Talaat Aya N, Ibrahim Nehal, Ayoub Iriny M, Labib Rola M, Singab Abdel Nasser B
Department of Pharmacognosy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Center for Drug Discovery Research and Development, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Chem Biodivers. 2025 Jul;22(7):e202402770. doi: 10.1002/cbdv.202402770. Epub 2025 Mar 1.
Alzheimer's disease (AD), one of the most common types of dementia, is an urgent and growing global challenge. AD pathogenesis is associated with increased activity of the acetylcholinesterase enzyme (AChE) and the β-site amyloid precursor protein cleaving enzyme (β-secretase, BACE1). This study aimed to evaluate the AChE and BACE1 inhibitory activities of the n-hexane soluble fraction of Crateva magna leaf extract (CMHF) and its cytotoxic properties against cancer and normal cell lines using MTT assay, also this study aimed to identify the volatile constituents of CMHF by gas chromatography-mass spectrometry (GC-MS) analysis. GC-MS analysis revealed a total of 13 metabolites which represent 92.42% of the detected compounds. Phytol was the major constituent of CMHF, representing 20.52% followed by (Z, Z, Z)-9,12,15-octadecatrienoic acid ethyl ester (19.04%), γ-sitosterol (13.71%), hexadecanoic acid ethyl ester (12.63%) and others. CMHF revealed potent AChE and BACE1 inhibitory activities with IC = 0.114 ± 0.006 and 1.723 ± 0.1 µg/mL, respectively. In conclusion, these findings indicate that CMHF may possess anti-Alzheimer efficacy. Furthermore, the absence of cytotoxicity against HepG-2, HCT-116, MCF-7, and WISH cell lines reinforces its safety profile. Therefore, CMHF could be considered as a natural and safe alternative for managing AD.
阿尔茨海默病(AD)是最常见的痴呆类型之一,是一项紧迫且日益严峻的全球挑战。AD的发病机制与乙酰胆碱酯酶(AChE)和β-淀粉样前体蛋白裂解酶(β-分泌酶,BACE1)活性增加有关。本研究旨在评估大花嘉赐树叶片提取物正己烷可溶部分(CMHF)对AChE和BACE1的抑制活性,以及使用MTT法检测其对癌细胞系和正常细胞系的细胞毒性,同时本研究旨在通过气相色谱-质谱联用(GC-MS)分析鉴定CMHF的挥发性成分。GC-MS分析共鉴定出13种代谢产物,占检测到的化合物的92.42%。叶绿醇是CMHF的主要成分,占20.52%,其次是(Z,Z,Z)-9,12,15-十八碳三烯酸乙酯(19.04%)、γ-谷甾醇(13.71%)、十六烷酸乙酯(12.63%)等。CMHF显示出较强的AChE和BACE1抑制活性,IC50分别为0.114±0.006和1.723±0.1μg/mL。总之,这些发现表明CMHF可能具有抗阿尔茨海默病的功效。此外,对HepG-2、HCT-116、MCF-7和WISH细胞系无细胞毒性,进一步证明了其安全性。因此,CMHF可被视为治疗AD的天然且安全的替代品。