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

2008; Springer Science+Business Media; Volume: 18; Issue: 1 Linguagem: Inglês

10.1590/s0102-695x2008000100008

1981-528X

Luciana P. Rangel, Lisandra Ferreira de Abreu, A. Andrade, Suzana Guimarães Leitão, Gilda Guimarães Leitão, Antônio Ferreira‐Pereira,

HIV/AIDS drug development and treatment

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 fixed concentration (200 µg/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 fistulifera Mart. and Virola oleifera (Schott) A. C. Sm. with concentrations ranging up to 400 µg/mL. The lower IC50 value was obtained for Virola oleifera, 22.8 µg/mL, followed by Bathysa australis, 35.3 µg/mL, and Mabea fistulifera, 42.5 µg/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 flavonoid derivatives, already reported for their ability to inhibit Pdr5p ATPase activity, as well as other classes of secondary metabolites such as lignans and alkaloids.