山药的临床应用

Background Cancer is a complex and debilitating physical health disease that is important for social and individual health. Astragalus and Dioscorea opposita are two herbs that are traditionally used in folk medicine to treat various diseases, and they also play a role in immunizing and alleviating cancer. Purpose This review aims to evaluate the anti-tumor potential of Astragalus and Dioscorea opposita by summarizing the active components and their known effects on tumor-related pathways, further illustrating the anti-tumor potential of traditional Chinese medicine. This study aims to explore the therapeutic effects of traditional Chinese medicines on different types of tumors. Methods A comprehensive summary of the literature has been compiled, gathering information on the phytochemical characteristics, anti-tumor mechanisms, and the current status of both traditional Chinese and Western medicine relating to Astragalus and Dioscorea opposita. It demonstrates the previously established links between Astragalus and Dioscorea opposita and their anti-tumor properties. Results The combined use of Astragalus and Dioscorea opposita enhances the immune regulatory effect through synergistic action, thereby improving the overall immune status of the body. Conclusion This review provides a reference for experimental research in the treatment of tumors.

ETHNOPHARMACOLOGICAL RELEVANCE Dioscoreae Rhizoma (DR), the dried rhizome of Dioscorea opposita Thunb., is commonly referred to as "Shan Yao" in China. It has been extensively used in traditional Chinese medicine as an immunomodulatory agent and an adjuvant therapy in the treatment of cancer. DR has been widely applied in traditional medicines, such as Liuwei Dihuang Concentrated Pills and Shanyao Shenqi Pills. AIM OF THIS WORK This review is intended to provide a comprehensive overview of botany, traditional application, phytochemistry, pharmacologic activities, clinical application, and quality control of DR. Meanwhile, the review focuses on immunomodulatory, anti-hyperglycemic mechanisms, antioxidant and anti-inflammatory provides new perspectives and identifies promising avenues for future studies. MATERIALS AND METHODS The review collected information from Web of Science, PubMed, X-MOL, SciFinder, Google Scholar, Researchgate and CNKI from January 1971 to March 2025. RESULTS To date, approximately 304 compounds isolated and identified from DR, including 78 polysaccharides, polyphenols (1-59), flavonoids (60-65), terpenoids and steroids (66-80), alkaloids (81-104), organic acids (105-166) and others (167-226). DR demonstrates numerous pharmacological activities, including anti-hyperglycemic, anti-hyperlipidemic, immunomodulatory and anti-tumor effects. Multiple pathways are implicated in the immunomodulatory activities of DR, for example, the TLR4/NF-κB and JAK-STAT signaling pathway. However, the mechanisms responsible for its anti-tumor effects have not been fully elucidated. Furthermore, we summarize the limitations of current research and propose promising future research directions. CONCLUSION This review encompasses a comprehensive overview of DR, covering its botany, traditional applications, phytochemistry, pharmacological activities, clinical applications and quality control of DR. Moreover, research has highlighted DR's broad pharmacological profile, with a notable emphasis on its immunomodulatory properties. While research has predominantly focused on Dioscoreae Rhizoma polysaccharides (DRP), the pharmacological mechanisms of its other compounds have consequently been underexplored.

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Hyperproduced prostaglandin E2 by cyclooxygenase-2 and microsomal prostaglandin E synthase-1 evokes several pathophysiological responses such as inflammation and carcinogenesis. Our recent study demonstrated that Dioscorea japonica extract suppressed the expression of cyclooxygenase-2 and microsomal prostaglandin E synthase-1 and induced apoptosis in lung carcinoma A549 cells. In the present study, we investigated the effects of Dioscorea japonica on squamous cell carcinoma of mouse skin. Dioscorea japonica feeding and Dioscorea japonica extract topical application suppressed the expression of cyclooxygenase-2, microsomal prostaglandin E synthase-1, interleukin-1β and interleukin-6 and inhibited tumor formation, hyperplasia and inflammatory cell infiltration. Immunohistochemical analyses showed the immunoreactivities of cyclooxygenase-2 and microsomal prostaglandin E synthase-1 in tumor keratinocytes and stronger immunoreactivities of cyclooxygenase-2 and hematopoietic prostaglandin D synthase in epidermal dendritic cells (Langerhans cells). Treatment with Dioscorea japonica decreased the immunoreactivity of cyclooxygenase-2 and microsomal prostaglandin E synthase-1. These results indicate that Dioscorea japonica may have inhibitory effects on inflammation and carcinogenesis via suppression of the prostaglandin E2 synthetic pathway.

In recent years, with the progress and development of the times, our eating habits and lifestyle changes have led to an increase in gouty arthritis annually, with the main use of nonsteroidal anti-inflammatory drugs and other drugs. These drugs are highly dependent, resulting in an unresponsive state, which is easy to recur. Therefore, more and more patients choose traditional Chinese medicine (TCM) to treat them. After years of continuous exploration and rich clinical experience accumulation, Academician TongXiaolin put forward the dialectical strategy of “combination of state and target” in TCM. He believed that the deficiency of liver and kidney is transformed into a state, with uric acid as the target. Through the target prescription Simiao decoction to clever heat and moisture, replenishing liver and kidney, the target medicine Bixie (Dioscorea Tokoro Makino) to rheumatism, Shujin;Tufuling (Rhizoma Smilacis Glabrae) for detoxification, dehydration gas, Weilingxian (Radix et Rhizoma Clematidis) to rheumatism, pass meridians, and the combination of the condition and target achieves a good clinical effect.

Yaosheng Zhang Zhongjing's Dioscorea Pill has been applied to skin diseases, respiratory diseases, immune systems, tumors and other diseases in clinic. In the past decade, the research on dioscorea pills has been widely conducted based on the development of modern Chinese medicine, and thus yield many significant outputs. For example, some research showed positive results regarding the application of yam pills in clinical pracices on diseases of many different systems, such as skin diseases, respiratory system, immune system and tumors. By contrast, others showed that dioscorea pills do not play a role in controlling disease progression and relieving symptoms when treating certain diseases.

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Abstract Hyperlipidemia is a disorder of lipid metabolism, which is a major cause of coronary heart disease. Although there has been considerable progress in hyperlipidemia treatment, morbidity and risk associated with the condition continue to rise. The first-line treatment for hyperlipidemia, statins, has multiple side effects; therefore, development of safe and effective drugs from natural products to prevent and treat hyperlipidemia is necessary. Diosgenin is primarily derived from fenugreek (Trigonella foenum graecum) seeds, and is also abundant in medicinal herbs such as Dioscorea rhizome, Dioscorea septemloba, and Rhizoma polygonati, is a well-known steroidal sapogenin and the active ingredient in many drugs to treat cardiovascular conditions. There is abundant evidence that diosgenin has potential for application in correcting lipid metabolism disorders. In this review, we evaluated the latest evidence related to diosgenin and hyperlipidemia from clinical and animal studies. Additionally, we elaborate the pharmacological mechanism underlying the activity of diosgenin in treating hyperlipidemia in detail, including its role in inhibition of intestinal absorption of lipids, regulation of cholesterol transport, promotion of cholesterol conversion into bile acid and its excretion, inhibition of endogenous lipid biosynthesis, antioxidation and lipoprotein lipase activity, and regulation of transcription factors related to lipid metabolism. This review provides a deep exploration of the pharmacological mechanisms involved in diosgenin-hyperlipidemia interactions and suggests potential routes for the development of novel drug therapies for hyperlipidemia.

Background：Cardiovascular disease is the leading cause of death in both developed and developing countries. Di'ao Xinxuekang (DAXXK) is a pure Chinese medicine herbal preparation refined from dioscin extracted from the roots of Dioscorea panthaica Prain et Burk and Diosorea nipponica Makino. Objective: To evaluate the application of DAXXK in Cardiovascular disease. Methods: We searched and summarized all the studies on DAXXK and Cardiovascular disease in pumend, Google, and CNKI. Results：Modern pharmacological studies have shown that DAXXK has pharmacological effects such as dilating blood vessels, lowering blood pressure and cardiac load, improving hemodynamics, lowering blood lipids and anti-platelet aggregation, and is widely used for the therapy of various kinds of cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease (CHD), angina pectoris (AP) and myocardial infarction. We provide an overview of the clinical efficacy, molecular mechanisms, safety and therapeutic potential of DAXXK in the treatment of cardiovascular disease, aiming to provide clues and evidence for clinical decision-making. Conclusion：DAXXK exerts cardiovascular protection by regulating a variety of cardiovascular disease-related signaling pathways.

Objectives Chinese yam and Rehmannia glutinosa, Henan province local medicinal herbs, have received attention owing to its positive nutritional and medicinal characteristics. The combination of Chinese yam and Rehmannia glutinosa, known as a ‘medicine pair’, has a long history of use. However, no published study has evaluated Chinese yam—Rehmannia glutinosa medicine pair (CYRG) as a dietary additive in broilers. This study aimed to evaluate the impact of dietary CYRG on growth performance, body measurements, slaughtering performance, antioxidant capacity and cecum microbiota of broilers. Methods Total of 300 23-day-old Arbor Acres female broilers were randomly assigned to the 5 treatment groups (CON, 0.5% CYRG, 1% CYRG, 1.5% CYRG, and 2% CYRG) with 6 replications and 10 birds/replicate. In the CON group, broilers received the basal diet, and other 4 groups received the basal diet supplemented with 0.5, 1, 1.5, and 2% CYRG, respectively. The feeding trial lasted for 19 days, until to 42 days. Results The results showed that 0.5% CYRG group had the highest of body weight gain, average daily gain, and average daily feed intake among the 5 groups. Supplementation CYRG significantly improved the slaughter percentage and semi-evisceration weight percentage of broilers (P < 0.05). Supplementation 0.5% CYRG and 1% CYRG significantly increased the level of anti-inflammatory cytokines (IL-4) and decreased the pro-inflammatory cytokines (IL-6) level (P < 0.05). Supplementation 1.5% CYRG improved the levels of serum immunoglobulins G (IgG) and IgM (P < 0.05). 0.5% CYRG significantly increased the levels of catalase (CAT), glutathione peroxidase (GSH-Px), and total antioxidant capacity (T- AOC), and decreased the levels of malondialdehyde (MDA) (P < 0.05). Microbiological analysis showed that CYRG supplementation increased the abundance of beneficial bacteria (Firmicutes) and decreased the quantity of harmful bacteria (Proteobacteria and Cyanobacteria). Correlation analysis indicated that Lactobacillus salivarius and Lactobacillus_crispatus were positively associated with serum IgA and IgG (P<0.05). And Ruminococcaceae were positively correlated with CAT and GSH-Px activities (P<0.05), and Unclassified Clostridia ucG 014 was negatively correlated with MDA (P<0.05). Conclusion Results showed that dietary CYRG improved the economic benefits of broilers by improving slaughter performance, physical and intestinal health. The 0.5% CYRG dose was recommended.

Objective Chinese yam (Shanyao in Chinese, SY) as one of the representatives for Chinese medicines can be used as both of medicine and food with rich nutritional and medicinal value. Most of Chinese herbal medicines need to be processed prior to be used in clinical practice. SY was divided into Maoshanyao (Hairy Shanyao, MSY) and Guangshanyao (Smooth Shanyao, GSY) based on different processing methods at the place of origin, and it also could be processed as stir-fried SY and bran stir-fried SY to meet the different clinical use. Moreover, during the processing of Chinese herbal medicines, more complicated Maillard reaction occurs compared to food processing. Therefore, the objective of this research is to quantify the firepower of SY processing, and combined this with the relevant parameters of Maillard reaction. Methods The MSY and GSY produced in Shanxi and Henan Provinces were chosen as the research objects. By using thermal analysis technology, we first established the correlation between pyrolysis and processing of SY and its mixtures. We also quantified the firepower of Shaoyao processing, and combined this with the relevant parameters of Maillard reaction (pH value, amino acid, and 5-HMF) and the changes in medicinal ingredients (allantoin). Results The SY was mainly fried with moderate-fire (190 °C−200 °C), and the starting temperatures of different SY–ingredient mixtures were (176.3 ± 5.33) °C for (honey) bran, and (205.9 ± 8.05) °C for rice. The upper limits of processing temperature were (289.9 ± 6.47) °C for (honey) bran and (298.9 ± 1.15) °C for rice. The cooking time was (10.80 ± 1.76) min for soil stir-fry, (10.31 ± 1.06) min for bran stir-fry, and (8.43 ± 0.68) min for rice stir-fry. Moreover, the pH values and the content of 5-HMF were increased (P < 0.001), while the content of glycine was decreased significantly (P < 0.001) after processing. Conclusion The results verified and quantified the firepower of traditional processing of SY, and also provided scientific reference for other studies related to SY processing.

Dioscorea polystachya and its closely related species are original plants of the tuber crop “yam”, which had been intensively use for medicinal and food purposes and widely cultivated in northern China and its surrounding areas with a long history. Many cultivars of these species are often confused with one another because of similar tuber morphology, however, conventional DNA barcoding faces practical limitations restricting the method to effectively identify closely related species. In addition, phylogenetic relationships among various cultivar groups of Chinese yam (D. polystachya) remains unclear. To solve these problems, genomic DNAs of 15 Dioscorea samples were sequenced to assemble and annotate chloroplast genomes, which were used for analyzing their structural characteristics and identifying phylogenetic relationships at the inter- and intraspecific levels. The size of chloroplast genomes of the tested samples is about 153 kb, and 79 protein-coding genes, 29 tRNA genes, and 4 rRNA genes are annotated. Phylogenetic analysis showed that D. polystachya were sister to Dioscorea japonica, and for Huaishan yams, Dioscorea persimilis did not cluster with Dioscorea alata and Dioscorea fordii. Four cultivar groups of Chinese yam were determined, namely Tiegun group, Anping group, Foshou group and Taihang complex group. Among these cultivar groups, Foshou and Taihang complex are clustered with different wild yams, respectively. Amino acid preferences are similar at the inter- and intraspecific levels, while synonymous codon usage reflects distinct patterns in the majority of cultivars of D. polystachya. There are distinct SSR variations among species, as well as four cultivar groups. Collinearity and SNP analyses show that nucleotide hypervariable regions among Dioscorea species are mainly concentrated in trnK–atpA, rps16–trnQ, atpA–atpH, rpoB–psbD, atpH–atpI, trnV–ndhC in the LSC region, and ccsA–ndhF in the SSC region, while intraspecific variation of Chinese yam is enriched in the intergenic spacers of rpoB–psbC, ndhD–ndhF, and trnQ-trnS, as well as the gene ycf1. Phylogenetic analysis supports that Huaishan yams are not of monophyletic origin and the cultivated Chinese yam has at least two wild origins of domestication, which is consistent with the historical records of these wild yams from Mt. Dabie and Mt. Taihang. The identification efficiency of the newly developed barcodes for cultivar groups based on chloroplast genome SNP screening is significantly better than those of conventional barcodes. This approach to generate viable candidate markers based on the comparison from interspecific and intraspecific hypervariable regions of chloroplast genomes can be applied to conduct phylogenetic relationships of more important crop species and their close relatives, which are difficult to identify, as well as their wild origins of domestication.

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O bjective: To study effects of nourishing kidney and detoxification prescriptions on virological response to chronic hepatitis B antiviral treatment. Methods: 98 patients with early antiviral treatment of chronic hepatitis b patients, were randomly divided into treatment group and control group, two groups all use lamivudine antiviral treatment, treatment group was added with Nourishing kidney and detoxification prescriptions (dodder, medlar, medicinal indianmulberry root, desertliving cistanche, turmeric, honeylocust thorn, giant knotweed, radix scutellariae, radix astragali, Chinese yam, batryticated silkworm, 12 sorts of traditional Chinese medicine, etc), virological response and virus Yin turn rate in patients with lamivudine antiviral treatment were observed. Results: the virological response rates, Yin turn rate of treatment group were obviously better than that of control group ( P <0.05). Conclusion: Nourishing kidney and detoxification prescriptions could improve the treatment of chronic hepatitis B antiviral treatment virological response rates and Yin turn rate.

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Yam (Dioscorea spp.), known as an edible and medicinal tuber crop in China, has been used historically for the treatment of diabetes, diarrhea, asthma, and other ailments in traditional Chinese medicine. Moreover, it has been consumed as starchy food for thousands of years in China. Modern phytochemistry and pharmacological experiments have been proved that non-starch polysaccharide is one of the main bioactive substances of yam. Many studies have been focused on the isolation and identification of polysaccharides and their bioactivities of Chinese yam. However, due to the difference in the variety of raw materials and the method of polysaccharides extracting, the structure and biological activity of the obtained polysaccharides also differ. It has been demonstrated that Chinese yam polysaccharide has various important biological activities, such as hypoglycemia, immunomodulatory, antioxidant, and antitumor activities. This paper is aimed at summarizing previous and current references of the isolation processes, structural features and bioactivities of yam polysaccharides. The review will serve as a useful reference material for further investigation and application of yam polysaccharides in functional foods and medicine fields.

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Abstract Two metal chelates of Dioscorea oppositifolia L. peel polysaccharides (DTP) were prepared: iron chelate (DTP-Fe) and zinc chelate (DTP-Zn). The physicochemical properties of the polysaccharide and its metal chelates were assessed by UV-Vis absorption spectroscopy, Fourier-transform infra-red spectroscopy, scanning electron microscopy, and thermogravimetric analysis. Antioxidant activities were evaluated by DPPH, ABTS + and hydroxyl radical scavenging assays. According to ICP-MS, the iron content of DTP-Fe was 9.47%, while the zinc content of DTP-Zn was 4.02%. The antioxidant capacity of DTP-Fe increased with the increase of concentration, and its overall activity was higher than that of DTP and DTP-Zn. This polysaccharide-iron chelate can be developed and utilised as an antioxidant and multifunctional iron supplement. DTP-Zn showed the potential to be a natural antioxidant and zinc supplement food. Graphical Abstract

The medicinal herb Dioscorea floribunda (Linn.) is very significant. Varahikanda's medicinal properties are quite important. It is used to treat various diseases in Ayurvedic literature. Here is a summary of studies on the antiquity and ayurvedic qualities of varahikanda, i.e. Dioscorea floribunda. Varahikanda has a variety of pharmacological characteristics, according to the research. Jeevaneeya, Rasayana, Balya, Krumighna, Pramehaghna, Kushtaghna, Vrushya, Nadivrun, Visarpa, Udarshool, Raktapitta are all Ayurvedic terms. It has antimicrobial action, wound healing activity, antihyperglycemic activity, dyslipidemic activity, anticancer activity, immunomodulatory activity, antioxidant activity, antiinflammatory and analgesic activity, antihelmintic activity, and aphrodisiac activity, according to contemporary research.

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A previously unknown, water-soluble polysaccharide, named DOTP-B, was isolated from the roots of the plant Dioscorea opposita Thunb, a well-known edible and medicinal plant in China. DOTP-B was found to be neutral in charge, with an average molecular weight of 5623 Da. Monosaccharide composition analysis by GC-MS revealed that DOTP-B was a hetero-polysaccharide consisting of glucose and galactose at a molar ratio of 14.6:1.0. Structural features of DOTP-B were investigated with a combination of chemical and instrumental methods, including complete acid hydrolysis, periodate oxidation, methylation, GC-MS, FTIR and several NMR spectra. Highly correlated results demonstrated that the main chain of DOTP-B consisted of →4)-α-d-glc(1 → residues, with about 6% internal →6)-β-d-gal(1 → residues. The antioxidant activity of DOTP-B was also evaluated as the EC50 values against DPPH and PTIO radicals were 2.1 ± 0.1 mg/mL and 1.6 ± 0.1 mg/mL, respectively. Therefore, the polysaccharide DOTP-B could be possibly developed as a promising natural antioxidant for application in medical and food industries.

To establish the quality control method of Dioscorea opposita Thunb., the multi-level fingerprinting of polysaccharides was established and the relationship between fingerprint and immune activity was analyzed. The two molecular weight segments Mw1 (1.38 × 105-1.63 × 106 Da) and Mw2 (3.27 × 103-4.37 × 103 Da), thirteen infrared absorption peaks (3399.26 cm-1, 2929.32 cm-1, 1631.78 cm-1, 1400.39 cm-1, 1351.80 cm-1, 1123.58 cm-1, 1024.76 cm-1, 931.53 cm-1, 854.76 cm-1, 760.43 cm-1, 708.14 cm-1, 616.47 cm-1, and 526.78 cm-1), and four monosaccharides (Man, Rha, GalA, and Glc) were used to evaluate the quality of Dioscorea opposita Thunb. The molecular weight fragments of Mw1, FT-IR absorption peaks of 1631.78 cm-1, and two monosaccharides (Man and Glc) would be used to identify Dioscorea opposita Thunb. polysaccharide (DOP) from different origins. The relationship of spectrum-effect showed that polysaccharides with features such as higher Mw1, a lower peak height of 1631.78 cm-1, higher content of Man, and lower content of Glc exerted stronger immune activity. In conclusion, this study established a polysaccharide-based quality evaluation method for Dioscorea opposita Thunb. and explored the relationship between polysaccharide fingerprints and in vitro immune activity, which provided a basis for further research on Dioscorea opposita Thunb.

The purified polysaccharides fraction, DOP-2, was prepared from Dioscorea opposita Thunb (D. opposita). This study combined in vitro and in vivo experiments to comprehensively investigate the index changes in RAW264.7 cells and immunocompromised mice under DOP-2 intervention, aiming to elucidate the potential mechanisms of immunomodulatory effects of DOP-2. DOP-2 (10 ∼ 500 μg/mL) significantly elevated the levels of NO, interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) factors secreted by RAW264.7 cells, and restored the body weight of immunosuppressed mice and improve the degree of injury to the immune organ index, resulting in significant immunomodulatory effects. Notably, DOP-2 promoted the production of short-chain fatty acids (SCFAs) in immunosuppressed mice and modulated the composition of their gut microflora. These findings highlight the potential benefits of DOP-2 therapy in improving immune function and gut health, and will provide a theoretical basis for the application of D. opposita polysaccharides as an immunomodulatory adjuvant.

As common complications of diabetes, long-term hyperglycemia and inflammatory infiltration often lead to prolonged unhealing of chronic diabetic wounds. The natural hydrogel-containing plant polysaccharides were recorded to have effective hypoglycemic and anti-inflammatory effects. This study focused on the accelerating effect of diabetic wound healing of hydrogels doped with Dioscorea opposita polysaccharide (DOP)─calcium carbonate (CaCO3) microspheres, which have glucose-responsive insulin release and anti-inflammatory effects. The hydrogel defined as PL-PVA/DOP-CaCO3 was designed via the borate ester bonds between polylysine-phenylboronic acids (PL-PBA) and dihydroxyl groups of poly(vinyl alcohol) (PVA). DOP modified on the surface of CaCO3 microspheres can simultaneously act with PBA to dope into the PL-PVA hydrogel and maintain glucose sensitivity. The mechanical and swelling properties of the hybrid hydrogels were reinforced by the incorporated microspheres. Meanwhile, the hyperglycemia was also regulated by the released insulin and DOP. The in vitro results indicated that the PL-PVA/DOP-CaCO3 hydrogel had good biocompatibility and inflammatory activity and could promote fibroblast proliferation and migration. In vivo experiments demonstrated that the INS@PL-PVA/DOP-CaCO3 hydrogel can significantly promote wound healing in diabetic rats by glucose-responsive regulation of hyperglycemia, inhibiting inflammation, improving angiogenesis, and accelerating the secretion of endothelial cells and proliferation of fibroblasts on wound tissues. The results bring new insights into the field of glucose-responsive hydrogels, showing their potential as drug delivery systems of macromolecular therapeutics to treat diabetic skin wounds.

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Yam is used as common herbal remedy in traditional Chinese medicine and is grown all over Asia. According to previous research, one of the primary bioactive components of yam is yam polysaccharide. To shed light on the mechanism of yam polysaccharide in ulcerative colitis (UC), a yam heteropolysaccharide named CYP-3a was isolated and purified using ultrasonic extraction, the trichloroacetic acid technique, DEAE cellulose-52 and a Sephadex G75 column. CYP-3a comprises rhamnus: arabinose:galactose:mannose:galacturonic acid glucuronic acid, with a molar ratio of 2.25:4.17:3.30:0.09:0.13:0.26. CCK-8 and ELISA analysis results showed that CYP-3a increased the number of dextran sodium sulphate (DSS)-induced Caco-2 cells and could reduce and inhibit their inflammatory response by lowering the amounts of secreted TNF-α and IL-6. Western blot data demonstrated that CYP-3a at various doses could suppress the endoplasmic reticulum stress-mediated apoptotic pathway generated by DSS-induced UC and down-regulate the protein levels of GRP78, CHOP and NF-κB.

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Background Diabetic nephropathy (DN) is a severe complication of diabetes, which has been increasingly associated with gut microbiota dysbiosis and inflammatory dysregulation. Objective This study investigates the dual therapeutic potential of diosgenin (DIO), a steroidal sapogenin, in modulating the gut-kidney axis and NLRP3 inflammasome activity in a streptozotocin (STZ)-induced DN rat model. Methods Oral DIO administration (20 mg/kg, 8 weeks) was used to treat the DN rats. The study assessed the effects on metabolic and renal function parameters, renal apoptosis and fibrosis, gut microbiota diversity, and NLRP3 inflammasome activation in the kidney. Results DIO treatment ameliorated the progression of DN, improving metabolic and renal function. It attenuated renal apoptosis and fibrosis and restored gut microbiota diversity, particularly enriching the abundance of Lachnospiraceae and Eubacterium. Mechanistically, DIO suppressed NLRP3 inflammasome activation in the kidney, disrupted the LPS-TLR4/NF-κB signaling cascade, and reduced systemic pro-inflammatory cytokines (IL-1β, IL-6). Conclusion DIO is a multitarget agent that addresses both gut microbiota homeostasis and NLRP3-driven inflammation, presenting a novel therapeutic strategy for DN through modulation of the gut-kidney axis.

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Acute liver failure (ALF) is a deadly clinical syndrome, which leads to a rapid loss of normal liver function. Diosgenin is a natural steroidal sapogenin found in various plant families. Various studies have shown that diosgenin have therapeutic or preventive effect in various diseases such as cancer, cardiovascular disorders, type 2 diabetes, and neurodegenerative disorders. In this study, we evaluated effects of diosgenin on mice model of ALF. Animal model of ALF was induced by intraperitoneal injection of lipopolysaccharide (LPS)/d-galactosamine (D-Gal). The male C57BL/6 mice were randomly divided into 3 groups: control group, LPS/D-Gal group, and LPS/D-Gal + diosgenin group (50 mg/kg). Mice in the LPS/D-Gal group received a combination of LPS (50 μg/kg) and D-Gal (400 mg/kg) intraperitoneally. LPS/D-Gal + diosgenin group received diosgenin twice orally 24 h and 1 h before receiving LPS/D-Gal. Markers of liver injury including ALT, AST and ALP were measured in blood samples in addition to determination of oxidative stress and inflammatory markers including MDA, nitrite, ROS, catalase, SOD, Nrf2, IL-1β, IL-6, TLR4, TNF-α and NF-κB in hepatic tissue. Administration of diosgenin could greatly reduce serum levels of ALT, AST, and ALP. Besides, hepatic levels of MDA, ROS, IL-1β, IL-6, TLR4, TNF-α, and NF-κB significantly decreased and SOD activity and Nrf2 level increased in comparison with the LPS/D-Gal group. In addition, myeloperoxidase activity as a marker of neutrophil infiltration decreased following diosgenin administration. In summary, diosgenin led to reduction of liver injury indices and oxidative stress and inflammatory events and diosgenin has probably hepatoprotecive effects in ALF.

In a mouse model of Graves’ disease (GD), diosgenin has been shown to have a therapeutic effect on GD by alleviating goitre. However, research on the effect of diosgenin on autoimmune thyroiditis (AIT) is lacking. In this study, transcriptomics was used to comprehensively analyse the protective effect of diosgenin against AIT in rats and the possible mechanism. The results showed that in the diosgenin-intervention group, compared to the model group, the expression of serum triiodothyronine, thyroxine, free triiodothyronine, and free thyroxine was decreased and that of thyroid-stimulating hormone was increased; these changes were accompanied by the downregulation of thyroglobulin, TSH receptor antibody and thyroid peroxidase expression in serum. Furthermore, transcriptome detection, RT-qPCR and immunohistochemistry verification revealed that in thyroid tissue, the relative mRNA and protein expression of cyclic adenosine 3′,5′-monophosphate (cAMP), protein kinase A (PKA) and cAMP response element-binding protein (Creb) were increased and the mRNA expression of S100 calcium-binding protein A9 (S100A9) was decreased in the diosgenin groups. In summary, diosgenin alleviates the development of AIT, possibly via the activation of the cAMP/PKA/Creb pathway and downregulation of S100A9 gene expression.

Background: Diosgenin, obtained from Dioscorea nipponica Makino, possesses anti-inflammatory properties. Objective: The objective of this study is to explore the therapeutic effects of diosgenin against collagen-induced arthritis (CIA) in DBA/1J mice. Materials and Methods: The CIA model was established using chicken type II collagen-immunized DBA1/J mice (0.1 mL/mouse), with the same stimulus repeated on day 21. Next, the CIA mouse model was selected, and inguinal lymph nodes were excised to obtain a single-cell suspension. Using CCK-8, control group, model group, and high-/medium-/low-dose diosgenin group were set based on drug toxicity. Next, the ratio of T-helper 17 cells (Th17) to CD3+ T cells was analyzed using flow cytometer. The levels of interleukin 17 (IL)-17 and IL-6 were determined by the enzyme-linked immunosorbent assay. The expression of RORγt was determined using the reverse-transcription quantitative real-time polymerase chain reaction and Western blot analysis. Results: An in vitro inhibitory rate of ≥ 70% was set as the cutoff value to select the high (25 μmol/L), medium (12.5 μmol/L), and low (6.25 μmol/L) doses of diosgenin. The Th17 cell ratio in CD3+ T cells, the levels of IL-17 and IL-6, and mRNA and protein expression of RORγt showed significantly increased tendency in the model group compared with the control group (P < 0.01 and/or P < 0.05). Diosgenin significantly decreased the Th17 cell ratio in CD3+ T cells, IL-17 and IL-6 levels, and RORγt expression when compared with the model group (P < 0.01 and/or P < 0.05). Conclusion: Diosgenin exhibited an antiarthritic effect in CIA mice by downregulating the differentiation of Th17 cells.

Silicosis is an occupational lung disease that is caused by chronic exposure to silica dust. Silica‐exposed workers are at higher risk of developing TB, resulting in lung fibrosis and significant respiratory dysfunction. Diosgenin is a steroidal saponin that has been shown to exert a therapeutic effect on lung injury. Therefore, we investigated the potential efficacy of diosgenin in treating silicotuberculosis by evaluating its effectiveness against Mycobacterium smegmatis, as well as its antifibrotic and antioxidant effects in silica‐induced TB in rats.

Introduction: Cardiovascular diseases are an important public health problem because they are the main causes of mortality in the world, especially in developing countries. Despite existing drug therapies, such diseases have particularities that hinder their control. For this reason many studies seek to identify new molecules, especially natural substances, with therapeutic potential to control cardiovascular diseases. Diosgenin is a steroidal saponin that has many biological activities and promotes cardiovascular action. Objective: Identify the cardiovascular effect of diosgenin and to describe the mechanisms of action involved in this activity. Methodology: An integrative review of the literature was carried out with articles that dealt with the topic researched in the last 10 years from 2009 to 2019, available in the PubMed, Web of Science, Scopus and BIREME/BVS databases, using advanced search with the descriptors "Diosgenin" "Cardiovascular System", "Heart" and “Diseases”, interspersed with the "and" or "or" boolean operators. Results: After initial selections and readings of some articles in their entirety, 14 studies integrated the present review. Diosgenin showed important cardioprotective activity in studies with animal models that mimic the multiple cardiac pathologies in humans, which allow it to be considered with great future pharmacological potential. The mechanisms of action of this substance are related to antioxidant, antithrombotic, antiapoptotic and antiproliferative capacity. Conclusion: Diosgenin has a beneficial cardiovascular effect when used in multiple models of animal experimentation with cardiac alterations. This fact makes this substance an important and promising molecule for future research, such as clinical trials in humans with cardiovascular changes similar to those presented by animals.

BACKGROUD Arsenic trioxide (ATO), the first-line drug in treating acute premyelogenous leukemia, has the profound side effect of inducing endothelial mesenchymal transition (EndMT) and causing cardiac fibrosis. Diosgenin (DIO), a pharmaceutical compound found in Paris polyphylla, exhibits promising potential in safeguarding cardiovascular health by mitigating EndMT. PURPOSE This study aims to explore the role and mechanism of DIO in ATO-induced myocardial fibrosis to provide a novel therapeutic agent for ATO-induced cardiac fibrosis. METHODS Wistar rats were given DIO by gavage and ATO by tail vein. Cardiac function and fibrosis were evaluated by echocardiography and Masson's trichrome staining in rats. Human aortic endothelial cells (HAECs) were utilized to analyze ATO-induced EndMT in vitro. The cytoskeleton of HAECs was visualized using F-actin staining to observe cell morphology, while Dil-Ac-LDL staining was employed to assess cell functionality. EndMT-related factors (CD31 and α-SMA), glucocorticoid receptor (GR) and interleukin-6 (IL-6) were detected by immunofluorescence and Western blot in vivo and in vitro. Furthermore, GR was knocked down by si-GR, and IL-6 was blocked by IL-6 neutralizing antibody to verify their role in the effect of DIO on ATO-induced EndMT in HAECs. RESULTS DIO exhibited significant efficacy in ATO-induced damage to both cardiac diastolic and systolic function, along with mitigating cardiac fibrosis. Additionally, DIO alleviated the loss of cytoskeletal anisotropy and enhanced the uptake of Dil-Ac-LDL in HAECs. Furthermore, it reversed the ATO-induced downregulation of endothelial-specific markers CD31 and GR, while suppressing the upregulation of mesenchymal markers α-SMA and IL-6, both in vivo and in vitro. Notably, the protective effect of DIO was compromised upon knockdown of GR, which also led to a reversal of DIO-induced IL-6 downregulation. Furthermore, the neutralization of IL-6 with specific antibodies abolished the ATO-induced changes related to EndMT. CONCLUSION In this study, we clarified the protective effect of DIO on ATO-induced myocardial fibrosis against EndMT via the GR/IL-6 axis for the first time and provided a potential therapeutic agent for preventing heart damage caused by ATO.

Plateau hyperuricemia is a common disease in the plateau area, and the incidence is much higher than that in the plain area. Dioscin (DIO) and its active metabolite Diosgenin (DG) exert therapeutic effects on hyperuricemia through oxidative stress and inflammation. In this study, DIO and its active metabolite DG were taken as the research objects to explore their therapeutic effects on high-altitude hyperuricemia in rats. To evaluate the therapeutic effect of DIO on the rat model of high-altitude hyperuricemia, the evaluation indexes include blood biochemical indexes, renal histopathology, oil red O staining of the kidney, rat kidney index, and rat renal inflammatory factors. Transcriptomics was used to analyze the control group, model group, and drug-administered group to preliminarily explore the protective mechanism of DIO in rats with high-altitude hyperuricemia. An HK-2 high-altitude hyperuricemia cell injury model was established to verify the therapeutic mechanism of DIO in rats with high-altitude hyperuricemia. Western blot was used to detect the expression of related proteins in renal tissues and cell models. The results showed that DIO and its active metabolite DG regulate renal lipid metabolism through the EPHX2 gene, attenuate renal inflammatory reaction, and then promote the excretion of uric acid and reduce its reabsorption, which ultimately achieves the effect of treating plateau hyperuricemia.

No abstract available

Nonalcoholic fatty liver disease (NAFLD) is the most common liver disease worldwide and has no approved treatment. The hepatic farnesoid X receptor (FXR) is one of the most promising therapeutic targets for NAFLD. Diosgenin (DG), a natural compound extracted from Chinese herbal medicine, is very effective in preventing metabolic diseases. Our research aims to determine the effects and molecular mechanisms of DG on NAFLD in vivo and in vitro. The effect of DG on hepatic steatosis was evaluated in Sprague‒Dawley (SD) rats induced by a high-fat diet (HFD) and in HepG2 cells exposed to free fatty acids (FFAs, sodium oleate:sodium palmitate = 2:1). DG treatment efficiently managed hepatic lipid deposition in vivo and in vitro. Mechanistically, DG upregulated the expression of FXR and small heterodimer partner (SHP) and downregulated the expression of genes involved in hepatic de novo lipogenesis (DNL), including sterol regulatory element-binding protein 1C (SREBP1C), acetyl-CoA carboxylase 1 (ACC1), and fatty acid synthase (FASN). Moreover, DG promoted the expression of peroxisome proliferator-activated receptor alpha (PPARα), which is related to fatty acid oxidation. In addition, DG inhibited the expression of the CD36 molecule (CD36) related to fatty acid uptake. However, hepatic FXR silencing weakened the regulatory effects of DG on these genes. Collectively, our data show that DG has a good effect on alleviating nonalcoholic hepatic steatosis via the hepatic FXR-SHP-SREBP1C/PPARα/CD36 pathway. DG promises to be a novel candidate FXR activator that can be utilized to treat NAFLD.

Inflammatory cascade plays a pivotal role in the onset and progression of major depressive disorder (MDD) and glioblastoma multiforme (GBM). Therefore, questing natural compounds with anti-inflammatory activity such as diosgenin can act as a double-edged sword targeting cancer and cancer-induced inflammation simultaneously. The blood–brain barrier limits the therapeutic efficiency of the drugs against intracranial pathologies including depression and brain cancers. Encapsulating a drug molecule in lipid nanoparticles can overcome this obstacle. The current study has thus investigated the anticancer and antidepressant effect of Tween 80 (P80) coated stearic acid solid lipid nanoparticles (SLNPs) encapsulating the diosgenin. Physio-chemical characterizations of SLNPs were performed to assess their stability, monodispersity, and entrapment efficiency. In vitro cytotoxic analysis of naked and drug encapsulated SLNPs on U-87 cell line indicated diosgenin IC50 value to be 194.4 μM, while diosgenin encapsulation in nanoparticles slightly decreases the toxicity. Antidepressant effects of encapsulated and non-encapsulated diosgenin were comprehensively evaluated in the concanavalin-A–induced sickness behavior mouse model. Behavior test results indicate that diosgenin and diosgenin encapsulated nanoparticles significantly alleviated anxiety-like and depressive behavior. Diosgenin incorporated SLNPs also improved grooming behavior and social interaction as well as showed normal levels of neutrophils and leukocytes with no toxicity indication. In conclusion, diosgenin and diosgenin encapsulated solid lipid nanoparticles proved successful in decreasing in vitro cancer cell proliferation and improving sickness behavioral phenotype and thus merit further exploration.

Hyperglycemia, hyperlipidemia, and atherosclerotic lesions may cause inflammation, which leads to chemokine production and changes in vascular responses. Hyperglycemia can impair normal protein folding by producing reactive oxygen species (ROS) and interacting with various signaling molecules, resulting in the activation of ER stress responses, that stimulates NF-kB, which regulates the expression of numerous genes involved in inflammation and vascular remodeling. Our previous studies have shown that diosgenin has a protective effect against streptozotocin (STZ) - induced oxidative damage in rat aorta. However, the therapeutic role of diosgenin on iRhom2/TACE signaling which has primarily been linked to the endoplasmic reticulum (ER)-stress induced inflammation is unknown. Diosgenin was administered (40 mg/kg b. wt, orally, for 4 weeks) to STZ-induced male albino rats. Fasting plasma glucose, blood pressure, nitrite level, lipid profile, and lipoprotein were assessed. Serum insulin and pro-inflammatory markers were analyzed using ELISA, mRNA and protein expression of iRhom2/TACE signaling molecules were analyzed using RT-PCR and western blotting analysis respectively. In silico study was also performed to find out the possible binding affinity of diosgenin with the ER stress signaling molecules. Through regulation of the iRhom2/TACE signaling molecules, diosgenin lowered dyslipidemia, hypertension, and pro-inflammatory cytokines (TNF-α, IL-1, IL-6, and IL-4) in the aorta of STZ induced diabetic rats. Results of molecular docking analysis also confirmed the potential binding interaction with iRhom2/TACE and TNF- α. These in silico and in vivo results indicated that a change in lipid profile and hypertension led to diabetes-related inflammation by promoting ER stress and, as a result, accelerating the aorta by generating proinflammatory cytokines and lipid deposition. This study concludes that diosgenin attenuates ER stress-induced inflammation in diabetic rat aorta by modulating the expression of pro-inflammatory, iRhom2/TACE mediated mechanism and hence diosgenin can be a therapeutic drug for the treatment of diabetes-induced inflammation.

Diosgenin, a natural steroidal saponin, can exert antitumor effect by regulating immune function and improving intestinal microbiota. The response to anti-PD-1 immunotherapy is associated with intestinal microbiota and effector T cells in tumor microenvironment. We hypothesize that the modulation of diosgenin on intestinal microbiota can facilitate antitumor immunity and the therapeutic efficacy of PD-1 antibody. In melanoma-bearing C57BL/6 mice, we observed that the anti-melanoma effect of diosgenin relied more on antitumor immunity than direct tumor inhibition activity evidenced by obvious CD4+/CD8+ T-cell infiltration and IFN-γ expression in tumor tissues, and it could improve the compositions of intestinal microbiota. Antibiotics impaired the therapeutic efficacy and immunity responses of diosgenin through disturbing intestinal microbiota, indicating the importance of intestinal microbiota in diosgenin’s in vivo antitumor activity. More importantly, the combined administration of PD-1 antibody with diosgenin aggravated the tumor necrosis and apoptosis by eliciting augmented T-cell responses. Taken together, diosgenin can be used as a microecological regulator to induce antitumor immunity and improve the efficacy of immune checkpoint antibody, making it more suitable for the treatment of malignant tumors.

No abstract available

ETHNOPHARMACOLOGICAL RELEVANCE Diabetic sarcopenia (DS), an emerging diabetes complication, poses an increasing challenge to the elderly population. Shenqi paste (SQP) consists of 8 medicine-food homology substances: Astragalus membranaceus (Fisch.) Bge., Codonopsis pilosula (Franch.) Nannf., Polygonatum sibiricum Red., Dioscorea opposita Thunb., Poria cocos (Schw.) Wolf, Eucommia ulmoides Oliv., Hordeum vulgare L., and Ophiopogon japonicus (L.f.) Ker Gawl.. SQP has shown potential benefits for sarcopenia in clinical practice. Its efficacy and safety in DS have not been validated in a randomized controlled trial. AIM OF THE STUDY This study aimed to evaluate the efficacy, safety, and limitations, and provide insights into methods and strategies for utilizing SQP in DS management. MATERIALS AND METHODS In this randomized, double-blind, placebo-controlled trial, community-dwelling older adults (≥ 60 years) with DS and spleen-kidney deficiency syndrome were allocated 1:1 to receive either SQP or placebo paste for 12 weeks. Primary outcomes were skeletal muscle mass index (SMI), handgrip strength, and five-time chair stand test (FCST) duration. Secondary outcomes included health-related scales and biochemical indicators. Assessments were conducted at the baseline (T0), week 6 (T1), and week 12 (T2). Safety evaluation included blood routine, liver and kidney function tests. Intention-to-treat analysis was applied to the primary outcomes data from all participants, with per-protocol analysis for sensitivity. Generalized estimating equations with covariate adjustment and t-tests or Wilcoxon rank-sum tests were used for statistical analysis. RESULTS Of 90 randomized participants, the SQP group showed greater improvements in handgrip strength (T2: interact p < 0.001), SMI (T2: interact p < 0.001), and FCST (T2: interact p < 0.001) versus control. Secondary outcome measures of 74 participants, including frailty, nutrition, physical activity, sleep quality, depression, and TCM syndrome scores, significantly improved (p < 0.05), with significant fasting blood glucose reduction (T2: interact p = 0.018) and C-reactive protein decrease (T2: interact p < 0.001). There was no statistically significant difference in the change in the difference between the two groups in fasting insulin, glycated hemoglobin and insulin resistance index before and after intervention (p > 0.05). Within-group analysis demonstrated significant reductions of SQP group in inflammatory cytokines, and sarcopenia-related biomarkers (p < 0.001) post-intervention. No serious adverse events occurred. CONCLUSION A 12-week SQP intervention enhanced muscle mass, strength, function, and metabolic and inflammatory profiles in older adults with DS, with good tolerability, supporting its potential as a safe, complementary therapy.

Background: Keeping in view the current scenario of increasing risk of dyslipidemia leading to coronary heart diseases in Indian population and dearth of conclusive evidences in support of homeopathic treatment of dyslipidemia, we intended to evaluate the efficacy of a frequently prescribed medicine Dioscorea villosa 6CH in comparison with placebo. Methods: In this prospective, double-blind, randomized, parallel arm, placebo-controlled trial, 100 patients diagnosed with dyslipidemia were randomized in 1:1 ratio to one of the two interventions – D. villosa 6CH or identical looking placebo in the mutual context of lifestyle modification advices. The outcome measure was the blood lipid profile – triglyceride, total cholesterol (TC), low-density lipoprotein cholesterol (LDLc), very LDLc (VLDLc), and high-density lipoprotein cholesterol (HDLc), assessed at baseline and 2 months after intervention. Comparative analysis was conducted on intention-to-treat basis to detect group differences using SPSS. Results: The groups were comparable at baseline. After 2 months of intervention, pre–post comparison showed significant changes in triglyceride, TC, and VLDLc in the verum group and triglyceride, TC, and LDLc in the placebo group; however, the group differences were non-significant: triglyceride (P = 0.809), TC (P = 0.316), HDLc (P = 0.430), LDLc (P = 0.192), and VLDLc (P = 0.251). Per protocol analysis also revealed similar non-significant trends. Conclusion: D. villosa 6CH could not produce any differentiable effect from placebo in treatment of dyslipidemia. Trial registration: Clinical Trials Registry – India/2018/04/013511.

Delayed bone defect repairs lead to severe health and socioeconomic impacts on patients. Hence, there are increasing demands for medical interventions to promote bone defect healing. Recombinant proteins such as BMP-2 have been recognized as one of the powerful osteogenic substances that promote mesenchymal stem cells (MSCs) to osteoblast differentiation and are widely applied clinically for bone defect repairs. However, recent reports show that BMP-2 treatment has been associated with clinical adverse side effects such as ectopic bone formation, osteolysis and stimulation of inflammation. Here, we have identified one new osteogenic protein, named ‘HKUOT-S2’ protein, from Dioscorea opposita Thunb. Using the bone defect model, we have shown that the HKUOT-S2 protein can accelerate bone defect repair by activating the mTOR signaling axis of MSCs-derived osteoblasts and increasing osteoblastic biomineralization. The HKUOT-S2 protein can also modulate the transcriptomic changes of macrophages, stem cells, and osteoblasts, thereby enhancing the crosstalk between the polarized macrophages and MSCs-osteoblast differentiation to facilitate osteogenesis. Furthermore, this protein had no toxic effects in vivo. We have also identified HKUOT-S2 peptide sequence TKSSLPGQTK as a functional osteogenic unit that can promote osteoblast differentiation in vitro. The HKUOT-S2 protein with robust osteogenic activity could be a potential alternative osteoanabolic agent for promoting osteogenesis and bone defect repairs. We believe that the HKUOT-S2 protein may potentially be applied clinically as a new class of osteogenic agent for bone defect healing.

Background and objectives Cyclophosphamide (CP) is widely used as a chemotherapy drug for the treatment of malignant tumors and autoimmune diseases, but it has strong toxic and side effects and can cause permanent damage to the ovaries, which affects women's quality of life. This study aimed to investigate the anti-premature ovarian failure protective effect of allantoin isolated from Dioscorea opposita Thunb. Methods Firstly, 75 mg/kg CP was injected into rats to establish an in vivo model of premature ovarian failure (POF). The POF rats were divided into the normal control group (NC), premature ovarian failure group (POF), and POF group treated with allantoin (ALL I 140 mg/kg and ALL II 70 mg/kg, daily 21 days). It investigated the estrous cycles, hormone levels, apoptosis rate, mitochondrial membrane potential (MMP), reactive oxygen species (ROS), mitophagy, and protein marker (Bax, Bcl2, LC3B, L-1β, caspase-1 and NLRP3). Results The results indicated that allantoin alleviated cyclophosphamide-induced premature ovarian failure in female rats, decreased the anoestrum, increased the level of estradiol (E2), and decreased the levels of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), decreased apoptosis rate, MMP, mitophagy and ROS in ovarian granulosa cells of POF rats, down-regulated L-1β, caspase-1, LC3B-II/LC3B-I in ovarian tissue, and up-regulated the Bcl2 and NLRP3. Conclusions Our study revealed the ovarian-protective effect of allantoin in CP-induced premature ovarian failure for the first time, the effect was achieved through attenuation of the apoptosis, autophagy, and pyroptosis. The study underlines the potential clinical application of allantoin as a protectant agent for premature ovarian failure.

Chinese yam (Dioscorea opposita Thunb), a traditional medicinal and edible plant, has attracted significant attention for its bioactive components. Chinese yam polysaccharides (CYPs) are regarded as the principal bioactive fraction responsible for its pleiotropic effects, notably immunomodulation. This review systematically summarizes recent advances in understanding the chemical structure, immunomodulatory mechanisms, and structure-activity relationships of CYPs. A core emphasis is placed on the intimate correlation between immunologic activity and specific structural determinants, including molecular weight, monosaccharide profile, glycosidic linkages, and higher-order conformation. Mechanistic studies demonstrate that CYPs are recognized by pattern recognition receptors, primarily TLR4, on the surface of immune cells such as macrophages. This recognition activates pivotal downstream signaling pathways, including NF-κB and MAPK. The subsequent orchestration of cytokine networks enables a homeostatic regulation of both innate and adaptive immunity, characterized by context-dependent immunostimulation and anti-inflammatory potential. Chemical modifications like sulfation and selenylation, alongside bioprocessing strategies such as physical, enzymatic, and fermentation treatments, significantly enhance their immunomodulatory potency. However, clinical translation faces significant hurdles, including incomplete structure-activity understanding, undefined pharmacokinetics, low oral bioavailability, challenges in quality control, and a paucity of systematic clinical safety and efficacy data. This review provides a comprehensive synthesis to inform future research and support the potential development of CYPs as novel immunomodulatory agents.

ETHNOPHARMACOLOGICAL RELEVANCE Autoimmune diseases (ADs) are characterized by high prevalence, severity, and a significant impact on quality of life. Conventional treatments, such as corticosteroids and biologics, often lead to adverse reactions. Traditional Chinese medicine, with its multi-component and multi-target characteristics, demonstrates potential as an alternative therapy for ADs. In traditional Chinese medicine, Dioscorea nipponica Makino (DnM) is often used in the treatment of rheumatic diseases and type 1 diabetes, among other autoimmune conditions. Therefore, we delve into the association of this herb with ADs. AIM OF THE STUDY We investigate the therapeutic potential and multi-target mechanisms of DnM (a traditional Chinese medicine with anti-inflammatory and immunomodulatory properties) in the treatment of ADs, elucidating its regulatory effects on immune cells and key signaling pathways. This work aims to provide a comprehensive phytopharmacological perspective for advancing ADs therapy and research. MATERIALS AND METHODS A systematic search was conducted across seven databases to analyze, compare, and review relevant studies. A comprehensive literature review was performed on the chemical components, quality control, clinical observations, pharmacological mechanisms, and toxicology of DnM, and DnM was compared to popular drug treatment strategies. RESULTS DnM and its bioactive constituents (notably dioscin, Diosgenin and Total Saponins of Rhizoma Dioscorea Nipponica (TSDN)) modulate T lymphocyte proliferation, regulate the TLR4/NF-κB pathway, suppress the release of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6), and bidirectionally regulate apoptosis through Fas/FasL and Bcl-2/Bax pathways (depending on disease-specific microenvironments in ADs). DnM demonstrates significant therapeutic efficacy in rheumatoid arthritis, autoimmune thyroiditis, psoriasis, and systemic lupus erythematosus, alleviating symptoms, delaying disease progression, and exhibiting a favorable safety profile. CONCLUSION DnM exerts multi-target effects by modulating key inflammatory and apoptotic pathways in ADs. The NF-κB, STAT3, and TGF-β/Smad signaling pathways may serve as key targets for DnM in modulating inflammatory states in ADs, while Fas/FasL and Bax/Bcl-2 are potential mediators of its apoptosis-regulating effects. Clinical evidence supports its efficacy in rheumatoid arthritis (RA) and Hashimoto's thyroiditis (HT), highlighting its multi-faceted therapeutic potential. This review systematically summarizes DnM's clinical outcomes, mechanisms, and toxicological profile, however, large-scale randomized controlled trials are required to validate its therapeutic potential across diverse ADs. Collectively, this work underscores DnM's promise as a candidate for AD therapeutics.

ETHNOPHARMACOLOGICAL RELEVANCE Clinical applications and pharmacological research suggest that Dioscorea opposita Thunb. (Chinese yam), a well-known traditional Chinese medicine which has been used for more than 2000 years to nourish kidney-yang and protect the male reproductive system, might be efficacious for the treatment of erectile dysfunction (ED). AIM OF THE STUDY This study aimed to investigate the active componentextract of Chinese yam, determine its effectiveness in hydrocortisone-induced "kidney-yang deficiency syndrome" (KDS-Yang) rats and in oxidatively damaged TM3 cells and explore the underlying mechanism on restoring erectile function. MATERIALS AND METHODS We clarified the Chinese yam cold-soaking extract (CYCSE) as the main active extract of Chinese yam by a CCK8 assay and further identified its composition. The KDS-Yang rats were induced by intragastric administration of hydrocortisone. After 10 d of CYCSE intervention, cavernous and testis morphology were stained with hematoxylin and eosin. Inducible nitric oxide synthase (iNOS), cyclic guanosine monophosphate (cGMP), testosterone, 8-hydroxy-2-deoxyguanosine (8-OHdG) and superoxide dismutase (SOD) levels were detected by enzyme-linked immunosorbent assay kits. Leydig cells were performed using immunohistochemistry. Reactive oxygen species were measured using a DCFH-DA fluorescent probe, and testicular collagenous fibers were stained with a Masson kit. Detection of testicular apoptosis was performed by a TUNEL assay. Nrf2 and NQO1 mRNA expression levels were measured by qRT-PCR. The protein expression levels of Nrf2, HO-1, TGF-β1 and SMAD2/3 were analyzed by Western blot. RESULTS We demonstrated in KDS-Yang rats and oxidatively damaged TM3 cells that CYCSE successfully restored erectile function through ameliorating testicular function. Our data suggested that CYCSE can stimulate the NO/cGMP pathway and restore the cavernous morphology to protect against KDS-Yang-induced ED. It also protected testis morphology, increased Leydig cell proliferation and stimulated testosterone secretion. In the damaged testes, excessive increases in 8-OHdG and inhibition of SOD activity were ameliorated, and the Nrf2/HO-1 signaling pathway was enhanced after treatment with CYCSE, indicating that the antioxidant defense system was activated. These findings were also validated in vitro. Additionally, fibrosis of the testes and TM3 cells was reversed by CYCSE through the TGF-β1/SMAD2/3 pathway. CONCLUSION CYCSE has a therapeutic effect on KDS-Yang-induced ED, and the mechanism includes stimulation of testosterone secretion, resistance to oxidative stress and prevention of fibrosis. These findings provide a new scientific verification for the application of Chinese yam in the treatment of KDS-Yang-induced ED.

No abstract available

ETHNOPHARMACOLOGICAL RELEVANCE Dioscorea zingiberensis C. H. Wright (D. zingiberensis), Dioscoreaceae, is used extensively in traditional Chinese medicines. The aim of the current review paper is to give a comprehensive overview of the traditional usage and phytochemistry of the plant. Clinical studies performed and products prepared from the plant and active principles will be mentioned. In addition a review of the taxonomy of the genus Dioscorea is given. MATERIALS AND METHODS A systematic search on literature has been performed in databases like Google Scholar, Science Direct, Scifinder, Web of Science, and in Chinese databases (China Knowledge Resource Integrated, i.e., CNKI and Wanfang) including Ph.D. and M.Sc. dissertations. These from the period 1983-2016 have been searched. RESULTS D. zingiberensis is an endemic plant in China widely distributed in some provinces, especially Hubei and Shaanxi. The rhizomes are the medicinal part in Dun-Ye-Guan-Xin-Ning tablets and are used for isolation of diosgenin. Steroidal saponins are believed to be the active principles. More than 70 compounds have been identified. Several of these have been tested in preclinical assays and clinical trials. A wide spectrum of biological effects including cardiovascular, anti-thrombosis, hyperlipidemia, neuroprotection, anti-inflammatory, and anthelmintic effect has been verified. CONCLUSIONS Because of the promising results from the investigations on the plant material of D. zingiberensis, further in depth analyses ought to be performed to evaluate its potential as either a traditional drug or a source of bioactive principle. The presently performed studies do not explain mechanism of action, pharmacokinetics (ADME properties), or toxicity. All of these topics need more elaborate investigations.

Ovarian cancer is among the deadliest gynecological cancer, primarily largely attributed to delayed clinical detection, significant metastatic abilities, coupled with reduced responsiveness to chemotherapy. These challenges have sparked interest in bioactive compounds derived from plants as potentially safer and more effective treatments. Diosgenin and dioscin, both steroidal saponins sourced mainly from Dioscorea species, have shown promise as anticancer agents with diverse mechanisms of action. Existing experimental studies assessing the anticancer potential of diosgenin and dioscin in ovarian cancer are outlined, with focus on their biological effects and underlying mechanisms. Studies conducted in vitro and in vivo indicate that diosgenin can inhibit the growth, migratory activity, and invasive capacity of ovarian cancer cells while promoting programmed cell death and cell cycle arrest by modulating essential molecular pathways, including PI3K/Akt/mTOR, PTEN, NF-κB, and Bcl-2 family proteins. Likewise, dioscin demonstrates notable anticancer effects mediated through the induction of apoptosis and autophagy, reducing metastasis, reversing multidrug resistance, and improving chemosensitivity. Advances in nanocarrier delivery systems have also enhanced the bioavailability and effectiveness of these compounds. Despite the promising experimental results, clinical validation is still lacking. Overall, diosgenin and dioscin are promising natural options for ovarian cancer treatment, highlighting the need for additional studies on their mechanisms and clinical trials to support their development as viable anticancer therapies.

No abstract available

Dioscorea species, known as “Yams”, belong to the Dioscoreaceae family. Members of the Dioscoreaceae family are widely distributed across subtropical and tropical regions. They are notable for their high content of starch, dietary fiber, and various bioactive compounds. In addition to serving as a staple food source, these tubers possess significant medicinal value in traditional medicine, particularly for treating diabetes, diarrhea, and various inflammatory diseases. This study aimed to comprehensively summarize the active components and food development potential of Dioscorea species from research over the past decade by searching commonly used databases such as PubMed, Web of Science, Scopus, and Google Scholar. This review highlights the classification of bioactive compounds in Dioscorea spp. using the NPClassifier tool. We discuss 60 representative bioactive metabolites, including terpenoids, phenylpropanoids, carbohydrates, fatty acids, alkaloids, and amino acids. Additionally, we discuss the functional food applications and regulations of Dioscorea spp., which possess antioxidant, anti-inflammatory, anti-diabetic, and anticancer properties. This review is expected to provide scientific ideas for future research related to prioritizing the optimization of extraction technologies, the execution of rigorous clinical trials to confirm therapeutic effects, and the exploration of novel applications of Dioscorea spp. bioactives to fully harness their potential in improving human health.

ABSTRACT Dioscorea oppositifolia L., also known as Cinnamon vine, has a longstanding history in traditional medicine due to its diverse bioactive compounds. However, comprehensive scientific evaluations of its phytochemical properties and therapeutic potential are still limited. This study provides an updated analysis of its nutritional composition, bioactive compounds, and pharmacological properties, emphasizing potential therapeutic applications. A comprehensive literature review was conducted using Google Scholar, Science Direct, and PubMed/MedLine, covering studies published between 2022 and 2023. Key bioactive constituents such as diosgenin and dioscorine were identified and evaluated for their biological activities, including antioxidant, anti‐inflammatory, antidiabetic, anticancer, and antimicrobial effects. The plant exhibits notable antioxidant activity by reducing oxidative stress, while its anti‐inflammatory effects are linked to cytokine inhibition. Antidiabetic properties are evidenced by blood glucose modulation and improved insulin sensitivity. Anticancer effects include apoptosis induction and suppression of cancer cell proliferation. Additionally, Dioscorea oppositifolia shows antimicrobial efficacy against various bacterial and fungal strains. Due to its broad‐spectrum bioactivities and rich phytochemical profile, Dioscorea oppositifolia emerges as a promising candidate for pharmaceutical applications. However, further research, including clinical trials and bioavailability studies, is essential to fully harness its therapeutic potential and facilitate its integration into modern medicine.

Abstract Dioscorea bulbifera (air potato), a climbing perennial of the Dioscoreaceae family, is widely distributed in tropical regions and valued in Ayurveda, Traditional Chinese Medicine, and African ethnomedicine for managing inflammatory, infectious, metabolic, and neoplastic disorders. This systematic review critically evaluates its phytochemistry, pharmacology, and toxicology. Primary metabolites contribute to its nutritional value, whereas secondary metabolites–predominantly steroidal saponins, flavonoids, and diterpenoids from bulbils and tubers–underlie its wide range of reported bioactivities. African accessions are rich in clerodane diterpenoids, while Asian ones are rich in saponins and flavonoids, underscoring the need for comparative metabolomic and chemotaxonomic studies. Preclinical studies confirm antiproliferative, antioxidant, anti-inflammatory, antimicrobial, antidiabetic, and neuroprotective effects. However, furanoid diterpenoids, particularly diosbulbin B and 8-epidiosbulbin E acetate, have been shown to induce hepatotoxicity, with additional risks of nephrotoxicity, cardiotoxicity, gastrointestinal irritation, and thyroid dysfunction. Traditional processing methods, such as boiling and roasting, as well as co-administration with protective herbs, mitigate toxicity. Despite promising activity, clinical translation remains hindered by phytochemical variability, non-standardised preparations, and the complete absence of human trials. Future research should therefore focus on developing detoxified, standardised extracts supported by pharmacokinetic studies and well-designed randomised controlled trials to establish D. bulbifera as a safe and effective phytotherapeutic agent.

The genus Dioscorea, commonly known as yam, represents a vital biological resource in India, with deep roots in traditional medicine and subsistence agriculture. This review systematically consolidates the multifaceted value of Indian Dioscorea species, exploring their journey from ethnobotanical use to modern nutraceutical and industrial applications. We begin by delineating the ethnopharmacological significance of key species such as D. deltoidea, D. bulbifera, and D. oppositifolia, which have been employed in various traditional systems for treating rheumatism, digestive disorders, and diabetes. The paper then provides a critical analysis of the phytochemical constituents, focusing on bioactive compounds like diosgenin, dioscorin, and various polyphenols, which are responsible for their observed pharmacological activities, including anti-inflammatory, antioxidant, antimicrobial, and anticancer effects. The transition of these species from traditional food sources to potential nutraceuticals is examined, highlighting their nutritional profile rich in carbohydrates, dietary fibers, and essential minerals. Furthermore, the review delves into the industrial potential of Dioscorea, particularly the pivotal role of diosgenin as a precursor for the synthesis of steroid hormones in the pharmaceutical industry. We also address the challenges of sustainable cultivation, conservation, and biotechnological interventions like tissue culture to meet industrial demand without compromising natural populations. Finally, the paper identifies future research directions, emphasizing the need for clinical trials, advanced extraction technologies, and value-added product development. This comprehensive assessment underscores the immense potential of Indian Dioscorea as a sustainable source for medicine, food, and industry, bridging traditional knowledge with contemporary scientific validation.

Yam (Dioscorea opposita Thunb.) is an important functional food in Asia. Yam starch usually has a low glycemic index. What is the structure requirement of starch to obtain a low glycemic index remains unknown. In order to understand the structure-glycemic index relationship, six yam starches from various regions with apparent structure difference were analyzed. Chinese yam starch (CYS) showed the lowest glycemic index. It presented as oval or round granules. Meanwhile, CYS showed a distinct A-type crystal structure while the others presented C-type crystal structure. The largest crystallinity, Rw, Mw/Mn, RS level, RS + SDS level, and the lowest peak viscosity, trough viscosity and C∞ values were found for CYS. These data explained the lowest glycemic index of CYS. The above results suggested that CYS was a good neutraceutical candidate and could be used in the diet of diabetes population.

Dioscorea esculenta (Dioscoreaceae) has been long used as an alternative food ingredient and traditional medicine. This panel aims to examine the use of D. esculenta as a food ingredient, traditional medicine and its bioactivity. The research method uses a literature review on various research reports, books, journals obtained online at Google Scholar by using the keywords D. esculenta, uses, and bioactivity D. esculenta. The tubers of D. esculenta are an alternative source of alternative carbohydrates and have been traded in traditional markets, but the supply is relatively small and decreasing. The nutritional content of tuber flour is protein (7.19%), fat (1.10%) dietary fiber (10.16%) inulin (7.49%), and total starch content (71.78%). Ethnomedicinally, D. esculenta tubers are used as antifatigue, anti-inflammatory, anti-stress, anti-spasmodic and immune. The bioactivity of D. esculenta is anti-inflammatory, anti-diabetic mellitus, anti-microbial, antioxidant, anti-fertility and anti-cancer. The D. esculenta tubers are very potential to be developed as an alternative food ingredient because they have a good glycemic index and are able to overcome diabetes mellitus.

ABSTRACT Dioscorea oppositifolia (Chinese yam) (DO) and Dioscorea hamiltonii (DH) are the plants of the genus Dioscorea and they are used as health food and traditional Chinese medicine. In order to development of the available DO and DH source, a comparative study of principal components and activities were carried on. DO and DH was qualitatively and quantitively profiled, and we comparatively evaluated their antioxidant (reducing power assay), anti-inflammatory (xylene-induced ear oedema test) and nonspecific immune regulating (carbon clearance test) activities. The 42 and 38 compounds were detected from DO and DH by the method UPLC-DAD-Q-TOF-MS/MS, respectively, as well as 14 compounds are quantified by HPLC and the methodology was examined. This is the first study of the composition and activities of DH, it also indicates that DO and DH consumption would be beneficial to the health. They may be useful in the production of functional food containing an efficacious dose.

Antioxidants are crucial in preventing cell and biomolecule damage caused by free radicals. These free radicals can eventually set off degenerative disorders, including inflammation. Dioscorea hispida tubers are plants that are widely used in the food sector. This study aims to establish the correlation between phytochemicals and the antioxidant and anti-inflammatory properties in extracts and derived fractions. The tubers were extracted by maceration using 96% ethanol and the liquid-liquid fractionation (n-hexane, ethyl acetate, and water) to obtain extract and fractions. Phytochemical screening and characterization were carried out on these samples. The ABTS method was used to evaluate the antioxidant, whereas the protein denaturation inhibition method was used to evaluate anti-inflammatory activity. The study shows dried plant materials and extracts contain alkaloids, flavonoids, glycosides, tannins, saponins, and triterpenoids/steroids. In fractions, triterpenoids/steroids were traced in the n-hexane fraction only; alkaloids, flavonoids, glycosides, and tannins in the ethyl acetate fraction, while alkaloids, flavonoids, glycosides, tannins, saponins in the water fraction. The IC50 values of the extract and fraction antioxidant assay are shown in the medium category, which aligns with the IC50 values of the ethyl acetate and water fraction anti-inflammatory assay. The secondary metabolites of ethanol extract and all fractions in this study are related to antioxidant activity, while anti-inflammatory activity was found only in the extract, ethyl acetate, and water- fraction.

Korean yams are abundant in bioactive compounds with significant health-promoting properties. This study evaluated the anti-inflammatory potential of ethanol and water extracts from Dioscorea polystachya and Dioscorea bulbifera in RAW 264.7 macrophage cells. Among the extracts, the 95% ethanol extract exhibited the most potent inhibition of reactive oxygen species (ROS) and nitric oxide (NO) production, warranting further exploration of its mechanisms of action. Further analysis revealed that the ethanol extract modulated key inflammatory signaling pathways, including MAPK and NF-κB, contributing to its anti-inflammatory activity. Additionally, mucilage polysaccharides, a key bioactive component of Korean yams, were extracted and characterized for their structural and functional properties. These polysaccharides demonstrated immune-enhancing effects by reducing ROS and NO production while increasing phagocytic activity in the RAW 264.7 cells. Their prebiotic potential was also assessed through microbial growth assays, which showed an enhanced proliferation of beneficial bacteria such as Lactobacillus and Bifidobacterium. Furthermore, the adhesion assays using Caco-2 intestinal epithelial cells revealed that these polysaccharides promoted probiotic adhesion while inhibiting the adhesion of pathogenic bacteria. These findings highlight the bioactive potential of ethanol extracts and mucilage polysaccharides from Korean yams, emphasizing their promising applications as anti-inflammatory, immune-modulating, and prebiotic agents for functional food and nutraceutical development.

Background Dioscorea bulbifera L. (Dioscoreaceae) has been traditionally used in Thai folk medicine as a diuretic and anthelmintic, for longevity preparations, and for wound and inflammation treatment. This plant is also commonly used in traditional Indian and Chinese medicines in the treatment of sore throat, gastric cancer, rectal carcinoma and goiters. However, the wound healing effects of the active compounds in this plant have not been investigated. Objective This study aimed to identify compounds responsible for the wound healing activity of D. bulbifera and determine their potential anti-inflammatory and antioxidant activities. Methods Crude extracts of D. bulbifera bulbils, their derived fractions and eleven purified compounds were tested for anti-inflammatory activity against LPS-induced NO production in RAW264.7 macrophages. The wound healing effects were evaluated via cell proliferation and migration assays using human dermal fibroblasts (HDFs), and the antioxidant effects were determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radical (•OH) scavenging activity assays. Results 15,16-Epoxy-6α-O-acetyl-8β-hydroxy-19-nor-clero-13(16),14-diene-17,12;18,2-diolide (2), (+)-catechin (5), quercetin (6) and myricetin (11) exhibited significantly potent wound healing effects and promoted marked cell proliferation, resulting in % viabilities of 107.4–137.6, 121.1–151.9, 98.0–131.9, 90.9–115.9, respectively. Among them, (+)-catechin produced the highest % cell migration, resulting in 100.0% wound closure sooner (at day 2) than the other compounds. In addition, 1 μg/ml (+)-catechin significantly increased fibroblast migration by 2.4-fold compared to that in the control after 24 h. Regarding anti-inflammatory properties, kaempferol (7) and quercetin (6) decreased (p < 0.005) NO production, with IC50 values of 46.6 and 56.2 μM, respectively. In addition, the crude extracts, solvent fractions and flavonoid compounds were also found to possess marked antioxidant activity in both DPPH and •OH radical scavenging assays. Conclusions These findings provide more evidence to support the traditional use of D. bulbifera for the treatment of wounds and inflammation.