Callizot N, Campanari M L, Rouvière L, Jacquemot G, Henriques A, Garayev E, Poindron P
Neuro-Sys SAS, Neuro-Pharmacology Department, Gardanne, France.
Neuralia SAS, Gardanne, France.
Front Pharmacol. 2021 Aug 30;12:681532. doi: 10.3389/fphar.2021.681532. eCollection 2021.
(Thunb.) Trevis is widely used in traditional asiatic medicine to treat many central disorders including, schizophrenia, cognitive dysfunction, and dementia. The major alkaloid, Huperzine A (HA), of is a well-known competitive reversible inhibitor of acetylcholinesterase (AChE) with neuroprotective effects. Inspired by the tradition, we developed a green one-step method using microwave assisted extraction to generate an extract of , called NSP01. This green extract conserves original neuropharmacological activity and chemical profile of traditional extract. The neuroprotective activity of NSP01 is based on a precise combination of three major constituents: HA and two phenolic acids, caffeic acid (CA) and ferulic acid (FA). We show that CA and FA potentiate HA-mediated neuroprotective activity. Importantly, the combination of HA with CA and FA does not potentiate the AChE inhibitory property of HA which is responsible for its adverse side effects. Collectively, these experimental findings demonstrated that NSP01, is a very promising plant extract for the prevention of Alzheimer's disease and memory deficits.
(石杉科石杉属植物)蛇足石杉在传统亚洲医学中被广泛用于治疗多种中枢神经系统疾病,包括精神分裂症、认知功能障碍和痴呆症。其主要生物碱石杉碱甲(HA)是一种著名的乙酰胆碱酯酶(AChE)竞争性可逆抑制剂,具有神经保护作用。受此传统启发,我们开发了一种绿色一步法,即微波辅助提取法来制备蛇足石杉提取物,称为NSP01。这种绿色提取物保留了传统提取物的原始神经药理活性和化学特征。NSP01的神经保护活性基于三种主要成分的精确组合:HA以及两种酚酸,咖啡酸(CA)和阿魏酸(FA)。我们发现CA和FA增强了HA介导的神经保护活性。重要的是,HA与CA和FA的组合并未增强HA的AChE抑制特性,而该特性是其产生不良副作用的原因。总体而言,这些实验结果表明,NSP01是一种非常有前景的植物提取物,可用于预防阿尔茨海默病和记忆缺陷。