Cai B C, Wang T S, Kurokawa M, Shiraki K, Hattori M
Institute of Traditional Chinese Medicine & Pharmacology, Nanjing University of Traditional Chinese Medicine, China.
Zhongguo Yao Li Xue Bao. 1998 Sep;19(5):425-8.
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.
Using cell culture, their inhibitory effects on Vero cell growth-inhibition assay, and host cell DNA synthesis by [3H]thymidine ([3H]TdR) uptake assay.
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.
Processing of nux vomica plays a critical role in its toxicity.
考察马钱子种子未经炮制及经多种传统炮制方法炮制后的6种马钱子生物碱粗提物及从中分离得到的13种马钱子生物碱单体的细胞毒性。
采用细胞培养技术，通过Vero细胞生长抑制试验及[3H]胸腺嘧啶核苷（[3H]TdR）掺入法检测其对宿主细胞DNA合成的抑制作用。
在细胞生长抑制试验及[3H]TdR掺入试验中，炮制后马钱子种子的半数抑制浓度（IC50）分别为未炮制马钱子种子的155%和212%。13种化合物的IC50分别为0.450.80 mmol·L-1和0.5012 mmol·L-1。与其他传统炮制方法或未炮制相比，砂烫法具有较宽的安全范围。马钱子生物碱的异构体及其氮氧化物在这些生物碱中细胞毒性较低。异布鲁生氮氧化物细胞毒性最低。马钱子生物碱异构体及氮氧化物含量在砂烫品中最高。
马钱子炮制对其毒性起关键作用。
