title: α-Mangostin: anti-inflammatory activity and metabolism by human cells.
abstract: Information about the anti-inflammatory activity and metabolism of α-mangostin (α-MG), the most abundant xanthone in mangosteen fruit, in human cells is limited. On the basis of available literature, we hypothesized that α-MG will inhibit the secretion of pro-inflammatory mediators by control and activated macrophage-like THP-1, hepatic HepG2, enterocyte-like Caco-2, and colon HT-29 human cell lines, as well as primary human monocyte-derived macrophages (MDM), and that such activity would be influenced by the extent of metabolism of the xanthone. α-MG attenuated TNF-α and IL-8 secretion by the various cell lines but increased TNF-α output by both quiescent and LPS-treated MDM. The relative amounts of free and phase II metabolites of α-MG and other xanthones present in media 24 h after addition of α-MG was shown to vary by cell type and inflammatory insult. Increased transport of xanthones and their metabolites across Caco-2 cell monolayers suggests enhanced absorption during an inflammatory episode. The anti-inflammatory activities of xanthones and their metabolites in different tissues merit consideration.
authors.affiliation: Interdisciplinary Ph.D. Program in Nutrition, The Ohio State University, Columbus, OH 43210, USA.
authors.forename: Fabiola
authors.initials: F
authors.lastname: Gutierrez-Orozco
authors.forename: Chureeporn
authors.initials: C
authors.lastname: Chitchumroonchokchai
authors.forename: Gregory B
authors.initials: GB
authors.lastname: Lesinski
authors.forename: Sunit
authors.initials: S
authors.lastname: Suksamrarn
authors.forename: Mark L
authors.initials: ML
authors.lastname: Failla
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D029762:Garcinia mangostana / Q000737:chemistry; D006801:Humans; D007202:Indicators and Reagents; D007249:Inflammation / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D044004:Xanthones / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D007202:Indicators and Reagents; D047428:Protein Kinase Inhibitors; D044004:Xanthones; C021053:mangostin