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Scholarinine A, a N3 type caged-monoterpene indole alkaloid as Cav3.1 T-type calcium channel inhibitor from Alstonia scholaris

Author:
Zhan, Rui, Du, Shu-Zong, Duan, Zhi-Hang, Nian, Yin, Chen, Ye-Gao
Source:
Tetrahedron letters 2019
ISSN:
0040-4039
Subject:
Alstonia scholaris, X-ray diffraction, calcium channels, chemical reactions, chemical structure, indole alkaloids, inhibitory concentration 50, monoterpenoids, nerve growth factor, neurites, spectral analysis
Abstract:
Scholarinine A (1), a new N3-type caged monoterpene indole alkaloid was isolated from the branches and leaves of Alstonia scholaris. Structurally, 1 is featured by unique 6/5/6/5/5/6 carbocyclic skeleton bearing a novel imidazolidine ring E. The structure of 1 was determined by extensive spectroscopic analyses and X-ray crystallography. Biological studies exhibited that compound 1 is a potent Cav3.1 T-type calcium channel inhibitor with an IC50 value of 4.28 μM. In addition, 1 enhanced the neurite outgrowth of nerve growth factor (NGF) mediated PC12 cells at 10 μM.
Agid:
6754615