The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells
10.3969/j.issn.1006-0111.2017.04.005
- VernacularTitle:靶向肺癌干细胞的海绵抗肿瘤活性化合物的发现
- Author:
Man LIU
1
;
Liyun LIU
;
Fan SUN
;
Houwen LIN
Author Information
1. 上海交通大学医学院附属仁济医院药学部
- Keywords:
aaptamine alkaloid;
lung cancer stem cell;
proliferation;
AP-1
- From:
Journal of Pharmaceutical Practice
2017;35(4):304-307
- CountryChina
- Language:Chinese
-
Abstract:
Objective To screen the active compounds targeting lung cancer stem cells (LCSCs) from the sponge Aaptos aaptos.Methods The A549-Nanog-GFP model of LCSCs was constructed.Western blot and immunofluorescence were used to examine the expression of pluripotency markers in screening model.The established LCSCs model was used to screen 8 fractions of Aaptos aaptos dichloromethane extract.The active fraction was separated by various chromatographic methods.CCK8 assay was used to screen the compounds for anti-LCSCs activity in vitro.Results LCSCs model with high expression of CD44 and ALDH1A1 protein was successfully constructed.The fraction D6 showed significant inhibitory activity in LCSCs(P<0.01).Four aaptamine alkaloids were isolated from this fraction.Compound AP-1 has good activity against LCSCs(P<0.01)with IC50 value(3.84±0.12) μmol/L.Conclusion AP-1 isolated from the spongeAaptos aaptos exhibited significant activity against LCSCs.
