title: Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
abstract: Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2-4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1-6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).
authors.affiliation: Department of Pharmaceutical Sciences, CCS, Universidade Federal de Santa Catarina, Florianópolis 88040-900, Santa Catarina, Brazil. Electronic address: p.l.sandjo@ufsc.br.
authors.forename: Louis P
authors.initials: LP
authors.lastname: Sandjo
authors.affiliation: Department of Microbiology, Immunology and Parasitology, Universidade Federal de Santa Catarina, 88040-900 Florianópolis, Santa Catarina, Brazil.
authors.forename: Milene H
authors.initials: MH
authors.lastname: de Moraes
authors.affiliation: Department of Biochemistry, Faculty of Science, University of Dschang, PO Box 67, Dschang, Cameroon.
authors.forename: Victor
authors.initials: V
authors.lastname: Kuete
authors.affiliation: Department of Organic Chemistry, University of Yaoundé 1, PO Box 812, Yaoundé, Cameroon.
authors.forename: Blaise C
authors.initials: BC
authors.lastname: Kamdoum
authors.affiliation: Department of Organic Chemistry, University of Yaoundé 1, PO Box 812, Yaoundé, Cameroon.
authors.forename: Bonaventure T
authors.initials: BT
authors.lastname: Ngadjui
authors.affiliation: Department of Microbiology, Immunology and Parasitology, Universidade Federal de Santa Catarina, 88040-900 Florianópolis, Santa Catarina, Brazil. Electronic address: mario.steindel@ufsc.br.
authors.forename: Mario
authors.initials: M
authors.lastname: Steindel
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology; D000880:Anthraquinones / Q000737:chemistry / Q000494:pharmacology; D000977:Antiparasitic Agents / Q000737:chemistry* / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology; D014355:Chagas Disease / Q000188:drug therapy; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology; D044950:Flavanones / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007894:Leishmania mexicana / Q000187:drug effects*; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy; D029586:Moraceae / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D010944:Plants / Q000737:chemistry*; D019666:Rubiaceae / Q000737:chemistry; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects*; D032106:Zanthoxylum / Q000737:chemistry
chemical_list: D000470:Alkaloids; D000880:Anthraquinones; D000977:Antiparasitic Agents; D000981:Antiprotozoal Agents; D047188:Chalcones; D044950:Flavanones; D010936:Plant Extracts; D014344:Trypanocidal Agents
keywords: Activity in combination; Antiparasitic effect; Secondary metabolites