Antileishmanial activity and ultrastructural changes of related tetrahydrofuran dineolignans isolated from Saururus cernuus L. (Saururaceae)

dc.contributor.authorBrito J.R.
dc.contributor.authorPassero L.F.D.
dc.contributor.authorBezerra-Souza A.
dc.contributor.authorLaurenti M.D.
dc.contributor.authorRomoff P.
dc.contributor.authorBarbosa H.
dc.contributor.authorFerreira E.A.
dc.contributor.authorLago J.H.G.
dc.date.accessioned2024-03-12T23:50:56Z
dc.date.available2024-03-12T23:50:56Z
dc.date.issued2019
dc.description.abstract© 2019 Royal Pharmaceutical SocietyObjective: This work describes the isolation of anti-Leishmania amazonensis metabolites from Saururus cernuus (Saururaceae). Additionally, ultrastructural changes in promastigotes were evidenced by electron microscopy. Methods: The MeOH extract from the leaves of S. cernuus was subjected to bioactivity-guided fractionation. Anti-L. amazonensis activity of purified compounds was performed in vitro against promastigote and amastigote forms. Key findings: Bioactivity-guided fractionation of the MeOH extract from the leaves of S. cernuus afforded two related tetrahydrofuran dineolignans: threo,threo-manassantin A (1) and threo,erythro-manassantin A (2). Compounds 1 and 2 displayed activity against promastigotes (EC50 of 35.4 ± 7.7 and 17.6 ± 4.2 μm, respectively) and amastigotes (EC50 of 20.4 ± 1.9 and 16.0 ± 1.1 μm, respectively), superior to that determined for the positive control miltefosine (EC50 of 28.7 ± 3.5 μm). Reduced cytotoxicity for host cells was observed for both compounds. Additionally, ultrastructural changes in promastigotes leading to an alteration of structural morphology were observed, as evidenced by electron microscopy. Furthermore, these compounds altered the morphology and physiology of the plasmatic membrane of L. amazonensis. Conclusions: The obtained results indicated that dineolignans 1 and 2 could be considered as a scaffold for the design of novel and selective drug candidates for the treatment of leishmaniasis.
dc.description.firstpage1871
dc.description.issuenumber12
dc.description.lastpage1878
dc.description.volume71
dc.identifier.doi10.1111/jphp.13171
dc.identifier.issn2042-7158
dc.identifier.urihttps://dspace.mackenzie.br/handle/10899/35147
dc.relation.ispartofJournal of Pharmacy and Pharmacology
dc.rightsAcesso Aberto
dc.subject.otherlanguageLeishmania amazonensis
dc.subject.otherlanguagemanassantin
dc.subject.otherlanguagemitochondrial membrane potential
dc.subject.otherlanguageSaururaceae
dc.subject.otherlanguageultrastructural changes
dc.titleAntileishmanial activity and ultrastructural changes of related tetrahydrofuran dineolignans isolated from Saururus cernuus L. (Saururaceae)
dc.typeArtigo
local.scopus.citations17
local.scopus.eid2-s2.0-85073945558
local.scopus.subjectAnimals
local.scopus.subjectAntiprotozoal Agents
local.scopus.subjectFurans
local.scopus.subjectLeishmania
local.scopus.subjectLeishmaniasis
local.scopus.subjectLignans
local.scopus.subjectMice
local.scopus.subjectMice, Inbred BALB C
local.scopus.subjectMicroscopy, Electron
local.scopus.subjectPhosphorylcholine
local.scopus.subjectPlant Leaves
local.scopus.subjectSaururaceae
local.scopus.updated2024-05-01
local.scopus.urlhttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85073945558&origin=inward
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