5－Fu佐剂包裹物的抗肿瘤机理的实验研究

Experimental Studying on Antitumor Mechanism of 5-Fu Entrapped by FCA

本文较系统地作了福氏完全佐剂（Ｆｒｅｕｎｄ＇ｓｃｏｍｐｌｅｔｅａｄｊｕｖａｎｔ，ＦＣＡ）包裹５－Ｆｕ的抗肿瘤机理的实验研究。ＦＣＡ包裹５－Ｆｕ相的对包封率平均为：８４．５％。５－Ｆｕ－ＦＣＡ体外缓释试验结果和Ｗｉｓｔａｒ大鼠体内５－Ｆｕ及５－Ｆｕ－ＰＣＡ吸收试验均表明：５－Ｆｕ用ＦＣＡ包裹后，在体内外具有缓慢释放的作用。５０～２００μｇ浓度的５－Ｆｕ在不同作用时间里对肿瘤细胞增殖抑制率随作用时间延长而增加，统计三次实验结果（对Ｈ＿（２２）肝癌细胞），５－Ｆｕ２００μｇ／ｍｌ作用１０分钟对肿瘤细胞增殖抑制率为３４．６６±６．０２；５０μｇ／ｍｌ作用２４小时的抑制率为６１．３５±７．１７。两者比较差别显著（Ｐ＜０．０８）。结果提示：在肿瘤局部低浓度５－Ｆｕ的持续存在，在一定情况下，对肿瘤的抑制作用更强。

FCA (Freund's Complete Adjuvant,FCA)is usually used to entrap antigen to immunize animal,We entrapped 5-Fu with FCA to slow their release in vivo and'by means of this to reduce their side effects and to augment their antituor effects.We called these FCA entrapped 5-Fu, 5- Fu-FCA.The average rate of entrapping 5-Fu by FCA is 84. 5%.The experiment showed that 5- Fu-FCA had a slow release of 5-Fu in vitro and in vivo.The proliferation inhibition rate of H22 tumorcells by higher concentration of 5-Fu (200μg/ml,10min )was 34. 66±6.02,significantly higher than that by lower concentration (50μg/ml)of 5-Fu and the same time(13.46±11.54,P<0.01),but lower than that by lower concentration(50μg/ml) of 5-Fu and longer time(24h,61.35 ±7.18,P<0.008).We conclude that:(1)the release of 5-Fu is markedly reduced in vivo by FCA entrapping;(2)lower concentration of 5-Fu aam longer time may have stronger antitumor effects.