Inhibition effect and mechanism of novel nitrogen mustard derivative 2 -(4 -di (2-chloroethyl) aminobutylamino)-1H-benz- de isoquinoline-1,3(2H) -dione on human hepatoma HepG2 cells

VernacularTitle:N－4－（二氯乙基）丁胺－1，8－萘酰亚胺对人肝癌HepG2细胞的抑制作用及其机制研究
Author: Jiu-Wang MIAO ¹ ; Zhong-Quan ZHANG ; Song-Qiang XIE
Author Information

1. 河南大学化学生物学研究所
Keywords: nitrogen mustard derivative; antitumor; apoptosis; caspase
From: The Chinese Journal of Clinical Pharmacology 2015;(20):2031-2033
CountryChina
Language:Chinese
Abstract: Objective To investigate the effects of 2-(4-di(2-chlo-roethyl) aminobutylamino)-1H-benz-[de]isoquinoline-1,3(2H)-dione( XHH) , a novel nitrogen mustard derivative, on the growth and apoptosis in human hepatoma HepG2 cells in vitro.Methods Cell pro-liferative effect was assessed by MTT assay.Changes of morphology and mitochondrial membrane potential ( MMP) were assessed by AnnexinV-FITC/Hoechst33342 , PI/Hoecsht33342 and Rh123/Hoechst33342 double staining using high content screening ( HCS ) .The expression of caspase-3 , caspase-9 , Bcl-2 , Bax was assessed by immunofluores-cence method using HCS. Results The results indicated that XHH could inhibit the proliferation of HepG2 cells, induce apoptosis, lose MMP, up-regulate the ratio of Bax/Bcl-2, increase the expression of caspase-3 , caspase-9.Conclusion XHH could inhibit proliferative of human hepatoma HepG2 cells and induce cell apoptosis via mitochon-drial pathway.