title: Inhibition of stromelysin-1 by caffeic acid derivatives from a propolis sample from Algeria.
abstract: Stromelysin-1 (matrix metalloproteinase-3: MMP-3) occupies a central position in collagenolytic and elastolytic cascades, leading to cutaneous intrinsic and extrinsic aging. We screened extracts of a propolis sample from Algeria with the aim to isolate compounds able to selectively inhibit this enzyme. A butanolic extract (B (3)) of the investigated propolis sample was found to potently inhibit MMP-3 activity (IC (50) = 0.15 ± 0.03 µg/mL), with no or only weak activity on other MMPs. This fraction also inhibited plasmin amidolytic activity (IC (50) = 0.05 µg/mL) and impeded plasmin-mediated proMMP-3 activation. B (3) was fractionated by HPLC, and one compound, characterized by NMR and mass spectroscopy and not previously identified in propolis, i.e., (+)-chicoric acid, displayed potent IN VITRO MMP-3 inhibitory activity (IC (50) = 6.3 × 10 (-7) M). In addition, both caffeic acid and (+)-chicoric acid methyl ester present in fraction B (3) significantly inhibited UVA-mediated MMP-3 upregulation by fibroblasts.
authors.affiliation: Unité Medyc, Université de Reims Champagne Ardennes, UFR de Médecine, Reims, France.
authors.forename: Narimane
authors.initials: N
authors.lastname: Segueni
authors.forename: Abdulmagid Alabdul
authors.initials: AA
authors.lastname: Magid
authors.forename: Martine
authors.initials: M
authors.lastname: Decarme
authors.forename: Salah
authors.initials: S
authors.lastname: Rhouati
authors.forename: Mesbah
authors.initials: M
authors.lastname: Lahouel
authors.forename: Frank
authors.initials: F
authors.lastname: Antonicelli
authors.forename: Catherine
authors.initials: C
authors.lastname: Lavaud
authors.forename: William
authors.initials: W
authors.lastname: Hornebeck
mesh_terms: D000328:Adult; D000462:Algeria; D000440:Butanols / Q000737:chemistry; D002109:Caffeic Acids / Q000737:chemistry / Q000494:pharmacology*; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D045424:Complex Mixtures / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D004789:Enzyme Activation / Q000187:drug effects; D005341:Fibrinolysin / Q000037:antagonists & inhibitors / Q000494:pharmacology; D005347:Fibroblasts / Q000187:drug effects / Q000201:enzymology / Q000528:radiation effects; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D019278:Matrix Metalloproteinase 3; D061965:Matrix Metalloproteinase Inhibitors; D008875:Middle Aged; D010636:Phenols / Q000494:pharmacology; D011429:Propolis / Q000737:chemistry*; D011480:Protease Inhibitors / Q000494:pharmacology*; D013386:Succinates / Q000737:chemistry / Q000494:pharmacology; D014466:Ultraviolet Rays; D055815:Young Adult
chemical_list: D000440:Butanols; D002109:Caffeic Acids; D045424:Complex Mixtures; D061965:Matrix Metalloproteinase Inhibitors; D010636:Phenols; D011480:Protease Inhibitors; D013386:Succinates; D011429:Propolis; D005341:Fibrinolysin; C511768:MMP3 protein, human; D019278:Matrix Metalloproteinase 3; C100435:chicoric acid; C040048:caffeic acid; C515101:caftaric acid