Anti-MMP-2 Activity and Skin-Penetrating Capability of the Chemical Constituents from Rhodiola rosea

Tzong Huei Lee, Chieh Chih Hsu, George Hsiao, Jia You Fang, Wei Min Liu, Ching Kuo Lee*

*此作品的通信作者

研究成果: 期刊稿件文章同行評審

14 引文 斯高帕斯(Scopus)

摘要

Based on the significant inhibitory activity toward matrix metalloproteinase-2 and collagenase noticed in preliminary studies, crude extracts of Rhodiola rosea were partitioned and chromatographed sequentially to afford three new compounds, 1,2,3,6-tetra-O-galloyl-4-O-p-hydroxybenzoyl-β-D-glucopyranoside (1), (E)-creoside I (2), and (R,Z)-2-methylhept-2-ene-1,6-diol (3), along with twenty-four known compounds (4-27). Their structures were determined by spectroscopic data analyses. All isolated compounds were subjected to bioactivity assays. In these, 1 specifically inhibited matrix metalloproteinase-2 activity with an IC50 value of 16.3 ± 1.6 μM, while its analogue 1,2,3,6-tetra-O-galloyl-β-D-glucopyranonoside (17) inhibited matrix metalloproteinase-2 with an IC50 value of 23.0 ± 4.8 μM. In the collagenase activity assay, the inhibitory effects of 1 and 17 at concentrations of both 20 and 40 μM were more potent than those of the positive control, 1,10-phenanthroline. In order to realize whether 17 could penetrate from the epidermal layer into the basal and dermal layers of the human skin to inhibit the activity of matrix metalloproteinase-2 and collagenase or not, a transdermal penetration test in nude and white mice skins was performed. Penetration percentages of 17 quantified by LC-MS were 27.8% and 74.8% in 24 hours, respectively.

原文英語
頁(從 - 到)698-704
頁數7
期刊Planta Medica
82
發行號8
DOIs
出版狀態已出版 - 01 05 2016

文獻附註

Publisher Copyright:
© Georg Thieme Verlag KG Stuttgart, New York.

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