果胶阿霉素的抗肿瘤活性研究

发布时间：2018-06-29 16:18

本文选题：PAC + ADM　；参考：《四川师范大学学报(自然科学版)》2016年06期

【摘要】：探讨果胶阿霉素的抗肿瘤活性,将果胶与阿霉素经过缩合反应生成果胶阿霉素轭合物(PAC);通过高压均质和冷冻干燥的方法制备成PAC纳米混悬剂;采用CCK-8方法考察PAC对8种人源性肿瘤细胞株的生长抑制作用;以KM小鼠H22腹水为模型,考察PAC对腹水瘤的抗肿瘤活性、对免疫器官的影响以及H22腹水小鼠生存期的影响;初步考察PAC对KM小鼠的急性毒性,并与阿霉素作对比.PAC对8种人源性肿瘤细胞株均有抑制作用,在阿霉素质量浓度为4、8μg/ml时,对各种肿瘤细胞的生长抑制率达到50%以上.PAC能有效地抑制H22腹水的生长,在阿霉素质量分数为2.5、5、10 mg/kg时产生的腹水量分别为3.32±0.41、0.96±0.17、0 m L.生存期方面,从接种肿瘤后至45 d时,PAC 10 mg/kg组未出现小鼠死亡,PAC 5 mg/kg组和2.5 mg/kg组存活率分别为75%、60%,阿霉素组2.5 mg/kg存活率80%,而对照组在25d以内全部死亡.PAC对KM小鼠的LD50为49.32 mg/kg,而阿霉素对KM小鼠的LD50为14.70 mg/kg.结论:PAC能有效地抑制细胞的生长,有良好的抗肿瘤作用.PAC能有效地抑制H22腹水的产生,对免疫器官的影响小于阿霉素,能明显延长腹水癌小鼠的生存期.PAC的LD50较ADM提高了2.36倍,毒性反应大大降低,有望开发成一种高效低毒的高分子抗癌药物.
[Abstract]:The antitumor activity of pectin doxorubicin was studied. The Pectin adriamycin conjugate (PAC) was synthesized by condensation of pectin and doxorubicin, and the suspension was prepared by high pressure homogenization and freeze-drying. The inhibitory effects of PAC on the growth of eight human tumor cell lines were investigated by CCK-8 method, and the antitumor activity of PAC on ascites, the effects of PAC on immune organs and the survival time of H22 ascites mice were investigated using KM mouse H22 ascites as a model. The acute toxicity of PAC to km mice was preliminarily investigated. Compared with adriamycin, PAC had inhibitory effects on eight human tumor cell lines, when the concentration of adriamycin was 4 渭 g/ml. The growth inhibition rate of various tumor cells was more than 50%. PAC could effectively inhibit the growth of H22 ascites. When the adriamycin content was 2. 5 渭 m / 10 mg/kg, the amount of ascites produced was 3. 32 卤0. 41 卤0. 96 卤0. 17mL, respectively. In terms of survival, From 45 days after inoculation to 45 days after inoculation, the survival rates of PAC5 mg/kg group and 2.5 mg/kg group were 7560mg / kg, respectively. The survival rate of doxorubicin group was 80%, while the LD50 of the control group was 49.32 mg / kg / kg of km mice, while the LD50 of the control group was 49.32 mg / kg / kg. The LD50 of mycin to km mice was 14.70 mg / kg. Conclusion the growth of H22 ascites can be effectively inhibited by% -PAC, and the effect on immune organs is less than that of adriamycin, and the LD50 of PAC can be increased 2.36 times than that of ADM, and the survival time of mice with ascites carcinoma can be prolonged by 2.36 times than that of ADM. The toxic reaction is greatly reduced, and it is expected to develop a high-efficient and low-toxic high-molecular anticancer drug.
【作者单位】：四川师范大学生命科学学院;重庆莱美药业股份有限公司;
【基金】：科技部新药创制“科技重大专项”(2011ZX09102-001)
【分类号】：R979.1

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