| Objective: To observe the effect of Small-molecule antagonists of apoptosis suppressor XIAP(Embelin)on the multidrug resistance cell line SGC-7901/VCR in vitro and in vivo, moreover to investigate the relationship between XIAP and GST-π.Methods: To observe the SGC-7901,SGC-7901/VCR cellular morphology with HE staining and Wright's staining in vitro; SGC-7901,SGC-7901/VCR cell lines were treated with Embelin,Embelin +VCR,VCR in vitro, MTT assay was performed to examine the IC50 and CI. The expressions of XIAP mRNA were examined by RT-PCR before and after treatment respectively, The levels of XIAP and GST-π's proteins in SGC-7901,SGC-7901/VCR were determined by Western blot befor and after treatment respectively. The influence of Embelin,Embelin combined with VCR,VCR on the weight of human gastric cancer xenograft in nude mice was observed in vivo.Results: MTT validated that the CI of SGC-7901/VCR was 48.17; The IC50 of VCR,Embelin and drug combination were 2.39μM, 6.48μM, 6.34μM respectively in SGC-7901/VCR cell line, The IC50 of Embelin and drug combination were 0.05μM, 6.37μM, 0.04μM respectively in SGC-7901 cell line;CI>1 at the different inhibition ratio by MTT assay. The Western blot validated that Between SGC-7901/VCR cell lines and SGC-7901 cell lines there was a significant difference in the expression of XIPA and GST-π(P<0.05), in vivo experiment weight inhibiton rates tumor were 40.28%, 88.58%, 48.43% respectively.Conclusion: Embein was good for multidrug resistance cell line SGC-7901/VCR,there is no Cross Resistance, but show antagonistic effect when combination with VCR on the dose of our experiment. There is some relationship between XIAP and GST-π. But the mechanism is not very clearly. |
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