García Mariana Vázquez, Poser Gilsane Lino von, Apel Miriam, Tlatilpa Rosa Cerros, Mendoza-Ruiz Aniceto, Villarreal María Luisa, Henriques Amelia Teresinha, Taketa Alexandre Cardoso
Centro de Investigación en Biotecnología, Universidad Autónoma del Estado de Morelos, Mexico.
Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Brazil.
Pak J Pharm Sci. 2017 Jan;30(1 Suppl):235-239.
Huperzine A (Hup A), the alkaloid produced by the Chinese medicinal plant Huperzia serrata, has been documented to be a promising agent for the treatment of Alzheimer's disease due to its potent acetylcholinesterase inhibitory (AChEI) activity. The search for anticholinesterase natural products, as well as for alternative sources of Hup A in Mexican lycopods, prompted us to investigate these plants. The action of methanolic and alkaloidal extracts of three Huperzia species (H. cuernavacensis, H. dichotoma, and H. linifolia) was evaluated using an in vitro anticholinesterase activity assay. Also, chromatographic and spectroscopic analyses were employed to detect the presence of Hup A. Methanolic and alkaloidal extracts of H. cuernavacensis showed IC =5.32±0.8μg/mL and 0.74±0.05μg/mL; H. dichotoma displayed AChEI with IC values =14.11±2.1μg/mL and 0.64±0.09μg/mL; and H. linifolia presented IC =158.37±8.7μg/mL and 4.2±1.24μg/mL, respectively, compared to the control Hup A (IC= 0.16±0.03μg/mL). Hup A was identified in the extracts of H. dichotoma, but it was not detected in the extracts of H. cuernavacensis and H. linifolia by H NMR techniques. This study reveals H. dichotoma as a new source of Hup A, and presents H. linifolia and H. cuernavacensis as potential candidates to obtain other anticholinesterase compounds useful in the Alzheimer's disease treatment.
石杉碱甲(Hup A)是中国药用植物蛇足石杉产生的一种生物碱,因其具有强大的乙酰胆碱酯酶抑制(AChEI)活性,已被证明是一种有前途的治疗阿尔茨海默病的药物。对抗胆碱酯酶天然产物的探索,以及在墨西哥石松类植物中寻找石杉碱甲的替代来源,促使我们对这些植物进行研究。使用体外抗胆碱酯酶活性测定法评估了三种蛇足石杉属植物(库埃纳瓦卡蛇足石杉、二叉蛇足石杉和线叶蛇足石杉)的甲醇提取物和生物碱提取物的作用。此外,还采用色谱和光谱分析来检测石杉碱甲的存在。库埃纳瓦卡蛇足石杉的甲醇提取物和生物碱提取物的IC50值分别为5.32±0.8μg/mL和0.74±0.05μg/mL;二叉蛇足石杉显示出乙酰胆碱酯酶抑制活性,IC50值分别为14.11±2.1μg/mL和0.64±0.09μg/mL;与对照石杉碱甲(IC50 = 0.16±0.03μg/mL)相比,线叶蛇足石杉的IC50值分别为158.37±8.7μg/mL和4.2±1.24μg/mL。通过1H NMR技术在二叉蛇足石杉的提取物中鉴定出了石杉碱甲,但在库埃纳瓦卡蛇足石杉和线叶蛇足石杉的提取物中未检测到。这项研究揭示了二叉蛇足石杉是石杉碱甲的新来源,并表明线叶蛇足石杉和库埃纳瓦卡蛇足石杉是获得其他可用于治疗阿尔茨海默病的抗胆碱酯酶化合物的潜在候选植物。