2,5-二羟基苯乙烷酮：一种从灵芝中分离的抗黑色素生成的生物活性化合物。

IF 5.4 2区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2025-12-01 Epub Date: 2025-04-29 DOI:10.1080/14756366.2025.2495364

Meng Ning, Xiao-Cui Liu, Min He, Xing-Rong Peng, Ming-Hua Qiu

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引用次数: 0

摘要

从灵芝子实体中提取的天然产物2,5-二羟基苯乙酮可以有效、安全地抑制斑马鱼模型中黑色素的产生。为了获得具有更明显抑制作用的类似物，我们合成了9个类似物，并购买了13个类似物。其中，有14个化合物能抑制黑色素的产生，其中5个化合物的抑制作用最为显著，与阳性对照SymWhite®377（苯乙基间苯二酚）相比，抑制率超过80%。本研究阐明了2,5-二羟基苯乙酮及其类似物的黑色素抑制作用，为其在抗黑色素生成试剂中的潜在应用提供了理论基础。

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2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear.

2,5-dihydroxyacetophenone, a natural product from the fruiting bodies of Ganoderma cochlear, can effectively and safely inhibit the production of melanin in zebrafish model. To achieve analogues with more significant inhibition, 9 analogs were synthesised and 13 analogues were purchased commercially. Among them, 14 compounds can inhibit melanin production, of which 5 compounds displayed the most significant inhibitory effects, with inhibitory rates of more than 80%, compared to positive control SymWhite^®377 (phenylethyl resorcinol). This study elucidated the melanin-inhibitory effects of 2,5-dihydroxyacetophenone and its analogs, providing a theoretical foundation for their potential applications in anti-melanogenic reagents.

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来源期刊

Journal of Enzyme Inhibition and Medicinal Chemistry 医学-生化与分子生物学

CiteScore

10.30

自引率

10.70%

发文量

195

审稿时长

4-8 weeks

期刊介绍： Journal of Enzyme Inhibition and Medicinal Chemistry publishes open access research on enzyme inhibitors, inhibitory processes, and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents. Journal of Enzyme Inhibition and Medicinal Chemistry aims to provide an international and interdisciplinary platform for the latest findings in enzyme inhibition research. The journal’s focus includes current developments in: Enzymology; Cell biology; Chemical biology; Microbiology; Physiology; Pharmacology leading to drug design; Molecular recognition processes; Distribution and metabolism of biologically active compounds.