羟基胆烷酸类和羟基胆甾烷类化合物的体内抗癌活性研究

The Study on Antitumor Activity of Hydroxycholestanes and Hydroxycholanic Acids

目的 考察3β,5α,6β-三羟基胆烷-4-酸甲酯(LS01)、胆甾烷-3β,5α,6β-三醇(LS19)和胆-4-烯-3β,6β-二醇(LS20)的体内抗癌活性和急性毒性.方法 体内抗癌活性实验按<抗肿瘤药药效学技术要求>的规定进行.急性毒性实验按常规方法进行.结果 灌服和腹腔注射LS20对小鼠S180无明显的抑制作用;灌服和腹腔注射LS19与LS01对小鼠S180皆有明显的抑制作用,且LS19较好.灌服和腹腔注射LS01的最大耐受量分别为8000,658 mg·kg-1;灌服LS19的最大耐受量为5 000 mg·kg-1, 腹腔注射LS19的LD50及其95%置信限分别为169 mg·kg-1、152～186 mg·kg-1.结论 LS19和LS01具有一定的体内抗癌活性.

OBJECTIVE To investigate the in vivo anticancer activity of methyl 3β,5α,6β-trihydroxycholan-24-oate(LS01),cholestan-3β,5α,6β-triol(LS19) and cholest-4-en-3β,6β-diol(LS20).METHODS The in vivo anticancer activity was proceeded in according to 'Technological requirements of Pharmacodynamics of Antitumor Drugs'.and acute toxicity was conducted with routine methods. RESULTS LS20 possessed no obvious inhibitory action on solid sarcoma 180 in mice administered orally and ip.LS19 and LS01 had obvious inhibitory action on solid sarcoma 180 in mice administered orally and ip,and LS19 was better.The acute LD50 value and 95% confidence limits of LS19 for mice was 169 mg·kg-1 and 152~186 mg·kg-1 by oral administration,and the maximum tolerance dosages of oral LS19,oral LS01 and ip LS01 were respectively 5 000 mg·kg-1,8000 mg·kg-1 and 658 mg·kg-1.CONCLUSION LS19 and LS01 possesses certain anticancer activities.