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作为潜在酪氨酸酶抑制剂的槲皮万寿菊素的抑制机制研究

Inhibition mechanism investigation of quercetagetin as a potential tyrosinase inhibitor.

作者信息

Liang Faliang

机构信息

Pharmacy Department, Jiang Men Maternity and Child Healthcare Hospital, Jiangmen, China.

出版信息

Front Chem. 2024 Jun 3;12:1411801. doi: 10.3389/fchem.2024.1411801. eCollection 2024.

Abstract

Tyrosinase is one important rate limiting enzyme in melanin synthesis, directly affecting the melanin synthesis. Quercetagetin is one active ingredient from marigold. Thence, the inhibition effects of quercetagetin against tyrosinase were investigated. The results showed quercetagetin could inhibit tyrosinase activity with IC value of 0.19 ± 0.01 mM and the inhibition type was a reversible mixed-type. Results of fluorescence quenching showed quercetagetin could quench tyrosinase fluorescence in static process. CD and 3D fluorescence results showed the interaction of quercetagetin to tyrosinase could change tyrosinase conformation to inhibit activity. Moreover, docking revealed details of quercetagetin's interactions with tyrosinase.

摘要

酪氨酸酶是黑色素合成中的一种重要限速酶,直接影响黑色素的合成。槲皮万寿菊素是金盏花中的一种活性成分。因此,研究了槲皮万寿菊素对酪氨酸酶的抑制作用。结果表明,槲皮万寿菊素能够抑制酪氨酸酶的活性,IC值为0.19±0.01 mM,抑制类型为可逆混合型。荧光猝灭结果表明,槲皮万寿菊素在静态过程中能够猝灭酪氨酸酶的荧光。圆二色光谱和三维荧光结果表明,槲皮万寿菊素与酪氨酸酶的相互作用能够改变酪氨酸酶的构象从而抑制其活性。此外,分子对接揭示了槲皮万寿菊素与酪氨酸酶相互作用的细节。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/53c5/11184945/b371a8692b81/fchem-12-1411801-g001.jpg

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