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LIU Man, LIU Liyun, SUN Fan, LIN Houwen. The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(4): 304-307. doi: 10.3969/j.issn.1006-0111.2017.04.005
Citation: LIU Man, LIU Liyun, SUN Fan, LIN Houwen. The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(4): 304-307. doi: 10.3969/j.issn.1006-0111.2017.04.005

The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells

doi: 10.3969/j.issn.1006-0111.2017.04.005
  • Received Date: 2017-03-28
  • Rev Recd Date: 2017-05-10
  • 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 sponge Aaptos aaptos exhibited significant activity against LCSCs.
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The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells

doi: 10.3969/j.issn.1006-0111.2017.04.005

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 sponge Aaptos aaptos exhibited significant activity against LCSCs.

LIU Man, LIU Liyun, SUN Fan, LIN Houwen. The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(4): 304-307. doi: 10.3969/j.issn.1006-0111.2017.04.005
Citation: LIU Man, LIU Liyun, SUN Fan, LIN Houwen. The discovery of antitumor compounds from marine sponge targeting lung cancer stem cells[J]. Journal of Pharmaceutical Practice and Service, 2017, 35(4): 304-307. doi: 10.3969/j.issn.1006-0111.2017.04.005
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