Effects of bovine serum albumin on zidovudine glucuronidated by UGT2B7 in human liver microsomes
Wang Yang
Gao Jie
Qiao Hailing
Abstract：Objective To investigate the effect of bovine serum albumin (BSA)on the activities of UDP -glucuronosyltrans-ferase (UGT)2B7 in human liver microsomes (HLMs).Methods HLMs were prepared by differential centrifugation methods. The kinetics of glucuronidation of zidovudine (AZT,3’-azido -3’-deoxy -thymidine),a selective UGT2B7 substrate,was measured to reflect the activity of UGT2B7 in HLMs.The formations of AZT and its metabolite,AZT -β-D -glucuronide,were analyzed using a reversed -phase high -performance liquid chromatography.Incubation systems were divided into two groups. One was control group and the other was BSA group which included 2% BSA.Results UGT2B7 -dependent AZT glucuronida-tion in control and BSA groups showed that the results were consistent with a typical Michaelis -Menten equation.The enzyme kinetics parameters of AZT in control and BSA groups were as follows:the Vmax were (1 359.0 ±1 35.8)and (1 268.4 ±300.1 ) pmol/(min·mg protein),the Km were (368.0 ±64.3)and (1 1 1 .4 ±6.9)μM,the CLint were (3.7 ±0.4)and (1 1 .4 ± 2.7)μl/(min·mg protein),respectively.Compared with control group,the Km value of UGT2B7 was significantly decreased and the CLint value was significantly increased in the BSA group (P <0.05).Conclusion The activity of UGT2B7 in HLMs was significantly influenced by BSA which decreased the value of Km and increased the value of CLint .
Keywords：bovine serum albuminHuman liver microsomesUGT2B7zidovudine
Publication Date：2016-01-01
Online Publishing Date：2026-09-12(First online date of this platform, not the publication date of the document)
Pages：5( 10-14 )