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 

机构地区：[1]College of Environmental Science and Engineering,Nankai University,Tianjin 300071,China [2]Research Center for Environmental Quality Management,Kyoto University,Otsu 5200811,Japan

出　　处：《Chinese Chemical Letters》2020年第10期2859-2863,共5页中国化学快报（英文版）

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)。

摘　　要：The occurre nce of biologically active pharmaceuticals in aquatic enviro nments raised the potential risks to aquatic species.Among 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 assay.However,as the most important producer and consumer of pharmaceuticals,the occurrence of GPCR targeted pharmaceuticals in China had remained unclear.In this study,we investigated the pharmaceutical activities of GPCR targeted pharmaceuticals in secondary effluents of Chinese wastewater treatment plants.We 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)receptor.Furthermore,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.

关 键 词：PCR targeted pharmaceutical Pharmaceutical activity TGFαshedding assay WASTEWATER 

分 类 号：O657.63[理学—分析化学] X703[理学—化学]