ABSTRACT
Crude extracts and fractions of five species of Polygala - P. campestris, P. cyparissias, P. paniculata, P. pulchella and P. sabulosa - were investigated for their in vitro antifungal activity against opportunistic Candida species, Cryptococcus gattii and Sporothrix schenckii with bioautographic and microdilution assays. In the bioautographic assays, the major extracts were active against the fungi tested. In the minimal concentration inhibitory (MIC) assay, the hexane extract of P. paniculata and EtOAc fraction of P. sabulosa showed the best antifungal activity, with MIC values of 60 and 30 µg/mL, respectively, against C. tropicalis, C. gattii and S. schenckii. The compounds isolated from P. sabulosa prenyloxycoumarin and 1,2,3,4,5,6-hexanehexol displayed antifungal activity against S. schenckii (with MICs of 125 µg/mL and 250 µg/mL, respectively) and C. gattii (both with MICs of 250 µg/mL). Rutin and aurapten isolated from P. paniculata showed antifungal activity against C. gattii with MIC values of 60 and 250 µg/mL, respectively. In the antifungal screening, few of the isolated compounds showed good antifungal inhibition. The compound á-spinasterol showed broad activity against the species tested, while rutin had the best activity with the lowest MIC values for the microorganisms tested. These two compounds may be chemically modified by the introduction of a substitute group that would alter several physico-chemical properties of the molecule, such as hydrophobicity, electronic density and steric strain.
Subject(s)
In Vitro Techniques , Plant Structures , Polygala , Polygalaceae/growth & development , Rutin/analysis , PlantsABSTRACT
A bioatividade das frações e compostos obtidos de Polygala sabulosa contra as formas epimastigota, tripomastigota sanguínea e amastigota de Trypanosoma cruzi foram avaliadas in vitro. Frações diclorometano e acetato de etila mostraram potente atividade tripanocida sob as formas epimastigotas (IC50 < 10,4 µg/mL). Análises por cromatografia em camada delgada destas frações confirmaram a presença de compostos previamente descritos (dihidroestiril-2-pironas, estiril-2-pironas e 6-metoxi-7-preniloxicumarina). Após o fracionamento da fração diclorometano por cromatografia em coluna, obteve-se o composto α-espinasterol e da fração acetato de etila obtiveram-se os compostos apigenina, quercetina e uma quercetina-3- O-glicosídeo, todos descritos pela primeira vez para o gênero Polygala. 4-metoxi-6-(11,12-metilenodioxi-14-metoxidihidroestiril)-2-pirona, 4-metoxi-6-(11,12-dimetoxi-14-metoxiestiril)-2-pirona, 6-metoxi-7-preniloxicumarina e quercetina-3- O-glicosídeo mostraram fraca atividade contra a forma tripomastigota sanguínea (IC50 < 1008,6 µg/mL). A cumarina prenilada foi o composto mais ativo contra ambas as formas epimastigota e tripomastigota, com IC50 10,5 e 88,2 µg/mL, respectivamente. A atividade hemolítica e a toxicidade celular de cada composto foram também avaliadas. Além disso, 4-metoxi-6-(11,12-metilenodioxi-14-metoxidihidroestiril)-2-pirona e 6-metoxi-7-preniloxicumarina reduziram em quatro vezes a infecção em ratos por Vero Cells nas concentrações de 100 e 50 µg/mL respectivamente. Esses resultados mostram, pela primeira vez, a atividade de compostos de P. sabulosa contra T. cruzi.
Bioactivity of fractions and compounds obtained from Polygala sabulosa against Trypanosoma cruzi epimastigote, blood trypomastigote and amastigote forms were evaluated in vitro. Dichloromethane and ethyl acetate fractions showed a strong trypanocidal activity on epimastigotes (IC50 < 10.4 µg/mL). Chromatographic analysis by TLC of these fractions confirmed the presence of previously described compounds (dihydrostyryl-2-pyrones, styryl-2-pyrones and 6-methoxy-7-prenyloxycoumarin). The dichloromethane fraction was fractioned by silica gel column chromatography to afford the compound α-spinasterol and the ethyl acetate fraction yielded apigenin, quercetin and a quercetin-3-O-glucoside, being the first description for the Polygala genus. 4-Methoxy-6-(11,12-methylenedioxy-14-methoxydihydrostyryl)-2-pyrone, 4-methoxy-6-(11,12-dimethoxystyryl)-2-pyrone, 6-methoxy-7-prenyloxycoumarin and quercetin-3-O-glucoside showed a weak activity against blood trypomastigotes (IC50 < 1008.6 µg/mL). The prenylated coumarin was the most active compound against both epimastigote and trypomastigote forms, IC50 10.5 and 88.2 µg/mL, respectively. The hemolytic activity and cell toxicity of each active compound was also assessed. Furthermore, 4-methoxy-6-(11,12-methylenedioxy-14-methoxydihydrostyryl)-2-pyrone and 6-methoxy-7-prenyloxycoumarin reduced 4 times the T. cruzi infection rate for Vero cells at 100 and 50 µg/mL, respectively. These results show for the first time active compounds against T. cruzi in P. sabulosa.
ABSTRACT
Os extratos obtidos pela maceração em CHCl3/MeOH (2:1) de 8 amostras de espécies medicinais e 11 amostras comerciais de chás foram analisados por cromatografia em camada delgada (CCD). Glicolipídios foram detectados em todas as amostras, porém com diferenças quali-quantitativas. Para as plantas medicinais, a maior concentração de glicolipídios foi detectada em Lippia alba e Cymbopogon citratus, enquanto em amostras comerciais, o melhor perfil glicolipídico foi encontrado nos extratos de C. citratus e Baccharis trimera.
The extracts obtained by maceration in CHCl3/MeOH (2:1) of 8 medicinal plants and 11 commercial samples (tea bags) were analysed by thin-layer chromatography. Glycolipids were detected in all the samples, with qualitative and quantitative differences. For the medicinal plants, the highest concentrations were detected in Lippia alba and Cymbopogon citratus. For the commercial samples, the best glycolipidic profiles were found in C. citratus and Baccharis trimera extracts.