In vitro evaluation of a chemical library of synthetic compounds using two consecutive assays has led to the discovery of fifteen compounds which have the ability to inhibit recombinant Plasmodium falciparum iron superoxide dismutase (PfSOD), suggested as a highly selective target for design of antiparasitic drugs. A large number of compounds were in fact excluded, because they were found to si...

Aphidicolin and a series of semisynthetic aphidicolan derivatives have been identified in in vitro tests as novel drugs with antiparasitic potential. All compounds have been tested against extracellular promastigotes of Leishmania donovani, L. infantum, L. enriettii, and L. major and against intracellular amastigotes of L. donovani in murine macrophages. The compounds showed antileishmanial act...

Biosynthesis of aromatic amino acids in plants, many bacteria, and microbes relies on the enzyme 5-enolpyruvylshikimate 3-phosphate (EPSP) synthase, a prime target for drugs and herbicides. We have identified the interaction of EPSP synthase with one of its two substrates (shikimate 3-phosphate) and with the widely used herbicide glyphosate by x-ray crystallography. The two-domain enzyme closes...

Trypanothione reductase (TryR) is a key validated enzyme in the trypanothione-based redox metabolism of pathogenic trypanosomes and leishmania parasites. This system is absent in humans, being replaced with glutathione and glutathione reductase, and as such offers a target for selective inhibition. As part of a program to discover antiparasitic drugs, the LOPAC1280 library of 1266 compounds was...

The occurrence of mixed infections of Trypanosoma cruzi and Leishmania spp. is becoming a common feature in Central and South America due to overlapping endemic areas. Unfortunately, the possibilities for treating flagellated kinetoplastid infections are still very limited and most of the available drugs exhibit severe side effects. Although the development of new drugs for Leishmania has marke...

Plasmodial resistance to a variety of plant-based antimalarial drugs has led toward the discovery more effective compounds having chemical or biological origin. Since natural are considered as safer drugs, in this study, yeast strains were identified and compared for production carotenoids that well-known antioxidants metabolite was tested its antiparasitic activity. Plasmodium falciparum 3D7 s...

Annona muricata L. (Annonaceae) is widely used in the Amazon and Carribean natural medicine as an antiparasitic, insecticidal, sedative astringent for diarrhea among others. In Nigeria however, under-utilized species of plants. This study investigated antidepressant ambulatory effect A. muricata, using open field test forced swim tests on Sprague-Dawley rats administered ethanol stem-bark extra...

Abstract Background Alpha-2u globulin nephropathy mainly shows toxicological pathology only in male rats induced by certain chemicals and drugs, such as levamisole (antiparasitic anticancer drugs). Streptozotocin (STZ) is also an anticancer-antibiotic agent that has been used for decades to induce a diabetic kidney disease model rodents. The purpose of this study determine if STZ causes alpha-2...

In this blinded, randomized, monocentric study, we evaluated the antiparasitic efficacy of a new fipronil formulation (Effipro® spot-on, Virbac) on dogs experimentally infested with ticks, Dermacentor reticulatus. The study was performed on three groups (three males and three females per group) of beagles: untreated control, reference drugtreated, and test drug-treated group. The reference drug...

Leishmaniasis is considered one of the most untreated tropical diseases in world. In this study, we investigated vitro leishmanicidal activity and cytotoxicity various isolated lichen substances, including atranorin (1), usnic acid (2), gyrophoric (3), salazinic (4), galbinic (5), parietin (6), some semi-synthetic imine derivatives (7, 8, 9) (10, 11, 12, 13). Imine condensation reactions with h...