马钱子生品及炮制品中马钱子类生物碱的细胞毒性

目的：测定６种中药马钱子生品及不同炮制品的总生物碱以及１３个单体生物碱的细胞毒性。方法：采用细胞培养法观察马钱子生物碱对Ｖｅｒｏ－细胞增殖抑制和［＾３Ｈ］胸腺啶核苷酸参入法对宿主细胞内ＤＮＡ合成的影响。结果：砂炒炮制品的ＩＣ５０值分别是生品的１５５％和２１２％。１３个化合物的ＩＣ５０值分别是０．４５－０．８０ｍｍｏｌ·Ｌ＾－１和０．５０－１２ｍｍｏｌ·Ｌ＾－１。马钱子中异型生物碱及氮氧化合物在砂炒

Cytotoxicities of alkaloids from processed and unprocessed seeds of Strychnos nux-vomica.

AIM: To examine the cytotoxicities of 6 crude Strychnos alkaloid fractions from the seeds of Strychnos nux-vomica unprocessed or processed with various traditional processing methods and 13 pure Strychnos alkaloids from the fractions. METHODS: Using cell culture, their inhibitory effects on Vero cell growth-inhibition assay, and host cell DNA synthesis by [3H]thymidine ([3H]TdR) uptake assay. RESULTS: The IC50 of processed seeds were 155% and 212% of unprocessed ones in cell growth-inhibition assay and in [3H]TdR uptake assay, respectively. The IC50 of 13 compounds were 0.45-0.80 mmol.L-1 and 0.50-12 mmol.L-1, respectively. The processing method with sand bath exhibited a wide safety margin compared with other traditional processing methods or no processing. The isomers of Strychnos alkaloids and their N-oxides showed much lower cytotoxicities among these alkaloids. Isobrucine N-oxide showed the lowest cytotoxicity. The contents of isomers and N-oxides of Strychnos alkaloids were the highest in the sand processing. CONCLUSION: Processing of nux vomica plays a critical role in its toxicity.