BACKGROUND Arginase is an enzyme that converts L-arginine to urea and L-ornithine, an essential substrate for the polyamine pathway supporting Leishmania (Leishmania) amazonensis replication and its survival in the mammalian host. L-arginine is also the substrate of macrophage nitric oxide synthase 2 (NOS2) to produce nitric oxide (NO) that kills the parasite. This competition can define the fa...

OBJECTIVES This study was performed to investigate the activity of tamoxifen, an antioestrogen widely used in the treatment of breast cancer, against Leishmania. METHODS Drug activity was assessed in vitro against axenically grown promastigotes and amastigotes through cell counting or by measuring the cleavage of MTT, and against intracellular amastigotes by treating infected macrophage cultu...

OBJECTIVES Solanum acueastrum Dunal. has been shown to have some chemotherapeutic value. Leaf and berry water and methanol compounds of S. acueastrum were evaluated for possible antileishmanial activity In vivo on BALB/c mice and in vitro against Leishmania major promastigotes, amastigotes and vero cells. MATERIALS AND METHODS Dry S. aculeastrum berry and leaf material were extracted in metha...

there is the need for new drugs with better action and lesser side effects. a lot of research is being undertaken to find out new plant drugs, their extraction and pharmacological evaluation. one of such plant is curcuma aromatica whichbelongs to the genus curcuma and reported to have high ethno-botanical values in traditional medicine. the present study evaluates comparative pharmacological ac...

The term leishmaniasis includes multiple clinical syndromes: visceral, cutaneous, and mucosal leishmaniasis, resulting from an infection of macrophages throughout the reticuloendothelial system in dermis naso-oropharyngeal mucosa, respectively. phenotype is mainly driven by leishmania biologic characteristics and, ultimately, also host immune status. disease endemic focal areas tropics, subtrop...

In this report, we have characterized two metacaspases of Leishmania donovani, L. donovani metacaspase-1 (LdMC1) and LdMC2. These two proteins show 98% homology with each other, and both contain a characteristic C-terminal proline-rich domain. Both genes are transcribed in promastigotes and axenic amastigotes of L. donovani; however, LdMC1 shows increased mRNA levels in axenic amastigotes. An a...

The 8-aminoquinoline tafenoquine showed significant in vitro activity against Leishmania species, including L. donovani amastigotes in macrophages, with 50% inhibitory concentrations (IC(50)s) between 0.1 and 4.0 μM for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in BALB/c mice, with 50% effective dose (ED(50)) values of 1.2 to 3.5 mg/kg for 5 ...

Drug combinations for the treatment of leishmaniasis represent a promising and challenging chemotherapeutic strategy that has recently been implemented in different endemic areas. However, the vast majority of studies undertaken to date have ignored the potential risk that Leishmania parasites could develop resistance to the different drugs used in such combinations. As a result, this study was...

Trypanosoma cruzi amastigotes present receptors for human transferrin as indicated by the saturable binding of 125I-transferrin to this form of the parasite. Computerized Scatchard analysis revealed one class of receptors present at 8.1 X 10(4) receptors per amastigote with a Kd of 2.82 microM. Immunofluorescence studies indicate that more than 90% of amastigotes bind human transferrin, whereas...

We report structure-activity studies of a large number of dialkyl imidazoles as inhibitors of Trypanosoma cruzi lanosterol-14R-demethylase (L14DM). The compounds have a simple structure compared to posaconazole, another L14DM inhibitor that is an anti-Chagas drug candidate. Several compounds display potency for killing T. cruzi amastigotes in vitro with values of EC50 in the 0.4-10 nM range. Tw...