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Li, Yong-mei; Li, Xiao-mian; Li, Guang-ming; Du, Wen-cai; Zhang, Jing; Li, Wei-xia; Xu, Jianshe; Hu, Ming; Zhu, Ze (2008)
Languages: English
Types: Article
Subjects: Article
Identifiers:pmc:PMC2782632
Hesperidin is an abundant flavanone glycoside in citrus fruits and has been reported to possess a wide range of biological activities. However, hesperidin has poor bioavailability. Here, we test the hypothesis that hesperetin found in Chenpi will have a better bioavailability than hesperidin and that treatment of hesperidin with glucosidase-like yeast Bg1A protein will increase its bioavailability. The results indicate that hesperidin in pure or extract form is hydrolyzed by BglA protein extracted from S. singularis or expressed in E coli BL21 (DE3). This biotransformation affected the plasma pharmacokinetics of total hesperetin in rats, in that the plasma Tmax was significantly shorter after administration of BglA protein-treated hesperidin than after administration of hesperidin extract. In addition, the AUC values for total hesperetin after administration of Bg1A-treated hesperidin were approximately 4-fold higher by oral administration and 3-fold higher by intravenous administration, respectively. In contract, the plasma clearance value and volume of distribution after administration of Bg1A-treated hesperidin extract or pure hesperetin was significant smaller than after administration of untreated hesperidin extract or pure hesperidin In conclusion, this is a first study that systemically determines the absolute bioavailability of hesperidin and hesperetin simultaneously, and the study shows clearly that hesperetin is more bioavailable than hesperidin regardless of the route of administration, and that prior transformation of hesperidin to hesperetin via fermentation should significantly increase its bioavailability because of the action of yeast glycosidase-like protein BglA.
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