Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6387
Title: Vascular L-type Ca2+ channel blocking activity of sulphur-containing indole alkaloids from Glycosmis petelotii
Authors: Cuong, N. M.
Khanh, P. N.
Huyen, P. T.
Duc, H. V.
Huong, T. T.
Ha, V. T.
Durante, Miriam
Sgaragli, GIAN PIETRO
Fusi, Fabio 
Issue Date: 2014
Project: None 
Journal: JOURNAL OF NATURAL PRODUCTS
Abstract: 
In the search for novel natural compounds endowed with potential antihypertensive activity, a new sulfur-containing indole alkaloid, N-demethylglypetelotine (2), and its known analogue glypetelotine (1), were isolated from the leaves of Glycosmis petelotii. Their structures were established on the basis of spectroscopic evidence. The two alkaloids were assessed for vasorelaxing activity on rat aorta rings and for L-type Ba(2+) current [I(Ba(L))] blocking activity on single myocytes isolated from rat tail artery. Both glypetelotine and N-demethylglypetelotine inhibited phenylephrine-induced contraction with IC50 values of 20 and 50 μM, respectively. The presence of endothelium did not modify their spasmolytic effect. Neither glypetelotine nor N-demethylglypetelotine affected Ca(2+) release from the sarcoplasmic reticulum induced by phenylephrine. The spasmolytic effect of glypetelotine increased with membrane depolarization. In the presence of 60 mM K(+), both compounds inhibited, in a concentration-dependent manner, the contraction induced by cumulative addition of Ca(2+), this inhibition being inversely related to Ca(2+) concentration. Glypetelotine and, less efficiently N-demethylglypetelotine, inhibited I(Ba(L)), the former compound also affecting I(Ba(L)) kinetics. In conclusion, glypetelotine is a novel vasorelaxing agent which antagonizes L-type Ca(2+) channels.
Description: 
61041
URI: http://hdl.handle.net/20.500.12779/6387
ISSN: 0163-3864
DOI: 10.1021/np500076v
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