期刊
PHYTOCHEMISTRY
卷 194, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2021.113017
关键词
Vinca minor; Apocynaceae; Alzheimer's disease; Docking studies; Alkaloids; Butyrylcholinesterase; Vincaminorudeine; (-)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H-indole
资金
- Charles University [SVV UK 260 548, Progres/UK Q42]
- project Modernization and extension of the doctoral study field of Pharmacognosy and toxicity of natural products in the study program Pharmacy [CZ.02.2.69/0.0/0.0/16_018/0002736]
- Czech Science Foundation [20-29633J]
- Long-term development plan (Faculty of Military Health Sciences)
- program Projects of Large Research, Development, and Innovations Infrastructures [LM2015042, LM2015085]
An undescribed indole alkaloid and twenty-two known compounds were isolated from aerial parts of Vinca minor L. The isolated alkaloids were identified using MS, HRMS, 1D, and 2D NMR techniques, with some revised NMR data. The (- )-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1Hindole showed significant inhibition activity against hBuChE and was studied further for its mode of inhibition and ability to cross the blood-brain barrier.
One undescribed indole alkaloid together with twenty-two known compounds have been isolated from aerial parts of Vinca minor L. (Apocynaceae). The chemical structures of the isolated alkaloids were determined by a combination of MS, HRMS, 1D, and 2D NMR techniques, and by comparison with literature data. The NMR data of several alkaloids have been revised, corrected, and missing data have been supplemented. Alkaloids isolated in sufficient quantity were screened for their in vitro acetylcholinesterase (AChE; E.C. 3.1.1.7) and butyrylcholinesterase (BuChE; E.C. 3.1.1.8) inhibitory activity. Selected compounds were also evaluated for prolyl oligopeptidase (POP; E.C. 3.4.21.26), and glycogen synthase 3 beta-kinase (GSK-3 beta; E.C. 2.7.11.26) inhibition potential. Significant hBuChE inhibition activity has been shown by (- )-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1Hindole with an IC50 value of 0.65 +/- 0.16 mu M. This compound was further studied by enzyme kinetics, along with in silico techniques, to reveal the mode of inhibition. This compound is also predicted to cross the blood-brain barrier (BBB) through passive diffusion.
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