Department of Genetics, Ribeirão Preto Medical School, University of São Paulo - USP, 14090-900, Ribeirão Preto, Brazil.
Department of Biology, Faculty of Philosophy, Sciences and Letters at Ribeirão Preto, University of São Paulo - USP, Ribeirão Preto, Brazil.
Neurochem Res. 2017 Oct;42(10):2826-2830. doi: 10.1007/s11064-017-2295-8. Epub 2017 May 11.
Alzheimer's disease (AD) is a progressive condition, where dementia symptoms gradually worsen. Biochemically the disease is characterized by the presence of neuritic plaques, neurofibrillary tangles, in addition to cholinergic dysfunction in the central nervous system. The role of the cholinergic neurotransmission in AD is the basis of the widely accepted cholinergic hypothesis. Some of the most relevant therapies for the treatment of the disease are based on the acetylcholinesterase (AChE) inhibitor activity; however, these therapies are not effective to stop the disease progression, but only can temporarily slow down the worsening of dementia symptoms, and improve quality of life of patients and their caregivers. In recent years, plant alkaloids extracted from Amaryllidaceae family have received great attention due to the well-known anti cholinergic activity. In this context, the purpose of this study was to apply the docking molecular in sílico analysis aiming to examine the recombinant human AChE enzyme (rhAChE) inhibitory activity displayed by different alkaloids from Amaryllidaceae family. Overall, the present results support the idea that alkaloids reported in this research are capable of interacting with rhAChE-binding sites.
阿尔茨海默病（AD）是一种进行性疾病，其痴呆症状逐渐恶化。从生化角度来看，该疾病的特征是存在神经纤维缠结，此外中枢神经系统还存在胆碱能功能障碍。胆碱能神经传递在 AD 中的作用是广泛接受的胆碱能假说的基础。一些治疗该疾病的最相关疗法基于乙酰胆碱酯酶（AChE）抑制剂活性；然而，这些疗法不能有效阻止疾病进展，只能暂时减缓痴呆症状的恶化，并改善患者及其护理人员的生活质量。近年来，由于其众所周知的抗胆碱能活性，从石蒜科中提取的植物生物碱受到了极大的关注。在这种情况下，本研究的目的是应用对接分子在硅分析，旨在检查不同石蒜科生物碱对重组人乙酰胆碱酯酶（rhAChE）的抑制活性。总的来说，本研究结果支持了这样一种观点，即本研究中报道的生物碱能够与 rhAChE 结合位点相互作用。
