Alterations in intestinal bacteria metabolism affect the pharmacokinetic property of hesperidin
- Alterations in intestinal bacteria metabolism affect the pharmacokinetic property of hesperidin
- Ming Ji Jin; 김운용; 김인숙; 김동현; 권오승; 유혜현
- Issue Date
- 2010년 춘계대한약학회 (Proceedings of the Spring International Convention of the Pharmaceutical Society of Korea)
- , 136-136
- Hesperidin is biologically active flavanone glycoside occurring abundantly in citrus fruits. in the present study, effects of intestinal microflora on pharmacokinetics of hesperidin were investigated using a pseudo germ-free rat model treated with anti-biotics. after administration of hesperidin to rats, hesperetin, hesperetin glucuronides and metabolites postulated to be eriodictyol, hemoeriodictyol, and their glucuronides were detected in urine while hesperetin glucuronide was predominantly found in plasma. The plasma concentration-time profile of hesperetin was also compared between normal (non=antibiotic) and pseudo germ-free rats administered this compound. The maximum concentration (Cmax)values of hesperetin in normal and pseudo germ-free rats were 0.58 and 0.20 μg/ml, respectively, and area under the curve(AUC) values were 6.3 and 2.8μg/ml, respectively. Thus, systemic exposure as evidenced by AUC and Cmax was significantly higher in normal compared to pseudo germ-free rats. fecal β-glucosidase activities of normal and pseudo germ-free rats were 0.21 and 0.11 nmol/min/mg;while, fecal α-rhamnosidase activities were 0.37 and 0.12 nmol/min/mg, respectively. The rate of hesperidin transformation to hesperetin was 6.9 and 2.9 nmol/min/g in fecal samples in normal and pseudo germ-free rats, respectively. Taken together, there result showed that pharmacokinetic differences between noraml and pseudo germ-free rats may be attributed to differing hesperidin uptake as well as alterations in metabolic activities of intestinal folra.
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