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迷迭香叶苷对黑色素生成的抑制作用。

Inhibition of melanogensis by a novel origanoside from Origanum vulgare.

机构信息

Department of Cosmetic Science, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.

出版信息

J Dermatol Sci. 2010 Mar;57(3):170-7. doi: 10.1016/j.jdermsci.2009.12.009. Epub 2010 Jan 7.

Abstract

BACKGROUND

Natural and synthetic substances are becoming increasingly utilized as tyrosinase inhibitors of depigmentation and developed cosmetics industry. However, few have been employed as skin-whitening agents, primarily because of numerous safety concerns.

OBJECTIVE

A novel compound was found, and then its safe concentrations and inhibition effect of hyperpigmentation by the regulation of the tyrosinase family of proteins were examined.

METHODS

A novel phenolic glucoside, origanoside (1), was isolated from Origanum vulgare. The structure of the origanoside (1) was established on the basis of spectral evidence and the safe concentrations were determined by MTT assay. Skin-whitening capacity in skin fibroblast Hs68 and melanoma B16 cells and in vivo animal test for origanoside (1) were investigated.

RESULTS

Origanoside (1) is non-toxic in concentrations of 0-100 microg/ml in both cells. The ability of origanoside (1) to inhibit cellular tyrosinase and DOPA oxidase in B16 cells was investigated. Origanoside (1) significantly reduced expressions of microphthalmia-associated transcription factor (MITF), tyrosinase and tyrosinase-related proteins 2 (TRP-2) in vitro and in vivo, suggesting that origanoside (1) is responsible for the antimelanogenic effect. Smearing origanoside (1)-gel samples on 12 mice for 10 days increased L*, reduced a* and erythema-melanin (E/M), and b* was almost unchanged compared with those of samples and untreated groups, indicating that the skin lightened.

CONCLUSION

Experimental data demonstrate that origanoside (1) causes depigmentation and may be useful for novel food additives and skin-whitening cosmetics.

摘要

背景

天然和合成物质作为抑制黑色素生成和开发化妆品行业的酪氨酸酶抑制剂越来越受到重视。然而,由于存在许多安全问题,很少有物质被用作美白剂。

目的

发现一种新型化合物,然后检测其安全浓度以及通过调节酪氨酸酶家族蛋白对皮肤色素沉着的抑制作用。

方法

从牛至(Origanum vulgare)中分离出一种新型酚糖苷——牛至苷(1)。基于光谱证据和 MTT 测定确定了牛至苷(1)的结构和安全浓度。研究了牛至苷(1)在皮肤成纤维细胞 Hs68 和黑色素瘤 B16 细胞中的美白作用以及在体内动物试验中的作用。

结果

牛至苷(1)在 0-100μg/ml 的浓度下对两种细胞均无毒性。研究了牛至苷(1)抑制 B16 细胞细胞内酪氨酸酶和多巴氧化酶的能力。牛至苷(1)在体外和体内显著降低小眼畸形相关转录因子(MITF)、酪氨酸酶和酪氨酸酶相关蛋白 2(TRP-2)的表达,表明牛至苷(1)具有抗黑色素生成作用。在 12 只小鼠身上涂抹牛至苷(1)-凝胶样品 10 天,与样品和未处理组相比,L增加,a降低,红斑黑色素(E/M)减少,b*几乎不变,表明皮肤变亮。

结论

实验数据表明,牛至苷(1)可导致皮肤脱色,可能对新型食品添加剂和皮肤美白化妆品有用。

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