Department of Chemistry, University of Alberta, Edmonton, AB, T6G 2G2, Canada.
Department of Chemistry, University of Iowa, Iowa City, IA, 52246, USA.
Org Biomol Chem. 2022 Mar 16;20(11):2187-2193. doi: 10.1039/d2ob00016d.
The synthesis and bioactivity of neurotrophic banglenes and derivatives is described, establishing a structure-activity relationship which enables future mechanistic studies. Neuritogenesis assays indicate that (-) -banglene is the active enantiomer. Assays performed with and without NGF protein suggest that neurotrophic activity and potentiation of NGF activity by (-) -banglene might be distinct unassociated processes. Interestingly, (-) -banglene potentiation of NGF-induced neuritogenesis is unaffected by the presence of Erk1/2, Akt and Pkc inhibitors.
本文描述了神经营养 banglenes 及其衍生物的合成和生物活性，建立了结构-活性关系，为未来的机制研究提供了依据。神经突生成试验表明（-）-banglene 是具有活性的对映异构体。在有和没有 NGF 蛋白的情况下进行的试验表明，（-）-banglene 的神经营养活性和对 NGF 活性的增强作用可能是两个不同的、不相关的过程。有趣的是，（-）-banglene 增强 NGF 诱导的神经突生成作用不受 Erk1/2、Akt 和 Pkc 抑制剂的影响。
