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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design, synthesis and evaluation of PEGylated lipoic acid derivatives with functionality as potent anti-melanogenic agents.
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Design, synthesis and evaluation of PEGylated lipoic acid derivatives with functionality as potent anti-melanogenic agents.

机译：具有功能强大的抗黑色素生成剂的聚乙二醇化硫辛酸衍生物的设计，合成和评估。

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摘要

The novel PEGylated lipoic acid (LA) derivatives with functionality were synthesized in satisfactory yield by simple procedures and evaluated about its anti-melanogenic activity on the B16F10 melanoma cells. Grafting a PEG moiety onto the carboxyl group of LA has reduced the cell cytotoxicity and provided the water solubility and functionality to incorporate the other bioactive moieties. We have found that derivatives showed inhibition of melanin formation by up to 36.5% at 0.1 mM, whereas LA decreased the melanin formation by 8.6%. In addition, it also inhibits at least 86.4% UV-induced MMP-1 expression at 0.1 mM which is higher than LA. These data suggest that the novel PEGylated LA derivatives with functionality may thus serve as a potentially effective anti-melanogenic and anti-aging agent.
机译：通过简单的程序以令人满意的产率合成了具有功能性的新型PEG化硫辛酸（LA）衍生物，并评估了其对B16F10黑色素瘤细胞的抗黑色素生成活性。将PEG部分接枝到LA的羧基上可降低细胞的细胞毒性，并提供水溶性和结合其他生物活性部分的功能。我们发现，衍生物在0.1 mM时可抑制黑色素形成达36.5％，而LA可将黑色素形成抑制达8.6％。另外，它还以0.1 mM抑制至少86.4％的紫外线诱导的MMP-1表达，高于LA。这些数据表明具有功能性的新的PEG化的LA衍生物因此可以用作潜在有效的抗黑色素和抗衰老剂。

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