Herba Epimediiis widely used as a traditional Chinese medicine for ＂strengthening the kidney＂ and ＂reinforcing bone＂ for a long time in China and other Asian countries. In this study, based on the large number of ...Herba Epimediiis widely used as a traditional Chinese medicine for ＂strengthening the kidney＂ and ＂reinforcing bone＂ for a long time in China and other Asian countries. In this study, based on the large number of domestic and international references and research results, the authors reviewed pharmacological effects and the clinical application of species in genus Epimedium L. Meanwhile, chemical conversion and biotransformation of the major active compounds during the processing of the plants in EpimediumL. and their metabolism in vivowere summarized. This provides a guidance for the application and development in clinical therapy in the future.展开更多
Epimedii Folium, a famous Chinese materia medica, is botanically originated from Epimedium L. species. Here Epimedium L. species were reviewed in phytochemistry, ethnopharmacology, ADME （absorption, distribution, met...Epimedii Folium, a famous Chinese materia medica, is botanically originated from Epimedium L. species. Here Epimedium L. species were reviewed in phytochemistry, ethnopharmacology, ADME （absorption, distribution, metabolism, and excretion）, and processing. They have been proven to possess the efficacy on anti-osteoporosis, antitumor, and treating sexual dysfunction in traditional Chinese medicines. More than 270 compounds have been isolated from the plants of Epimedium L., some of which could be metabolized into a series of metabolites after oral absorption by the active enzymes and intestinal microflora leading to various bioactivities. Polyglucosides （epimendins A-C） and the coresponding oligoglycosides （icariin and baohuoside I） play important roles in clinical application.展开更多
Objective Icaritin is the main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese materia medica Epimedii Herba. Modern pharmacological studies have demonstrated that icaritin has a wi...Objective Icaritin is the main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese materia medica Epimedii Herba. Modern pharmacological studies have demonstrated that icaritin has a wide range of biological activities. However, its metabolites and biotransformation pathways have not yet been comprehensively investigated. The present study aims to identify icaritin metabolites in rats by using a sensitive and effective LC-MS/MS method. Methods The plasma and urine samples of rats were collected before （blank） and after oral administration of icaritin, and subjected to liquid-liquid extraction with ethyl acetate. The full-scan LC-MS chromatograms of the plasma and urine samples were compared with those of blank samples to detect the possible metabolites, which were later detected by their product ion spectra. Results A total of 23 metabolites were identified, and conjugated icaritins produced by glucuronidation, glycosylation, and sulfation were its major metabolites. Minor demethylation, hydrogenation, and oxidation metabolites were also found. Conclusion Phase II metabolism is the main metabolic pathway of icaritin.展开更多
文摘Herba Epimediiis widely used as a traditional Chinese medicine for ＂strengthening the kidney＂ and ＂reinforcing bone＂ for a long time in China and other Asian countries. In this study, based on the large number of domestic and international references and research results, the authors reviewed pharmacological effects and the clinical application of species in genus Epimedium L. Meanwhile, chemical conversion and biotransformation of the major active compounds during the processing of the plants in EpimediumL. and their metabolism in vivowere summarized. This provides a guidance for the application and development in clinical therapy in the future.
文摘Epimedii Folium, a famous Chinese materia medica, is botanically originated from Epimedium L. species. Here Epimedium L. species were reviewed in phytochemistry, ethnopharmacology, ADME （absorption, distribution, metabolism, and excretion）, and processing. They have been proven to possess the efficacy on anti-osteoporosis, antitumor, and treating sexual dysfunction in traditional Chinese medicines. More than 270 compounds have been isolated from the plants of Epimedium L., some of which could be metabolized into a series of metabolites after oral absorption by the active enzymes and intestinal microflora leading to various bioactivities. Polyglucosides （epimendins A-C） and the coresponding oligoglycosides （icariin and baohuoside I） play important roles in clinical application.
基金EU-China Scientific and Technological Cooperation(1108)National Mega-project for Innovative Drugs(2012ZX09301002-001)Macao Science and Technology Development Fund(No.044/2011/A2)
文摘Objective Icaritin is the main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese materia medica Epimedii Herba. Modern pharmacological studies have demonstrated that icaritin has a wide range of biological activities. However, its metabolites and biotransformation pathways have not yet been comprehensively investigated. The present study aims to identify icaritin metabolites in rats by using a sensitive and effective LC-MS/MS method. Methods The plasma and urine samples of rats were collected before （blank） and after oral administration of icaritin, and subjected to liquid-liquid extraction with ethyl acetate. The full-scan LC-MS chromatograms of the plasma and urine samples were compared with those of blank samples to detect the possible metabolites, which were later detected by their product ion spectra. Results A total of 23 metabolites were identified, and conjugated icaritins produced by glucuronidation, glycosylation, and sulfation were its major metabolites. Minor demethylation, hydrogenation, and oxidation metabolites were also found. Conclusion Phase II metabolism is the main metabolic pathway of icaritin.
