棉酚类衍生物的抗肿瘤作用

Experimental antitumor activity of taurine gossypol and harbital gossypol

用小鼠Ｌｅｗｉｓ肺癌、肝癌和肉瘤１８０移植瘤模型研究了牛磺酸棉酚和巴比妥棉酚的抑瘤活性，并用细胞集落形成法研究了牛磺酸棉酚对人胃癌ＢＧＣ８２３和人肝癌ＳＭＭＣ７７２１细胞系的细胞毒作用。结果表明，牛磺酸棉酚２０．０ｍｇ／ｋｇ（ｉｐ）对Ｌｅｗｉｓ肺癌抑瘤率为４２．５％～６９．２％，２５０ｍｇ／ｋｇ（ｉｐ）对肝癌腹水型小鼠生命延长率为７４．３％～１２０％，对肉瘤１８０抑瘤率为２９．５％～３４．７％，１０．０～１２．５ｍｇ／ｋｇ则无抗肿瘤作用。牛磺酸棉酚不同浓度与ＢＧＣ８２３和ＳＭＭＣ７７２１在３７℃作用２４ｈ用集落形成法检测结果表明，该药对两种人癌细胞系的细胞杀灭作用具有剂量依赖性，ＩＣ＿（５０）浓度分别为１９．０和２３．５ｍｇ／Ｌ巴比妥棉酚１００ｍｇ／ｋｇ（ｉｐ）对小鼠肝癌和肉瘤１８０治疗无效。

The antitumor activities of gossypol derivatives,taurine gossypol and barbital gassypol,were studied in vivo and in vitro. The results showed that taurine gossypol could inhibit thegrowth of Lewis lung carcinoma and sarcoma 180 in mice. The inhibitory rates were42.5 %-69.2% and 29.5%- 34.7%,respectively.It also produced a 74.3%- 120% increase inlifespan of hepaloma- bearing miee. Barbital gossypol showed no effect in murine tumor models. Taurine gossypol showed notable cytotoxic activity against two cultured human tumor cell lines,BGC823 and SMMC7721.The IC_(50) values were 19.0 and 23.5 mg/ L,respectively.