文献类型：期刊文献

中文题名：Discovery of a natural fluorescent probe targeting the Plasmodium falciparum cysteine protease falcipain-2

作者：Lili Zhu[1];Lei Shan[2];Junsheng Zhu[1];Li Li[2];Shiliang Li[1];Liyan Wang[1];Jiawei Wang[1];Shoude Zhang[1,2];Hongchang Zhou[3];Weidong Zhang[2];Honglin Li[1]

机构：[1]Shanghai Key Laboratory of New Drug Design,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China;[2]Department of Natural Product Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;[3]School of Medicine,Huzhou University,Huzhou ho u Central Hospital,Huzhou 313000,China

年份：2020

卷号：63

期号：7

起止页码：1016

中文期刊名：Science China(Life Sciences)

外文期刊名：中国科学（生命科学英文版）

收录：Scopus;CSCD:【CSCD2019_2020】；PubMed;

基金：supported by the National Key Research and Development Program (2016YFA0502304 to H.L.);the National Natural Science Foundation of China (81825020);the National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program”, China (2018ZX09711002);the Fundamental Research Funds for the Central Universities;Special Program for Applied Research on Super Computation of the NSFC-Guangdong Joint Fund (the second phase) (U1501501);Professor of Chang Jiang Scholars Program (to W.Z.);the Natural Science Foundation of Zhejiang Province (LY15H190007);sponsored by the National Program for Special Supports of Eminent Professionals and National Program for Support of Top-notch Young Professionals。

语种：英文

中文关键词：falcipain-2;malaria diagnosis;antimalarial agent;acylated flavonol monoglycoside;fluorescent probe

摘要：The Plasmodium falciparum cysteine protease falcipain-2(FP-2) is an attractive antimalarial target. Here, we discovered that the natural compound NP1024 is a nonpeptidic inhibitor of FP-2 with an IC50 value of 0.44 μmol L–1. The most exciting finding is that both in vitro and in vivo, NP1024 directly targets FP-2 in malaria parasite-infected erythrocytes as a natural fluorescent probe, thereby paving the way for an integration of malaria diagnosis and treatment.