Flavonoids of Tripodanthus acutifolius inhibit TNF-α production in LPS-activated THP-1 and B16-F10 cells.
ETHNOPHARMACOLOGICAL RELEVANCE
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.


MATERIALS AND METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
['Apaza T|L|L|', 'Serban|Andreea Madalina|AM|', 'Cabanillas|A H|AH|', 'Villacampa|A|A|', 'Rumbero|Angel|A|']
D000818:Animals D045744:Cell Line, Tumor D002470:Cell Survival D005419:Flavonoids D006801:Humans D008070:Lipopolysaccharides D028183:Loranthaceae D008546:Melanoma, Experimental D051379:Mice D018515:Plant Leaves D018547:Plant Stems D014409:Tumor Necrosis Factor-alpha
Flavonoids Tripodanthus Chalcones Anti–inflammatory TNF–α