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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 braziliensis. One of the cationic Au^I bis-N-heterocyclic carbenes (3) has low EC₅₀ values (ca. 4??M) 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.

SUBMITTER: Minori K

PROVIDER: S-EPMC7756297 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature

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

Minori Karen K Rosa Letícia B LB Bonsignore Riccardo R Casini Angela A Miguel Danilo C DC

ChemMedChem 20200928 22

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 ...[more]

PMID: 32830445

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