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RESEARCH PRODUCT

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

Riccardo BonsignoreDanilo C. MiguelAngela CasiniLeticia B. RosaKaren Minori

subject

StereochemistryAntiprotozoal Agentsamastigotes01 natural sciencesBiochemistryMiceGold iiiParasitic Sensitivity TestsGold CompoundsDrug Discoverygold compoundsmedicineAnimalsGeneral Pharmacology Toxicology and PharmaceuticsAmastigoteleishmaniasisCells CulturedEC50LeishmaniaPharmacologyMice Inbred BALB CMolecular Structurebiology010405 organic chemistryChemistryCommunicationOrganic ChemistryLeishmaniasismedicine.diseasebiology.organism_classificationLeishmania braziliensisCommunicationsIn vitroddc:0104 chemical sciences010404 medicinal & biomolecular chemistryMolecular MedicinepromastigotesOrganogold CompoundsIntracellular

description

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’ plasma membrane integrity.

yearjournalcountryeditionlanguage
2020-09-28ChemMedChem
https://doi.org/10.1002/cmdc.202000536