Comparing the Antileishmanial Activity of Gold(I) and Gold(III) Compounds in <i>L. amazonensis</i> and <i>L. braziliensis in Vitro</i>
Karen Minori, Letícia B. Rosa, Riccardo Bonsignore, Angela Casini, Danilo C. Miguel
Abstract
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 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.