Sandjo Louis P, de Moraes Milene H, Kuete Victor, Kamdoum Blaise C, Ngadjui Bonaventure T, Steindel Mario
Department of Pharmaceutical Sciences, CCS, Universidade Federal de Santa Catarina, Florianópolis 88040-900, Santa Catarina, Brazil.
Department of Microbiology, Immunology and Parasitology, Universidade Federal de Santa Catarina, 88040-900 Florianópolis, Santa Catarina, Brazil.
Bioorg Med Chem Lett. 2016 Apr 1;26(7):1772-5. doi: 10.1016/j.bmcl.2016.02.044. Epub 2016 Feb 17.
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).
对六种植物代谢产物进行了评估,包括异补骨脂查耳酮(1)、4-羟基隆果豆碱(2)、(E)-1-(2,2-二甲基-2H-色烯-6-基)-3-(4-羟基苯基)丙-2-烯-1-酮(3)、6,8-(二-3-甲基-丁-2-烯基)圣草酚(4)、虎刺醛(5)和布氏木宁(6),考察它们对亚马逊利什曼原虫和克氏锥虫细胞内无鞭毛体的杀利什曼原虫和杀锥虫活性。化合物2 - 4和6表现出抗利什曼原虫活性,而3和5表现出杀锥虫作用。6表现出最低的半数抑制浓度(IC50)(5.70μg/mL)的抗利什曼原虫活性,而杀锥虫活性最强的代谢产物(5)的IC50为11.14μg/mL。此外,还研究了以不同比例(3:1、1:1和1:3)配制的1 - 6混合物的抗原虫作用。有趣的是,最初对克氏锥虫无活性的1和2混合在一起时表现出杀锥虫活性。当3(13.63μg/mL)与1按1:1(10.01μg/mL)和3:1(7.78μg/mL)的比例混合时,这种活性增强。此外,在混合物6/4(1:3)中,4对亚马逊利什曼原虫的抗利什曼原虫作用增强。