氯化两面针碱体外和体内的抗肿瘤作用

目的观察氯化两面针碱(NC)的抗肿瘤作用。方法采用MTT法观察NC体外对肿瘤细胞存活的影响。移植性S180肉瘤模型小鼠,ip给予NC,每天1次,共10d,测瘤重,计算抑瘤率,并在电镜下观察移植瘤细胞的超微结构。腹水型H22肝癌模型小鼠,sc给予NC,每天1次,共10d,观察小鼠的存活时间,计算生命延长率。结果体外给予NC0.625,1.25,2.5,5.0和10.0mg·L-1可浓度依赖性地降低人鼻咽癌细胞CNE1、人肺癌细胞SPC-A-1和人乳腺癌细胞MDA-MB-231等9种肿瘤细胞的存活率,作用48h平均IC50为(3.33±0.28)mg·L-1。体内给予NC2.5,5.0和10.0mg·kg-1对小鼠S180肉瘤的抑瘤率分别为1.95%,27.3%和42.9%,对腹水型H22肝癌小鼠的生命延长率分别为35.7%,71.4%和85.7%。电镜下可见NC10.0mg·kg-1组S180移植瘤细胞核染色质浓缩并边缘化,核碎裂,胞浆空泡化明显。结论NC体内外应用均具有明显的抗肿瘤作用。

Antitumor effect of nitidine chloride in vitro and in vivo

AIM To investigate the antitumor effect of nitidine chloride（NC） in vitro and in vivo. METHODS MTT assay was used to examine the survival of tumor cells in vitro. The implanted sarcoma 180 (S180) model mice were ip given NC, once daily for 10 d, then the tumor weights were measured and the tumor inhibition rates were calculated. The ultrastructure of implanted S180 cells was observed with electron microscope. The ascitic-tumor model mice induced by hepatocarcinoma H22 were sc given NC, once daily for 10 d, then mouse life span was recorded, and the life prolonged rates were calculated. RESULTS In vitro, NC 0.625, 1.25, 2.5, 5.0 and 10.0 mg·L^-1 decreased survival rates of tumor cells in a concentration-dependent manner, and the average of IC₅₀ value for 48 h was （3.33±0.28） mg·L^-1. In vivo, NC 2.5, 5.0 and 10.0 mg·kg^-1 inhibited the growth of S180 tumor and tumor inhibition rates were 1.95%, 27.3% and 42.9%, respectively. NC significantly prolonged survival time of H22 ascitic-tumor mice, and life prolongation rate was 35.7%, 71.4% and 85.7%, respectively. Condensation of chromatin at margins of nuclei, disintegration of nucleoli and vacuoles in cytoplasm were observed in NC 10.0 mg·kg^-1 group with electron microscope. CONCLUSION NC has significant antitumor effect in vitro and in vivo.