Programa de Pós Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Av Ipiranga, 2752 90610-000, Porto Alegre - RS, Brazil.
J Ethnopharmacol. 2012 Jan 6;139(1):58-67. doi: 10.1016/j.jep.2011.10.042. Epub 2011 Nov 15.
The study was aimed at evaluating medicinal and therapeutic potentials of two Lycopodiaceae species, Lycopodium clavatum (L.) and Lycopodium thyoides (Humb. & Bonpl. ex Willd), both used in South American folk medicine for central nervous system conditions. Alkaloid extracts were evaluated for chemical characterization, acetylcholinesterase and antioxidant activities.
The alkaloid extracts obtained by alkaline extraction were determined for each species by GC/MS examination. The evaluation of the anticholinesterase and the antioxidant activities of the extracts were tested by determining in vitro and ex vivo models. Effects on acetylcholinesterase (AChE) were tested in vitro using rat brain homogenates and ex vivo after a single administration (25, 10 and 1mg/kg i.p.) of the alkaloid extracts in mice. The in vitro antioxidant effects were tested for the 2-deoxyribose degradation, nitric oxide (NO) interaction, 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging activity and total reactive antioxidant potential (TRAP). After an acute administration (25 and 10mg/kg i.p.) of the extracts in middle-aged (12 months) mice, the antioxidant effects were estimated through the thiobarbituric acid reactive substances test (TBARS), and the antioxidant enzymes activities for catalase (CAT) and superoxide dismutase (SOD) were measured.
AChE activity was inhibited in vitro by the alkaloid-enriched extracts of both Lycopodium species in a dose and time-dependent manner in rat cortex, striatum and hippocampus. A significant inhibition was also observed in areas of the brain after acute administration of extracts, as well as decreased lipid peroxidation and increased CAT activity in the cortex, hippocampus and cerebellum. A moderate antioxidant activity was observed in vitro for the extracts. Chemically, the main alkaloids found for the two species were lycopodine and acetyldihidrolycopodine.
This study showed that the biological properties of the folk medicinal plants Lycopodium clavatum and Lycopodium thyoides include AChE inhibitory activity and antioxidant effects, two possible mechanisms of action in Alzheimer's related processes.
本研究旨在评估两种石松科植物（Lycopodium clavatum（L.）和 Lycopodium thyoides（Humb.＆Bonpl. ex Willd）的药用和治疗潜力，这两种植物均在南美民间医学中用于治疗中枢神经系统疾病。通过 GC/MS 检查评估生物碱提取物的化学特征、乙酰胆碱酯酶和抗氧化活性。
通过碱性提取获得的生物碱提取物分别用 GC/MS 检查来确定每种物种的含量。通过确定体外和体内模型来评估提取物的抗胆碱酯酶和抗氧化活性。在体外使用大鼠脑匀浆测试提取物对乙酰胆碱酯酶（AChE）的影响，在体内通过单次给予（25、10 和 1mg/kg i.p.）生物碱提取物后在小鼠中进行。体外抗氧化作用通过 2-脱氧核糖降解、一氧化氮（NO）相互作用、2,2-二苯基-1-苦基肼（DPPH）自由基清除活性和总反应性抗氧化能力（TRAP）进行测试。在给予提取物（25 和 10mg/kg i.p.）后，通过丙二醛（TBARS）测试来评估中年（12 个月）小鼠体内的抗氧化作用，并测量抗氧化酶活性如过氧化氢酶（CAT）和超氧化物歧化酶（SOD）。
生物碱富集提取物以剂量和时间依赖性方式在大鼠皮质、纹状体和海马中抑制 AChE 活性。在急性给予提取物后，大脑的各个区域也观察到显著抑制，以及皮质、海马和小脑的脂质过氧化减少和 CAT 活性增加。提取物在体外具有适度的抗氧化活性。化学上，这两种植物的主要生物碱是石松碱和乙酰二氢石松碱。
本研究表明，民间药用植物石松和卷柏的生物学特性包括 AChE 抑制活性和抗氧化作用，这是阿尔茨海默病相关过程的两种可能作用机制。
