کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2545031 1560399 2015 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Characterization of Pterocarpus erinaceus kino extract and its gamma-secretase inhibitory properties
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی داروشناسی
پیش نمایش صفحه اول مقاله
Characterization of Pterocarpus erinaceus kino extract and its gamma-secretase inhibitory properties
چکیده انگلیسی

Ethnopharmacological relevanceThe aqueous decoction of Pterocarpus erinaceus has been traditionally used in Benin against memory troubles.Aim of the studyNew strategies are needed against Alzheimer׳s disease (AD), for, to date, AD treatment is symptomatic and consists in drugs treating the cognitive decline. An interesting target is the β-amyloid peptide (Aβ), whose accumulation and progressive deposition into amyloid plaques are key events in AD aetiology.Identifying new and more selective γ-secretase inhibitors or modulators (none of the existing has proven so far to be selective or fully efficient) appears in this respect of particular interest. We studied the activity and mechanisms of action of Pterocarpus erinaceus kino aqueous extract, after the removal of catechic tannins (KAST).Methods and resultsWe tested KAST at non-toxic concentrations on cells expressing the human Amyloid Precursor Protein (APP695), as well as on primary neurons. Pterocarpus erinaceus extract was found to inhibit Aβ release in both models. We further showed that KAST inhibited γ-secretase activity in cell-free and in vitro assays, strongly suggesting that KAST is a natural γ-secretase inhibitor. Importantly, this extract did not inhibit the cleavage of Notch, another γ-secretase substrate responsible for major detrimental side effects observed with γ-secretase inhibitors. Epicatechin was further identified in KAST by HPLC-MS.ConclusionPterocarpus erinaceus kino extract appears therefore as a new γ-secretase inhibitor selective towards APP processing.

Pterocarpus erinaceus kino extract acts as a natural and selective γ-secretase inhibitor towards APP processing.Figure optionsDownload high-quality image (184 K)Download as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Ethnopharmacology - Volume 163, 2 April 2015, Pages 192–202
نویسندگان
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