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Valeriaquinone A,a unique anthraquinone–coumarin hybrid with selective inhibition of PTP1B from Knoxia valerianoides
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作者 Yan Jiang ren-yong yang +4 位作者 Zhao-Xia Qu Gui-Ge Hou Wei Cong Chun-Hua Wang Feng Zhao 《Chinese Chemical Letters》 SCIE CAS CSCD 2022年第6期2919-2922,共4页
Valeriaquinone A(1),an unprecedented anthraquinone–coumarin hybrid,was isolated from the roots of Knoxia valerianoides.Its structure was determined by extensive spectroscopic analyses and X-ray diffraction.The plausi... Valeriaquinone A(1),an unprecedented anthraquinone–coumarin hybrid,was isolated from the roots of Knoxia valerianoides.Its structure was determined by extensive spectroscopic analyses and X-ray diffraction.The plausible biosynthetic pathways for 1 were proposed.Compound 1 exhibited strong protein tyrosine phosphatase 1 B(PTP1 B)inhibition with high selectivity(>30 fold)over homologous T cell protein tyrosine phosphatase(TCPTP)potentially by binding to an allosteric site predicted by kinetic analysis and molecular docking.Moreover,compound 1 showed significant cytotoxic activities against three human hepatoma cell lines(HepG2,QGY-7703,and SMMC-7721)with half maximal inhibitory concentration(IC_(50))values of 1.39±0.2,10.34±2.09,and 5.56±0.47μmol/L,respectively. 展开更多
关键词 Knoxia valerianoides Anthraquinone–coumarin hybrid PTP1B inhibitory activity Cytotoxic activity Allosteric inhibition
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