Biological Activities and Cytotoxicity of Eperua oleifera Ducke Oil-resin

BACKGROUND: The oil-resin of Eperua oleifera Ducke has been used in popular medicine similarly to the copaiba oil (Copaifera spp.). OBJECTIVE: This study aimed to investigate the effects of the acid fraction of E. oleifera oil-resin (AFEOR) on cell proliferation, collagen production in human fibroblasts, inhibition of metalloproteinases, and cytotoxicity against tumor cell lines. MATERIALS AND METHODS: Acid fraction of E. oleifera was fractionated in the ion exchange column chromatography. Cytotoxicity and genotoxicity were evaluated by Alamar Blue(®) and Cometa assay. The inhibition of metalloproteinases was performed by zymography and Western blotting. RESULTS: The predominant acidic diterpenes in the AFEOR were copalic and hardwickiic acids. AFEOR caused morphology alteration and decrease of proliferation at concentrations higher than 5 μg/mL. It also caused significant collagen proliferation in fibroblasts. It showed cytotoxicity against tumoral and nontumoral cell lines, with IC(50) values ranging from 13 to 50 μg/mL, and a hemolytic activity with an IC(50) value of 38.29 μg/mL. AFEOR inhibited collagenase activity, with an IC(50) value of 46.64 μg/mL, and matrix metalloproteinase-2 (MMP)-2 and MMP-9 in HaCaT cells or MMP-1 expression in MRC-5 cells. AFEOR induced genotoxicity in MRC-5 cells with a DNA damage index between 40% and 60% when compared to the negative controls (0%–20%). CONCLUSION: For the first time, biological activities from oil-resin E. oleifera demonstrated ratifying somehow its popular use. SUMMARY: Analysis of crude oil-resin and fractionation of diterpenic fraction was performance using selective ion-exchange column chromatography. Cytotoxicity analysis and morphology were performed with different cell lines. Collagen production in human fibroblasts, inhibition of metalloproteinases were demonstrated by zymography and Western blotting. [Image: see text] Abbreviations used: AFEOR: Eperua oleifera oil-resin.