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Molecules 2014, 19(1), 177-203; doi:10.3390/molecules19010177
Article

A Comparative Study on the Metabolism of Epimedium koreanum Nakai-Prenylated Flavonoids in Rats by an Intestinal Enzyme (Lactase Phlorizin Hydrolase) and Intestinal Flora

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1,* , 1,2
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1 Key Laboratory of New Drug Delivery System of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, 100 Shizi Road, Nanjing 210028, Jiangsu, China 2 College of Pharmacy, Jiangsu University, Zhenjiang 212013, Jiangsu, China 3 College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, Jiangsu, China
* Author to whom correspondence should be addressed.
Received: 6 November 2013 / Revised: 11 December 2013 / Accepted: 17 December 2013 / Published: 24 December 2013
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Abstract

The aim of this study was to compare the significance of the intestinal hydrolysis of prenylated flavonoids in Herba Epimedii by an intestinal enzyme and flora. Flavonoids were incubated at 37 °C with rat intestinal enzyme and intestinal flora. HPLC-UV was used to calculate the metabolic rates of the parent drug in the incubation and LC/MS/MS was used to determine the chemical structures of metabolites generated by different flavonoid glycosides. Rates of flavonoid metabolism by rat intestinal enzyme were quicker than those of intestinal flora. The sequence of intestinal flora metabolic rates was icariin > epimedin B > epimedin A > epimedin C > baohuoside I, whereas the order of intestinal enzyme metabolic rates was icariin > epimedin A > epimedin C > epimedin B > baohuoside I. Meanwhile, the LC/MS/MS graphs showed that icariin produced three products, epimedin A/B/C had four and baohuoside I yielded one product in incubations of both intestinal enzyme and flora, which were more than the results of HPLC-UV due to the fact LC/MS/MS has lower detectability and higher sensitivity. Moreover, the outcomes indicated that the rate of metabolization of flavonoids by intestinal enzyme were faster than those of intestinal flora, which was consistent with the HPLC-UV results. In conclusion, the metabolic pathways of the same components by intestinal flora and enzyme were the same. What’s more, an intestinal enzyme such as lactase phlorizin hydrolase exhibited a more significant metabolic role in prenylated flavonoids of Herba Epimedi compared with intestinal flora.
Keywords: lactase phlorizin hydrolase; intestinal flora; prenylated flavonoids; metabolite; Epimedium lactase phlorizin hydrolase; intestinal flora; prenylated flavonoids; metabolite; Epimedium
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Zhou, J.; Chen, Y.; Wang, Y.; Gao, X.; Qu, D.; Liu, C. A Comparative Study on the Metabolism of Epimedium koreanum Nakai-Prenylated Flavonoids in Rats by an Intestinal Enzyme (Lactase Phlorizin Hydrolase) and Intestinal Flora. Molecules 2014, 19, 177-203.

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