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- W2791740279 abstract "Abstract Bioactive molecules isolated from plants are promising sources for the development of new therapies against leishmaniasis. We investigated the leishmanicidal activity of cariphenone A (1), isouliginosin B (2) and uliginosin B (3) isolated from Hypericum species. Promastigotes and amastigotes of Leishmania amazonensis were incubated with compounds 1–3 at concentrations 1–100 µ m for 48 h. The anti-promastigote effect of compounds was also tested in combinations. The cytotoxicity against macrophages and human erythrocytes were determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) method and hemolysis assay, respectively. The compounds 1–3 showed high leishmanicidal activity against promastigotes, IC 50 values of 10.5, 17.5 and 11.3 µ m , respectively. Synergistic interactions were found to the associations of compounds 1 and 2 [Σ fractional inhibitory concentration (FIC) = 0.41], and 2 and 3 (ΣFIC = 0.28) on promastigotes. All Hypericum compounds induced mitochondrial hyperpolarization and reactive oxygen species production in promastigotes. The compounds showed low cytotoxicity toward mammalian cells, high selectivity index and killed intracellular amastigotes probably mediated by oxidative stress. These results indicate that these compounds are promising candidates for the development of drugs against leishmaniasis." @default.
- W2791740279 created "2018-03-29" @default.
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- W2791740279 date "2018-02-27" @default.
- W2791740279 modified "2023-10-12" @default.
- W2791740279 title "Phloroglucinol derivatives from <i>Hypericum</i> species trigger mitochondrial dysfunction in <i>Leishmania amazonensis</i>" @default.
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- W2791740279 doi "https://doi.org/10.1017/s0031182018000203" @default.
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