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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Anti-tumor-promoting activity of simple models of galactoglycerolipids with branched and unsaturated acyl chains.
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Anti-tumor-promoting activity of simple models of galactoglycerolipids with branched and unsaturated acyl chains.

机译：具有分支和不饱和酰基链的半乳糖甘油脂简单模型的抗肿瘤促进活性。

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摘要

Six new galactoglycerolipid analogs, in which one or two 4-methylpentanoyl or trans-2-butenoyl groups are linked to the 2-O-beta-D-galactosylglycerol skeleton, were tested for their anti-tumor-promoting activity using a short-term in vitro assay for Epstein-Barr virus early antigen (EBV-EA) activation. All these compounds were more active than their linear or saturated reference compounds in inhibiting the EBV activation promoted by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA), the diester 1-O-(4-methylpentanoyl)-2-O-[6-O-(4-methylpentanoyl)-beta-D-galactopyranos yl]-sn-glycerol resulting the most active glycoglycerolipid analog till now tested. Four compounds (three butenoates and one 4-methylpentanoate), when tested in the in vivo two-stage carcinogenesis test, exhibited also inhibitory effects on mouse skin tumor promotion.
机译：测试了六个新的半乳糖甘油类似物，其中一个或两个4-甲基戊酰基或反-2-丁烯酰基与2-O-β-D-半乳糖基甘油骨架相连，并通过短期测试了它们的抗肿瘤活性EB病毒早期抗原（EBV-EA）激活的体外测定。所有这些化合物在抑制肿瘤启动子12-O-十四烷酰基phorbol-13-乙酸酯（TPA），二酯1-O-（4-甲基戊酰基）-2--促进的EBV活化方面均比其线性或饱和参照化合物更具活性。直到现在测试的O- [6-O-（4-甲基戊酰基）-β-D-吡喃并吡喃糖基] -sn-甘油产生最活跃的糖脂类类似物。在体内两阶段致癌性试验中测试时，四种化合物（三种丁烯酸酯和一种4-甲基戊酸酯）也表现出对小鼠皮肤肿瘤促进作用的抑制作用。

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