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Identification of Icaritin Metabolites in Rats by LC-MS/MS
Lin-hu Ye1; Bing-xin Xiao1; Fang-rui Cao1; Ying Zheng2; Rui-le Pan1; Qi Chang1
Source PublicationChinese Herbal Medicines


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.


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.


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.


Phase II metabolism is the main metabolic pathway of icaritin.

KeywordEpimedium L. Icaritin Lc-ms/ms Metabolites
Indexed By其他
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000433671400003
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorQi Chang
Affiliation1.Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China
Recommended Citation
GB/T 7714
Lin-hu Ye,Bing-xin Xiao,Fang-rui Cao,et al. Identification of Icaritin Metabolites in Rats by LC-MS/MS[J]. Chinese Herbal Medicines,2015,7(4):296-302.
APA Lin-hu Ye,Bing-xin Xiao,Fang-rui Cao,Ying Zheng,Rui-le Pan,&Qi Chang.(2015).Identification of Icaritin Metabolites in Rats by LC-MS/MS.Chinese Herbal Medicines,7(4),296-302.
MLA Lin-hu Ye,et al."Identification of Icaritin Metabolites in Rats by LC-MS/MS".Chinese Herbal Medicines 7.4(2015):296-302.
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