Role of Intestinal Hydrolase in the Absorption of Prenylated Flavonoids Present in Yinyanghuo 英文参考文献.docVIP

Molecules 2011, 16, 1336-1348; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Role of Intestinal Hydrolase in the Absorption of Prenylated Flavonoids Present in Yinyanghuo Yan Chen 1, Jinyan Wang 1, Xiaobin Jia 1,*, Xiaobin Tan 1 and Ming Hu 2 1 Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 100 Shizi Road, Nanjing 210028, China; E-Mails: ychen202@ (Y.C.); wwind924@ (J.W.); jakytan2005@ (X.T.) 2 Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, 1441 Moursund Street, Houston, TX 77030, USA; E-Mail: mhu@ (M.H) * Author to whom correspondence should be addressed; E-Mail: jxiaobin2005@; Tel.: +86-25 Fax: +86-25 Received: 13 December 2010; in revised form: 25 January 2011 / Accepted: 27 January 2011 / Published: 1 February 2011 Abstract: Purpose: Yinyanghuo (Herba Epimdii) is a traditional Chinese herb containing prenylated flavonoids as its active constituents. The aim of this study was to examine the significance of the intestinal hydrolysis of prenylated flavonoids by lactase phlorizin hydrolase (LPH), an enzyme at the brush border membrane of intestinal cells. Methods: A four-site perfused rat intestinal model was used. The concentration of the flavonoids of interest and their metabolites in different intestinal segements were analyzed by HPLC, and the apparent permeabilities were calculated. A lactase phlorizin hydrolase inhibitor (gluconolactone) was employed to investigate the mechanism of the intestinal absorption, and the metabolites of the four flavonoids were identified using LC/MS/MS. Results: Diglycosides (icariin) or triglycosides (epimedin A, epimedin B, and epimedin C) were hydrolyzed rapidly in duodenum and jejunum producing one or two metabolites, while a monoglycoside (b