AbstractBackgroundStem bark ofLuehea ochrophylla(L. ochrophylla) is used by the traditional Brazilian medicine for treatment of rheumatic diseases and tumors. This study aimed to investigate inhibition of acute and chronic inflammations and cytotoxic activity of extracts, fractions, and isolated compounds fromL. ochrophylla.MethodsHexane (HE) and ethanol (EE) extracts obtained from stem bark ofL.ochrophyllawere submitted to chromatographic fractionation. In order to test acute inflammation, experimental model of impact injury was used, followed by transdermal application of gels using phonophoresis. Histological analysis was based on scores assigned by the capacity of decreasing the lesion. To evaluate the effect EE and fractions on cell proliferation, human lymphocytes were stimulated with phytohemagglutinin and analyzed using flow cytometry. Proliferation was measured using VPD 450 staining and the calculated proliferative index (PI). The cytotoxic activity was evaluated using MTT colorimetric method against MDA-MB-231, MCF-7, HCT-116, and Vero cells. GraphPad Prism Version 5 was used for statistical analysis.ResultsHE and EE provided friedelin,β-friedelinol, lupeol, mixture of lupeol and pseudotaraxasterol,β-sitosterol, betulinic acid, mixture of lupeol and taraxasterol, (−)-epicatechin,β-sitosterol-3-O-β-D-glucopyranoside, and (+)-epicatechin-(4β-8)-epicatechin. HE, ethyl acetate fraction (AF), betulinic acid, andβ-sitosterol promoted regeneration of muscle fibers caused by muscle injury. AF significantly (p < 0.05) reduced the lymphocyte proliferation index (1.36 for cultures stimulated with PHA, 0.7 for untreated cultures and 0.12 for cultures stimulated with PHA and treated with AF 25 μg/mL and AF 50 μg/mL, respectively).β-Sitosterol-3-O-β-D-glucopyranoside exhibited high cytotoxic activity (IC₅₀ = 1.279 μg/mL) against HCT-116 cell line.ConclusionThese results suggest that extracts, fractions, and chemical constituents fromL. ochrophylladecreases inflammatory processes generated by muscle injury. The anti-inflammatory activity may be justified by high inhibition of T cell proliferation. These extracts, fractions, and chemical constituents fromL. ochrophyllamay be useful as a therapeutic agent against rheumatic diseases. Moreover, chemical constituents fromL. ochrophyllashow potent cytotoxic activity against colon and rectal carcinomas.