Inhibition of the gastric H+,K+-ATPase by plectrinone A, a diterpenoid isolated from Plectranthus barbatus Andrews

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dc.contributor.authorSchultz, Carla
dc.contributor.authorBossolani, Myllene P.
dc.contributor.authorTorres, Luce M. B.
dc.contributor.authorLima-Landman, Maria Teresa R.
dc.contributor.authorLapa, Antonio J.
dc.contributor.authorSouccar, Caden
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionBot Garden São Paulo
dc.date.accessioned2016-01-24T13:48:36Z
dc.date.available2016-01-24T13:48:36Z
dc.date.issued2007-04-20
dc.description.abstractThis work assessed the mechanism underlying the antisecretory gastric acid effect of Plectranthus barbatus Andrews (Lamiaceae) and active constituents. Popularly known as false-boldo, this plant is used in Brazilian folk medicine to treat gastrointestinal and hepatic ailments. the plant aqueous extract (AE) and isolated compounds were assayed in vivo in pylorus-ligated mice, and in vitro on acid secretion measured as [C-14] -arninopyrine ([C-14]-AP) accumulation in rabbit gastric glands and gastric H+,K+-ATPase preparations. Injected into the duodenal lumen, the AE of the plant leaves (0.5 and 1.0g/kg) decreased the volume (62 and 76%) and total acidity (23 and 50%) of gastric acid secretion in pylorus-ligated mice. Bioguided purification of the AE yielded an active fraction (IC50 = 24 kg/ml) that inhibited acid secretion in rabbit gastric glands with a potency 10 to 18 times greater than that of the originating extract, on both the basal and stimulated acid secretion by histamine (His) (1 mu M) or bethanechol (100 mu M). At the same concentrations the gastric H+,K+-ATPase activity was also inhibited. the active constituent was chemically identified as the abietanoid dienedione plectrinone A which reduced the H+,(+)-ATPase activity with IC50 = 171 mu M. the results indicate that inhibition of the gastric proton pump by this diterpenoid may account for the antisecretory acid effect and reputed antiulcer activity of Plectranthus barbatus. (c) 2006 Elsevier Ireland Ltd. All rights reserved.en
dc.description.affiliationUniversidade Federal de São Paulo, Escola Paulista Med, Dept Pharmacol, Nat Prod Sect, BR-04044020 São Paulo, Brazil
dc.description.affiliationBot Garden São Paulo, Inst Bot, São Paulo, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, Escola Paulista Med, Dept Pharmacol, Nat Prod Sect, BR-04044020 São Paulo, Brazil
dc.description.sourceWeb of Science
dc.format.extent1-7
dc.identifierhttp://dx.doi.org/10.1016/j.jep.2006.09.046
dc.identifier.citationJournal of Ethnopharmacology. Clare: Elsevier B.V., v. 111, n. 1, p. 1-7, 2007.
dc.identifier.doi10.1016/j.jep.2006.09.046
dc.identifier.issn0378-8741
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/29671
dc.identifier.wosWOS:000246059600001
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofJournal of Ethnopharmacology
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rights.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.subjectPlectranthus barbatusen
dc.subjectLamiaceaeen
dc.subjectacid secretionen
dc.subjectrabbit gastric glandsen
dc.subjectH+,K+-ATPaseen
dc.subjectplectrinone Aen
dc.titleInhibition of the gastric H+,K+-ATPase by plectrinone A, a diterpenoid isolated from Plectranthus barbatus Andrewsen
dc.typeinfo:eu-repo/semantics/article
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