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目的制备苦参碱-美法仑复合物(MAT-MEL),测定其抗肿瘤活性。方法以槐果碱和美法仑为原料,利用拼合原理制备MAT-MEL;采用MTT法在体外测定复合物对人乳腺癌MCF-7细胞、人肝癌SMMC-7721细胞及小鼠骨肉瘤S_(180)细胞的生长抑制作用;采用S_(180)小鼠移植肿瘤模型评价复合物的体内抗肿瘤活性。结果 MAT-MEL的收率为61%,其结构通过核磁、质谱和元素分析得到确证;对3种细胞株的IC_(50)分别为116.7±27.8、56.3±19.5、1.9±1.0 nmol·m L~(-1);3、6、9μmol·kg~(-1)的复合物对小鼠S_(180)的抑瘤率分别为49.56%、54.58%、77.18%。结论 MAT-MEL具有显著的抗肿瘤活性。
Objective To prepare matrine-melphalan complex (MAT-MEL) and measure its anti-tumor activity. Methods MAT-MEL was prepared by the combination principle of sophocarpine and melphalan. MTT assay was used to determine the inhibitory effect of the complex on human breast cancer MCF-7 cells, human hepatocellular carcinoma SMMC-7721 cells and mouse osteosarcoma S 180 ) Cell growth inhibition; S_ (180) mice transplanted tumor model to evaluate the in vivo antitumor activity of the complex. Results The yield of MAT-MEL was 61%. The structure of MAT-MEL was confirmed by NMR, MS and elemental analysis. The IC 50 of the three cell lines were 116.7 ± 27.8, 56.3 ± 19.5 and 1.9 ± 1.0 nmol · m L ~ (-1). The inhibitory rates of 3, 6, 9μmol · kg ~ (-1) complex on mice S_ (180) were 49.56%, 54.58% and 77.18%, respectively. Conclusion MAT-MEL has significant anti-tumor activity.