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

Karen Minori; Letícia B. Rosa; Riccardo Bonsignore; Angela Casini; Danilo C. Miguel

doi:10.1002/cmdc.202000536

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

Karen Minori, Letícia B. Rosa, Riccardo Bonsignore, Angela Casini, Danilo C. Miguel

Chair of Medicinal and Bioinorganic Chemistry

Research output: Contribution to journal › Article › peer-review

29 Scopus citations

Abstract

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 EC₅₀ 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.

Original language	English
Pages (from-to)	2146-2150
Number of pages	5
Journal	ChemMedChem
Volume	15
Issue number	22
DOIs	https://doi.org/10.1002/cmdc.202000536
State	Published - 18 Nov 2020

Keywords

amastigotes
antiprotozoal agents
gold compounds
leishmaniasis
promastigotes

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10.1002/cmdc.202000536

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

abstract = "Abstract: A series of mononuclear coordination or organometallic AuI/AuIII 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 AuI bis-N-heterocyclic carbenes (3) has low EC50 values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other AuIII 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{\textquoteright} plasma membrane integrity.",

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AU - Rosa, Letícia B.

AU - Bonsignore, Riccardo

AU - Casini, Angela

AU - Miguel, Danilo C.

PY - 2020/11/18

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N2 - Abstract: A series of mononuclear coordination or organometallic AuI/AuIII 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 AuI bis-N-heterocyclic carbenes (3) has low EC50 values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other AuIII 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.

AB - Abstract: A series of mononuclear coordination or organometallic AuI/AuIII 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 AuI bis-N-heterocyclic carbenes (3) has low EC50 values (ca. 4 μM) in promastigotes cells and no toxicity in host macrophages. Together with two other AuIII 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.

KW - amastigotes

KW - antiprotozoal agents

KW - gold compounds

KW - leishmaniasis

KW - promastigotes

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

Abstract

Keywords

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