Imbricaric Acid and Perlatolic Acid: Multi-Targeting Anti-Inflammatory Depsides from Cetrelia monachorum

• DOI: 10.1371/journal.pone.0076929
• Publication Date: 2013-10-11T03:52:41Z
• Authors: Sarah K. Oettl; Jana Gerstmeier; Shafaat Y. Khan; Katja Wiechmann; Julia Bauer; Atanas G. Atanasov; Clemens Malainer; Ezzat M. Awad; Pavel Uhrin; Elke H. Heiss; Birgit Waltenberger; Daniel Remias; Johannes M. Breuss; Joel Boustie; Verena M. Dirsch; Hermann Stuppner; Oliver Werz; Judith M. Rollinger
• Keywords: IC50; Anti-inflammatory

In vitro screening of 17 Alpine lichen species for their inhibitory activity against 5-lipoxygenase, microsomal prostaglandin E2 synthase-1 and nuclear factor kappa B revealed Cetrelia monachorum (Zahlbr.) W.L. Culb. & C.F. As conceivable source novel anti-inflammatory compounds. Phytochemical investigation the ethanolic crude extract resulted in isolation identification 11 constituents, belonging to depsides derivatives orsellinic acid, olivetolic acid olivetol. The two imbricaric (4) perlatolic (5) approved dual activities on (IC50 = 1.9 0.4 µM, resp.) 5-lipoxygenase tested a cell-based assay 5.3 1.8 purified enzyme 3.5 resp.). Additionally, these main constituents quantified with 15.22% 9.10% showed significant inhibition tumor necrosis alpha-induced activation luciferase reporter cells IC50 values 2.0 7.0 respectively. murine vivo model inflammation, 5 impaired inflammatory, thioglycollate-induced recruitment leukocytes peritoneum. potent effects three identified targets attest 4 pronounced multi-target profile which warrants further pharmacokinetics efficacy.