Abstract：ObjectiveTo synthesize novel (-) -huperzine A derivatives and explore their neuroprotective effects.MethodsA series of (-) -huperzine A derivatives were synthesized through the reaction of (-) -huperzine A with multiple substituent sulfonyl chloride. Their structural information was extensively characterized by using melt point, ESR-MS and HRMS. Aβ25-35was used to induce the nerve cell SH-SY5Y injury and apoptosis, and the neuroprotective effects of (-) -huperzine A and its novel derivatives was also evaluated on SH-SY5Y cells in vitro by using an MTT-assay.ResultsEight novel (-) -huperzine A sulfonyl substituted derivatives HA-1 ~ HA-8 were synthesized. The (-) -huperzine A, HA-4, Ha-6 and HA-7 can reverse the injury of Aβ25-35on SH-SY5Y cells. The activities of derivatives HA-4 and HA-7 were better than (-) -huperzine A.ConclusionThe (-) -huperzine A derivatives HA-4 and HA-7 show better neuroprotective effects than (-) -huperzine A.
杨昌华, 胡文胜, 李树华, 邓春雷. 石杉碱甲新型衍生物的合成及其对神经细胞活性的影响[J]. 金宝搏官方188学报(医学版), 2023, 20(3): 155-157. YANG Changhua, HU Wengsheng, LI Shuhua, DENG Chunlei. Synthesis of novel (-) -huperzine A derivatives and the effects on nerve cell viability. HuNan ShiFan DaXue XueBao(YiXueBan), 2023, 20(3): 155-157.
[1] Ma X, Tan C, Zhu D, et al.Huperzine A from Huperzia species—An ethnopharmacolgical review[J]. J Ethnopharmacol, 2007, 113: 15-34. [2] Wang R, Yan H, Tang XC.Progress in studies of huperzine A, a natural cholinesterase inhibitor from Chinese herbal medicine[J]. Acta Pharmacol Sin, 2006, 27(1): 1-26. [3] Li X, Li W, Tian P, et al.Delineating biosynthesis of Huperzine A, A plant-derived medicine for the treatment of Alzheimer's disease[J]. Biotechnol Adv, 2022, 60: 108026. [4] 易家宝, 颜杰, 李旭明. 石杉碱甲结构改造的研究进展[J]. 天然产物研究与开发, 2009, 21: 1080-1083+987. [5] Yan J, Sun L, Wu G, et al.Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives[J]. Bioorg Med Chem, 2009, 17(19): 6937-6941. [6] Li C, Du F, Yu C, et al.A sensitive method for the determination of the novel cholinesterase inhibitor ZT-1 and its active metabolite huperzine A in rat blood using liquid chromatography/ tandem mass spectrometry[J]. Rapid Commun Mass Spectrom, 2004, 18(6): 651-656.
2023,Vol. 20
