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天然化妆品活性成分与嗅觉受体 OR2AT4 之间的结构-功能关系。

Structure-function relationship between a natural cosmetic active ingredient and the olfactory receptor OR2AT4.

机构信息

SILAB R&D Department, Brive, France.

出版信息

Int J Cosmet Sci. 2019 Apr;41(2):194-199. doi: 10.1111/ics.12526. Epub 2019 Mar 29.

Abstract

OBJECTIVE

Although the olfactory receptor OR2AT4 was described as involved in epidermal renewal, there is no data about a cosmetic active ingredient activating this receptor. The aim of this research work was thus to identify a natural molecule binding to this receptor in order to stimulate keratinocyte migration.

METHODS

For this purpose, natural molecules were extracted from Cocos nucifera flour. Then, efficacy of this natural extract was evaluated on keratinocyte migration in vitro. Molecules of the Cocos nucifera flour extract were then identified by UPLC-MS/MS. Molecular docking was finally conducted to investigate the potential interaction between identified molecules and the olfactory receptor OR2AT4.

RESULTS

The Cocos nucifera flour extract significantly increased keratinocyte migration and results demonstrated that this effect was mediated by the olfactory receptor OR2AT4. Metabolomic analysis revealed two molecules, nonioside D and butyl 4-O-alpha-D-glucopyranosyl-beta-D-glucopyranoside, as significantly present in the Cocos nucifera flour extract compared to both Cocos nucifera oil and water. Finally, molecular docking revealed that butyl 4-O-alpha-D-glucopyranosyl-beta-D-glucopyranoside could interact with the extracellular domain 2 of the OR2AT4.

CONCLUSION

This study highlighted for the first time a natural molecule, extracted from Cocos nucifera flour, able to interact with the olfactory receptor OR2AT4 and promote the keratinocyte migration and thus the epithelialization.

摘要

目的

尽管嗅觉受体 OR2AT4 被描述为参与表皮更新,但目前尚无关于激活该受体的化妆品活性成分的数据。因此,本研究旨在鉴定一种与该受体结合的天然分子,以刺激角质形成细胞迁移。

方法

为此,从椰子粉中提取天然分子。然后,评估该天然提取物对体外角质形成细胞迁移的功效。然后通过 UPLC-MS/MS 鉴定椰子粉提取物中的分子。最后进行分子对接,以研究鉴定出的分子与嗅觉受体 OR2AT4 之间的潜在相互作用。

结果

椰子粉提取物显著增加了角质形成细胞的迁移,结果表明这种作用是由嗅觉受体 OR2AT4 介导的。代谢组学分析显示,与椰子油和水相比,非甾体 D 和丁基 4-O-α-D-吡喃葡萄糖基-β-D-吡喃糖苷这两种分子在椰子粉提取物中明显存在。最后,分子对接显示丁基 4-O-α-D-吡喃葡萄糖基-β-D-吡喃糖苷可以与 OR2AT4 的细胞外结构域 2 相互作用。

结论

本研究首次强调了一种从椰子粉中提取的天然分子,能够与嗅觉受体 OR2AT4 相互作用并促进角质形成细胞迁移,从而促进上皮化。

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