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Xenobiotica
the fate of foreign compounds in biological systems
Volume 45, 2015 - Issue 3
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Research Article

Regulation profile of phosphatidylcholines (PCs) and lysophosphatidylcholines (LPCs) components towards UDP-glucuronosyltransferases (UGTs) isoforms

Xin GaoDepartment of Clinical Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China,
,
Hengyan QuDepartment of Clinical Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China,
,
Chun-Zhi AiJoint Center for Translational Medicine, Dalian Institute of Chemical Physics Chinese Academy of Sciences and The first Affiliated Hospital of Liaoning Medical University, Dalian, China,
,
Yun-Feng CaoKey Laboratory of Contraceptives and Devices Research (NPFPC), Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai, China, and
,
Ting HuangKey Laboratory of Contraceptives and Devices Research (NPFPC), Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai, China, and
,
Jian-Xing ChenKey Laboratory of Contraceptives and Devices Research (NPFPC), Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai, China, and
,
Jia ZengKey Laboratory of Contraceptives and Devices Research (NPFPC), Shanghai Engineer and Technology Research Center of Reproductive Health Drug and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai, China, and
,
Xiao-Yu SunJoint Center for Translational Medicine, Dalian Institute of Chemical Physics Chinese Academy of Sciences and The first Affiliated Hospital of Liaoning Medical University, Dalian, China,
,
Mo HongJoint Center for Translational Medicine, Dalian Institute of Chemical Physics Chinese Academy of Sciences and The first Affiliated Hospital of Liaoning Medical University, Dalian, China,
,
Frank J. GonzalezLaboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA
,
Zeyuan LiuDepartment of Clinical Pharmacology, Affiliated Hospital of the Academy of Military Medical Sciences, Beijing, China, Correspondence[email protected]
&
Zhong-Ze FangDepartment of Toxicology, School of Public Health, Tianjin Medical University, Tianjin, China, Correspondence[email protected]
 show all
Pages 197-206 | Received 07 Aug 2014, Accepted 12 Sep 2014, Published online: 26 Sep 2014
 
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Abstract

1. Endogenous compounds have been reported to be the regulators of UDP-glucuronosyltransferases (UGTs) isoforms. This study aims to investigate the regulatory effects of the activity of UGT isoforms by two important lipid components phosphatidylcholine (PC) and lysophosphatidylcholines (LPC) using in vitro incubation system.

2. UGTs supersomes-catalyzed 4-methylumbelliferone (4-MU) glucuronidation was used as the probe reaction to evaluate the inhibition of compounds towards UGT isoforms except UGT1A4, and UGT1A4-catalyzed trifluoperazine (TFP) glucuronidation reaction was utilized to phenotype the activity of UGT1A4.

3. About 50 μM of LPC15:0, LPC16:0, LPC17:0, LPC18:0, LPC18:1 and PC16:0, 2:0 exhibited inhibition towards more than 90% activity of UGT isoforms, and other LPC and PC components showed negligible inhibitory potential towards all the UGT isoforms. UGT1A6 and UGT1A8 were identified to be the most sensitive UGT isoforms susceptible for the inhibition by LPC15:0, LPC16:0, LPC17:0, LPC18:0, LPC18:1 and PC16:0, 2:0, indicating the strong influence of these LPC and PC components towards UGT1A6 and UGT1A8-catalyzed metabolic reaction when the concentrations of these components increased.

Declaration of interest

The authors have declared no conflict of interest. This work was supported by the National Natural Science Foundation of China (No. 81202586).

Supplementary material available online.

Supplemental Table S1.

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