title: Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3',4',5'-Pentamethoxyflavone Isolated from Lantana ukambensis.
abstract: Lantana ukambensis (Vatke) Verdc. is an African food and medicinal plant. Its red fruits are eaten and highly appreciated by the rural population. This plant was extensively used in African folk medicinal traditions to treat chronic wounds but also as anti-leishmanial or cytotoxic remedies, especially in Burkina Faso, Tanzania, Kenya, or Ethiopia. This study investigates the in vitro bioactivity of polymethoxyflavones extracted from a L. ukambensis as anti-proliferative and pro-apoptotic agents. We isolated two known polymethoxyflavones, 5,6,7,3',4',5'-hexamethoxyflavone (1) and 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) from the whole plant of L. ukambensis. Their chemical structures were determined by spectroscopic analysis and comparison with published data. These molecules were tested for the anti-proliferative, cytotoxic and pro-apoptotic effects on human cancer cells. Among them, 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) was selectively cytotoxic against monocytic lymphoma (U937), acute T cell leukemia (Jurkat), and chronic myelogenous leukemia (K562) cell lines, but not against peripheral blood mononuclear cells (PBMCs) from healthy donors, at all tested concentrations. Moreover, this compound exhibited significant anti-proliferative and pro-apoptotic effects against U937 acute myelogenous leukemia cells. This study highlights the anti-proliferative and pro-apoptotic effects of 5-hydroxy-6,7,3',4',5'-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.
authors.affiliation: Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg. richard.sawadogo@lbmcc.lu.|Institut de Recherche en Sciences de la Santé, Ouagadougou 03 BP 7192, Burkina Faso. richard.sawadogo@lbmcc.lu.
authors.forename: Wamtinga Richard
authors.initials: WR
authors.lastname: Sawadogo
authors.affiliation: Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg. claudia.cerella@lbmcc.lu.
authors.forename: Claudia
authors.initials: C
authors.lastname: Cerella
authors.affiliation: Institut de Chimie des Substances Naturelles, CNRS-ICSN UPR 2301, Université Paris-Sud, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France. Ali.ALMOURABIT@cnrs.fr.
authors.forename: Ali
authors.initials: A
authors.lastname: Al-Mourabit
authors.affiliation: Institut de Chimie des Substances Naturelles, CNRS-ICSN UPR 2301, Université Paris-Sud, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France. Celine.Moriou@cnrs.fr.
authors.forename: Céline
authors.initials: C
authors.lastname: Moriou
authors.affiliation: Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg. marie_helene.teiten@lbmcc.lu.
authors.forename: Marie-Hélène
authors.initials: MH
authors.lastname: Teiten
authors.affiliation: Institut de Recherche en Sciences de la Santé, Ouagadougou 03 BP 7192, Burkina Faso. ip_guissou@yahoo.fr.|Laboratoire de Pharmacologie et Toxicologie de l'UFR-SDS, Université de Ouagadougou, BP 7021 Ouagadougou, Burkina Faso. ip_guissou@yahoo.fr.
authors.forename: Innocent Pierre
authors.initials: IP
authors.lastname: Guissou
authors.affiliation: Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg. mdicato@gmail.com.
authors.forename: Mario
authors.initials: M
authors.lastname: Dicato
authors.affiliation: Research Institute of Pharmaceutical Sciences, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Korea. marcdiederich@snu.ac.kr.
authors.forename: Marc
authors.initials: M
authors.lastname: Diederich
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D047309:Flavones / Q000737:chemistry / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D019169:Jurkat Cells; D020014:K562 Cells; D032410:Lantana / Q000737:chemistry*; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry; D020298:U937 Cells
chemical_list: D047309:Flavones; D005419:Flavonoids; D010936:Plant Extracts; C057913:umuhengerin; C008661:nobiletin; C059006:tangeretin
keywords: Lantana ukambensis; anti-proliferative; cancer; cytotoxic; polymethoxyflavone; pro-apoptotic