Phenolic Glycoside Monomer from Reed Rhizome Inhibits Melanin Production via PI3K-Akt and Ras-Raf-MEK-ERK Pathways.

IF 3.5 4区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current medicinal chemistry Pub Date : 2025-01-01 DOI:10.2174/0109298673341645240919072455

Meijun Pang, Hong Yao, Kechen Bao, Ruitian Xu, Rongjiao Xi, Rui Peng, Hui Zhi, Kuo Zhang, Runnan He, Yunfei Du, Yanfang Su, Xiuyun Liu, Dong Ming

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Abstract

Introduction: Melanogenesis, the process responsible for melanin production, is a critical determinant of skin pigmentation. Dysregulation of this process can lead to hyperpigmentation disorders.

Methods: In this study, we identified a novel Reed Rhizome extract, (1'S, 2'S)-syringyl glycerol 3'-O-β-D-glucopyranoside (compound 5), and evaluated its anti-melanogenic potential in zebrafish models and in vitro assays. Compound 5 inhibited melanin synthesis by 36.66% ± 14.00% and tyrosinase in vivo 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 hsp90aa1.1, hrasa, and pik3r1, and subsequently down-regulating mitfa, tyr, and tyrp1, critical genes in melanogenesis.

Conclusion: These findings suggest that compound 5 inhibits melanin production via PI3K-Akt and Ras-Raf-MEK-ERK signaling pathways, positioning it as a promising candidate for the treatment of hyperpigmentation.

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芦苇酚苷单体通过 PI3K-Akt 和 Ras-Raf-MEK-ERK 途径抑制黑色素生成

简介黑色素生成是黑色素产生的过程，是皮肤色素沉着的关键因素。这一过程的失调可导致色素沉着症：在这项研究中，我们发现了一种新型芦苇根茎提取物--(1'S, 2'S)-syringyl glycerol 3'-O-β-D-glucopyranoside （化合物 5），并在斑马鱼模型和体外试验中评估了其抗黑色素生成的潜力。化合物 5 对黑色素合成的抑制率为 36.66% ± 14.00%，对体内酪氨酸酶的抑制率为 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可能参与化合物 5 抗黑色素生成作用的关键靶点，包括 HSP90AA1、HRAS 和 PIK3R1：分子对接研究证实了化合物 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 能上调 hsp90aa1.1、hrasa 和 pik3r1，随后下调黑色素生成的关键基因 mitfa、tyr 和 tyrp1：这些研究结果表明，化合物 5 可通过 PI3K-Akt 和 Ras-Raf-MEK-ERK 信号通路抑制黑色素生成，因此有望成为治疗色素沉着的候选药物。

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来源期刊

Current medicinal chemistry 医学-生化与分子生物学

CiteScore

8.60

自引率

2.40%

发文量

468

审稿时长

3 months

期刊介绍： Aims & Scope Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.