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来自槐树的活性成分在人表皮黑素细胞中表现出细胞酪氨酸酶抑制作用。

Active constituents from Sophora japonica exhibiting cellular tyrosinase inhibition in human epidermal melanocytes.

作者信息

Lo Yuan-Hsin, Lin Rong-Dih, Lin Yi-Pei, Liu Yan-Ling, Lee Mei-Hsien

机构信息

Department of Dermatology, Shin Kong Wu Ho-Su Memorial Hospital, Taipei 111, Taiwan.

出版信息

J Ethnopharmacol. 2009 Jul 30;124(3):625-9. doi: 10.1016/j.jep.2009.04.053. Epub 2009 May 5.

Abstract

AIM OF THE STUDY

There is greater consumer awareness of plant-based skin-care products. Sophora japonica L. (Fabaceae) has been used traditionally as a hemostatic agent and also has skin-care and whitening benefits. The effect of the isolated active compounds of Sophora japonica L. (Fabaceae) that inhibits tyrosinase activity in human epidermal melanocytes (HEMn) was examined.

MATERIALS AND METHODS

We used the mushroom tyrosinase inhibitory assay to isolate active constituents from the extracts. The structures of these constituents were characterized by physical and spectroscopic analyses. Cellular tyrosinase kinetics were analyzed and showed by Lineweaver-Burk plot.

RESULTS

A new compound, N-feruloyl-N'-cis-feruloyl-putrescine (8), together with four flavonoids and three putrescine derivatives were obtained after assay-guided isolation of S. japonica. In HEMn, compound 8 was minimally cytotoxic (cell viability >90% at 100 microM) and the IC(50) value for suppression of cellular tyrosinase activity was estimated as 85.0 microM. Zymography analysis demonstrated the compound's concentration-dependent effects and the kinetic analysis indicated the compound's mixed-inhibitory action.

CONCLUSIONS

We concluded that the new compound 8 is the most potent component of S. japonica yet discovered. Its pigment inhibition activity may be exploitable cosmetically.

摘要

研究目的

消费者对植物性护肤品的认知度越来越高。槐(豆科)传统上用作止血剂,也具有护肤和美白功效。本研究考察了从槐中分离得到的活性化合物对人表皮黑素细胞(HEMn)酪氨酸酶活性的抑制作用。

材料与方法

我们采用蘑菇酪氨酸酶抑制试验从提取物中分离活性成分。通过物理和光谱分析对这些成分的结构进行了表征。采用Lineweaver-Burk图分析并展示细胞酪氨酸酶动力学。

结果

通过对槐进行活性导向分离,得到了一种新化合物N-阿魏酰基-N'-顺式阿魏酰基腐胺(8),以及四种黄酮类化合物和三种腐胺衍生物。在HEMn细胞中,化合物8的细胞毒性极小(在100 microM时细胞活力>90%),抑制细胞酪氨酸酶活性的IC50值估计为85.0 microM。酶谱分析证明了该化合物的浓度依赖性作用,动力学分析表明该化合物具有混合抑制作用。

结论

我们得出结论,新化合物8是迄今发现的槐中最有效的成分。其色素抑制活性在化妆品领域可能具有开发价值。

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