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.

Original languageEnglish
Pages (from-to)698-704
Number of pages7
JournalPlanta Medica
Issue number8
Publication statusPublished - May 1 2016


  • (E)-creoside I
  • (Z)-2-methyl-2-hepten-1 6-diol
  • 1 2 3 6-tetra- O -galloyl-4- O - p -hydroxybenzoyl- β -D-glucopyranoside
  • Crassulaceae
  • Rhodiola rosea
  • collagenase
  • matrix metalloproteinase

ASJC Scopus subject areas

  • Drug Discovery
  • Analytical Chemistry
  • Molecular Medicine
  • Complementary and alternative medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry


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