Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6387
DC FieldValueLanguage
dc.contributor.authorCuong, N. M.en_us
dc.contributor.authorKhanh, P. N.en_us
dc.contributor.authorHuyen, P. T.en_us
dc.contributor.authorDuc, H. V.en_us
dc.contributor.authorHuong, T. T.en_us
dc.contributor.authorHa, V. T.en_us
dc.contributor.authorDurante, Miriamen_us
dc.contributor.authorSgaragli, GIAN PIETROen_us
dc.contributor.authorFusi, Fabioen_us
dc.date.accessioned2021-03-30T16:01:47Z-
dc.date.available2021-03-30T16:01:47Z-
dc.date.issued2014-
dc.identifier.issn0163-3864en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/6387-
dc.description61041en_US
dc.description.abstractIn 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.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofJOURNAL OF NATURAL PRODUCTSen_US
dc.titleVascular L-type Ca2+ channel blocking activity of sulphur-containing indole alkaloids from Glycosmis petelotiien_US
dc.typeArticleen_US
dc.identifier.doi10.1021/np500076ven_US
dc.identifier.pmid24949913en_US
dc.identifier.scopus2-s2.0-84904959822en_US
dc.identifier.isiWOS:000339604300006en_US
dc.relation.volume77en_US
dc.relation.issue7en_US
dc.description.firstpage1586en_US
dc.description.lastpage1593en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0002-5737-8309-
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