Verbascum xanthophoeniceum-derived phenylethanoid glycosides are potent inhibitors of inflammatory chemokines in dormant and interferon-gamma-stimulated human keratinocytes

Milen Georgiev, Saveria Pastore, Daniela Lulli, Kalina Alipieva, Vladimir Kostyuk, Alla Potapovich, Mariangela Panetta, Liudmila Korkina

Research output: Contribution to journalArticle

Abstract

Ethnopharmacological relevance: Verbascum xanthophoeniceum is a representative of mullein species with a strong tradition of use in folk medicine as a remedy in inflammatory and infectious contexts. This plant accumulates phenylethanoid and iridoid metabolites with a partially characterized bioactivity. Materials and methods: Here, we compared anti-inflammatory effects of Verbascum xanthophoeniceum crude extract, its fractions, isolated iridoid glycosides, including aucubin, ajugol, harpagide, harpagoside, nigroside III and nigroside VI, and phenylethanoid glycosides verbascoside and forsythoside B in primary cultures of normal human keratinocytes (NHK). The gene expression, synthesis, and release of soluble pro-inflammatory chemokines, such as IL-8, MCP-1 and IP-10, in dormant and IFN-γ-activated NHK were investigated, and IC50 for each extract/individual substance was determined. Results: We found that the phenylethanoid glycosides verbascoside and forsythoside B were effective, dose-dependent inhibitors of gene expression and de novo synthesis of all the chemokines, whereas the iridoid glycosides and phenylpropanoid aglycone rosmarinic acid displayed a poor and selective inhibition. Accordingly, the fraction of the crude extract containing verbascoside effectively impaired both spontaneous and induced chemokine expression in NHK. Conclusion: This is the first report on the identification of active constituents of Verbascum xanthophoeniceum possessing anti-inflammatory properties towards human keratinocytes. Phenylethanoid glycosides exerted exquisite corticosteroid-like inhibition of pro-inflammatory chemokines at transcriptional and translational levels.

Original languageEnglish
Pages (from-to)754-760
Number of pages7
JournalJournal of Ethnopharmacology
Volume144
Issue number3
DOIs
Publication statusPublished - Dec 18 2012

Keywords

  • Chemokines
  • Human keratinocytes
  • Interferon gamma
  • Iridoid glycosides
  • Phenylethanoids
  • Verbascum xanthophoeniceum

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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