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目的:检验构建的蜂毒素改造物是否达到减轻溶血副作用、保留或增强抗肿瘤活性的目的。方法:比较蜂毒素改造物与蜂毒素的体外溶血作用及急性毒性作用;MTT法检测其对H22肝癌细胞的增殖抑制作用;观察蜂毒素改造物瘤内注射对荷肝癌小鼠的抗肿瘤作用。结果:蜂毒素改造物致溶血浓度约为蜂毒素的2.2倍,LD50约为蜂毒素的4倍;蜂毒素改造物对H22肝癌细胞具有增殖抑制作用,呈浓度依赖性;蜂毒素改造物瘤内注射3 d后,荷瘤鼠肿瘤增长速度减缓(P<0.05),中位生存时间长于蜂毒素及生理盐水组,但差异无统计学意义(P>0.05)。结论:对蜂毒素分子一级结构进行适当修饰和改造,理论上和实践上均具有可行性,能达到降低蜂毒素溶血副作用、继续保留其抗肿瘤活性的目的。
OBJECTIVE: To test if the constructed melittin modified material has the purpose of alleviating hemolytic side effects and preserving or enhancing anti-tumor activity. Methods: The in vitro hemolysis and acute toxicity of melittin remover and melittin were compared. MTT assay was used to detect the inhibitory effect on proliferation of H22 hepatoma cells. The antitumor effect of melittin modified tumor on mice bearing hepatoma was observed. Results: The melittin concentration induced by melittin was about 2.2 times higher than that of melittin and the LD50 was about 4 times of that of melittin. The melittin modified substance had inhibitory effect on H22 hepatoma cells in a concentration-dependent manner. After 3 days of injection, tumor growth of tumor-bearing mice slowed down (P <0.05), and the median survival time was longer than that of melittin and saline group, but the difference was not statistically significant (P> 0.05). CONCLUSION: The modification and modification of the primary structure of melittin molecules are both theoretically and practically feasible, and can reduce the melittin hemolytic side effects and keep the antitumor activity.