首页|Rapid discovery of a novel"green"and natural GST inhibitor for sensitizing hepatocellular carcinoma to Cisplatin by visual screening strategy

Rapid discovery of a novel"green"and natural GST inhibitor for sensitizing hepatocellular carcinoma to Cisplatin by visual screening strategy

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  • 国家科技期刊平台
  • NETL
  • NSTL
  • 万方数据
Over-expression of glutathione S-transferase(GST)can promote Cisplatin resistance in hepatocellular carcinoma(HCC)treatment.Hence,inhibiting GST is an attractive strategy to improve Cisplatin sensi-tivity in HCC therapy.Although several synthesized GST inhibitors have been developed,the side effects and narrow spectrum for anticancer seriously limit their clinical application.Considering the abundance of natural compounds with anticancer activity,this study developed a rapid fluorescence technique to screen"green"natural GST inhibitors with high specificity.The fluorescence assay demonstrated that schisanlactone B(hereafter abbreviated as C1)isolated from Xue tong significantly down-regulated GST levels in Cisplatin-resistant HCC cells in vitro and in vivo.Importantly,C1 can selectively kill HCC cells from normal liver cells,effectively improving the therapeutic effect of Cisplatin on HCC mice by down-regulating GST expression.Considering the high GST levels in HCC patients,this compound demon-strated the high potential for sensitizing HCC therapy in clinical practice by down-regulating GST levels.

GSTDrug resistanceFluorescenceHepatocarcinomaNatural compound C1"Green"GST inhibitor

Linxi Mao、Yan Qin、Jialong Fan、Wei Yang、Bin Li、Liang Cao、Liqin Yuan、Mengyun Wang、Bin Liu、Wei Wang

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TCM and Ethnomedicine Innovation & Development International Laboratory,School of Pharmacy,Hunan University of Chinese Medicine,Changsha,410208,China

College of Biology,Hunan University,Changsha,410082,China

College of Foreign Languages,Hunan Women's University,Changsha,410004,China

Department of General Surgery,The Second Xiangya Hospital,Central South University,Changsha,410011,China

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National Natural Science Foundation of ChinaNational Natural Science Foundation of ChinaNational Natural Science Foundation of ChinaOutstanding Youth Foundation of Hunan Provincial Education Department of ChinaHunan Youth Science and Technology Innovation Talents Project,ChinaChinese Postdoctoral Science foundationChangjiang Scholars Program in Ministry Education,People's Republic of ChinaScientific Research Project of Hunan Provincial Education Department

82003931822047668137406220B4452021RC31002021M690974Program :T2019133Project :21B0394

2024

10.1016/j.jpha.2023.12.013

药物分析学报(英文)
西安交通大学

药物分析学报(英文)

影响因子：0.244
ISSN：2095-1779
年,卷(期)：2024.14(5)
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