title: Bioactive phloroglucinols from Mallotus oppositifolius.
abstract: The two new acylphloroglucinol derivatives, methylene-bis-aspidinol AB (1) and mallopposinol (2), together with the nine known compounds, aspidinol B (3), methylene-bis-aspidinol (4), (+)-α-tocopherol (5), lupeol (6), stigmasterol (7), phytol (8), bergenin (9), squalene (11) and methyl gallate (10) were isolated from the leaves of Mallotus oppositifolius. Their structures were elucidated by spectral analysis including MS, 1D and 2D-NMR spectroscopy. In vitro trypanocidal and antileishmanial activities of compounds 1-9 were evaluated. Mallopposinol (2) and aspidinol B (3) displayed weak antileishmanial activities against Leishmania donovani promastigotes, with EC50 values of 21.3 and 38.8μM, respectively. Only the methylene-bis-aspidinol (4) exhibited trypanocidal activity against Trypanosoma brucei brucei trypomastigotes (LC100=0.8μM) similar to the reference drug pentamidine (LC100=0.4μM).
authors.affiliation: Laboratoire de Chimie Organique Biologique, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphouët-Boigny, 22 BP 582 Abidjan 22, Côte d'Ivoire; Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France. Electronic address: kabranakafaustin@yahoo.fr.
authors.forename: Faustin A
authors.initials: FA
authors.lastname: Kabran
authors.affiliation: Laboratoire de Chimie Organique Biologique, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphouët-Boigny, 22 BP 582 Abidjan 22, Côte d'Ivoire.
authors.forename: Timothée A
authors.initials: TA
authors.lastname: Okpekon
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: François
authors.initials: F
authors.lastname: Roblot
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Blandine
authors.initials: B
authors.lastname: Séon-Méniel
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Karine
authors.initials: K
authors.lastname: Leblanc
authors.affiliation: Laboratoire de Chimiothérapie Antiparasitaire, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Christian
authors.initials: C
authors.lastname: Bories
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Pierre
authors.initials: P
authors.lastname: Champy
authors.affiliation: Laboratoire de Chimie Analytique, UFR des Sciences Pharmaceutiques et Biologiques, Université Félix Houphouët-Boigny, 22 BP 714 Abidjan 22, Côte d'Ivoire.
authors.forename: Séri F
authors.initials: SF
authors.lastname: Yolou
authors.affiliation: Laboratoire de Chimiothérapie Antiparasitaire, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Philippe M
authors.initials: PM
authors.lastname: Loiseau
authors.affiliation: Laboratoire de Chimie Organique Biologique, UFR Sciences des Structures de la Matière et Technologie, Université Félix Houphouët-Boigny, 22 BP 582 Abidjan 22, Côte d'Ivoire.
authors.forename: Léon A
authors.initials: LA
authors.lastname: Djakouré
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France.
authors.forename: Bruno
authors.initials: B
authors.lastname: Figadère
authors.affiliation: Laboratoire de Pharmacognosie, UMR BioCIS, CNRS, Univ. Paris-Sud, Université Paris-Saclay, 92296 Châtenay-Malabry, France. Electronic address: alexandre.maciuk@u-psud.fr.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Maciuk
mesh_terms: D000981:Antiprotozoal Agents / Q000302:isolation & purification / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D036461:Mallotus Plant / Q000737:chemistry*; D015394:Molecular Structure; D010696:Phloroglucinol / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D010936:Plant Extracts; D010696:Phloroglucinol
keywords: (+)-tocophérol (PubChem CID: 14985); Aspidinol B (PubChem CID: 122841); Euphorbiaceae; Leishmania donovani; Mallotus oppositifolius; Methylene-bis-aspidinol (PubChem CID: 617027); Phloroglucinol; Trypanosoma brucei brucei; bergenin (PubChem CID: 66065); lupeol (PubChem CID: 259846); methyl gallate (PubChem CID: 7428); phytol (PubChem CID: 5280435); squalene (PubChem CID: 638072); stigmasterol (PubChem CID: 5280794)