Anti-MMP-2 Activity and Skin-Penetrating Capability of the Chemical Constituents from Rhodiola rosea
| Autor: | Chieh Chih Hsu, George Hsiao, Wei Min Liu, Ching Kuo Lee, Tzong-Huei Lee, Jia You Fang |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Mice Nude Pharmaceutical Science Human skin Matrix Metalloproteinase Inhibitors Matrix metalloproteinase Analytical Chemistry Mice 03 medical and health sciences Drug Discovery medicine Animals IC50 Cells Cultured Skin Pharmacology Chromatography biology Plant Extracts Chemistry Organic Chemistry Penetration (firestop) biology.organism_classification Crassulaceae 030104 developmental biology Rhodiola rosea Complementary and alternative medicine Chemical constituents Collagenase Matrix Metalloproteinase 2 Molecular Medicine Rhodiola medicine.drug |
| Zdroj: | Planta Medica. 82:698-704 |
| ISSN: | 1439-0221 0032-0943 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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