dc.contributor.author
Wulsten, Imke E.
dc.contributor.author
Costa-Silva, Thais A.
dc.contributor.author
Mesquita, Juliana T.
dc.contributor.author
Lima, Marta L.
dc.contributor.author
Galuppo, Mariana K.
dc.contributor.author
Taniwaki, Noemi N.
dc.contributor.author
Borborema, Samanta E. T.
dc.contributor.author
Costa, Fernando B. da
dc.contributor.author
Schmidt, Thomas J.
dc.contributor.author
Tempone, Andre G.
dc.date.accessioned
2018-06-08T10:43:47Z
dc.date.available
2017-09-04T11:25:56.186Z
dc.identifier.uri
https://refubium.fu-berlin.de/handle/fub188/20978
dc.identifier.uri
http://dx.doi.org/10.17169/refubium-24275
dc.description.abstract
Leishmaniases are neglected infectious diseases caused by parasites of the
‘protozoan’ genus Leishmania. Depending on the parasite species, different
clinical forms are known as cutaneous, muco-cutaneous, and the visceral
leishmaniasis (VL). VL is particularly fatal and the therapy presents
limitations. In the search for new anti-leishmanial hit compounds, seven
natural sesquiterpene lactones were evaluated against promastigotes and
intracellular amastigotes of Leishmania (Leishmania) infantum, a pathogen
causing VL. The pseudoguaianolides mexicanin I and helenalin acetate
demonstrated the highest selectivity and potency against intracellular
amastigotes. In addition, promastigotes treated with helenalin acetate were
subject to an ultrastructural and biochemical investigation. The lethal action
of the compound was investigated by fluorescence-activated cell sorting and
related techniques to detect alterations in reactive oxygen species (ROS)
content, plasma membrane permeability, and mitochondrial membrane potential.
Helenalin acetate significantly reduced the mitochondrial membrane potential
and the mitochondrial structural damage was also confirmed by transmission
electron microscopy, displaying an intense organelle swelling. No alteration
of plasma membrane permeability or ROS content could be detected.
Additionally, helenalin acetate significantly increased the production of
nitric oxide in peritoneal macrophages, probably potentiating the activity
against the intracellular amastigotes. Helenalin acetate could hence be a
useful anti-leishmanial scaffold for further optimization studies. View Full-
Text
en
dc.rights.uri
http://creativecommons.org/licenses/by/4.0/
dc.subject
sesquiterpene lactones
dc.subject
pseudoguaianolides
dc.subject
helenalin acetate
dc.subject
Leishmania (L.) infantum
dc.subject.ddc
600 Technik, Medizin, angewandte Wissenschaften::610 Medizin und Gesundheit
dc.title
Investigation of the Anti-Leishmania (Leishmania) infantum Activity of Some
Natural Sesquiterpene Lactones
dc.type
Wissenschaftlicher Artikel
dcterms.bibliographicCitation
Molecules. - 22 (2017), 5, Artikel Nr. 685
dcterms.bibliographicCitation.doi
10.3390/molecules22050685
dcterms.bibliographicCitation.url
http://www.mdpi.com/1420-3049/22/5/685
refubium.affiliation
Biologie, Chemie, Pharmazie
de
refubium.mycore.fudocsId
FUDOCS_document_000000027814
refubium.note.author
Der Artikel wurde in einer reinen Open-Access-Zeitschrift publiziert.
refubium.resourceType.isindependentpub
no
refubium.mycore.derivateId
FUDOCS_derivate_000000008697
dcterms.accessRights.openaire
open access