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薯蓣皂苷元衍生物的抗肿瘤活性研究

The antitumor activity of the Diosgenin derivatives

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【作者】 吴亚克何谷傅微微郑微曾春玲范举正

【Author】 WU Ya-ke1,HE Gu2,FU Wei-wei1,ZHENG Wei1,ZENG Chun-ling1,FAN Ju-zheng 1(1.West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;2.State Key Laboratory of Biotherapy and Cancer Center,West China Hospital,Sichuan University,Chengdu,Sichuan,610041 P.R.China)

【机构】 四川大学华西药学院四川大学华西医院生物治疗国家重点实验室

【摘要】 目的研究薯蓣皂苷元衍生物在体外的抗肿瘤活性。方法采用MTT法对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2及人慢性髓原白血病细胞株K562进行体外抗肿瘤活性试验。结果薯蓣皂苷元衍生物对4个肿瘤细胞株A375、A549、K562、HepG-2具有不同程度的抗肿瘤活性。结论绝大部分薯蓣皂苷元衍生物对4个肿瘤细胞株有较好的抗肿瘤活性,IC50值都低于30μmol.L-1。化合物22对细胞株A375的IC50=4.48μmol.L-1,化合物9、10对细胞株K562的IC50分别为2.51、2.38μmol.L-1;显示其抗肿瘤活性与对照化合物1-(3β-薯蓣皂苷元)-3-苄基咪唑溴盐相当。

【Abstract】 OBJECTIVE To investigate the anti-tumor activity of diosgenin derivatives in vitro.METHODS The anti-tumor activities of diosgenin derivatives were studied using human malignant melanoma A375 cells,human lung adenocarcinoma A549 cells,human hepatoma HepG-2 cells and Human myeloid leukemia K562 cells in vitro by MTT assay.RESULTS Their anti-tumor activities against cell lines A375,A549,K562,and HepG-2 were tested.Most of the diosgenin derivatives exhibited good anti-tumor activities against all the four cancer cell lines.CONCLUSION Most of the diosgenin derivatives exhibited good anti-tumor activities against all the four cancer cell lines,and all IC50 values were below 30 μmol·L-1.Among these compounds,IC50 value of compound 22 against A375 was 4.48 μmol·L-1,and IC50 values of compound 9,10 against K562 were 2.51 μmol·L-1 and 2.38 μmol·L-1.These showed they had the same anti-tumor activity as 1-(3β-diosgenin)-3-benzylimidazole bromo salt which was used as positive control.

【关键词】 薯蓣皂苷元衍生物抗肿瘤活性K562A375
【Key words】 Diosgenin derivativesAntitumor activityK562A375
  • 【文献出处】 华西药学杂志 ,West China Journal of Pharmaceutical Sciences , 编辑部邮箱 ,2012年01期
  • 【分类号】R285
  • 【被引频次】11
  • 【下载频次】409
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