Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Marine Biomedical Research Institute of Qiangdao, Qingdao 266237, China.
Mar Drugs. 2022 Apr 12;20(4):262. doi: 10.3390/md20040262.
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--alkylated permethylated Neolamellarin A derivatives. In this report, another series of 15 different 3,4-bisaryl--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.
从海绵中提取的海洋生物碱具有多种生物活性和潜在的药用价值。吡咯衍生的 lamellarin 类似生物碱，特别是它们的全甲基衍生物，显示出低细胞毒性和有效的多药耐药逆转活性。Neolamellarin A 是一种从海洋动物海绵中提取的新型 lamellarin 类似生物碱。我们于 2015 年报道了通过会聚策略合成全甲基化 Neolamellarin A 及其衍生物的方法。2018 年，我们报道了 3,4-双芳基-烷基化全甲基化 Neolamellarin A 衍生物的合成及其在 PC12 细胞中的神经保护活性。在本报告中，我们又合成了另一系列 15 种不同的 3,4-双芳基-酰化全甲基化 Neolamellarin A 衍生物，并对这些化合物对谷氨酸诱导的 PC12 细胞凋亡的显著保护作用进行了呈现和讨论。这些具有低细胞毒性和优越神经保护活性的 Neolamellarin A 衍生物可能有潜力开发成为对抗谷氨酸诱导的神经细胞凋亡的拮抗剂。
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