Bioactivity of prenylated hydroxybenzoic acids from Piper garagaranum C. DC

Abstract

A bio-assay guided fractionation of Piper garagaranum C. DC. led to the isolation of two prenylated hydroxybenzoic acids (1-2) with anti-inflammatory and cytotoxic activities. The anti-inflammatory action was determined in an LPS stimulated RAW 264.7 murine macrophage assay with IC50 values for inhibition of NO production of (18 ± 3) and (26 ± 5) μM, for 1 and 2, respectively. These compounds do not inhibit NO production by a competitive inhibition of the iNOS enzyme and show anti-inflammatory properties by lowering the expression of pro-inflammatory genes (TNF-α, IL-1β, CXCL2 and CCL2), as determined by qRT-PCR. Electrochemical measurements using cyclic voltammetry (CV) show that compound 1 exhibits anti-oxidant properties. This is the first phytochemical study of this plant, and we report a preliminary study of the biological activity of the isolated compounds.