Effect of different extracts from the Brazilian Atlantic Forest on the Pdr5p ATPase activity

Abstract

RESUMO: "Efeito de extratos de plantas da Floresta Atlântica Brasileira sobre a atividade da Pdr5p ATPase" No presente estudo, testamos o efeito de 27 extratos e frações de plantas de diferentes famílias botânicas sobre a atividade da proteína Pdr5p de membranas plasmáticas de leveduras, responsável pelo fenótipo de resistência a múltiplas drogas em leveduras. Alguns dos extratos foram capazes de produzir uma boa inibição na concentração fi xa de 200 g/mL e foram selecionados para uma investigação mais aprofundada. Curvas de dose-resposta foram obtidas para os extratos brutos etanólicos de Bathysa australis (A. St.-Hill.) Benth. & Hook f., Mabea fi stulifera Mart. e Virola oleifera (Schott) A. C. Sm., com concentrações até 400 g/mL. O menor valor de IC 50 foi obtido para Virola oleifera, 22,8 g/mL, seguido por Bathysa australis, 35,3 g/mL e Mabea fi stulifera, 42,5 g/mL. Após o fracionamento dos extratos brutos por partição líquido-líquido com diferentes solventes orgânicos, cada fração foi novamente testada, sendo que apenas algumas das frações mantiveram a habilidade de inibir a atividade enzimática. Quando analisadas por HPLC/DAD, as frações ativas demonstraram a presença de derivados de fl avonóides, que já demonstraram ter a habilidade de inibir a atividade ATPasica da Pdr5p, assim como outras classes de metabólitos secundários, tais como lignanas e alcalóides. Unitermos:Resistência a múltiplas drogas, levedura, Pdr5p, extratos de plantas, Mata Atlântica. ABSTRACT:In the current study, we tested the effect of 27 plant extracts and fractions from different botanical families on the activity of Pdr5p from yeast plasma membrane, responsible for the multidrug resistance phenotype in yeast cells. Some of the extracts were able to produce a good inhibition in the fi xed concentration (200 g/mL) and were selected for a deeper investigation. Dose-response curves were obtained for the crude ethanol extracts of Bathysa australis (A. St.-Hill.) Benth. & Hook f., Mabea fi stulifera Mart. and Virola oleifera (Schott) A. C. Sm. with concentrations ranging up to 400 g/mL. The lower IC 50 value was obtained for Virola oleifera, 22.8 g/mL, followed by Bathysa australis, 35.3 g/mL, and Mabea fi stulifera, 42.5 g/mL. After fractionation of the crude extracts by liquid-liquid partition with different organic solvents and each fraction was tested again, only some of the fractions retained the ability to inhibit the enzymatic activity. When analyzed by HPLC/DAD, the active fractions showed the presence of fl avonoid derivatives, already reported for their ability to inhibit Pdr5p ATPase activity, as well as other classes of secondary metabolites such as lignans and alkaloids.

Avaliação da atividade de Casearia sylvestris Swartz (Flacourtiaceae) sobre os níveis séricos de triglicerídeos em ratos

“…A literatura tem destacado várias atividades para a planta, algumas delas já comprovadas cientificamente, como seu efeito antiulcera (Basile et al, 1990), atividade antiinflamatória (Ruppelt et al, 1991) e a habilidade de inibir a atividade ATPasica da Pdr5p (Rangel et al, 2008), entretanto não foram encontrados estudos da ação da planta sobre os níveis de triglicerideos sanguíneos, apenas a medicina popular a indicava como hipotrigliceridemiante.…”

Chemistry and Biological Activity of Condamineeae Tribe: A Chemotaxonomic Contribution of Rubiaceae Family

“…Positive results are found for indolic alkaloids and flavonoids on chromatographic tests with B. australis extracts analyzed by HPLC [20]. For B. cuspidata the presence of alkaloids was evaluated by thin layer chromatography [21] and phytochemical analyzes were done through chromatographic reagent tests to the presence of flavonoids, phenolic compounds, alkaloids, tannins, cumarins and triterpenes [22].…”

“…Based on this result the ethanolic extract was fractionated by liquid-liquid partition resulting in hexane, dichloromethane, ethyl acetate and butanol fractions. After the solubilization in 20% of dimethylsulfoxid, the fractions were tested in Pdr5p ATPase on fixed concentration of 200 μg/mL and it was observed that the ethyl acetate, dichloromethane and hexane fractions presented and inhibition on the Pdr5p ATPase activity very similar (around 80%) compared with the ethanolic raw extract, while the butanol fraction produced a very small inhibition (around 20%) [20]. The antifungal evaluation of B. meridionalis, against Alternaria anternata, that causes diseases on tangerines.…”

Inhibition of Saccharomyces cerevisiae Pdr5p by a natural compound extracted from Brazilian Red Propolis

“…Plasma membrane fractions were obtained from yeast S. cerevisiae mutants AD124567 and AD 1234567 (Decottignies et al, 1998) as previously reported by Rangel et al (2008). The plasma membranes highly enriched in Pdr5p were stored in liquid nitrogen.…”