Lignan Derivatives from Krameria lappacea Roots Inhibit Acute Inflammation in Vivo and Pro-inflammatory Mediators in Vitro

• DOI: 10.1021/np200343t
• Publication Date: 2011-07-29T17:27:15Z
• Authors: Lisa Baumgartner; Silvio Sosa; Atanas G. Atanasov; Antje Bodensieck; Nanang Fakhrudin; Julia Bauer; Giorgia Del Favero; Cristina Ponti; Elke H. Heiss; Stefan Schwaiger; Angela Ladurner; Ute Widowitz; Roberto Della Loggia; Judith M. Rollinger; Oliver Werz; Rudolf Bauer; Verena M. Dirsch; Aurelia Tubaro; Hermann Stuppner
• Keywords: Croton oil; Anti-inflammatory; HaCaT; Croton

The roots of Krameria lappacea are used traditionally against oropharyngeal inflammation. So far, the astringent and antimicrobial properties its proanthocyanidin constituents considered to account for anti-inflammatory effect. aim present study was characterize pharmacologically a lipophilic extract K. several isolated lignan derivatives (1–11) in terms their putative activity. dichloromethane (ID50 77 μg/cm2) as well compounds 1–11 0.31–0.60 μmol/cm2) exhibited topical antiedematous comparable those indomethacin 0.29 mouse ear vivo model. Two most potent compounds, 2-(2-hydroxy-4-methoxyphenyl)-5-(3-hydroxypropyl)benzofuran (5) (+)-conocarpan (7), were studied regarding time-dependent edema development leukocyte infiltration up 48 h after croton oil-induced dermatitis induction, they showed activity profiles similar that hydrocortisone. In vitro studies demonstrated inhibition NF-κB, cyclooxygenase-1 -2, 5-lipoxygenase, microsomal prostaglandin E2 synthase-1 antioxidant properties, mechanisms possibly contributing observed effects. findings not only support ethnopharmacological use but also reveal contribute strongly this herbal drug.