The Inhibitory Effect and Possible Mechanism of a Novel 7-azaisoindigo on Proliferation of A549 Cells

Abstract: The anticancer effect of a newly synthesized 7-azaisoindigo derivative (namely N1-(n-butyl)-7-azaisoindigo， 7-AI-b) was investigated in human lung cell line A549， and the underlying mechanism of action was analysed. Cell proliferation was assessed by MTT assay; Autophagy induced by 7-AI-b was evaluated by MDC staining and the expression of LC3 by Western blot; Cell cycle was detected by flow cytometry (FCM) following PI staining; The alteration of intracellular Ca2+ level was detected following Fluo-3-AM loading. It was found that 7-AI-b inhibited A549 cell proliferation in a dose- and time-dependent way. 7-AI-b-induced autophagy occurred showing enhanced MDC staining， and increased in both expressions of LC3 and conversion of LC3-I to LC3-II; Cell cycle was arrested in the G0/G1 phase; Meanwhile， 7-AI-b was found to increase intracellular Ca2+ level. Generally speaking， the novel compound 7-AI-b could inhibit the proliferation of cancer cells effectively. Its mechanism might be related to arrest cell cycle and induce cell autophagy. The intracellular Ca2+ overloading was involved in cell death process.

CSTR: 32200.14.cjcb.2010.02.0008