Synthesis and in vitro anti-tumor effects screening of sinomenine-nitrate conjugates
Objective:To find effective structural modification methods for discovering the anti-tumor activity of sinomenine.Methods:Based on the structural characteristics of sinomenine,a series of sinomenine-nitrate conjugates were designed and synthesized.The structures of all these compounds were confirmed by infrared spectroscopy,nuclear magnetic resonance hydrogen spectroscopy,nuclear magnetic resonance carbon spectroscopy and high-resolution mass spectrometry.MTT assay was used to test the inhibitory effects of sinomenine-nitrate conjugates on the proliferation of human tumor cells(cervical cancer Hela cells,lung cancer A549 cells,liver cancer HepG2 cells,breast cancer MCF-7 cells and colon cancer HT-29 cells)in vitro.Results:Nine nitrate derivatives were effectively synthesized.Compared with other conjugates,6-phenylhydrazone sinomenine-nitrate conjugates showed outstanding anti-tumor activity in vitro.The anti-proliferation ability of derivative 10d on Hela,MCF-7 and HT-29 was better than that of the positive drug cisplatin,with IC50 being(9.72±0.53),(15.46±8.16),(8.19±1.05)μmol·L-1,respectively.Conclusion:Compound10d has good anti-tumor activity against various tested tumor cells and can be used as a precursor molecule for anti-cancer drugs,which needs to be further studied.
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