Programa de Pós Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
J Enzyme Inhib Med Chem. 2013 Feb;28(1):218-22. doi: 10.3109/14756366.2011.633908. Epub 2011 Nov 25.
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.
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。