Evaluation of pharmaceutical activities of G-protein coupled receptor targeted pharmaceuticals in Chinese wastewater effluent

作     者：Han Zhang Yingchao Lin Zhengyu Men Masaru Ihara Weizun Li Kai He Han Zhang;Yingchao Lin;Zhengyu Men;Masaru Ihara;Weizun Li;Kai He

作者机构：College of Environmental Science and EngineeringNankai UniversityTianjin 300071China Research Center for Environmental Quality ManagementKyoto UniversityOtsu 5200811Japan 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2020年第31卷第10期

页      面：2859-2863页

核心收录：

学科分类：083002[工学-环境工程] 0830[工学-环境科学与工程（可授工学、理学、农学学位）] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070302[理学-分析化学] 0703[理学-化学] 

基　　金：The Fundamental Research Funds for the Central Universities Japan Society for the Promotion of science(JSPS)for Grant-in-Aid for Scientific Research(B)(No.17H01907) Keihanshin Consortium for Fostering the Next Generation of Global Leaders in Research(No.K-CONNEX),established by Human Resource Development Program for Science and Technology,MEXT financial support from the National Natural Science Foundation of China(No.21806082) Key Technologies R&D Program of Tianjin(Nos.18YFZCNC01410,16YFZCSF00410) 

主　　题：PCR targeted pharmaceutical Pharmaceutical activity TGFαshedding assay Wastewater 

摘      要：The occurre nce of biologically active pharmaceuticals in aquatic enviro nments raised the potential risks to aquatic *** these marketed biological active pharmaceuticals,it has been estimated that40%of them target G-protein-coupled receptors(GPCRs).We have illustrated pharmaceutical activities of GPCR targeted pharmaceuticals in English and Japanese wastewater by the in vitro transforming growth factor-α(TGFα)shedding ***,as the most important producer and consumer of pharmaceuticals,the occurrence of GPCR targeted pharmaceuticals in China had remained *** this study,we investigated the pharmaceutical activities of GPCR targeted pharmaceuticals in secondary effluents of Chinese wastewater treatment *** discovered antagonistic activities against angiotensin(AT1)receptor at up to 7.2×102 ng-valsartan-equivalent quantity/L in Chinese wastewater for the first time as well as agonistic activities against dopamine(D2)***,in parallel with the assay,we determined concentrations of GPCR targeted pharmaceuticals in target wastewater by liquid chromatography coupled with tandem mass spectrometry(LC-MS/MS).Through the comparison of predicted antagonistic activities calculated by concentrations and potency values from the assay,we found that the measured antagonistic activities against AT1 receptor from the assay were higher than the predicted AT1 activities from valsartan,irbesartan,and losartan,indicating the potential existence of other unknown AT1 antagonists in wastewater.