异紫堇碱衍生物抗菌及抑肿瘤作用的研究

研究异紫堇碱（isocorydine，ICD）半合成衍生物8-氨基-异紫堇碱（8-NH2-ICD）的抗菌及抑制肿瘤生长作用。用琼脂扩散法和最低抑菌浓度测定法测定8-NH2-ICD的抑菌作用，用MTT法测定该化合物对细胞增殖的抑制作用。不同浓度的8-NH2-ICD对7种常见致病菌具有明显抑制作用，其中对伤寒沙门氏菌和大肠埃希菌的抑制作用显著高于其它菌，8-NH2-ICD对产气杆菌的抑制作用相对较弱。8-NH2-ICD对9种肿瘤细胞系生长抑制程度不同，对胃腺癌细胞MGC803和胶质瘤细胞M059K的增殖具有较强的抑制作用，对人正常细胞生长抑制作用较弱。8-NH2-ICD具有较强的抑制病原菌和抑制肿瘤细胞生长的作用。
To investigate the bacteriostasis activity and tumour inhibitory effect of semi-synthetic derivate of isocorydine 8-amino-isocorydine (8-NH2-ICD). The bacteriostasis activities of alkaloid in vitro were tested with agar diffusion method and minimal inhibitory concentrations (MIC). Inhibitory activity on proliferation of tumour cells with treated by 8-NH2-ICD were measured by MTT assay. The results show there is a dramatic bacteriostasis activity on Salmonella typhi and Escherichia coli, and relatively mild effect on Enterobacter aerogenes. MGC803 cell and M059K cell proliferation effect were dramatically inhibited by 8-NH2-ICD in vitro. The anti-tumour activity was gradually enhanced with the alkaloid variety of dose. However, 8-NH2-ICD have been demonstrated with low toxity to normal fibroblasts MRC-5 till concentration up to 200 mol/L. To our knowledge, this is the first time that 8-NH2-ICD has anticancer and antibacterial activity is reported