论文部分内容阅读
目的为进一步提高苦参碱的抗肿瘤活性,基于分子杂合策略,设计合成N-苄基苦参酸一氧化氮杂合体衍生物,并对其体外抗肿瘤活性进行初步研究。方法将NO供体硝酸酯通过连接基团与N-苄基苦参酸的羧基连接制得NO供体型N-苄基苦参酸衍生物。采用MTT法测定了目标化合物对人肝癌细胞(HepG2)增殖的体外抑制活性。结果与结论合成了14个结构新颖的N-苄基苦参酸一氧化氮杂合体衍生物,其结构经MS、IR、1H-NMR确证,且目标化合物均具有较苦参碱强的增殖抑制活性。
OBJECTIVE To further improve the antitumor activity of matrine, based on the molecular hybrid strategy, a derivative of N-benzyl-matrine nitric oxide was designed and synthesized, and its antitumor activity was studied in vitro. Methods NO donor nitric acid ester was linked to the carboxyl group of N-benzyl kensoic acid via a linker to prepare NO donor N-benzyl kuh acid derivative. The inhibitory activity of the target compounds on the proliferation of human hepatocellular carcinoma cells (HepG2) was measured by MTT assay. RESULTS AND CONCLUSIONS A total of 14 novel derivatives of N-benzyl-matrine nitric oxide were synthesized and their structures were confirmed by MS, IR and 1H-NMR. All of the target compounds exhibited stronger inhibition of proliferation than matrine active.