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目的比较抗菌肽Maximin衍生物(M1~M19)的体外杀精效果和细胞毒性作用,筛选有进一步研究价值的候选体外杀精剂。方法利用Sander-Cramer方法评价抗菌肽的体外杀精效果;CCK-8试剂盒测定抗菌肽对Hela-229的细胞毒性,筛选出具有较强杀精作用和低细胞毒性的抗菌肽。结果 19种抗菌肽衍生物中,M1、M7、M11、M15和M17五种抗菌肽在2 000mg/L时均能完全制动精子,其中100%制动精子的最低浓度EC100分别是:M7=M11=2 000mg/L,M1=M15=M17=1 500mg/L;利用Hela-229细胞分析细胞毒性时,M11的细胞毒性明显低于其他4种抗菌肽,表现出较高的安全性。结论对19种抗菌肽衍生物的体外研究表明,抗菌肽M11具有较强的杀精作用,且细胞毒性低,有望成为体外杀精剂的候选药物。
Objective To compare the in vitro spermicidal and cytotoxic effects of the antibacterial peptide Maximin derivatives (M1 ~ M19), and to screen for candidate in vitro spermicides with further research value. Methods Sander-Cramer method was used to evaluate the in vitro spermicidal effect of antimicrobial peptides. CCK-8 kit was used to determine the cytotoxicity of antimicrobial peptides to Hela-229 cells. The antimicrobial peptides were screened with strong killing effect and low cytotoxicity. Results Among the 19 antimicrobial peptide derivatives, the five antimicrobial peptides M1, M7, M11, M15 and M17 could completely brake sperms at 2000mg / L, among which the lowest EC100 of 100% brake sperm were M7 = M11 = 2000mg / L, M1 = M15 = M17 = 1500mg / L; when using Hela-229 cells to analyze cytotoxicity, M11 cytotoxicity was significantly lower than the other four kinds of antimicrobial peptides, showing higher safety. Conclusion In vitro studies of 19 antimicrobial peptide derivatives showed that the antimicrobial peptide M11 has strong spermicidal activity and low cytotoxicity and is expected to be a candidate drug for in vitro spermicide.