强效卤代黄酮衍生物：合成、分子对接及抗酪氨酸酶活性研究。

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2024-05-03 DOI:10.1080/10286020.2023.2264784

Fatin Farhana Baharuddin , Nadiah Mad Nasir , Bimo Ario Tejo , Soo Peng Koh , Shuruti Ramakrishnan , Nur Qurratu Ain A. Nordin , Anis Nasuha Adzahar , Pavithren Devakrishnan , Salsabiilaa Mohd Razib

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引用次数: 0

摘要

酪氨酸酶抑制剂可以减少皮肤美白中黑色素的产生，但现有的一些产品可能会伤害皮肤。本研究在蘑菇双孢蘑菇中发现了六种抑制酪氨酸酶50%以上的化合物。化合物11对L-酪氨酸和L-DOPA底物显示出强抑制作用（92.2%和86.7%），而化合物13对这两种底物显示出高抑制作用（96.0%和62.0%）。分子对接模拟显示，化合物11和13在酶的变构位点结合。基于这些发现，黄酮衍生物具有作为安全的皮肤增白剂和治疗化妆品行业色素沉着相关疾病的潜力。

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Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity

Tyrosinase inhibitors can reduce melanin production for skin whitening, but some existing products may harm the skin. This study discovered six compounds that inhibit tyrosinase in the mushroom Agaricus bisporus by over 50%. Compound 11 displayed strong inhibition (92.2% and 86.7%) for L-tyrosine and L-DOPA substrates, while compound 13 showed high inhibition (96.0% and 62.0%) for both substrates. Molecular docking simulations revealed compounds 11 and 13 bind at the allosteric site of the enzyme. Xanthone derivatives, based on these findings, hold potential as safe skin whitening agents and for pigmentation-related diseases in the cosmetic industry.

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

审稿时长

2.3 months

期刊介绍： The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.