title: Anti-Trichomonas vaginalis activity of Hypericum polyanthemum extract obtained by supercritical fluid extraction and isolated compounds.
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.
authors.affiliation: Laboratório de Farmacognosia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, RS, Brazil.
authors.forename: Simone Tasca
authors.initials: ST
authors.lastname: Cargnin
authors.forename: Patrícia de Brum
authors.initials: Pde B
authors.lastname: Vieira
authors.forename: Samuel
authors.initials: S
authors.lastname: Cibulski
authors.forename: Eduardo
authors.initials: E
authors.lastname: Cassel
authors.forename: Rubem Mário Figueiró
authors.initials: RM
authors.lastname: Vargas
authors.forename: Jarbas
authors.initials: J
authors.lastname: Montanha
authors.forename: Paulo
authors.initials: P
authors.lastname: Roehe
authors.forename: Tiana
authors.initials: T
authors.lastname: Tasca
authors.forename: Gilsane Lino
authors.initials: GL
authors.lastname: von Poser
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001578:Benzopyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002462:Cell Membrane / Q000187:drug effects; D002470:Cell Survival; D002522:Chlorocebus aethiops; D025924:Chromatography, Supercritical Fluid / Q000379:methods*; D020902:Hypericum / Q000737:chemistry*; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008795:Metronidazole / Q000494:pharmacology; D010696:Phloroglucinol / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015800:Protozoan Proteins / Q000378:metabolism; D014246:Trichomonas vaginalis / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D014709:Vero Cells
chemical_list: C539960:5-hydroxy-6-isobutyryl-7-methoxy-2,2-dimethyl-benzopyran; C539958:6-isobutyryl-5,7-dimethoxy-2,2-dimethyl-benzopyran; C539959:7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethyl-benzopyran; D000981:Antiprotozoal Agents; D001578:Benzopyrans; D010936:Plant Extracts; D015800:Protozoan Proteins; D008795:Metronidazole; D010696:Phloroglucinol; D007770:L-Lactate Dehydrogenase; C547933:uliginosin B