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

引用

Chinese Chemical Letters 2020年第10期31卷 2859-2863页

作者： Han Zhang Yingchao Lin Zhengyu Men Masaru Ihara Weizun Li Kai He College of Environmental Science and Engineering Nankai UniversityTianjin 300071China Research Center for Environmental Quality Management Kyoto UniversityOtsu 5200811Japan

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.

关键词： pcr targeted pharmaceutical pharmaceutical activity TGFαshedding assay Wastewater

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