穿山龙的化学成分

Dioscorea nipponica Makino is a perennial twining herbs belonging to the family Dioscoreaceae, which is mainly distributed in the northeastern, northern, eastern and central regions of China. Traditionally, the rhizome of this herb has been commonly used by Miao and Meng ethnic groups of China to treat rheumatoid arthritis, pain in the legs and lumbar area, Kashin Beck disease, bruises, sprains, chronic bronchitis, cough and asthma. Modern pharmacological studies have discovered that this herb possesses anti-tumor, anti-inflammatory, anti-diuretic, analgesic, anti-tussive, panting-calming and phlegm-dispelling activities, along with enhancing immune function and improving cardiovascular health. In recent years, both fat-soluble and water-soluble steroidal saponins were isolated from the rhizomes of D. nipponica using silica gel column chromatography, thin layer chromatography and high performance liquid chromatography methods. Saponin and sapogenins are mainly responsible for most of the pharmacological effects of this plant. Further, the chemical components of the aboveground parts contain more than 10 kinds of phenanthrene derivatives. The present review summarizes the knowledge concerning the geographical distribution, chemical composition, pharmacological effects, toxicology studies and clinical applications of D. nipponica.

Ethnopharmacological relevance: Dioscorea nipponica Makino is a traditional medicinal plant widely used in East Asia for the treatment of rheumatic disorders, inflammatory diseases, and cardiovascular conditions. Its rhizome has long been applied in clinical practice for relieving pain, promoting blood circulation, and reducing swelling. Aim of the study: This narrative review aims to provide a comprehensive and critical overview of the phytochemical constituents, pharmacological activities, and underlying mechanisms of D. nipponica and to identify current research gaps and future perspectives. Materials and methods: The literature was searched in PubMed, Web of Science, ScienceDirect, CNKI and Wanfang Data from database inception to December 2025. The combined retrieval keywords were set as: (Dioscorea nipponica Makino OR Chuanshanlong) AND (chemical constituents OR steroidal saponins OR flavonoids OR phenols) AND (biological activity OR anti-inflammatory OR cardioprotective OR hepatotoxicity OR clinical application). Both English and Chinese publications were retrieved, and studies written in other languages were excluded. Results: Phytochemical studies have identified diverse secondary metabolites, particularly steroidal saponins, along with diarylheptanoids and phenanthrenes. These compounds exhibit multiple pharmacological activities, including anti-inflammatory, anti-tumor, immunomodulatory, and cardioprotective effects. Mechanistic studies indicate that these activities are mediated through the modulation of key signaling pathways such as NF-κB, PI3K/Akt, AMPK, and the NLRP3 inflammasome. However, current research remains fragmented, with limited integration of chemical composition, molecular targets, and therapeutic outcomes. Conclusions: D. nipponica represents a promising source of bioactive natural products, with steroidal saponins as the major contributors to its pharmacological effects. Future studies should focus on multi-component interactions, pharmacokinetics, quality control, and clinical validation to support its rational development and sustainable utilization.

… Dioscorea nipponica (Dioscoreaceae) have been used as traditional medicines for diabetes… isolate the bioactive components from the rhizomes of Dioscorea nipponica and to evaluate …

This study reported the isolation and identification of bioactive compounds from Dioscorea nipponica Makino, a plant used in traditional medicine for various ailments. Nine compounds were isolated, including a new compound named as diosniposide E, which was elucidated by analyzing its ^1H-NMR, ^13C-NMR, DEPT, COSY, HMBC and MS data and comparing them with data available in literature. The other eight compounds were identified as known compounds. Theoretical calculations of energy and the generation of a molecular electrostatic potential surface map were employed to assess the antioxidant capacity of nine compounds, the calculation results exhibited that compounds 5 and 6 had strong antioxidant capacities. To further evaluate the antioxidant activities of the investigated compounds, the DPPH and ABTS assays were conducted. The results from the DPPH scavenging activity test revealed that compounds 4 – 6 exhibited enhanced scavenging activities compared to L-ascorbic acid, while displaying similar efficacy to trolox. Moreover, the ABTS scavenging activities of compounds 4 – 6 were found to surpass those of L-ascorbic acid and trolox. In terms of α-glucosidase inhibition, compounds 3 and 4 displayed remarkable inhibitory activities that surpassed the effects of acarbose. Additionally, compound 2 exhibited potent anticholinesterase activities, outperforming donepezil. This research provides insights into the potential bioactive compounds present in Dioscorea nipponica Makino and may contribute to its use in traditional medicine.

… Recently, we reported bioactive constituents from Dioscorea … search for bioactive components from Dioscoreaceae medicinal … Therefore, we suggest that compounds 8 and 11 isolated …

Objectives This study aimed to screen potential antitumor compounds from Dioscorea nipponica Makino subsp. rosthornii, validate them in cellular models, and investigate their mechanisms underlying the inhibition of proliferation in A549 cells. Methods The chemical constituents in 12 batches of D. nipponica Makino subsp. rosthornii were identified using ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). The antitumor activity of these samples was assessed in A549 cells through cell proliferation, wound healing, migration, and invasion assays. A multivariate regression spectrum-effect relationship model was developed, treating the peak areas of common chromatographic peaks as independent variables and the antitumor activity as the dependent variable. Potential antitumor components were identified based on this spectrum-effect correlation and subsequently validated. The protein expression levels of N-cadherin, MMP2, and E-cadherin in A549 cells were measured to investigate the underlying mechanisms. Results A comprehensive chemical analysis was conducted on 12 batches of D. nipponica Makino subsp. rosthornii from varied geographical origins using UPLC-QTOF-MS, resulting in the identification of 23 distinct chemical constituents. The extract derived from D. nipponica Makino subsp. rosthornii notably inhibited the proliferation, migration, and invasion of A549 cells. Spectrum-effect relationship analysis pinpointed three potential antitumor compounds: protodioscin, diosgenin, and gracillin. Further mechanistic investigations demonstrated that these saponins inhibit the malignant phenotype of A549 cells through a dual regulatory mechanism. Specifically, they markedly reduced the expression of pro-metastatic proteins N-cadherin and MMP2, while simultaneously enhancing the expression of E-cadherin. Conclusion This study elucidated the key active constituents responsible for the antitumor effects of D. nipponica Makino subsp. rosthornii, thereby providing scientific evidence to support its potential application in cancer therapy.

Nine glycosides of spirostan (1–7) and furostan (8 and 9) type steroids including a new compound, 7-oxodioscin (1), were isolated from the rhizomes of Dioscorea nipponica. The structure of 1 was established as (25R)-3β-O-[(α-L-rhamnopyranosyl-(1→4)-O-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranosyl)oxy]spirost-5-en-7-one by extensive spectroscopic techniques including HRESI-TOFMS, 1D and 2D NMR, and chemical methods. Known compounds were elucidated as dioseptemloside G (2), (25R)-dracaenoside G (3), orbiculatoside B (4), dioscin (5), progenin III (6), gracillin (7), (3β,22α,25R)–26-(β-D-glucopyranosyloxy)-22-methoxyfurost-5-en-3-yl O-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside (8), and methylprotodioscin (9).

… Based on the comparative results described above, for the intraspecies difference in chemical composition it was shown in our study that the major composition of either DN or DP …

The rhizome of Dioscorea nipponica Makino (RDN) is a widely used herbal medicine, which has significant anti-inflammatory activities on various inflammatory diseases. However, the bioactive compositions responsible for the anti-inflammatory activity of RDN are still unknown. This study aimed to identify the anti-inflammatory bioactive compounds in RDN using high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (HPLC-Q/TOF-MS), quantitative analysis of multiple components by single marker (QAMS) and chemometric methods. Firstly, an HPLC-Q/TOF-MS method was employed for identification of bioactive steroidal saponins in RND, and a total of twelve steroid saponins were identified. Then, QAMS method was employed to determine the contents of seven bioactive steroidal saponins, including protodioscin, protogracillin, methyl protodioscin, pseudoprotodioscin, pseudoprogracillin, dioscin and gracillin in RND samples using dioscin as the reference analyte. The anti-inflammatory effects of RDN samples were then evaluated by inhibition of NO production in LPS-induced RAW264.7 cells. Furthermore, chemometric methods, including Pearson correlation analysis and partial least squares regression (PLSR) were employed to investigate the correlations between chemical components and anti-inflammatory activities, and explore the potential anti-inflammatory bioactive compounds of RDN. The results indicated that protodioscin, dioscin and gracillin were selected as the major anti-inflammatory compounds in RND. The further verification experiments showed that protodioscin, dioscin and gracillin exhibited great inhibition on NO production with IC50 values (the half maximal inhibitory concentration) of 0.712 μM, 0.469 μM and 0.815 μM, respectively. They also significantly reduced the levels of TNF-α, IL-1β, and IL-6 in LPS-induced RAW264.7 cells. The present study provided evidences for the anti-inflammatory activity of RND and identification of the anti-inflammatory components in RDN.

To prevent confusing Dioscorea nipponica (DN), an Oriental medicine, with Dioscorea quinquelobata (DQ) and Dioscorea septemloba (DS), a simple and accurate quantitative analysis method using HPLC combined with ultraviolet (UV) detection was developed and verified with UPLC-QTOF/MS through identification of five saponin glycosides: protodioscin (1), protogracillin (2), pseudoprotodioscin (3), dioscin (4), and gracillin (5). The newly developed analysis method showed sufficient reproducibility (<1.91%) and accuracy (92.1%–102.6%) and was able to identify DN based on the presence of compound 3 (13.821 ± 0.037 mg/mL) and the absence of 5. Compound 1, which is present in DN at a relatively high level (159.983 ± 0.064 mg/mL), was also an important marker for identification. Among the three species, DN showed the strongest activation of apoptotic signaling in osteosarcoma cells, while the four compounds detected in DN showed IC50 values of 6.43 (1), 10.61 (2), 10.48 (3), and 6.90 (4). In conclusion, the strong inhibitory effect of DN against osteosarcoma was confirmed to be associated with 1 and 4, which is also related to the quantitative results. Therefore, the results of this study might provide important information for quality control related to Oriental medicine.

… Currently, a lot of attention is focused on the active components deriving from natural … complex chemical composition of herbal extracts, the absence of well-identified active compounds …

… Dioscorea nipponica Makino showed the strongest inhibitory eŠect against pancreatic lipase. Dioscorea nipponica … In the present study, the active component from the herb was puriˆed, …

Activation of microglial cells by intrinsic or extrinsic insult causes neuroinflammation, a common phenomenon in neurodegenerative diseases. Prevention of neuroinflammation may ameliorate many neurodegenerative disease progressions. Dioscorea nipponica Makino (DN) extract can alleviate muscular atrophy and inflammatory diseases; however, the efficacy and mechanism of action in microglial cells remain unknown. The current study investigates the possible anti-inflammatory effects and mechanisms of Dioscorea nipponica Makino ethanol extract and its steroidal saponin dioscin. Our in vitro study shows that Dioscorea nipponica rhizome ethanol extract (DNRE) and dioscin protect against lipopolysaccharide (LPS)-activated inflammatory responses in BV-2 microglial cells by inhibiting phosphorylation and the nuclear translocation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), resulting in the downregulation of pro-inflammatory cytokines and enzymes. Consistent with our previous report of dioscin-mediated enhancement of neurotrophic factors in dopaminergic cells, here we found that dioscin upregulates brain-derived neurotrophic factor (BDNF) and cAMP-response element binding protein (CREB) phosphorylation (pCREB) in the cerebral cortex and hippocampus regions of the mouse brain. Scopolamine treatment increased pro-inflammatory enzyme levels and reduced the expression of BDNF and pCREB in the hippocampus and cortex regions, which led to impaired learning and referencing memory in mice. Pre-treatment of dioscin for 7 days substantially enhanced mice performances in maze studies, indicating amelioration in cognitive deficits. In conclusion, DNRE and its active compound dioscin protect against neurotoxicity most likely by suppressing NF-κB phosphorylation and upregulating neurotrophic factor BDNF.

… of Dioscorea nipponica is the major part of medicine, and the identified active components … Saponin of Dioscorea nipponica possesses various pharmacological activities. Among them…

… Because DG has a similar chemical structure to ruscogenin, the active chemical moiety of spicatoside A, we hypothesized that DG might also have neurotrophic activity. …

… These secondary metabolites consist of various chemical compounds called … nipponica, is a kind of steroidal saponin, which is isolated as antifungal constituents from medicinal plants. …

… Studies of the detailed mechanism of these extracts as well as identification of the active components are warranted for the development of an anti-DPN drug from DJ and DN. …

INTRODUCTION Dioscorea species, which contain abundant steroidal saponins, have been used as folk medicines or raw materials to synthesise steroid drugs. OBJECTIVE To establish a rapid chemotaxonomic method that will comprehensively resolve confusions about genetic relationships of genus Dioscorea. METHODS A comprehensive strategy using ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UHPLC-QTOF-MS/MS) was firstly proposed to evaluate the chemotaxonomy of 12 species (27 taxa) from China by hierarchical cluster analysis (HCA) based on the variations of the identified metabolites. RESULTS Twenty-eight secondary metabolites (mainly steroidal saponins) were identified. The MSn fragmentation patterns of DA (a new acetylated steroidal saponin at C-7 position) were firstly reported. Moreover, eight major steroidal saponins were further quantified simultaneously by UPLC-QTOF-MS method. According to HCA results, D. bulbifera L. was distinguished with species of sect. Stenophora Uline for pennogenin-type steroidal saponins. Dioscorea zingiberensis exhibited far distance from other members of sect. Stenophora Uline for two unique saponins. Dioscorea banzhuana may be reclassified into sect. Stenophora. Dioscorea nipponica subsp. rosthornii and D. collettii var. hypoglauca might be separated from their original subspecies/varieties as new species, respectively. CONCLUSION The chemotaxonomic method was successfully applied in the study of genetic relationships of Dioscorea species. This study not only enhanced the understanding of chemical constituents, but also laid basic theoretical foundations for the rational utilisation and chemotaxonomy of genus Dioscorea.

The Dioscoreaceae, a family of monocotyledonous flowering plants comprising about 650 species across four genera, is prevalent in tropical regions and plays a vital role in diets across the Global South. Its edible tubers, known as yams, are both nutritional staples and widely used in traditional medicine. This review of 121 studies synthesizes knowledge on the traditional uses, biological activities, phytochemistry, nutritional value, and technological applications of Dioscoreaceae species. The most used species, Dioscorea alata and D. bulbifera, are employed across Asia, Africa, and South America to treat gastrointestinal disorders, diabetes, rheumatism, and infections. In Africa, species such as D. dregeana and D. smilacifolia are primarily used for inflammatory and respiratory conditions, while in Asia, particularly China and India, D. cirrhosa, D. japonica, and D. polystachya are associated with digestive, metabolic, and endocrine disorders. Phytochemical studies consistently identify steroidal saponins, pregnane glycosides, and phenanthrene glycosides, underscoring their potential for drug discovery. These species also exhibit diverse evaluated biological activities, including anti-inflammatory, anticancer, antidiabetic effects, supporting some of their traditional uses. With a global production of 75 million tons, yam tubers are nutrient-dense, supplying carbohydrates, proteins, and essential minerals to food-insecure populations. Additionally, polysaccharides from Dioscoreaceae demonstrate technological applications, including bioplastics, hydrogels, and functional food enhancement. Overall, this synthesis highlights the Dioscoreaceae family’s nutritional, medicinal, and technological significance, bridging traditional knowledge with modern applications, and emphasizing its cultural and innovative potential.

Dioscorea, consisting of over 600 species, is the most important genus in the Dioscoreaceae family; however, the practically used plants, which are commonly called yam, are restricted to a remarkably smaller number of species. Numerous studies have reported the high nutritional value of yam, particularly as an alternative source of starch and some important micronutrients. Several Dioscorea species are widely used for various medicinal purposes as well. In many studies, the bioactivities and health benefits of Dioscorea extracts and other preparations have been related to the presence of phytochemicals, which possess antioxidant properties; they are related mainly to radical-scavenging capacity in chemical assays and positive effects on the endogenous antioxidant system in cell-based and in vivo assays. Considering the increasing number of publications on this topic and the absence of comprehensive and focused review papers on antioxidant potential, this article summarizes the results of studies on the antioxidant properties of Dioscorea spp. and their relation to phytochemicals and health benefits. A comprehensive survey of the published articles has revealed that the majority of studies have been performed with plant tubers (rhizomes, roots), while reports on leaves are rather scarce. In general, leaf extracts demonstrated stronger antioxidant potential than tuber preparations. This may be related to the differences in phytochemical composition: saponins, phenanthrenes and, for some pigment-rich species (purple yams), anthocyanins are important constituents in tubers, while phenolic acids and flavonoids are characteristic phytochemicals in the leaves. The review may assist in explaining ethnopharmacological knowledge on the health benefits of Dioscorea plants and their preparations; moreover, it may foster further studies of poorly investigated species, as well as their wider application in developing new functional foods and nutraceuticals.

The dried rhizome of Dioscorea nipponica Makino ("Chuanshanlong" in Chinese) is a medicinal herb with multiple major producing areas. The main objective of this study was the comparative profiling of Dioscoreae Nipponicae Rhizoma (DNR) from various geographical origins. A hypoxia/reoxygenation-induced H9c2 cell injury model was established, and the antimyocardial ischemia activity of DNR samples from different origins was detected using the cell counting kit-8 (CCK-8) method. The result showed that the antimyocardial ischemia potential of DNR samples from the Heilongjiang province was higher than that of the other studied samples. Subsequently, a plant metabolomics technique utilizing ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q TOF-MS) was used to determine the differences in DNR samples from various geographical origins. Forty compounds, including steroidal saponins, free fatty acids, and organic acids, were tentatively identified based on UPLC-Q TOF-MS fragmentation pathways and via comparison with available reference standards. Partial least squares discriminant analysis was performed to estimate the differences in DNR samples from different origins. Five compounds were significantly up-regulated and correlated with antimyocardial ischemia in DNR samples from Heilongjiang province. Molecular docking was used to discern the interactions of key markers with the active sites of the target protein. The findings signified that UPLC-Q TOF-MS metabolomics coupled with molecular docking is a powerful tool to rapidly identify the quality control characteristics of DNR samples and their products. The research provides a direction for the rational utilization of DNR.

… The most common sugars encountered in saponins are pentoses (arabinose, xylose, … Steroidal saponins are widely spread throughout the plant kingdom, such as Dioscorea nipponica …

… activities of Dioscorea steroid saponins from the liter… steroid saponins of furostane-, spirostane-, and pregnane-type skeleton have been discovered and characterized from 13 Dioscorea …

Dioscin, a steroidal saponin isolated from Dioscorea nipponica Makino, has previously been shown to possess antiarthritic effects. However, the underlying mechanism is still elusive. Herein, we investigated the therapeutic effects of dioscin on collagen-induced arthritis (CIA) in DBA/1 mice and related mechanism. Cytokine production in CII-specific immune responses were measured by enzyme-linked immunosorbent assay (ELISA); Th17 cell-related gene expression, including IL-17A, ROR γτ and IL-23p19, were detected by qPCR analysis; Surface marker, T regulatory (Treg) cells and intracellular cytokines (IL-17A and IFN- γ ) were evaluated by flow cytometry. We performed Th17 cell differentiation assay in vitro. Results showed that, in vivo, dioscin treatment significantly reduced the severity of CIA, which was accompanied by decreased Th17 response, but not Th1 and Treg response; dioscin-treated mice also showed lower percentage of CD11b + Gr-1 + neutrophils; In vitro, dioscin treatment suppressed the differentiation of naive CD4 + T cells into Th17 cell and decreased IL-17A production. Collectively, our results indicate that dioscin exerts antiarthritic effects by inhibiting Th17 cell immune response.

In the present study, a simple and environmentally friendly extraction method based on natural deep eutectic solvents (NADESs) was established to extract four bioactive steroidal saponins from Dioscoreae Nipponicae Rhizoma (DNR). A total of twenty-one types of choline chloride, betaine, and L-proline based NADESs were tailored, and the NADES composed of 1:1 molar ratio of choline chloride and malonic acid showed the best extraction efficiency for the four steroidal saponins compared with other NADESs. Then, the extraction parameters for extraction of steroidal saponins by selected tailor-made NADES were optimized using response surface methodology and the optimal extraction conditions are extraction time, 23.5 min; liquid–solid ratio, 57.5 mL/g; and water content, 54%. The microstructure of the DNR powder before and after ultrasonic extraction by conventional solvents (water and methanol) and the selected NADES were observed using field emission scanning electron microscope. In addition, the four steroidal saponins were recovered from NADESs by D101 macroporous resin with a satisfactory recovery yield between 67.27% and 79.90%. The present research demonstrates that NADESs are a suitable green media for the extraction of the bioactive steroidal saponins from DNR, and have a great potential as possible alternatives to organic solvents for efficiently extracting bioactive compounds from natural products.

… nipponica [3–7]. As a continuing work to search for diversified steroidal saponins from natural … nipponica led to the isolation of two new steroidal saponins, along with nine known …

… Dioscorea nipponica Makino exhibits many biological activities, … total saponins extraction from Dioscorea nipponica Makino. In this study, the optimal extraction process of total saponins …

Objective: Dioscorea nipponica Makino is one of the most common used traditional Chinese drugs which are used to treat gouty arthritis (GA). Nuclear factor-κB (NF-κB) pathway plays an important role during this process. In the present study, we investigated the effects of total saponins from D. nipponica Makino (TDN) on NF-κB pathway in interleukin-1β (IL-1β) induced fibroblast-like synoviocytes (FLS). Materials and Methods: FLS were divided into three groups: Normal group, model group, which was given 10 μg/L IL-1β to induce the proliferation, and TDN group (10 μg/L IL-1β +100 μg/L TDN). 1 h, 24 h, 48 h, and 72 h after treating, immune fluorescence method was used to detect the cell location of NF-κB p65. Electrophoretic mobility shift assay was used to detect the activation of NF-κB p65. Western blot method was used to detect the protein expressions of NF-κB p65, IκBα, and p-IκBα. Results: TDN could inhibit the activation and transfer of NF-κB p65. As time went on, the expression of NF-κB p65 in the cytoplasm was decreased while it was increased in the nucleus. The expression of p-IκBα was increased, whereas the expression of IκBα was not changed. TDN could regulate these abnormal expressions. Conclusion: TDN may treat GA by regulating NF-κB signal pathway. SUMMARY TDN could inhibit the transfer of NF-κB p65. TDN could inhibit the activation of NF-κB p65. TDN could inhibit the expression of p-IκBα Abbreviations used: TDN: Total saponins from Dioscorea nipponica Makino, GA: Gouty arthritis, FLS: Fibroblast-like synoviocytes, IL-1β: Interleukin-1 beta, IF: Immune fluorescence, EMSA: Electrophoretic mobility shift assay, WB: Western blot.

Asthma is a heterogeneous disease characterized by symptoms of chronic inflammation and airway structural and functional changes. It affects about 300 million people worldwide and causes 250 000 deaths annually, but its symptoms can be greatly relieved by regular use of inhaled glucocorticoids (GCs). GCs exert their function through interacting with glucocorticoid receptors (GRs). Diosgenin is a naturally occurring steroidal saponin abundantly present in many medicinal plants, including Dioscorea nipponica, which shares a similar steroidal structure with GC. In this study, ovalbumin (OVA)-induced asthmatic mice and primary tracheal epithelial cells (TECs) were used as research models. ELISAs were applied to measure the secretion of TNF-α, IL-1β, and IL-6, while quantitative PCR and western blotting were applied to evaluate expression of GRs SLPI, TTP, GILZ, MKP-1, and NF-κB. Our data demonstrated that diosgenin suppressed the secretion of TNF-α, IL-1β, and IL-6 by enhancing the expression of GRs, SLPI, GILZ, and MKP-1, and inhibiting the expression of HSP70. These data provide some evidence on the molecular mechanism of diosgenin, which might facilitate its clinical applications.

Studying the biotransformation of natural products by intestinal microflora is an important approach to understanding how and why some medicines—particularly natural medicines—work. In many cases, the active components are generated by metabolic activation. This is critical for drug research and development. As a means to explore the therapeutic mechanism of Dioscorea nipponica (DN), a medicinal plant used to treat myocardial ischemia (MI), metabolites generated by intestinal microflora from DN were identified, and the cardioprotective efficacy of these metabolites was evaluated. Our results demonstrate that diosgenin is the main metabolite produced by rat intestinal microflora from DN. Further, our results show that diosgenin protects the myocardium against ischemic insult through increasing enzymatic and nonenzymatic antioxidant levels in vivo and by decreasing oxidative stress damage. These mechanisms explain the clinical efficacy of DN as an anti-MI drug.

Dioscorea nipponica is an important medicinal and edible plant in northern China, and its extract dioscin is an important raw material for the modern pharmaceutical industry. To investigate the key environmental factors influencing diosgenin accumulation in the rhizomes of D. nipponica and their action mechanism, we collected wild D. nipponica plants from 60 plots on Zhongtiao Mountain and analyzed the effects of environmental conditions on both plant growth and diosgenin synthesis. Additionally, physiological parameters of D. nipponica were investigated under different intervals of watering treatments: control (CK, 3 days), mild drought (MID, 5 days), moderate drought (MD, 8 days) and severe drought (SD, 10 days). The results showed that the water content of rhizome was the main factor affecting the diosgenin content, and soil nutrients, especially nitrogen, played an important role in the growth of D. nipponica. The results of a drought stress gradient test showed that diosgenin increased significantly under mild drought compared to the control, reaching 103.19 ± 2.63%. SD inhibited the growth of plants, and the indexes decreased by 10.08 ± 0.03–34.94 ± 5.60% compared with MID but increased the proliferation rate of rhizomes (83.33%), which is the reproductive strategy of D. nipponica when faced with drought stress. It provides a scientific basis for imitation of wild cultivation of D. nipponica.

… and their contributions to plant growth and diosgenin production is limited. The present … potential of diosgenin biotransformation by endophytes isolates associated with D. nipponica for …

… nipponica) was usually subjected to the multiple processes such as extraction, hydrolysis, … In this study, a novel method for rapid production and recovery of diosgenin from D. nipponica …

… Extraction of diosgenin from the rhizome of Dioscorea by … and extract diosgenin from Dioscorea nipponica Makino (DNM). … application value for the extraction of diosgenin from plants. …

… diosgenin from Dioscorea nipponica Makino (DNM). The effects of extraction temperature (75–175 C) and time (15–45 min) on the diosgenin … Results showed that diosgenin extraction …

… extraction (SFE) was used to extract diosgenin following acid hydrolysis from Dioscorea nipponica tuber. … The tuber of Dioscorea nipponica is extensively used in China for extraction of …

Dioscorea nipponica rhizoma (DNR) is commonly used for the cure of hyperthyroidism resulting from Graves’ disease (GD) or thyroid nodules. However, its therapeutic mechanism remains unclear. This study aimed to utilize network pharmacology integrated molecular docking and experimental verification to reveal the potential pharmacological mechanism of DNR against GD. First, the active componds of DNR were collected from the HERB database and a literature search was conducted. Then, according to multisource database, the predicted genes of DNR and GD were collected to generate networks. The analysis of protein–protein interaction and GO enrichment and KEGG pathway were employed to discover main mechanisms associated with therapeutic targets. Moreover, molecular docking simulation was applied in order to verify the interactions between the drug and target. Finally, our experiments validated the ameliorated effects of diosgenin, the main component of DNR, in terms of phosphorylation deactivation in IGF-1R, which in turn inhibited the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and GD remission. Our present study provided a foundation for further investigation of the in-depth mechanisms of diosgenin in GD and will provide new scientific evidence for clinical application.

Phytochemicals found in foods and spices are progressively gaining popularity over conventional synthetic drugs mainly because they act via multiple molecular targets that synergize to efficiently prevent or treat chronic illnesses. Phytochemicals are also safe (with minimal or no toxic or side effects) with better bioavailability. Food saponins have been used in complimentary and traditional medicine against a variety of diseases including several cancers. Diosgenin, a naturally-occurring steroid saponin is found abundantly in legumes (Trigonella sp.) and yams (Dioscorea sp.). Diosgenin is a precursor of various synthetic steroidal drugs that are extensively used in the pharmaceutical industry. Over the past two decades, a series of pre-clinical and mechanistic studies have been independently conducted to understand the beneficial role of diosgenin against metabolic diseases (hypercholesterolemia, dyslipidemia, diabetes and obesity), inflammation and cancer. In experimental models of obesity, diosgenin decreases plasma and hepatic triglycerides and improves glucose homeostasis plausibly by promoting adipocyte differentiation and inhibiting inflammation in adipose tissues. A limited number of experiments have been conducted to understand the preclinical efficacy of diosgenin as a chemopreventive/therapeutic agent against cancers of several organ sites. Mechanistic studies using in vitro models suggest that diosgenin suppresses cancer cell growth through multiple cell signaling events associated with proliferation, differentiation, apoptosis, inflammation and oncogenesis. This chapter provides a comprehensive review of the biological activity of diosgenin that contributes to several diseases in its role as a health beneficial phytochemical by citing new studies. In addition, diosgenin’s safety with regards to its potential toxicity is also critically discussed. Altogether, the findings from pre-clinical and mechanistic studies strongly implicate the use of diosgenin as a novel multi-target based chemopreventive or therapeutic agent against several chronic diseases.

… The goal of this study was to evaluate whether memory enhancement effect of Dioscorea species depends on the diosgenin content in the extracts. To clarify this issue, we compared …

… Dioscorea nipponica Makino, as well as on the formation and localization of phenolic compounds … The object of the study was intact plants Dioscorea nipponica Makino and microclones …

… compounds. Such interactions may lead to discrepancies in the accurate measurement of phenolic … when assessing phenolic levels in Dioscorea spp. and similar botanical extracts. …

… Twenty-three phenolic compounds were isolated from Dioscorea opposita by bioactivity-guided method and their inhibitory effect against pancreatic lipase was evaluated. A total of 15 …

Dioscorea spp. belongs to the Dioscoreaceae family, known as “yams”, and contains approximately 600 species with a wide distribution. It is a major food source for millions of people in tropical and subtropical regions. Dioscorea has great medicinal and therapeutic capabilities and is a potential source of bioactive substances for the prevention and treatment of many diseases. In recent years, increasing attention has been paid to the phytochemicals of Dioscorea, such as steroidal saponins, polyphenols, allantoin, and, in particular, polysaccharides and diosgenin. These bioactive compounds possess anti-inflammatory activity and are protective against a variety of inflammatory diseases, such as enteritis, arthritis, dermatitis, acute pancreatitis, and neuroinflammation. In addition, they play an important role in the prevention and treatment of metabolic diseases, including obesity, dyslipidemia, diabetes, and non-alcoholic fatty liver disease. Their mechanisms of action are related to the modulation of a number of key signaling pathways and molecular targets. This review mainly summarizes recent studies on the bioactive compounds of Dioscorea and its treatment of inflammatory and metabolic diseases, and highlights the underlying molecular mechanisms. In conclusion, Dioscorea is a promising source of bioactive components and has the potential to develop novel natural bioactive compounds for the prevention and treatment of inflammatory and metabolic diseases.

Dioscoreae nipponica Makino (D. nipponica) as the rhizome of dioscoreaceae rich in steroidal saponins, have been reported to have the hypolipidemic effects etc. However, it is still unclear which exact active components are primary responsible for the beneficial effects. This study was conducted to fish out the lipase inhibitors from D. nipponica, and evaluate the inhibitory activity on porcine pancreatic lipase (PPL) through in vitro kinetic assay using p-nitrophenyl palmitate as substrate. Accordingly, the ethanolic extract was subjected to D101 macroporous resin purification for spectrophotometric screening, high performance liquid chromatography (HPLC) separation and structural characterization by ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. Through orlistat validation, the PPL inhibitory activity and IC50 value of the extract were respectively 68.34 ± 1.47 % and 107.05 μg/mL under the optimized inhibition conditions. From 6 steroidal saponins identified, the inhibitory components named the protodioscin, protogracillin, dioscin and gracillin were fished out by grouping separation and HPLC analysis. Furthermore, dioscin and gracillin with the parent structure of diogenin were confirmed as the major inhibitors by virtue of stability tests based on transformation of protodioscin and protogracillin. Finally, the inhibitory mechanism of the major inhibitors toward PPL was further clarified by kinetic analysis and molecular docking analysis. The proposed method not only revealed the PPL inhibitory components in D. nipponica, but also provided an effective approach to hierarchical screening of PPL inhibitors from natural plants.

… Dioscorea nipponica Makino is well known as a traditional edible plant in oriental countries. To date, no investigation has been carried out on polysaccharides that may account for the …

Abstract The tubers of Dioscorea persimilis have been widely consumed as a food and for the treatment of sonasthenia, intestinal disease, diarrhea, long-term dysentery, spermatorrhea, metritis, kidney failure, back pain, dizziness, and night sweats. The present study describes the isolation of 11 secondary metabolites, including three new phenanthrenes namely diospersimilosides A (1) and B (2) and diosbiphenanthrene (3), and eight known phenolic compounds: 2,4,6,7-tetrahydroxy-9,10-dihydrophenanthrene (4), aerosin (5), gastrodin (6), 2-phenylethyl-β- d -glucopyranoside (7), afzelechin (8), catechin (9), eucomic acid (10), and vanillic acid-4-O-β- d -glucopyranoside (11) from the tubers of D. persimilis. Their chemical structures were elucidated based on comprehensive analyses of the NMR and mass spectra. Evaluation of their cytotoxicity against three human cancer cell lines, including liver (HepG2), breast (MCF7), and melanoma (SK-Mel-2) revealed that the phenanthrene metabolites (3-5) possess cytotoxicity toward all the cell lines, with IC50 values ranging from 8.2–68.4 μM. Our results revealed that the free of the hydroxy groups plays an important role in cytotoxicity of the phenanthrenes and suggests that pohydroxylated dihydrophenanthrene and biphenanthrene metabolites could be considered as promising cytotoxic agents against human cancer cells.

… compounds: diosgenin-3-O-α-l-rhamnopyranosyl (1 → 2)–β-d-glucopyranoside (DBS1) content, total phenolic … GAE/g dry extract total phenolic and DPPH radical scavenging assay with …

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 Saponin derived from natural extracts can alleviate muscle atrophy. Dioscorea nipponica Makino (DNM) is commonly used in herbal medicine and contains various steroidal saponins, although its efficacy and mechanisms of action for treating muscle atrophy remain unknown. Here, differentiated myoblast cells treated with DNM showed increased MyoD and MyoG expression and effectively promoted muscle formation. DNM effectively inhibited muscle atrophy induced by tumor necrosis factor alpha (TNFα) monotherapy, and combination treatment with protodioscin and protogracillin (among the tested DNM constituents) showed a synergistic effect on differentiated myoblast cells. DNM and this combination repressed TNFα-induced increased MuRF1 and Atrogin1/MAFbx expression by inhibiting nuclear factor-kappa B (NF-κB) expression. DNM also effectively promoted the recovery of muscle formation in injured mice. Therefore, DNM and its multi-constituents can potentially be used as therapeutic agents for muscle-related diseases and represent prospective food supplements.

This study conducted the solid fermentation process of Dioscorea nipponica using endophytic fungi C39 to determine the changes in the diosgenin concentration. The results revealed that endophytic fungi C39 could effectively biotransform the saponin components in D. nipponica. Moreover, the maximum increase in the diosgenin concentration reached 62.67% in 15 days of solid fermentation. MTT assay results demonstrated that the inhibitory effects of the fermentation drugs on four types of cancer cells (liver cancer cells (HepG2), stomach cancer cells (BGC823), cervical cancer cells (HeLa), and lung cancer cells (A549)) were better than those of the crude drugs obtained from D. nipponica. The chemical composition of the samples obtained before and after the biotransformation of D. nipponica was analyzed by UPLC-Q-TOF-MS. A total of 32 compounds were identified, 21 of which have been reported in Dioscorea saponins and the ChemSpider database and 11 compounds were identified for the first time in D. nipponica. The biotransformation process was inferred based on the variation trend of saponins, which included transformation pathways pertaining to glycolytic metabolism, ring closure reaction, dehydrogenation, and carbonylation. The cumulative findings provide the basis for the rapid qualitative analysis of the saponin components of D. nipponica before and after biotransformation. The 11 metabolites obtained from biotransformation are potential active ingredients obtained from D. nipponica, which can be used to further identify pharmacodynamically active substances.

… The present study was to investigate the effects and possible mechanisms of the total saponins from Dioscorea nipponica Makino (TSDN) against CCl 4 -induced hepato-toxicity in mice. …

… possible mechanisms of the total saponins from Dioscorea nipponica Makino (TSDN) against type 2 … Protection of the flavonoid fraction from Rosa laevigata Michx fruit against carbon …

… of four furostanol glycosides … saponins showed rapid excretion and relative high plasma concentrations when the validated method was applied to the PK study of Dioscorea nipponica …

… In conclusion, the structures of two new furostanol saponins (1–2), along with ten known compounds (3–12) isolated from the rhizomes of D. japonica were identified. While steroidal …

Steroidal saponins are an important type of plant-specific metabolite that are essential for plants’ responses to biotic and abiotic stresses. Because of their extensive pharmacological activities, steroidal saponins are also important industrial raw materials for the production of steroidal drugs. In recent years, more and more studies have explored the biosynthesis of steroidal saponins in plants, but most of them only focused on the biosynthesis of their molecular skeleton, diosgenin, and their subsequent glycosylation modification mechanism needs to be further studied. In addition, the biosynthetic regulation mechanism of steroidal saponins, their distribution pattern, and their molecular evolution in plants remain unclear. In this review, we summarized and discussed recent studies on the biosynthesis, molecular regulation, and function of steroidal saponins. Finally, we also reviewed the distribution and molecular evolution of steroidal saponins in plants. The elucidation of the biosynthesis, regulation, and molecular evolutionary mechanisms of steroidal saponins is crucial to provide new insights and references for studying their distribution, diversity, and evolutionary history in plants. Furthermore, a deeper understanding of steroidal saponin biosynthesis will contribute to their industrial production and pharmacological applications.

… new furostanol saponins from the Dioscorea panthaica were isolated. ► The structures of the new saponins … Two saponins were found to exhibit potent activities against α-glucosidase. …

… In this study, the separation of three furostanol saponins and four spirostanol saponins were successfully accomplished by HSCCC-ELSD utilising an nhexane:n-butanol:water system [3…

Fusarium sp. C39 is an endophytic fungus of Dioscorea nipponica Makino. Symbiosis of Fusarium sp. C39 with Rhizoma Dioscoreae Nipponicae (RDN) can significantly increase the content of saponin, which provides a new approach for saponin production and reduces the pressure on natural sources of saponins. However, the underlying mechanism is not clear, limiting its application. In this study, the genome of Fusarium sp. C39 was sequenced, the gene functions were predicted via gene annotation, and the genome was compared to the genomes of four related species. Fusarium sp. C39 is predicted to encode many key enzyme genes involved in saponin synthesis, which could transform the mevalonate, isopentenyl pyrophosphate, and various intermediate compounds present in the RDN extract into saponins. The Fusarium sp. C39 genome contains specific genes that are conducive to its endophytic lifestyle and can provide abundant raw materials for saponin synthesis. Based on the genomic analysis, we proposed the mechanism by which Fusarium sp. C39 generates saponins and provides a theoretical basis for rapid, efficient, low‐cost production of saponins.

Dioscorea nipponica and the preparations made from it have been used for long to prevent and treat coronary heart disease in traditional Chinese medicine. A group of steroidal saponins present in the plant are believed to be the active ingredients. It has been a challenge to study the individual saponins separately due to the similarities in their chemical and physical properties. In this work, human serum albumin (HSA) functionalized magnetic nanoparticles (MNPs) were used to isolate and identify saponin ligands that bind to HSA from D. nipponica extract. Electrospray ionization mass spectrometry (ESI-MS) was used for compound identification and semi-quantification. Three saponins, i.e. dioscin, gracillin, and pseudo-protodioscin showed affinity to HSA-MNPs and thus isolated effectively from the extract. The other two saponins detected in the extract (i.e. protodioscin and 26-O-β-D-glucopyranosyl-3β, 20α, 26-triol-25 (R) -Δ5, 22-dienofurostan-3-O-α-L-rhamnopyranosyl (1→2)-[α-L-rhamnopyranosyl (1→4)]-β-D-glucopyranoside) exhibited no affinity at all. Among the three saponins fished out, dioscin bound to HSA much stronger than gracillin and pseudo-protodioscin did. The results indicated that affinity interaction between HSA immobilized on MNPs and small molecule compounds were highly dependent on chemical structures and, potentially, medicinal usefulness. The present work demonstrates a facile and effective way to isolate and identify ligands of receptors from medicinal plants.

Dioscorea contains critically important species which can be used as staple foods or sources of bioactive substances, including Dioscorea nipponica, which has been used to develop highly successful drugs to treat cardiovascular disease. Its major active ingredients are thought to be sterol compounds such as diosgenin, which has been called “medicinal gold” because of its valuable properties. However, reliance on naturally growing plants as a production system limits the potential use of D. nipponica, raising interest in engineering metabolic pathways to enhance the production of secondary metabolites. However, the biosynthetic pathway of diosgenin is still poorly understood, and D. nipponica is poorly characterized at a molecular level, hindering in-depth investigation. In the present work, the RNAs from five organs and seven methyl jasmonate treated D. nipponica rhizomes were sequenced using the Illumina high-throughput sequencing platform, yielding 52 gigabases of data, which were pooled and assembled into a reference transcriptome. Four hundred and eighty two genes were found to be highly expressed in the rhizomes, and these genes are mainly involved in stress response and transcriptional regulation. Based on their expression patterns, 36 genes were selected for further investigation as candidate genes involved in dioscin biosynthesis. Constructing co-expression networks based on significant changes in gene expression revealed 15 gene modules. Of these, four modules with properties correlating to dioscin regulation and biosynthesis, consisting of 4,665 genes in total, were selected for further functional investigation. These results improve our understanding of dioscin biosynthesis in this important medicinal plant and will help guide more intensive investigations.

… b LC/MS analysis of crude extract of Proteus sp. R60 and c LC/MS analysis of crude extract … As role of rhizobacteria on secondary metabolism enhancement is least investigated, the …