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Flavonoids of Tripodanthus acutifolius inhibit TNF–α production in LPS–activated THP–1 and B16–F10 cells

Apaza T, L., Serban, Andreea Madalina, Cabanillas, A.H., Villacampa, A., Rumbero, Angel
Journal of ethnopharmacology 2019 v.242 pp. 112036
chalcone, flavones, heptane, indigenous species, inhibitory concentration 50, leaves, methanol, methylene chloride, stems, traditional medicine, tumor necrosis factor-alpha, South America
T. acutifolius is an endemic species from South America which has been used in traditional medicine since ancient times due to its biological properties, including its anti–inflammatory effects.Aim of the study: The aim of the article is to investigate the inhibitory activity of T. acutifolius over TNF–α production in THP–1 and B16–F10 cells. To achieve this, phytochemical analysis has been used to determine the compounds present in the species with anti–inflammatory effects.Leaves and stems of T. acutifolius were extracted with n–heptane, dichloromethane, methanol and water. The resulting extracts were analysed in THP–1 and B16–F10 cells by measuring their inhibitory capacity over the production of TNF–α stimulated with LPS.The guided–bioassay led to the isolation of 6,2',4'–trimethoxyflavone (1), 5,3',4'–trihydroxy–6,7,8–trimethoxyflavone (2), (E)–2',4'–dihydroxy–6'–methoxy–chalcone (3) and 5,4'–dihydroxy–6,7,8–trimethoxyflavone (4) from the dichloromethanic extract. Compounds showed an inhibitory activity of TNF–⍺ production in THP–1 cells, with IC50 of 2.38 ± 0.02 μM, 12.36 ± 0.17 μM, 1.12 ± 0.01 μM and 8.09 ± 0.04 μM, respectively. In addition, the compounds showed an inhibitory activity of TNF–⍺ production in B16–F10 cells with IC50 of 1.32 ± 0.03 μM, 5.63 ± 0.09 μM, 0.60 ± 0.02 μM and 3.77 ± 0.15 μM, respectively.We identified 3 flavones (6,2',4'–trimethoxyflavone, 5,3',4'–trihydroxy–6,7,8–trimethoxyflavone, 5,4'–dihydroxy–6,7,8–trimethoxyflavone) and a chalcone ((E)–2',4'–dihydroxy–6'–methoxy–chalcone) present in the leaves and stems of T. acutifolius. These compounds are an alternative for the treatment of immune–mediated inflammatory disorders, acting as negative modulators over the TNF–α production.