Biological Activities and Cytotoxicity of Eperua oleifera Ducke Oil-resin

摘要

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 IC₅₀ values ranging from 13 to 50 μg/mL, and a hemolytic activity with an IC₅₀ value of 38.29 μg/mL. AFEOR inhibited collagenase activity, with an IC₅₀ 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. Abbreviations used: AFEOR: Eperua oleifera oil-resin.