首页> 美国卫生研究院文献>Molecules >An Isoxazole Chalcone Derivative Enhances Melanogenesis in B16 Melanoma Cells via the Akt/GSK3β/β-Catenin Signaling Pathways
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An Isoxazole Chalcone Derivative Enhances Melanogenesis in B16 Melanoma Cells via the Akt/GSK3β/β-Catenin Signaling Pathways

机译:异恶唑查尔酮衍生物通过Akt /GSK3β/β-Catenin信号通路增强B16黑色素瘤细胞的黑色素生成

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摘要

Plants or plant-derived products have been routinely used in several traditional medicine systems for vitiligo treatment. It is well-known that melanogenesis can be promoted by certain flavonoid compounds isolated from the traditional Uyghur medicinal plant, Kaliziri. Therefore, Chalcones, one class of flavonoid compounds, has become an interesting target for the development of anti-vitiligo agents. A series of novel isoxazole chalcone derivatives have been designed, synthesized, and evaluated for biological activities by our group. Among them, derivative 1-(4-((3-phenylisoxazol-5-yl)methoxy)phenyl)-3-phenylprop-2-en-1-one (PMPP) was identified as a potent tyrosinase activator with better activity and lower toxicity than the positive control 8-methoxypsoralen (8-MOP) in this study. Further investigations revealed that Akt and GSK3β were the signaling pathways involved in the hyperpigmentation of PMPP. Overall, these studies may provide a convenient and novel approach for the further development of anti-vitiligo agents.
机译:植物或植物来源的产品已常规用于几种传统药物系统中以治疗白癜风。众所周知,从传统维吾尔族药用植物Kaliziri分离出的某些类黄酮化合物可促进黑色素生成。因此,作为一种类黄酮化合物的查耳酮已成为开发抗玻璃体药物的有趣目标。我们小组已设计,合成和评估了一系列新型异恶唑查尔酮衍生物。其中,衍生物1-(4-((3-苯基异恶唑-5-基)甲氧基)苯基)-3-苯基丙-2-烯-1-酮(PMPP)被认为是一种有效的酪氨酸酶激活剂,具有更好的活性和更低的活性。毒性大于阳性对照的8-甲氧基补骨脂素(8-MOP)。进一步的研究表明,Akt和GSK3β是参与PMPP色素沉着过度的信号传导途径。总体而言,这些研究可能为进一步开发抗玻璃胶剂提供方便和新颖的方法。

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