{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,12]],"date-time":"2026-06-12T22:50:57Z","timestamp":1781304657023,"version":"3.54.1"},"reference-count":32,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2015,12,10]],"date-time":"2015-12-10T00:00:00Z","timestamp":1449705600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Nutrients"],"abstract":"<jats:p>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\u2032,4\u2032,5\u2032-hexamethoxyflavone (1) and 5-hydroxy-6,7,3\u2032,4\u2032,5\u2032-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\u2032,4\u2032,5\u2032-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\u2032,4\u2032,5\u2032-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.<\/jats:p>","DOI":"10.3390\/nu7125537","type":"journal-article","created":{"date-parts":[[2015,12,14]],"date-time":"2015-12-14T02:57:29Z","timestamp":1450061849000},"page":"10388-10397","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3\u2032,4\u2032,5\u2032-Pentamethoxyflavone Isolated from Lantana ukambensis"],"prefix":"10.3390","volume":"7","author":[{"given":"Wamtinga","family":"Sawadogo","sequence":"first","affiliation":[{"name":"Laboratoire de Biologie Mol\u00e9culaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg"},{"name":"Institut de Recherche en Sciences de la Sant\u00e9, Ouagadougou 03 BP 7192, Burkina Faso"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9308-8176","authenticated-orcid":false,"given":"Claudia","family":"Cerella","sequence":"additional","affiliation":[{"name":"Laboratoire de Biologie Mol\u00e9culaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ali","family":"Al-Mourabit","sequence":"additional","affiliation":[{"name":"Institut de Chimie des Substances Naturelles, CNRS-ICSN UPR 2301, Universit\u00e9 Paris-Sud, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"C\u00e9line","family":"Moriou","sequence":"additional","affiliation":[{"name":"Institut de Chimie des Substances Naturelles, CNRS-ICSN UPR 2301, Universit\u00e9 Paris-Sud, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marie-H\u00e9l\u00e8ne","family":"Teiten","sequence":"additional","affiliation":[{"name":"Laboratoire de Biologie Mol\u00e9culaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Innocent","family":"Guissou","sequence":"additional","affiliation":[{"name":"Institut de Recherche en Sciences de la Sant\u00e9, Ouagadougou 03 BP 7192, Burkina Faso"},{"name":"Laboratoire de Pharmacologie et Toxicologie de l\u2019UFR-SDS, Universit\u00e9 de Ouagadougou, BP 7021 Ouagadougou, Burkina Faso"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mario","family":"Dicato","sequence":"additional","affiliation":[{"name":"Laboratoire de Biologie Mol\u00e9culaire et Cellulaire du Cancer, 9 Rue Edward Steichen, L-2540 Luxembourg, Luxembourg"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0115-4725","authenticated-orcid":false,"given":"Marc","family":"Diederich","sequence":"additional","affiliation":[{"name":"Research Institute of Pharmaceutical Sciences, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2015,12,10]]},"reference":[{"key":"ref_1","unstructured":"WHO (2014). Cancer, Fact Sheet N\u00b0297, WHO."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"765","DOI":"10.1016\/j.ejca.2009.12.014","article-title":"Estimates of cancer incidence and mortality in Europe in 2008","volume":"46","author":"Ferlay","year":"2010","journal-title":"Eur. J. Cancer"},{"key":"ref_3","unstructured":"WHO (2011). Global Status Report on Noncommunicable Diseases 2010, WHO."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"311","DOI":"10.1021\/np200906s","article-title":"Natural products as sources of new drugs over the 30 years from 1981 to 2010","volume":"75","author":"Newman","year":"2012","journal-title":"J. Nat. Prod."},{"key":"ref_5","doi-asserted-by":"crossref","first-page":"3641","DOI":"10.3390\/molecules18043641","article-title":"A survey of marine natural compounds and their derivatives with anti-cancer activity reported in 2011","volume":"18","author":"Sawadogo","year":"2013","journal-title":"Molecules"},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"1225","DOI":"10.1016\/j.bcp.2012.07.021","article-title":"Traditional West African pharmacopeia, plants and derived compounds for cancer therapy","volume":"84","author":"Sawadogo","year":"2012","journal-title":"Biochem. Pharmacol."},{"key":"ref_7","unstructured":"Ruffo, C.K., Birnie, A., and Tengnas, B. (2002). Edible Wild Plants of Tanzania. Regional Land Management Unit: Nairobi, RELMA\/Sida ICRAF House."},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"1779","DOI":"10.1007\/s00436-011-2699-3","article-title":"In vitro antileishmanial and antitrypanosomal activities of five medicinal plants from Burkina Faso","volume":"110","author":"Sawadogo","year":"2012","journal-title":"Parasitol. Res."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"575","DOI":"10.1080\/14786419.2010.534737","article-title":"Mutagenic effect, antioxidant and anticancer activities of six medicinal plants from Burkina Faso","volume":"26","author":"Sawadogo","year":"2012","journal-title":"Nat. Prod. Res."},{"key":"ref_10","doi-asserted-by":"crossref","first-page":"9","DOI":"10.1016\/j.pharmthera.2010.01.009","article-title":"Dietary flavonoids in cancer therapy and prevention: Substrates and inhibitors of cytochrome P450 CYP1 enzymes","volume":"126","author":"Androutsopoulos","year":"2010","journal-title":"Pharmacol. Therap."},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"555","DOI":"10.1016\/j.tiv.2003.12.012","article-title":"Prooxidant property of green tea polyphenols epicatechin and epigallocatechin-3-gallate: Implications for anticancer properties","volume":"18","author":"Azam","year":"2004","journal-title":"Toxicol. Vitro"},{"key":"ref_12","doi-asserted-by":"crossref","first-page":"13","DOI":"10.1016\/j.bcp.2010.08.025","article-title":"UNBS1450, a steroid cardiac glycoside inducing apoptotic cell death in human leukemia cells","volume":"81","author":"Juncker","year":"2011","journal-title":"Biochem. Pharmacol."},{"key":"ref_13","doi-asserted-by":"crossref","first-page":"781","DOI":"10.1016\/j.jep.2011.01.038","article-title":"Characterization of the anticancer properties of monoglycosidic cardenolides isolated from Nerium oleander and Streptocaulon tomentosum","volume":"134","author":"Rashan","year":"2011","journal-title":"J. Ethnopharmacol."},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"606","DOI":"10.1016\/j.phymed.2009.12.013","article-title":"Effects of triterpenes from Ganoderma lucidum on protein expression profile of HeLa cells","volume":"17","author":"Yue","year":"2010","journal-title":"Phytomedicine"},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"1207","DOI":"10.1016\/0031-9422(96)00058-1","article-title":"Highly oxygenated flavonoids from Murraya paniculata","volume":"42","author":"Kinoshita","year":"1996","journal-title":"Phytochemistry"},{"key":"ref_16","doi-asserted-by":"crossref","first-page":"966","DOI":"10.1021\/np50059a026","article-title":"Umuhengerin, a new antimicrobially active flavonoid from Lantana trifolia","volume":"51","author":"Rwangabo","year":"1988","journal-title":"J. Nat. Prod."},{"key":"ref_17","doi-asserted-by":"crossref","first-page":"3850","DOI":"10.1016\/j.bmc.2013.04.024","article-title":"Anticancer effect of altersolanol A, a metabolite produced by the endophytic fungus Stemphylium globuliferum, mediated by its pro-apoptotic and anti-invasive potential via the inhibition of NF-\u03baB activity","volume":"21","author":"Teiten","year":"2013","journal-title":"Bioorg. Med. Chem."},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/j.bcp.2009.01.018","article-title":"UNBS1450 from Calotropis procera as a regulator of signaling pathways involved in proliferation and cell death","volume":"78","author":"Juncker","year":"2009","journal-title":"Biochem. Pharmacol."},{"key":"ref_19","doi-asserted-by":"crossref","first-page":"1087","DOI":"10.1007\/s10637-013-9984-1","article-title":"Cardiac glycosides in cancer therapy: From preclinical investigations towards clinical trials","volume":"31","author":"Slingerland","year":"2013","journal-title":"Investig. New Drugs"},{"key":"ref_20","doi-asserted-by":"crossref","first-page":"225","DOI":"10.1016\/j.mito.2012.06.003","article-title":"Assembling the puzzle of anti-cancer mechanisms triggered by cardiac glycosides","volume":"13","author":"Cerella","year":"2013","journal-title":"Mitochondrion"},{"key":"ref_21","doi-asserted-by":"crossref","first-page":"e1782","DOI":"10.1038\/cddis.2015.134","article-title":"Early downregulation of MCL-1 regulates apoptosis triggered by cardiac glycoside UNBS1450","volume":"6","author":"Cerella","year":"2015","journal-title":"Cell Death Dis."},{"key":"ref_22","doi-asserted-by":"crossref","first-page":"1277","DOI":"10.1016\/j.bcp.2011.06.028","article-title":"COX-2 inhibitors block chemotherapeutic agent-induced apoptosis prior to commitment in hematopoietic cancer cells","volume":"82","author":"Cerella","year":"2011","journal-title":"Biochem. Pharmacol."},{"key":"ref_23","doi-asserted-by":"crossref","first-page":"2978","DOI":"10.4161\/cc.10.17.16460","article-title":"COX-2 inhibitors induce early c-Myc downregulation and lead to expression of differentiation markers in leukemia cells","volume":"10","author":"Sobolewski","year":"2011","journal-title":"Cell Cycle"},{"key":"ref_24","doi-asserted-by":"crossref","first-page":"641","DOI":"10.1007\/s10495-009-0328-8","article-title":"Cell cycle arrest in early mitosis and induction of caspase-dependent apoptosis in U937 cells by diallyltetrasulfide (Al2S4)","volume":"14","author":"Cerella","year":"2009","journal-title":"Apoptosis Int. J. Program. Cell Death"},{"key":"ref_25","doi-asserted-by":"crossref","first-page":"999","DOI":"10.1002\/mc.22169","article-title":"Celecoxib prevents curcumin-induced apoptosis in a hematopoietic cancer cell model","volume":"54","author":"Sobolewski","year":"2015","journal-title":"Mol. Carcinog."},{"key":"ref_26","doi-asserted-by":"crossref","first-page":"322","DOI":"10.1124\/jpet.115.225011","article-title":"2,5-Dimethyl-Celecoxib Inhibits Cell Cycle Progression and Induces Apoptosis in Human Leukemia Cells","volume":"355","author":"Sobolewski","year":"2015","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"ref_27","doi-asserted-by":"crossref","first-page":"7592","DOI":"10.1016\/j.bmc.2008.07.018","article-title":"Inhibitory effects of polymethoxy flavones isolated from Citrus reticulate on degranulation in rat basophilic leukemia RBL-2H3: Enhanced inhibition by their combination","volume":"16","author":"Itoh","year":"2008","journal-title":"Biorg. Med. Chem."},{"key":"ref_28","doi-asserted-by":"crossref","first-page":"4524","DOI":"10.1016\/j.bmc.2010.04.061","article-title":"Synthesis and antitumor activity of 2,5-bis(3\u2032-indolyl)-furans and 3,5-bis(3\u2032-indolyl)-isoxazoles, nortopsentin analogues","volume":"18","author":"Diana","year":"2010","journal-title":"Bioorg. Med. Chem."},{"key":"ref_29","first-page":"261","article-title":"A novel adriamycin analogue derived from marine microbes induces apoptosis by blocking AKT activation in human breast cancer cells","volume":"4","author":"Yuan","year":"2011","journal-title":"Mol. Med. Rep."},{"key":"ref_30","doi-asserted-by":"crossref","first-page":"643","DOI":"10.3390\/md11030643","article-title":"Synthesis and Antiproliferative Activity of 2,5-bis(3\u2032-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin","volume":"11","author":"Carbone","year":"2013","journal-title":"Mar. Drugs"},{"key":"ref_31","doi-asserted-by":"crossref","first-page":"235","DOI":"10.1016\/S1056-8719(00)00107-6","article-title":"Drug-like properties and the causes of poor solubility and poor permeability","volume":"44","author":"Lipinski","year":"2000","journal-title":"J. Pharmacol. Toxicol. Methods"},{"key":"ref_32","doi-asserted-by":"crossref","first-page":"3","DOI":"10.1016\/S0169-409X(00)00129-0","article-title":"Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings","volume":"46","author":"Lipinski","year":"2001","journal-title":"Adv. Drug Deliv. Rev."}],"container-title":["Nutrients"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/2072-6643\/7\/12\/5537\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T20:53:48Z","timestamp":1760216028000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/2072-6643\/7\/12\/5537"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2015,12,10]]},"references-count":32,"journal-issue":{"issue":"12","published-online":{"date-parts":[[2015,12]]}},"alternative-id":["nu7125537"],"URL":"https:\/\/doi.org\/10.3390\/nu7125537","relation":{},"ISSN":["2072-6643"],"issn-type":[{"value":"2072-6643","type":"electronic"}],"subject":[],"published":{"date-parts":[[2015,12,10]]}}}