Pharmacognosy Research Group, Louvain Drug Research Institute, Université Catholique de Louvain, Avenue E Mounier 72-30, B-1200 Brussels Woluwe-Saint-Lambert, Belgium.
J Ethnopharmacol. 2010 Oct 5;131(3):585-91. doi: 10.1016/j.jep.2010.07.044. Epub 2010 Jul 29.
The aim of the study was to investigate the activity on β-amyloid peptide production of crude extracts of 9 plant species traditionally used in Benin or in Madagascar for the treatment of cognitive disorders, in order to select candidates for Alzheimer's disease treatment.
For each species, hexane, dichloromethane, ethyl-acetate and water extracts were tested, at non-toxic concentrations, on CHO cells overexpressing the human neuronal β-amyloid peptide precursor (APP695) to measure variations of APP processing (by Western-blotting) and, for the most active, of Aβ-amyloid production (by ECLIA).
We observed, at non-toxic concentrations, a significant increase in CTF/APP ratio with Oldenlandia affinis cyclotide-enriched fraction, Prosopis africana EtOAc extract, Pterocarpus erinaceus aqueous extract and Trichilia emetica hexane extract. We also showed that the Pterocarpus erinaceus extract significantly decreased Aβ production, displaying effects similar to those of DAPT (γ-secretase inhibitor) on APP processing, but may act on another inhibition site.
These active extracts are worth further studies to isolate the compounds responsible for the observed activities, to analyze their mode of action and determine their clinical potentials.
本研究旨在探讨 9 种植物粗提取物对β-淀粉样肽生成的活性,这些植物在贝宁或马达加斯加传统上用于治疗认知障碍,以选择用于治疗阿尔茨海默病的候选药物。
对于每种植物,在非毒性浓度下,用表达人神经元β-淀粉样肽前体(APP695)的 CHO 细胞测试正己烷、二氯甲烷、乙酸乙酯和水提取物,以测量 APP 加工的变化(通过 Western blot),对于最活跃的提取物,还测量 Aβ-淀粉样肽生成的变化(通过 ECLIA)。
我们观察到,在非毒性浓度下,Oldenlandia affinis 环肽富集部分、Prosopis africana EtOAc 提取物、Pterocarpus erinaceus 水提取物和 Trichilia emetica 正己烷提取物显著增加了 CTF/APP 比值。我们还表明,Pterocarpus erinaceus 提取物显著降低了 Aβ的产生,其对 APP 加工的影响类似于 DAPT(γ-分泌酶抑制剂),但可能作用于另一个抑制位点。
这些具有活性的提取物值得进一步研究,以分离出引起观察到的活性的化合物,分析其作用模式,并确定其临床潜力。