title: Pharmacological properties of Myrtacine® and its potential value in acne treatment.
abstract: This study aimed at evaluating the antiproliferative, antibacterial, and anti-inflammatory properties of an ethanolic myrtle extract (Myrtacine®) in vitro, characterising its potential active compounds (myrtucommulones A and B') by structural analysis, and evaluating their biological activity. Antiproliferative activity was assessed by the BrdU incorporation assay in HaCat keratinocytes and inhibitory and bactericidal activities against P. ACNES strains by measuring the minimal inhibitory concentration (MIC) and D value. Anti-inflammatory effect was evaluated by measuring 6-keto-prostaglandin F1 α and [³H]-arachidonic acid metabolite production in keratinocytes stimulated for inflammation. Myrtacine® inhibited keratinocyte proliferation by 27 % and 76 % at 1 and 3 µg/mL, respectively (p < 0.001). A comparable effect, though less marked, was observed with 5 µg/mL myrtucommulones A and B' (-36 % and -28 %, respectively). Myrtacine® inhibited erythromycin-sensible and -resistant P. ACNES strains growth with MICs of 4.9 µg/mL and 2.4 µg/mL, respectively. Myrtucommulone B' and myrtucommulone A displayed a similar inhibitory activity against both strains (for both strains, MIC = 1.2 µg/mL and about 0.5 µg/mL, respectively). At 3 and 10 µg/mL, Myrtacine® significantly decreased all metabolite production from cyclooxygenase (81 % and 107 %, p < 0.0001) and lipoxygenase (52 % and 95 %, p < 0.001) pathways. Finally, Myrtacine® exhibited a concentration-dependent anti-lipase activity at 100 µg/mL and 1 mg/mL, as it decreased lipase activity by respectively 53 % and 100 % (p < 0.01 for both). In conclusion, in vitro, Myrtacine® demonstrated antiproliferative, antibacterial, and anti-inflammatory properties that may be of value to exert a global action in the treatment of acne lesions.
authors: Laboratoire des Produits Végétaux, Institut de Recherche Pierre Fabre, Centre de R & D Pierre Fabre 3, Toulouse, France.
authors: Christel
authors: C
authors: Fiorini-Puybaret
authors: Marie-Françoise
authors: MF
authors: Aries
authors: Bernard
authors: B
authors: Fabre
authors: Stelianos
authors: S
authors: Mamatas
authors: Joëlle
authors: J
authors: Luc
authors: Arnaud
authors: A
authors: Degouy
authors: Marco
authors: M
authors: Ambonati
authors: Carine
authors: C
authors: Mejean
authors: Florence
authors: F
authors: Poli
mesh_terms: D000152:Acne Vulgaris / Q000188:drug therapy* / Q000382:microbiology; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D051546:Cyclooxygenase 2 / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects; D008049:Lipase / Q000187:drug effects / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D031651:Myrtus / Q000737:chemistry*; D010696:Phloroglucinol / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry; D011425:Propionibacterium acnes / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D010936:Plant Extracts; C455139:myrtucommulone A; C579604:myrtucommulone B; D010696:Phloroglucinol; D051546:Cyclooxygenase 2; C496540:PTGS2 protein, human; D008049:Lipase