Acetylcholinesterase inhibition by somes promising Brazilian medicinal plants

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 (IC 50 = 0.12 mg/mL), Jatropha curcas (IC 50 = 0.25 mg/mL), Jatropha gossypiifolia (IC 50 = 0.05 mg/mL), Kalanchoe brasiliensis (IC 50 = 0.16 mg/mL) and Senna alata (IC 50 = 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 (IC 50 = 0.37 x 10 -3 mg/ mL) should be present.Keywords: Brazilian medicinal plants, Alzheimer's disease, acetylcholinesterase inhibitors, microplate assay. Plantas medicinais brasileiras promissoras para inibição da acetilcolinesterase ResumoOs ensaios de microplaca e cromatografia em camada delgada com base no ensaio de Ellman foram usados para triagem de inibidores da acetilcolinesterase dos extratos acetato de etila e metanol de plantas medicinais brasileiras de famílias que, segundo a literatura, tem usos tradicionais que podem estar relacionadas com a inibição da acetilcolinesterase, enzima associada ao mal de Alzheimer. Dezoito plantas das famílias: Convolvulaceae, Crassulaceae, Euphorbiaceae, Leguminosae, Malvaceae, Moraceae, Nyctaginaceae e Rutaceae foram testadas. As espécies mais ativas foram Ipomoea asarifolia (CI 50 = 0,12 mg/mL), Jatropha curcas (CI 50 = 0,25 mg/mL), Jatropha gossypiifolia (CI 50 = 0,05 mg/mL), Kalanchoe brasiliensis (CI 50 = 0,16 mg/mL) e Senna alata (CI 50 = 0,08 mg/mL). Os extratos mais promissores foram os das espécies Jatropha gossypiifolia e Senna alata, assumindo a presença de compostos com atividade semelhante à galantamina que deve conter cerca de 1% de um composto ativo, ou se presentes em menores níveis ainda mais compostos ativos que a galantamina (CI 50 = 0,37 x10 -3 mg/mL) devem estar presentes.Palavras-chave: plantas medicinais brasileiras, doença de Alzheimer, inibidores da acetilcolinesterase, microplaca.

A comparative study of Bulgarian and Turkish Asphodeline lutea root extracts: HPLC–UV profiles, enzyme inhibitory potentials and anti-proliferative activities against MCF-7 and MCF-10A cell lines

“…This is consistent with the results from the present study, where the relative ratio of the bianthraquinones in the total anthraquinone content seems a feature responsible for the higher AChE inhibitory effect of ALT compared with that of ALB. Our results are in good correlation with the findings of Feitosa, Freitas, Luz, Bezerra, and Trevisan (2011) who observed high AChE inhibitory potential of Cassia alata (Senna alata), which is well known for its anthraquinone content. However, further studies are needed to discover the individual components responsible for the discussed inhibition potential.…”

<b>Larvicidal, cytotoxic and genotoxic effects of aqueous leaf extract of <i>Jatropha mollissima</i> (Pohl) Baill

“…Coumarins, as well as alkaloids, may act as inhibitors of acetylcholinesterase (ACheI), an enzyme that promotes the uptake of acetylcholine at the neuronal synapses, thus leading to paralysis and death of the larvae (Khanikor, Parida, Yadav, & Bora, 2013). The activity of ACheI has been confirmed in the leaf extracts of J. curcas and J. gossypiifolia (Feitosa, Freitas, Luz, Bezerra, & Trevisan, 2011). However, the presence of the mentioned phytochemicals at lower concentrations (0.005, 0.01, 0.02 and 0.04 mg mL -1 ) might possibly have a protective effect, thus justifying the absence of larvicidal potential.…”

Evaluation of Acetylcholinesterase inhibition by Alnus rugosa L. stems methanol extract and phytochemical content

“…Table 1 Alnus rugosa stems methanol extract seems of interest for further study. Plants that have shown favorable effects in relation to cognitive disorders, including anticholinesterase, anti-inflammatory and antioxidant activities or other relevant pharmacological activities are potentially of interest to clinical use for Alzheimer's disease 13 . Eighteen medicinal plants of Brazil were screened for inhibitory activity on AchE, the results show that various plants are very interesting for further isolation of acetylcholinesterase inhibitors, which are widely used in the treatment of Alzheimer's disease, galanthamine, an alkaloid from plants of the Amaryllidaceae family, is a selective reversible long-acting and competitive acetylcholinesterase inhibitor (AChEI).…”