芦苇根茎中的酚苷单体通过PI3K-Akt和Ras-Raf-MEK-ERK途径抑制黑色素生成。
Phenolic Glycoside Monomer from Reed Rhizome Inhibits Melanin Production via PI3K-Akt and Ras-Raf-MEK-ERK Pathways.
作者信息
Pang Meijun, Yao Hong, Bao Kechen, Xu Ruitian, Xi Rongjiao, Peng Rui, Zhi Hui, Zhang Kuo, He Runnan, Du Yunfei, Su Yanfang, Liu Xiuyun, Ming Dong
机构信息
Medical School, Tianjin University, 92 Weijin Road, Nankai District, 300072, Tianjin, China.
State Key Laboratory of Advanced Medical Materials and Devices, 300072, Tianjin, China.
出版信息
Curr Med Chem. 2024 Sep 27. doi: 10.2174/0109298673341645240919072455.
INTRODUCTION
Melanogenesis, the process responsible for melanin production, is a critical determinant of skin pigmentation. Dysregulation of this process can lead to hyperpigmentation disorders.
METHOD
In this study, we identified a novel extract, (1'S, 2'S)-syringyl glycerol 3'-O-β-D-glucopyranoside (compound 5), and evaluated its anti-melanogenic potential in zebrafish models and assays. Compound 5 inhibited melanin synthesis by 36.66% ± 14.00% and tyrosinase by 48.26% ± 6.94%, surpassing the inhibitory effects of arbutin. Network pharmacological analysis revealed key targets, including HSP90AA1, HRAS, and PIK3R1, potentially involved in the anti-melanogenic effects of compound 5.
RESULTS
Molecular docking studies supported the interactions between compound 5 and these targets. Further, gene expression analysis in zebrafish indicated that compound 5 up-regulates and and subsequently down-regulating tyr, and tyrp1, critical genes in melanogenesis.
CONCLUSION
These findings suggest that compound 5 inhibits melanin production PI3K-Akt and Ras-Raf-MEK-ERK signaling pathways, positioning it as a promising candidate for the treatment of hyperpigmentation.
引言
黑色素生成是负责黑色素产生的过程，是皮肤色素沉着的关键决定因素。这一过程的失调会导致色素沉着紊乱。
方法
在本研究中，我们鉴定出一种新型提取物，（1'S，2'S）-丁香基甘油3'-O-β-D-吡喃葡萄糖苷（化合物5），并在斑马鱼模型和实验中评估了其抗黑色素生成潜力。化合物5抑制黑色素合成36.66%±14.00%，抑制酪氨酸酶48.26%±6.94%，超过了熊果苷的抑制作用。网络药理学分析揭示了关键靶点，包括HSP90AA1、HRAS和PIK3R1，可能参与化合物5的抗黑色素生成作用。
结果
分子对接研究支持了化合物5与这些靶点之间的相互作用。此外，斑马鱼的基因表达分析表明，化合物5上调和，随后下调tyr和tyrp1，这是黑色素生成中的关键基因。
结论
这些发现表明，化合物5通过PI3K-Akt和Ras-Raf-MEK-ERK信号通路抑制黑色素生成，使其成为治疗色素沉着紊乱的有前途的候选药物。
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