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Anticancer and Anti-inflammatory Effects of Cysteine Metabolites of the Green Tea Polyphenol,(-)-Epigallocatechin-3-gallate

机译:绿茶多酚(-)-表没食子儿茶素-3-没食子酸酯的半胱氨酸代谢产物的抗癌和抗炎作用

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(-)-Epigailocatechin-3-gallate (EGCG) has been shown to have cancer preventive activity in vitro and in vivo. We have previously shown that EGCG can undergo conjugation to cysteine to form 2'-cysteinyl-EGCG and 2"-cysteinyl-EGCG. Studies of thiol-conjugated metabolites of methamphe-tamine indicate that such metabolites are not detoxified but retain biological activity. Here, we examined the growth inhibitory, pro-oxidant, and anti-inflammatory activities of the cysteine metabolites of EGCG. Both compounds dose-dependently inhibited the growth of colon cancer and intestinal cell lines. Both metabolites prevented aberrant arachidonic acid release and nitric oxide production by lipopoly-saccharide-stimulated RAW264.7 cells. Under cell culture conditions, 2"-cysteinyl-EGCG produced H2O2 at a faster rate than EGCG. The results of the present study show that cysteine conjugates of EGCG retain the growth inhibitory, anti-inflammatory, and pro-oxidant activities of EGCG in vitro and may play a role in disease prevention in vivo. These results remain to be confirmed in vivo.
机译:(-)-Epigailocatechin-3-gallate(EGCG)已显示出在体内和体外具有癌症预防活性。先前我们已经证明EGCG可以与半胱氨酸结合形成2'-半胱氨酸-EGCG和2“-半胱氨酸-EGCG。对甲基苯丙胺的硫醇结合代谢产物的研究表明,这种代谢产物没有排毒,但保留了生物活性。 ,我们研究了EGCG的半胱氨酸代谢产物的生长抑制,促氧化剂和抗炎活性,两种化合物均剂量依赖性地抑制结肠癌和肠道细胞的生长,两种代谢产物均能阻止花生四烯酸的异常释放和一氧化氮的产生。通过脂多糖刺激的RAW264.7细胞。在细胞培养条件下,2“-半胱氨酰-EGCG生成H2O2的速度比EGCG更快。本研究的结果表明,EGCG的半胱氨酸缀合物在体外保留了EGCG的生长抑制,抗炎和促氧化活性,并可能在体内预防疾病中发挥作用。这些结果仍有待在体内证实。

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