MC1R天然拮抗剂的高通量初步筛选

为了寻找高效稳定的黑色素皮质激素受体1(melanocortin 1 receptor, MC1R)的拮抗剂，利用作者前期工作中建立的高通量筛选方法对 1 000种中草药提取物进行了筛选，并检测了这些提取物对小鼠B16-F1细胞系黑色素生成量的影响.结果表明，补骨脂等10种粗提物具有拮抗促黑激素（MSH）激活MC1R的作用.其中，补骨脂、破茎松萝、桑根和太白树粗提物能明显降低B16-F1细胞的产黑色素能力，但其机制有所不同，补骨脂主要作用于MSH对C1R的激活过程，而其余3种提取物基本上直接作用于cAMP通路.本实验为利用上述中草药调控皮肤细胞中的黑色素生成提供了初步线索.

High-Throughput Screening of Crude Antagonists of MC1R

To find high effect and stable properties crude antagonists of melanocortin 1 receptor (MC1R), one thousand refreshants from Chinese herbs were screened with the high throughput method established in our earlier work, and the effect on melanogenesis of B16-F1 mice malenoma cells were measured. The results show that ten Chinese herb refreshants inhibited the activity of MSH on MC1R, in which malaytea scurfpea fruit, Pojingsongluo mulberry root and Taibai tree reduced the melanogenesis of B16-F1 cell, but the reduced mechanism were different. The inhibitory effect of malaytea scurfpea fruit mainly aim at MSH's active progress for MC1R, while other three Chinese herbs directly act on cAMP pathway. The results provide elementary clew for control of melanogenesis in skin cell with these Chinese herbs. 