Comparative oral and intravenous pharmacokinetics of phlorizin in rats having type 2 diabetes and in normal rats based on phase II metabolism

Food & Function
Zhanguo WangHuiling Hu

Abstract

Phlorizin (PHZ), a type of dihydrochalcone widely found in Rosaceae such as apples, is the first compound discovered as a sodium-glucose cotransporter (SGLT) inhibitor. It has been confirmed to improve the symptoms of diabetes and diabetic complications effectively. Like other flavonoids, the bioavailability challenge of PHZ is the wide phase I and II metabolism in the digestive tract. In this study, we investigated the pharmacokinetics and contribution of phase II metabolism after the oral and intravenous administrations of PHZ in rats having type 2 diabetes (T2D) and in normal rats. The phase II metabolism characteristics of PHZ were investigated by treating plasma samples with β-glucuronidase/sulfatase. The contribution ratio of phase II metabolism of PHZ ranged from 41.9% to 69.0% after intravenous injection with three doses of PHZ in normal rats. Compared with the observations for normal rats, AUC0-t and Cmax of PHZ significantly increased and T1/2 of PHZ significantly decreased in T2D rats. PHZ was converted into phloretin (PHT) through an enzyme-catalyzed hydrolysis reaction, and PHT was further transformed into conjugates with glycose after both oral and intravenous administrations. Moreover, it was found that the bioav...Continue Reading

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Citations

Dec 11, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Monika StomporAgata Bajek-Bil
Aug 23, 2019·Critical Reviews in Toxicology·Tian YangYing-Yong Zhao
Aug 17, 2020·The Journal of Biological Chemistry·Rachel J Perry, Gerald I Shulman
Jul 17, 2021·International Journal of Biological Macromolecules·Dong Yu-HaoLiu Rui-Hai
Nov 19, 2021·Critical Reviews in Food Science and Nutrition·Yao ChenZhiyong He

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