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南美洲石松科生物碱分析及乙酰胆碱酯酶抑制活性研究。

Alkaloid profiling and anticholinesterase activity of South American Lycopodiaceae species.

机构信息

Programa de Pós Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.

出版信息

J Enzyme Inhib Med Chem. 2013 Feb;28(1):218-22. doi: 10.3109/14756366.2011.633908. Epub 2011 Nov 25.

Abstract

The alkaloid extracts of four Huperzia and one Lycopodiella species, from Brazilian habitats, were tested for their in vitro anticholinesterase activities. IC(50) values showed a potent acetylcholinesterase inhibition for H. reflexa (0.11 ± 0.05 μg/mL), followed by H. quadrifariata (2.0 ± 0.3 μg/mL), H. acerosa (5.5 ± 0.9 μg/mL), H. heterocarpon (25.6 ± 2.7 μg/mL) and L. cernua (42.6 ± 1.5 μg/mL). A lower inhibition of butyrylcholinesterase was observed for all species with the exception of H. heterocarpon (8.3 ± 0.9 μg/mL), whose alkaloid extract presented a selectivity for pseudocholinesterase. Moreover, the chemical study of the bioactive extracts performed by GC-MS, revealed the presence of a number of Lycopodium alkaloids belonging to the lycopodane, flabellidane and cernuane groups. Surprisingly, the potent acetylcholinesterase inhibitors huperzines A and B were not detected in the extracts, suggesting that other alkaloids may be responsible for such an effect.

摘要

从巴西生境中分离得到的 4 种鳞毛蕨属和 1 种石松属植物的生物碱提取物进行了体外抗胆碱酯酶活性测试。IC50 值显示 H. reflexa(0.11±0.05μg/mL)对乙酰胆碱酯酶具有很强的抑制作用,其次是 H. quadrifariata(2.0±0.3μg/mL)、H. acerosa(5.5±0.9μg/mL)、H. heterocarpon(25.6±2.7μg/mL)和 L. cernua(42.6±1.5μg/mL)。除 H. heterocarpon(8.3±0.9μg/mL)外,所有物种对丁酰胆碱酯酶的抑制作用较低,而 H. heterocarpon 的生物碱提取物对拟胆碱酯酶具有选择性。此外,通过 GC-MS 对生物活性提取物进行的化学研究表明,存在许多属于石松烷、扁柏烷和石松烷组的石松生物碱。令人惊讶的是,在提取物中未检测到强效乙酰胆碱酯酶抑制剂石杉碱甲和石杉碱乙,这表明可能是其他生物碱引起了这种作用。

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