Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana-124001, India.
Department of Pharmaceutical Sciences, Guru Jambeshwar University of Science & Technology, Hisar, Haryana-125001, India.
Biomolecules. 2021 Feb 25;11(3):350. doi: 10.3390/biom11030350.
Alzheimer's disease (AD) is a gradually growing irreversible illness of the brain that almost affects every fifth person (aged > 80 years) in the world. World Health Organization (WHO) also revealed that the prevalence of this disease will enhance (upto double) significantly upto 2030. The poor cholinergic transmission at the synapse is considered to be one of the main reasons behind the progression and occurrence of this disorder. Natural inhibitors of acetylcholine (ACh) such as galanthamine and rivastigmine are used commercially in the treatmentof AD. The biomolecules such assesquiterpenes, possess a great structural diversity and are responsible for a plethora of pharmacological properties. The potential of various sesquiterpenes as anticholinesterase has been reviewed in this article. For this purpose, the various databases, mainly PubMed, Scopus, and Web of Science were investigatedwith different keywords such as "sesquiterpenes+acetylcholinesterase" and "sesquiterpenes+cholinesterase+inhibitors" in the surveyed time frame (2010-2020). A vast literature was evident in the last decade, which affirms the potential of various sesquiterpenes in the improvement of cholinergic transmission by inhibiting the AChE. After data analysis, it was found that 12 compounds out of a total of 58 sesquiterpenes were reported to possess IC < 9μM and can be considered as potential candidates for the improvement of learning and memory. Sesquiterpene is an important category of terpenoids, found to possess a large spectrum of biological activities. The outcome of the review clearly states that sesquiterpenes (such as amberboin, lipidiol,etc) from herbs could offer fresh, functional compounds for possible prevention and treatment of AD.
阿尔茨海默病(AD)是一种逐渐发展的不可逆的大脑疾病,几乎影响到世界上每五分之一(年龄> 80 岁)的人。世界卫生组织(WHO)还透露,这种疾病的患病率将显著提高(高达两倍),到 2030 年。突触处的胆碱能传递不良被认为是这种疾病发展和发生的主要原因之一。天然乙酰胆碱(ACh)抑制剂,如加兰他敏和利伐斯的明,已被商业用于 AD 的治疗。生物分子如倍半萜,具有巨大的结构多样性,并负责多种药理性质。本文综述了各种倍半萜作为乙酰胆碱酯酶抑制剂的潜力。为此,主要使用了 PubMed、Scopus 和 Web of Science 等各种数据库,使用了不同的关键词,如“倍半萜+乙酰胆碱酯酶”和“倍半萜+胆碱酯酶抑制剂”,在调查的时间范围内(2010-2020 年)。在过去的十年中,有大量的文献证实了各种倍半萜通过抑制乙酰胆碱酯酶来改善胆碱能传递的潜力。经过数据分析,发现总共 58 种倍半萜中有 12 种化合物被报道具有 IC < 9μM,可被视为改善学习和记忆的潜在候选物。倍半萜是萜类化合物的一个重要类别,被发现具有广泛的生物活性。综述的结果清楚地表明,草药中的倍半萜(如琥珀醇、脂醇等)可能为 AD 的预防和治疗提供新的、有功能的化合物。