Abstract
The anti-Trichomonas vaginalis activity of Hypericum polyanthemum extract obtained by supercritical fluid extraction (50°C, 150bar) and the chemical compounds isolated and purified from this extract (benzopyrans HP1, HP2, HP3, and phloroglucinol derivative uliginosin B) were assessed. All samples had anti-T. vaginalis activity; however, HP1 demonstrated the best selectivity against this protozoan (metronidazole-resistant and susceptible isolates), with no cytotoxicity on mammalian cells (selectivity index of 73.97). Moreover, HP1 had activity against a metronidazole-resistant isolate (52% of viable trophozoites), and this effect was higher when tested with a low concentration of metronidazole (23% of viable trophozoites). Experiments demonstrated that all isolated compounds caused damage to the parasites' membrane (>90% of LDH release) and do not present a notable hemolytic effect, although HP2 and uliginosin B exhibited cytotoxicity against mammalian cells. Therefore, the analyzed molecules are promising prototypes for new antiprotozoal drugs, especially HP1, which seems to improve metronidazole's effect on a resistant T. vaginalis isolate.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / isolation & purification
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Antiprotozoal Agents / pharmacology*
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Benzopyrans / chemistry
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Benzopyrans / isolation & purification
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Benzopyrans / pharmacology
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Cell Membrane / drug effects
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Cell Survival
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Chlorocebus aethiops
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Chromatography, Supercritical Fluid / methods*
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Hypericum / chemistry*
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L-Lactate Dehydrogenase / metabolism
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Metronidazole / pharmacology
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Phloroglucinol / analogs & derivatives
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Phloroglucinol / chemistry
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Phloroglucinol / isolation & purification
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Phloroglucinol / pharmacology
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Plant Components, Aerial / chemistry
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Protozoan Proteins / metabolism
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Trichomonas vaginalis / drug effects*
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Trichomonas vaginalis / enzymology
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Trichomonas vaginalis / physiology
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Vero Cells
Substances
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5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl-benzopyran
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6-isobutyryl-5,7-dimethoxy-2,2-dimethyl-benzopyran
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7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran
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Antiprotozoal Agents
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Benzopyrans
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Plant Extracts
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Protozoan Proteins
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Metronidazole
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Phloroglucinol
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L-Lactate Dehydrogenase
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uliginosin B