Hydroalcoholic extract of Tagetes minuta L. inhibits inflammatory bowel disease through the activity of pheophytins on the NF-κB signalling pathway

• Published in: Journal of ethnopharmacology Vol. 268; p. 113603
• Main Authors: Apaza Ticona, Luis, Lacheva, Ginka Ilieva, Serban, Andreea Madalina, Rumbero Sánchez, Ángel
• Format: Journal Article
• Language: English
• Published: Ireland Elsevier B.V 25.03.2021
• Subjects: Anti-inflammatory; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; Cell Line; Dose-Response Relationship, Drug; Ethanol - isolation & purification; Ethanol - pharmacology; Ethanol - therapeutic use; Humans; Inflammatory Bowel Diseases - drug therapy; Inflammatory Bowel Diseases - metabolism; NF-kappa B - antagonists & inhibitors; NF-kappa B - metabolism; NF-κB; Pheophytins; Pheophytins - isolation & purification; Pheophytins - pharmacology; Pheophytins - therapeutic use; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Signal Transduction - drug effects; Signal Transduction - physiology; Tagetes; Tagetes minuta; TNF-α; Water - pharmacology; Pheophytins; NF-κB; Tagetes minuta; TNF-α; Anti-inflammatory
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2020.113603

Species of the genus Tagetes are well known for their anti-inflammatory properties. Tagetes minuta “Huacatay” is an endemic species of South America that has been used in traditional medicine since ancient times as a remedy for stomach and intestinal discomfort. The aim of this study is to investigate the anti-inflammatory activity of the aqueous and hydroalcoholic extracts of the Huacatay, identifying the compounds responsible for this activity. Anti-inflammatory activity of the compounds, fractions and extracts was evaluated in Hs 746T (stomach), HIEC-6 (intestine) and THP-1 (monocytes peripheral blood) cells by measuring their inhibitory capacity against the NF-κB production. Aqueous and hydroalcoholic extracts of Tagetes minuta displayed anti-inflammatory activity in vitro, the hydroalcoholic extract being the most active (IC50 between 59.72 and 66.42 μg/mL) in all cell lines. Bio-guided hydroalcoholic extract fractionation led to the isolation and characterisation of two pheophytins, pheophytin a (1) and 132-hydroxy pheophytin a (2). Both compounds inhibited the production of NF-κB with IC50 values in the low micromolar range, with an IC50 between 12.32 and 16.01 μM for compound 1 and 7.91–9.87 μM for compound 2. The two pheophytins isolated in this study inhibit the production of NF-κB, thus showing that the traditional anti-inflammatory use of Tagetes minuta can be proved through pharmacological assays. This contributes to understanding the anti-inflammatory activity of the Huacatay extracts and their use in the treatment of stomach and intestinal discomfort. [Display omitted] •Tagetes minuta L. extracts inhibit NF-κB production in vitro.•Pheophytin a and 132-hydroxy pheophytin a have been isolated from Tagetes minuta L.•Pheophytin a and 132-hydroxy pheophytin a inhibit NF-κB production in vitro