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Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in L. amazonensis and L. braziliensis in Vitro
Author(s) -
Minori Karen,
Rosa Letícia B.,
Bonsignore Riccardo,
Casini Angela,
Miguel Danilo C.
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000536
Subject(s) - amastigote , leishmania braziliensis , leishmania , in vitro , intracellular , parasite hosting , leishmaniasis , chemistry , biology , microbiology and biotechnology , biochemistry , cutaneous leishmaniasis , immunology , world wide web , computer science
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.