期刊
MARINE DRUGS
卷 20, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/md20040262
关键词
synthesis; marine alkaloids; Neolamellarin A; PC12 cells; glutamate
资金
- Natural Science Foundation of China [82003583, 82073759]
- Fund of Greater Bay Area Institute of Precision Medicine (Guangzhou) [IPM2021C009]
- National Science and Technology Major Project for Significant New Drugs Development [2018ZX09735004]
Marine alkaloids obtained from sponges have various biological activities and potential medicinal value. Neolamellarin A and its derivatives possess low cytotoxicity and superior neuroprotective activity, suggesting their potential as antagonists against nerve cell apoptosis.
Marine alkaloids obtained from sponges possess a variety of biological activities and potential medicinal value. The pyrrole-derived lamellarin-like alkaloids, especially their permethyl derivatives, show low cytotoxicity and potent MDR reversing activity. Neolamellarin A is a novel lamellarin-like alkaloid which was extracted from marine animal sponges. We reported the synthetic method of permethylated Neolamellarin A and its derivatives by a convergent strategy in 2015. In 2018, we reported the synthesis and the neuroprotective activity in PC12 cells of 3,4-bisaryl-N-alkylated permethylated Neolamellarin A derivatives. In this report, another series of 15 different 3,4-bisaryl-N-acylated permethylated Neolamellarin A derivatives were synthesized, and the outstanding protective effects of these compounds against glutamate induced PC12 cell apoptosis were presented and discussed. These Neolamellarin A derivatives which possessed low cytotoxicity and superior neuroprotective activity may have the potential to be developed into antagonists against glutamate induced nerve cell apoptosis.
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