Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro

Abstract: A series of mononuclear coordination or organometallic Au(I)/Au(III) complexes (1–9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, of Leishmania amazonensis and Leishmania braziliens...

Descripción completa

Detalles Bibliográficos
Autores principales: Minori, Karen, Rosa, Letícia B., Bonsignore, Riccardo, Casini, Angela, Miguel, Danilo C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7756297/
https://www.ncbi.nlm.nih.gov/pubmed/32830445
http://dx.doi.org/10.1002/cmdc.202000536
_version_ 1783626509528858624
author Minori, Karen
Rosa, Letícia B.
Bonsignore, Riccardo
Casini, Angela
Miguel, Danilo C.
author_facet Minori, Karen
Rosa, Letícia B.
Bonsignore, Riccardo
Casini, Angela
Miguel, Danilo C.
author_sort Minori, Karen
collection PubMed
description Abstract: A series of mononuclear coordination or organometallic Au(I)/Au(III) complexes (1–9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, of Leishmania amazonensis and Leishmania braziliensis. One of the cationic Au(I) bis‐N‐heterocyclic carbenes (3) has low EC(50) values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other Au(III) complexes (6 and 7), the compound is also extremely effective in intracellular amastigotes from L. amazonensis. Initial mechanistic studies include an evaluation of the gold complexes′ effect on L. amazonensis’ plasma membrane integrity.
format Online
Article
Text
id pubmed-7756297
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher John Wiley and Sons Inc.
record_format MEDLINE/PubMed
spelling pubmed-77562972020-12-28 Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro Minori, Karen Rosa, Letícia B. Bonsignore, Riccardo Casini, Angela Miguel, Danilo C. ChemMedChem Communications Abstract: A series of mononuclear coordination or organometallic Au(I)/Au(III) complexes (1–9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, of Leishmania amazonensis and Leishmania braziliensis. One of the cationic Au(I) bis‐N‐heterocyclic carbenes (3) has low EC(50) values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other Au(III) complexes (6 and 7), the compound is also extremely effective in intracellular amastigotes from L. amazonensis. Initial mechanistic studies include an evaluation of the gold complexes′ effect on L. amazonensis’ plasma membrane integrity. John Wiley and Sons Inc. 2020-09-28 2020-11-18 /pmc/articles/PMC7756297/ /pubmed/32830445 http://dx.doi.org/10.1002/cmdc.202000536 Text en © 2020 The Authors. Published by Wiley-VCH GmbH This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited and is not used for commercial purposes.
spellingShingle Communications
Minori, Karen
Rosa, Letícia B.
Bonsignore, Riccardo
Casini, Angela
Miguel, Danilo C.
Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title_full Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title_fullStr Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title_full_unstemmed Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title_short Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
title_sort comparing the antileishmanial activity of gold(i) and gold(iii) compounds in l. amazonensis and l. braziliensis in vitro
topic Communications
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7756297/
https://www.ncbi.nlm.nih.gov/pubmed/32830445
http://dx.doi.org/10.1002/cmdc.202000536
work_keys_str_mv AT minorikaren comparingtheantileishmanialactivityofgoldiandgoldiiicompoundsinlamazonensisandlbraziliensisinvitro
AT rosaleticiab comparingtheantileishmanialactivityofgoldiandgoldiiicompoundsinlamazonensisandlbraziliensisinvitro
AT bonsignorericcardo comparingtheantileishmanialactivityofgoldiandgoldiiicompoundsinlamazonensisandlbraziliensisinvitro
AT casiniangela comparingtheantileishmanialactivityofgoldiandgoldiiicompoundsinlamazonensisandlbraziliensisinvitro
AT migueldaniloc comparingtheantileishmanialactivityofgoldiandgoldiiicompoundsinlamazonensisandlbraziliensisinvitro

Ejemplares similares