基于均匀设计法对蟾酥中单体体外抗癌配伍研究  

Optimized compatibility of anticancer monomers from Venenum Bufonis by uniform design

作　　者：杨爽[1] 马晓兵[2] 张波[3] 

机构地区：[1]沈阳医学院附属中心医院药剂科,沈阳110024 [2]中国人民解放军第205医院器材科,锦州121004 [3]中山大学中山医学院,广州510080

出　　处：《中国新药杂志》2014年第17期2077-2080,共4页Chinese Journal of New Drugs

摘　　要：目的:优选蟾酥中3种单体(蟾蜍灵、华蟾蜍精、脂蟾毒配基)体外抗癌最佳配伍。方法:采用均匀设计法分成7组给药,分别为丝裂霉素组及给药A-F组,分别作用于肺癌(H441)宫颈癌(Hela)和白血病(HL-60)细胞株,采用WST-8细胞计数试剂盒,评价对3种癌细胞的抑制作用,筛选蟾蜍灵、华蟾蜍精、脂蟾毒配基最佳配伍。对最佳配伍进行比较和验证试验。结果:与对照组比较,在肺癌(H441)和宫颈癌(Hela)细胞上A,B组抑制作用与丝裂霉素相当(P>0.05),在白血病(HL-60)细胞上A组抑制作用于丝裂霉素相当(P>0.05)。经多元统计分析,蟾蜍灵、华蟾蜍精、脂蟾毒配基最佳配伍组合为100,100,15μmol·L^(-1)。结论:应用均匀设计和体外抗癌作用评价相结合确定蟾酥中3种单体蟾蜍灵、华蟾蜍精、脂蟾毒配基最佳配伍的方法是可行的,验证实验表明,蟾蜍灵、华蟾蜍精、脂蟾毒配基最佳配伍体外抑制癌细胞的作用与丝裂霉素相当,略好于组合中的每个单体。Objective： To optimize the compatibility of three anticancer monomers （bufalin, cinobufagin, resibufogenin） from Venenum Bufonis. Methods： Dosage regimen were divided into seven （mitomycin and the test agents A - F） groups by uniform design, and their inhibitory effect was evaluated in lung cancer （ H441 ） , cervical cancer （Hela） and leukemia （HL-60） cells, respectively, by WST-8 cell count kits. The best compatibility of bu- falin, cinobufagin and resibufogenin was screened. Then a further experiment for comparing and verifying the effi- cacy of the best compatibility was conducted. Results： Compared with the control group, inhibitory effect of A and B was similar to that of mitomycin in lung cancer （H441） and cervical cancer （Hela） cells （P 〉0.05）, and in- hibitory effect of A was similar to that of mitomycin in leukemia （HL-60） ceils （P 〉 0.05）. Multiple regression a- nalysis showed that the best compatibility of bufalin, cinobufagin and resibufogenin was 100, 100 and 15 μmol.L-1. Conclusion： It is feasible to screen the best compatible ratio of bufalin, cinobufagin and resibufogenin by combi- ning uniform design with anticancer evaluation in vitro. The verification experiment indicates that anticancer effect of the optimized compatibility of bufalin, cinobufagin and resibufogenin are the same as mitomycin in vitro, slightlybetter than other combinations of the monomers.

关 键 词：蟾蜍灵 华蟾蜍精 脂蟾毒配基 均匀设计 抑制作用 

分 类 号：R961[医药卫生—药理学]