The Potential Role of Sanguinarine as an Inhibitor of Leishmania PP2C in the Induction of Apoptosis.

Leishmania spp. cause a wide range of human diseases, localized skin lesions, mucocutaneous and visceral infections. In the present study, the aim was to investigate the potential role of sanguinarine as a specific inhibitor of Leishmania PP2C that can induce apoptosis in the parasite.

Exploring the Mechanisms Underlying Cellular Uptake and Activation of Dendritic Cells by the GK-1 Peptide.

The use of peptides for cancer immunotherapy is a promising and emerging approach that is being intensively explored worldwide. One such peptide, GK-1, has been shown to delay the growth of triple-negative breast tumors in mice, reduce their metastatic capacity, and reverse the intratumor immunosuppression that characterizes this model. Herein, it is demonstrated that GK-1 is taken up by bone marrow dendritic cells in a dose-dependent manner 15 min after exposure, more efficiently at 37 °C than at 4 °C, implying an entrance into the cells by energy-independent and -dependent processes through clathrin-mediated endocytosis.

Compared Antileishmanial Activity of Clomiphene and Tamoxifen.

Drug repositioning is an efficient strategy to search for new treatment alternatives that is especially valuable for neglected parasitic diseases such as leishmaniasis. Tamoxifen and raloxifene are selective estrogen receptor modulators (SERMs) that have shown antileishmanial activity. Clomiphene is a SERM structurally similar to tamoxifen, whose antileishmanial potential is unknown.

3-Alkoxy-1-Benzyl-5-Nitroindazole Derivatives Are Potent Antileishmanial Compounds.

Indazoles have previously been identified as molecules with antiprotozoal activity. In this study, we evaluate the in vitro activity of thirteen 3-alkoxy-1-benzyl-5-nitroindazole derivatives (series D) against , and . In vitro, cytotoxicity against mouse peritoneal macrophages and growth inhibitory activity in promastigotes were evaluated for all compounds, and those showing adequate activity and selectivity were tested against intracellular amastigotes.

In Vitro and In Vivo Antileishmanial Activity of Thioridazine.

Introduction: Leishmaniasis is a neglected disease with high prevalence and incidence in tropical and subtropical areas. Existing drugs are limited due to cost, toxicity, declining efficacy and unavailability in endemic places. Drug repurposing has established as an efficient way for the discovery of drugs for a variety of diseases.

Antileishmanial activity of 5-nitroindazole derivatives.

Background: Currently, there is no safe and effective vaccine against leishmaniasis and existing therapies are inadequate due to high toxicity, cost and decreased efficacy caused by the emergence of resistant parasite strains. Some indazole derivatives have shown and activity against and . On that basis, 20 indazole derivatives were tested against .

Detergent-free parasite transformation and replication assay for drug screening against intracellular Leishmania amastigotes.

Leishmaniasis is an infectious disease caused by protozoan species in the genera Leishmania and Endotrypanum. Current antileishmanial drugs are limited due to adverse effects, variable efficacy, the development of resistant parasites, high cost, parenteral administration and lack of availability in endemic areas. Therefore, active searching for new antileishmanial drugs has been done for years, mainly by academia.

Characterization of Actinobacterial Strains as Potential Biocontrol Agents against and , the Main Soil-Borne Pathogens of in Cuba.

Macrophomina phaseolina and Rhizoctonia solani are considered two major soil-borne pathogens of Phaseolus vulgaris in Cuba. Their management is difficult, not only due to their intrinsic biology as soil-borne pathogens, but also because the lack of active ingredients available against these pathogens. Actinobacteria, a heterogeneous bacterial group traditionally known as actinomycetes have been reported as promising biological control agents (BCAs) in crop protection.

Antichagasic, Leishmanicidal, and Trichomonacidal Activity of 2-Benzyl-5-nitroindazole-Derived Amines.

Three different series of new 5-nitroindazole derivatives-1-(ω-aminoalkyl)-2-benzylindazolin-3-ones (series A; ten compounds), 3-(ω-aminoalkoxy)-2-benzylindazoles (series B; four compounds) and 3-alkylamino-2-benzylindazoles (series C; five compounds)-have been synthesized and evaluated against the protozoan parasites Trypanosoma cruzi, Leishmania amazonensis, and Trichomonas vaginalis: etiological agents of Chagas disease, cutaneous leishmaniasis, and trichomoniasis, respectively. Many indazoles of series A, B, and C were efficient against T. cruzi.

The efficacy of 2-nitrovinylfuran derivatives against Leishmania in vitro and in vivo.

Despite recent advances in the treatment of some forms of leishmaniasis, the available drugs are still far from ideal due to inefficacy, parasite resistance, toxicity and cost. The wide-spectrum antimicrobial activity of 2-nitrovinylfuran compounds has been described, as has their activity against Trichomonas vaginalis and other protozoa. Thus, the aim of this study was to test the antileishmanial activities of six 2-nitrovinylfurans in vitro and in a murine model of leishmaniasis.

Toxicological Assessment of the Cochleate Derived from Neisseria meningitidis Proteoliposome in Sprague Dawley Rats.

Background: The AFCo1 cochleate is a potential novel adjuvant derived from Neisseria meningitidis B proteoliposome.

Aim: The aim was to assessing the safety of AFCo1 by single and repeated doses in Sprague Dawley rats.

Materials And Methods: Rats were grouped for treatment with AFCo1, placebo formulation or control.

A fluorometric method for evaluation of pharmacological activity against intracellular Leishmania amastigotes.

In this work a simple and novel method to evaluate the efficacy of compounds on intracellular Leishmania amastigotes by using a fluorometric assay has been developed. The new method is sensitive, easy to perform and scalable for high throughput and therefore it could be validated for screening of new anti-leishmanial agents.

Repeated dose toxicity study of a live attenuated oral cholera vaccine in Sprague Dawley rats.

Background And Aims: A live attenuated vaccine candidate against human cholera has been developed from the genetically modified Vibrio cholerae O1, biotype El Tor, serotype Ogawa, 638 strain. Previous single dose toxicity and local tolerance studies have demonstrated that the product is innocuous in Sprague Dawley rats by oral route and single dose. The present paper describes a repeated dose toxicity study using a further dose compared to the proposed clinical schedule.

Evaluation of the antimeningococcal immunoglobin activity against five strains of Neisseria meningitidis group B from Latin America using mice as model.

To know the activity of antimeningococcal immunoglobulin, Balb/c mice of 18-22 g of body weight were challenged with 5 serotype B strains of Neisseria meningitidis (Nm) isolated from patients of different Latin American countries. The specific antimeningococcal Ig was extracted from the serum of volunteers previously vaccinated with the antimeningococcal BC vaccine VA-MENGOC-BC (Finlay Institute, Havana, Cuba). The Ig was intraperitoneally (IP) administered in a unique dose of 10 mg/mouse.