甲氧基-4′氨基查尔酮衍生物对白血病细胞的细胞毒活性

Arina Novilla, M. Mustofa, I. Astuti, J. Jumina, Hery Suwito
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引用次数: 8

摘要

背景:化疗是白血病和其他癌症的常用治疗方法。肿瘤选择性的缺乏和化疗对肿瘤多药耐药的发展,使得肿瘤治疗新策略的开发成为迫切需要。研究了7种查尔酮衍生物对K562和HL-60白血病细胞的抗癌活性和选择性。材料与方法:采用MTS(3-(4,5-二甲基噻唑-2-基)-5-(3-羧基-thoxyphenyl)-2-(4-磺苯基)- 2h -四唑)法测定查尔酮的7个衍生物(化合物1-7)的细胞毒性。计算细胞死亡数据的百分比,然后使用probit分析(SPSS 17)分析IC50。然后根据正常淋巴细胞和癌细胞系(HL-60和K562)的IC50比值计算选择性指数(SI)。结果:除化合物7外,7种化合物在HL-60细胞株中的IC50均低于K562细胞株。查尔酮衍生物中甲氧基的数目和位置影响查尔酮衍生物的抗癌和抗癌选择性。结论:查尔酮衍生物中甲氧基的数目和位置影响查尔酮衍生物的抗癌和抗癌选择性。关键词:抗癌,查尔酮衍生物,甲氧基-4′-氨基查尔酮,白血病,细胞毒性,选择性
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Cytotoxic Activity of Methoxy-4’amino Chalcone Derivatives Against Leukemia Cell Lines
Background: Chemotherapy is a common treatment for leukemia as well as in other cancer treatment. The lack of tumor selectivity and development of multi-drug resistance by chemotherapy caused the development of new strategy in cancer treatment become a pressing need. This study was performed to evaluate the anticancer activity and selectivity of seven derivatives of chalcones against K562 and HL-60 leukemia cell lines. Materials and Methods: The cytotoxicity of chalcone’s seven derivatives (compound 1-7) was tested by using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxyme-thoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) method. The percentage of cell mortality data was calculated then the IC50 was analyzed using probit analysis (SPSS 17). The selectivity index (SI) then calculated from IC50 ratio of normal lymphocyte cells and cancerous cells line (HL-60 and K562).Results: The IC50 of almost all seven tested compounds were lower in HL-60 cell lines than K562 cell lines, except for Compound 7. The number and position of methoxy groups in chalcone derivatives influenced the anticancer and cancer selectivity of chalcone derivatives.Conclusion: The results revealed that the number and position of methoxy groups in chalcone derivatives influenced the anticancer and cancer selectivity of chalcone derivatives.Keywords: anticancer, chalcone derivatives, methoxy-4’-amino chalcone, leukemia, cytotoxic, selectivity
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