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J Pharm Pharmacol ; 71(12): 1784-1791, 2019 Dec.
Article in English | MEDLINE | ID: mdl-31579947

ABSTRACT

The alkylaminoalkanethiosulfuric acids (AAATs) are amphipathic compounds effective against experimental schistosomiasis, of low toxicity, elevated bioavailability after a single oral dose and prompt tissue absorption. OBJECTIVES: To explore the in-vitro antileishmanial potential of AAATs using five compounds of this series against Leishmania (Viannia) braziliensis. METHODS: Their effects on promastigotes and axenic amastigotes, and cytotoxicity to macrophages were tested by the MTT method, and on Leishmania-infected macrophages by Giemsa stain. Effects on the mitochondrial membrane potential of promastigotes and axenic amastigotes and DNA of intracellular amastigotes were tested using JC-1 and TUNEL assays, respectively. KEY FINDINGS: The 2-(isopropylamino)-1-octanethiosulfuric acid (I) and 2-(sec-butylamino)-1-octanethiosulfuric acid (II) exhibit activity against both promastigotes and intracellular amastigotes (IC50 25-35 µm), being more toxic to intracellular parasites than to the host cell. Compound I induced a loss of viability of axenic amastigotes, significantly reduced (30%) the mitochondrial membrane potential of both promastigotes and axenic amastigotes and promoted selective DNA fragmentation of the nucleus and kinetoplast of intracellular amastigotes. CONCLUSIONS: In this previously unpublished study of trypanosomatids, it is shown that AAATs could also exhibit selective antileishmanial activity, a new possibility to be investigated in oral treatment of leishmaniasis.


Subject(s)
Antiprotozoal Agents/pharmacology , Leishmania braziliensis/isolation & purification , Leishmaniasis/drug therapy , Sulfuric Acids/pharmacology , Administration, Oral , Animals , Antiprotozoal Agents/administration & dosage , Antiprotozoal Agents/chemistry , Inhibitory Concentration 50 , Leishmania braziliensis/drug effects , Membrane Potential, Mitochondrial/drug effects , Mice , Mice, Inbred BALB C , Structure-Activity Relationship , Sulfuric Acids/administration & dosage , Sulfuric Acids/chemistry
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