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Synthesis of novel (-) -huperzine A derivatives and the effects on nerve cell viability |
YANG Changhua, HU Wengsheng, LI Shuhua, DENG Chunlei |
School of Medicine, Changsha 410006, China |
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Abstract Objective To synthesize novel (-) -huperzine A derivatives and explore their neuroprotective effects. Methods A 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. Aβ25-35 was 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. Results Eight 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 Aβ25-35 on SH-SY5Y cells. The activities of derivatives HA-4 and HA-7 were better than (-) -huperzine A. Conclusion The (-) -huperzine A derivatives HA-4 and HA-7 show better neuroprotective effects than (-) -huperzine A.
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Received: 30 September 2022
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