Hsp90抑制剂木犀草苷对非小细胞肺癌的体外抑制活性及作用机理研究

doi:10.16088/j.issn.1001-6600.2015.03.014

Abstract

Abstract: A fluorescence polarization technique was established to screen Hsp90 inhibitors and was selected as candidate for further anti-proliferation study. Thermal shift assay was used to confirm the binding effect of cynaroside and Hsp90. Then it was found that cynaroside showed potent and selective antiproliferation activities against non-small lung cancer cells among 14 strains of cancer cells. The colonial assay, western blot and flow cytometry were employed to investigate its possible mechanism. The results showed that cynaroside could inhibit the proliferation of non-small lung cancer cells in a dose-dependent manner and induce the degradation of Raf-1, and HER2 expression. Moreover, cynaroside induced G2/M arrest in H460 cell and triggered apoptosis by up-regulatiing Bax expression. Finally, the results displayed that cynaroside, one of the flavonoids, formed antineoplastic activity by inhibiting Hsp90 activity to degrade its client proteins in H460 cells, inducing G2/M phase arrest and triggering apoptosis by up-regulating Bax expression.

Key words: Hsp90, cynaroside, non-small lung cancer, cell cycle arrest, apoptosis

CLC Number:

R962

MEI Han-bing, WANG Wei, YAO Xue, CHENG Lian-biao, HUANG Jin. Inhibitory Activity and Mechanism of Hsp90 Inhibitor Cynaroside Against Non-small Cell Lung Cancer in Vitro[J].Journal of Guangxi Normal University(Natural Science Edition), 2015, 33(3): 91-97.

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Inhibitory Activity and Mechanism of Hsp90 Inhibitor Cynaroside Against Non-small Cell Lung Cancer in Vitro

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