Abstract
A microplate assay and a thin-layer chromatography (TLC) "in situ" assay based on the Ellman assay was used to screen for acetylcholinesterase inhibitors from ethyl acetate and methanol extracts of Brazilian medicinal plants of families that, according to the literature, have traditional uses that might be connected with acetylcholinesterase inhibition. Eighteen species belonging to Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae and Rutaceae families were tested. The most active plants were Ipomoea asarifolia (IC50 = 0.12 mg/mL), Jatropha curcas (IC50 = 0.25 mg/mL), Jatropha gossypiifolia (IC50 = 0.05 mg/mL), Kalanchoe brasiliensis (IC50 = 0.16 mg/mL) and Senna alata (IC50 = 0.08 mg/mL). The most promising extracts were the Jatropha gossypiifolia and Senna alata species assuming there were compounds with a similar activity to galanthamine, which should contain about 1% of an active compound, or if present at lower levels even more active compounds than galanthamine (IC50 = 0.37 x 10-3 mg/mL) should be present.
Highlights
Based on the cholinergic hypothesis, acetylcholinesterase inhibitors (AChEIs) are widely used to treat Alzheimer’s disease (Francis et al, 1999)
In order to discover novel potential sources for AChEIs, a microplate assay and a thin-layer chromatography (TLC) assay were used to screen for AChE inhibitory activity in ethyl acetate and methanol extracts from Brazilian medicinal plants (Ellman et al, 1961; Ingkaninan et al, 2001)
Eighteen species were screened and the results show that several plants are very interesting candidates for further isolation of AChEIs
Summary
Based on the cholinergic hypothesis, acetylcholinesterase inhibitors (AChEIs) are widely used to treat Alzheimer’s disease (Francis et al, 1999). Galanthamine, an alkaloid from plants of the Amaryllidaceae family, is a selective reversible long-acting and competitive acetylcholinesterase inhibitor (AChEI). This compound is considered to be more effective in the treatment of Alzheimer’s disease (AD) and to have fewer limitations than physostigmine and tacrine (Gordon et al, 2000). In order to discover novel potential sources for AChEIs, a microplate assay and a TLC assay were used to screen for AChE inhibitory activity in ethyl acetate and methanol extracts from Brazilian medicinal plants (Ellman et al, 1961; Ingkaninan et al, 2001).
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