精制鱼油、磷脂和脂肪酸甘油酯对5-氟尿嘧啶抗癌活性及毒性的影响

Effect of polyunsaturated fatty acids, phospholipid and glyce-ride on the anti-cancer activities and toxicities of 5-fluorouracil

用精制鱼油、磷脂、脂肪酸甘油酯分别与5-氟尿嘧啶制成3种口服制剂:5-FU-PUFA、5-FU-P、5-FU-G,以小鼠肉瘤180（Sarcoma 180,S180）、艾氏实体瘤（Ehrlich carcinoma,ESC）为模型,进行抗癌活性研究,实验结果表明的抑瘤率较市售5-FU片剂提高10％,毒性显著降低（5-FU-PUFA和5-FU片剂的LD50分别为231.26mg·kg-1和104.29mg·kg-1）;5-FU-P、5-FU-G的抑瘤率及毒性与5-FU片剂无显著差别。

Three 5-Fluorouracil (5-FU) oral preparations were formulated by 5-FU with poly-unsaturated fatty acids (PUFAs), phospholipid,glyceride respectively (designated 5-FU-PUFA, 5-FU-P and 5-FU-G). The anti-cancer activities and toxicities of the three 5-Fluorouracil oral preparations were studied with the pharmacodynamic models of sarcoma 180 (S180) and Ehrlich carcinoma (ESC) in mice. The results showed that; the inhibition tumor indexes of S180, EAC in mice of 5-FU-PUFA were about ten percent higher than that of the tablet on market and the toxicity of 5-FU-PUFA was remarkably lower than that of the 5-FU tablet on market (LD50 of 5-FU-PUFA and the tablet on market are 231. 26mg · kg-1 and 104. 29mg · kg-1 in mice respectively); the inhibition tumor indexes of S180 , EAC of 5-FU-P, 5-FU-G and the toxicities of 5-FU-P, 5-FU-G were not greatly different from the 5-FU tablet on market in mice.