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L. 花芽中黄酮类化合物对酪氨酸酶活性的抑制机制

Inhibitory mechanism on tyrosinase activity of flavonoids from flower buds of L.

作者信息

Ma Yunfeng, Zhang Chaoyang, Li Jinlin, Xiong Jiayan, Xiao Bao-Lin

机构信息

School of Life Sciences, Henan University, Kaifeng, 475004, China.

Institute of Microbial Engineering, Laboratory of Bioresource and Applied Microbiology, Henan University, Kaifeng, 475004, China.

出版信息

Heliyon. 2024 Sep 21;10(19):e38252. doi: 10.1016/j.heliyon.2024.e38252. eCollection 2024 Oct 15.

Abstract

The flower buds of L. (FBSJ) have long been applied as Traditional Chinese Medicine (TCM) and functional food in East Asia. In this study, extracts of FBSJ from 11 different locations were analyzed using the HPLC method to establish their HPLC fingerprints. By determining the IC50 on tyrosinase activity, it was discovered that the extract from Kunming, Yunnan Province exhibited the strongest inhibitory activity. Further analysis, including partial least squares regression coefficient analysis and grey correlation analysis, regarded kaempferol, isorhamnetin, and quercetin as the compounds with significant tyrosinase inhibitory activities. To understand the inhibition mechanism of tyrosinase activity, various analytical techniques such as enzymatic kinetic analysis, fluorescence quenching, circular dichroism (CD), molecular docking, and molecular dynamics simulation were employed. The results revealed that quercetin, isorhamnetin, and kaempferol exhibited higher inhibitory activity and binding energy compared with kojic acid, indicating their potential value as natural tyrosinase inhibitors. This research provides a solid theoretical foundation for studying the application and mechanism of flavonoids against tyrosinase in FBSJ.

摘要

长瓣金莲花(FBSJ)的花蕾长期以来在东亚地区被用作传统中药(TCM)和功能性食品。在本研究中,采用高效液相色谱(HPLC)法对来自11个不同地点的FBSJ提取物进行分析,以建立其HPLC指纹图谱。通过测定对酪氨酸酶活性的半数抑制浓度(IC50),发现云南省昆明市的提取物表现出最强的抑制活性。进一步的分析,包括偏最小二乘回归系数分析和灰色关联分析,将山柰酚、异鼠李素和槲皮素视为具有显著酪氨酸酶抑制活性的化合物。为了解酪氨酸酶活性的抑制机制,采用了多种分析技术,如酶动力学分析、荧光猝灭、圆二色性(CD)、分子对接和分子动力学模拟。结果表明,与曲酸相比,槲皮素、异鼠李素和山柰酚表现出更高的抑制活性和结合能,表明它们作为天然酪氨酸酶抑制剂的潜在价值。本研究为研究黄酮类化合物在FBSJ中对酪氨酸酶的应用及作用机制提供了坚实的理论基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/799e/11462347/42b055bda956/gr1.jpg

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