Oleanolic acid (OA) as an antileishmanial agent: Biological evaluation and in silico mechanistic insights

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dc.contributor.authorMelo T.S.
dc.contributor.authorGattass C.R.
dc.contributor.authorSoares D.C.
dc.contributor.authorCunha M.R.
dc.contributor.authorFerreira C.
dc.contributor.authorTavares M.T.
dc.contributor.authorSaraiva E.
dc.contributor.authorParise-Filho R.
dc.contributor.authorBraden H.
dc.contributor.authorDelorenzi J.C.
dc.date.accessioned2024-03-13T00:53:09Z
dc.date.available2024-03-13T00:53:09Z
dc.date.issued2016
dc.description.abstract© 2016 Elsevier Ireland Ltd.Although a worldwide health problem, leishmaniasis is considered a highly neglected disease, lacking efficient and low toxic treatment. The efforts for new drug development are based on alternatives such as new uses for well-known drugs, in silico and synthetic studies and naturally derived compounds. Oleanolic acid (OA) is a pentacyclic triterpenoid widely distributed throughout the Plantae kingdom that displays several pharmacological activities. OA showed potent leishmancidal effects in different Leishmania species, both against promastigotes (IC50 L. braziliensis 30.47±6.35μM; IC50 L. amazonensis 40.46±14.21μM; IC50 L. infantum 65.93±15.12μM) and amastigotes (IC50 L. braziliensis 68.75±16.55μM; IC50 L. amazonensis 38.45±12.05μM; IC50 L. infantum 64.08±23.52μM), with low cytotoxicity against mouse peritoneal macrophages (CC50 235.80±36.95μM). Moreover, in silico studies performed to evaluate OA molecular properties and to elucidate the possible mechanism of action over the Leishmania enzyme sterol 14α-demethylase (CYP51) suggested that OA interacts efficiently with CYP51 and could inhibit the ergosterol synthesis pathway. Collectively, these data indicate that OA is a good candidate as leading compound for the development of a new leishmaniasis treatment.
dc.description.firstpage227
dc.description.issuenumber3
dc.description.lastpage237
dc.description.volume65
dc.identifier.doi10.1016/j.parint.2016.01.001
dc.identifier.issn1873-0329
dc.identifier.urihttps://dspace.mackenzie.br/handle/10899/35970
dc.relation.ispartofParasitology International
dc.rightsAcesso Restrito
dc.subject.otherlanguageCYP51
dc.subject.otherlanguageIn silico studies
dc.subject.otherlanguageLeishmania spp.
dc.subject.otherlanguageLeishmaniasis
dc.subject.otherlanguageOleanolic acid
dc.titleOleanolic acid (OA) as an antileishmanial agent: Biological evaluation and in silico mechanistic insights
dc.typeArtigo
local.scopus.citations30
local.scopus.eid2-s2.0-84954528607
local.scopus.subjectAnimals
local.scopus.subjectAntiprotozoal Agents
local.scopus.subjectFemale
local.scopus.subjectHumans
local.scopus.subjectLeishmania
local.scopus.subjectLeishmaniasis
local.scopus.subjectMacrophages, Peritoneal
local.scopus.subjectMale
local.scopus.subjectMice
local.scopus.subjectModels, Molecular
local.scopus.subjectModels, Structural
local.scopus.subjectOleanolic Acid
local.scopus.updated2024-05-01
local.scopus.urlhttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84954528607&origin=inward
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