ArticlePlanta medica2013
Characterization of in vitro ADME properties of diosgenin and dioscin from Dioscorea villosa.
Article in Planta medica, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 55 citations in OpenAlex.
- Risks, Benefits, and Molecular Targets of Fenugreek Administration in the Treatment of Hepatocellular Carcinoma.Cancers · 2026Review
- Therapeutic potential of diosgenin in hepatocellular carcinoma through molecular mechanisms and nanodelivery strategies.Discover oncology · 2026Review
- Dioscin in liver diseases: pharmacological mechanisms, translational potential and future perspectives.Frontiers in pharmacology · 2026Review
- Molecular entities for the anti-melanoma effect ofBioinformation · 2025Article
- An Updated Review of Molecular Mechanisms Implicated with the Anticancer Potential of Diosgenin and Its Nanoformulations.Drug design, development and therapy · 2025Review
- Pre-ADMET studies of 5-(3',4'-dihydroxyphenyl)-γ-valerolactone, the bioactive intestinal metabolite of proanthocyanidins.Archiv der Pharmazie · 2025Article
- Integrating network pharmacology and experimental validation to decipher the pharmacological mechanism of DXXK in treating diabetic kidney injury.Scientific reports · 2024Article
- An overview on pharmacological significance, phytochemical potential, traditional importance and conservation strategies ofHeliyon · 2024Review
- Role of diosgenin extracted fromHeliyon · 2024Article
- Effect of Verapamil, a P-glycoprotein-1 and Cytochrome P450 3A4 Inhibitor, on Pharmacokinetics and Metabolic Stability of Ripretinib: A Drug-Drug Interaction Study in Rats.European journal of drug metabolism and pharmacokinetics · 2023Article
- Protective effects of dioscin against Parkinson's disease via regulating bile acid metabolism through remodeling gut microbiome/GLP-1 signaling.Journal of pharmaceutical analysis · 2023Article
- Identification of the Natural Steroid Sapogenin Diosgenin as a Direct Dual-Specific RORα/γ Inverse Agonist.Biomedicines · 2022Article
- Diosgenin: An Updated Pharmacological Review and Therapeutic Perspectives.Oxidative medicine and cellular longevity · 2022Review
- Diosgenin and Its Analogs: Potential Protective Agents Against Atherosclerosis.Drug design, development and therapy · 2022Review
- Synthesis of Anti-Inflammatory Spirostene-Pyrazole Conjugates by a Consecutive Multicomponent Reaction of Diosgenin with Oxalyl Chloride, Arylalkynes and Hydrazines or Hydrazones.Molecules (Basel, Switzerland) · 2021Article
- Potential Herb-Drug Interactions in the Management of Age-Related Cognitive Dysfunction.Pharmaceutics · 2021Review
- The Effects of Diosgenin on Hypolipidemia and Its Underlying Mechanism: A Review.Diabetes, metabolic syndrome and obesity : targets and therapy · 2021Review
- Tubulin colchicine site binding agent LL01 displays potent antitumor efficiency both in vitro and in vivo with suitable drug-like properties.Investigational new drugs · 2020Article
- Recent Advances in the Pharmacological Activities of Dioscin.BioMed research international · 2019Review
- Modulation of Cytochrome P450, P-glycoprotein and Pregnane X Receptor by Selected Antimalarial Herbs-Implication for Herb-Drug Interaction.Molecules (Basel, Switzerland) · 2017Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
Dioscorea villosa (wild yam) is native to North America and has been widely used as a natural alternative for estrogen replacement therapy to improve women's health as well as to treat inflammation, muscle spasm, and asthma. Diosgenin and dioscin (glycoside form of diosgenin) are reported to be the pharmacologically active compounds. Despite the reports of significant pharmacological properties of dioscin and diosgenin in conditions related to inflammation, cancer, diabetes, and gastrointestinal ailments, no reports are available on ADME properties of these compounds. This study was carried out to determine ADME properties of diosgenin and dioscin and their effects on major drug metabolizing enzymes (CYP 3A4, 2D6, 2C9, and 1A2). The stability was determined in simulated gastric and intestinal fluids (SGF, pH 1.2 and SIF, pH 6.8), and intestinal transport was evaluated in Caco-2 model. Phase I and phase II metabolic stability was determined in human liver microsomes and S9 fractions, respectively. Quantitative analysis of dioscin and diosgenin was performed by UPLC-MS system. Dioscin degraded up to 28.3 % in SGF and 12.4 % in SIF, which could be accounted for by its conversion to diosgenin (24.2 %. in SGF and 2.4 % in SIF). The depletion of diosgenin in SGF and SIF was < 10 %. Diosgenin was stable in HLM but disappeared in S9 fraction with a half-life of 11.3 min. In contrast, dioscin was stable in both HLM and S9 fractions. Dioscin showed higher permeability across Caco-2 monolayer with no significant efflux, while diosgenin was subjected to efflux mediated by P-glycoprotein. Diosgenin and dioscin inhibited CYP3A4 with IC50 values of 17 and 33 µM, respectively, while other CYP enzymes were not affected. In conclusion, dioscin showed better intestinal permeability. Conversion of dioscin to diosgenin was observed in both gastric and intestinal fluids. No phase I metabolism was detected for both compounds. The disappearance of diosgenin in S9 fraction indicated phase II metabolism.
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