scholarly journals Defeating the trypanosomatid trio: proteomics of the protozoan parasites causing neglected tropical diseases

2020 ◽  
Vol 11 (6) ◽  
pp. 625-645 ◽  
Author(s):  
Anutthaman Parthasarathy ◽  
Karunakaran Kalesh
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanosoma Brucei ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Protozoan Parasites ◽  
Proteomic Techniques

This review highlights the key roles of proteomic techniques in the study of Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei parasites.

The use of Sulfonamide Derivatives in the Treatment of Trypanosomatid Parasites including Trypanosoma cruzi, Trypanosoma brucei, and Leishmania ssp

2020 ◽  
Vol 16 (1) ◽  
pp. 24-38 ◽  
Author(s):  
Cauê B. Scarim ◽  
Rafael C. Chelucci ◽  
Jean L. dos Santos ◽  
Chung M. Chin
Keyword(s):  
Trypanosoma Cruzi ◽  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Neglected Tropical Diseases ◽  
Economic Incentive ◽  
Tropical Diseases ◽  
Lipinski’S Rule ◽  
Novel Drugs ◽  
Trypanosomatid Parasites ◽  
Research And Policy

More than 10 million people around the world are afflicted by Neglected Tropical Diseases, such as Chagas Disease, Human African Trypanosomiasis, and Leishmania. These diseases mostly occur in undeveloped countries that suffer from a lack of economic incentive, research, and policy for new compound development. Sulfonamide moieties are effective scaffolds present in several compounds that are determinants to treat various diseases, principally neglected tropical diseases. This review article examines the contribution of these scaffolds in medicinal chemistry in the last five years, focusing on three trypanosomatid parasites: Trypanosoma cruzi, Trypanosoma brucei, and Leishmania ssp. We also present perspectives for their use in drug designs in an effort to contribute to new drug development. In addition, we consider the physicochemical parameters, whose molecules all presented according to Lipinski's rule. The correlation between the selective index and LogP was evaluated, showing that sulfonamide derivatives can act differently against each trypanosomatid parasite. Moreover, the approaches of novel drugs and technologies are very important for the eventual drug discovery against trypanosomatid diseases.

Quinoline-based Compounds as Key Candidates to Tackle Drug Discovery Programs of Microbicidal Agents

2020 ◽  
Vol 26 ◽  
Author(s):  
Aline Nefertiti Silva da Gama ◽  
Maria de Nazaré Correia Soeiro
Keyword(s):  
Drug Discovery ◽  
Trypanosoma Brucei ◽  
Anticancer Agents ◽  
Biological Effect ◽  
Heterocyclic Compounds ◽  
Neglected Tropical Diseases ◽  
Pharmacological Properties ◽  
Tropical Diseases ◽  
Clinical Use ◽  
Leishmania Spp

: Quinolines are nitrogen heterocyclic compounds ubiquitous in nature and largely used as a structural component of dyes, solvent for resins, terpenes as well as during the production of several other chemical stuffs, including pesticides. Quinolines, such as quinine and chloroquine, exhibit various pharmacological properties, acting as antimalarial drugs, antiparasitic, antibacterial, antiviral, antifungal, and anticancer agents, besides being in clinical use for autoimmune diseases. Presently, a brief review is present regarding the biological effect and clinical use of quinolines and derivatives upon two trypanosomatids agents of important neglected tropical diseases; Trypanosoma cruzi, Trypanosoma brucei spp and Leishmania spp, which trigger Chagas disease, sleeping sickness and leishmaniasis, respectively, also extending to a glance update of their potential application towards other microbes relevant for emerging illness caused by fungi, bacteria and virus, including the pandemic Covid-19.

scholarly journals Host-Directed Drug Therapies for Neglected Tropical Diseases Caused by Protozoan Parasites

2018 ◽  
Vol 9 ◽  
Author(s):  
Sanjay Varikuti ◽  
Bijay Kumar Jha ◽  
Greta Volpedo ◽  
Nathan M. Ryan ◽  
Gregory Halsey ◽  
...  
Keyword(s):  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Protozoan Parasites

scholarly journals Bixa orellana L. (Bixaceae) and Dysphania ambrosioides (L.) Mosyakin & Clemants (Amaranthaceae) Essential Oils Formulated in Nanocochleates against Leishmania amazonensis

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4222 ◽  
Author(s):  
Laura Machín ◽  
Beatriz Tamargo ◽  
Abel Piñón ◽  
Regla C. Atíes ◽  
Ramón Scull ◽  
...  
Keyword(s):  
Animal Model ◽  
Essential Oils ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Bixa Orellana ◽  
Protozoan Parasites ◽  
Cytotoxic Effects ◽  
Hydrophobic Materials

Leishmaniasis is a group of neglected tropical diseases caused by protozoan parasites of the Leishmania genus. The absence of effective vaccines and the limitations of current treatments make the search for effective therapies a real need. Different plant-derived essential oils (EOs) have shown antileishmanial effects, in particular from Bixa orellana L. (EO-Bo) and Dysphania ambrosioides (L.) Mosyakin & Clemants (EO-Da). In the present study, the EO-Bo and EO-Da, formulated in nanocochleates (EO-Bo-NC and EO-Da-NC, respectively), were evaluated in vitro and in vivo against L. amazonensis. The EO-Bo-NC and EO-Da-NC did not increase the in vitro inhibitory activity of the EOs, although the EO-Bo-NC showed reduced cytotoxic effects. In the animal model, both formulations (30 mg/kg/intralesional route/every 4 days/4 times) showed no deaths or weight loss greater than 10%. In the animal (mouse) model, EO-Bo-NC contributed to the control of infection (p < 0.05) in comparison with EO-Bo treatment, while the mice treated with EO-Da-NC exhibited larger lesions (p < 0.05) compared to those treated with EO-Da. The enhanced in vivo activity observed for EO-Bo-NC suggests that lipid-based nanoformulations like nanocochleates should be explored for their potential in the proper delivery of drugs, and in particular, the delivery of hydrophobic materials for effective cutaneous leishmaniasis treatment.

scholarly journals Antiprotozoal Activity of 1-Phenethyl-4-Aminopiperidine Derivatives

2009 ◽  
Vol 53 (9) ◽  
pp. 3815-3821 ◽  
Author(s):  
Christophe Dardonville ◽  
Cristina Fernández-Fernández ◽  
Sarah-Louise Gibbons ◽  
Nadine Jagerovic ◽  
Lidia Nieto ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Trypanosoma Cruzi ◽  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
Antiprotozoal Activity ◽  
Protozoan Parasites ◽  
Trypanosoma Brucei Rhodesiense ◽  
Reference Drug ◽  
Axenic Amastigotes

ABSTRACT A series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum). This screening identified 29 molecules selectively active against bloodstream-form T. b. rhodesiense trypomastigotes, with 50% inhibitory concentrations (IC50) ranging from 0.12 to 10 μM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 μM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 μM) but were also cytotoxic to L-6 cells, showing little selectivity for T. cruzi. None of the molecules tested showed interesting antileishmanial activity against axenic amastigotes of L. donovani. To our knowledge, this is the first report of the antitrypanosomal activity of molecules bearing the 4-aminopiperidine skeleton.

scholarly journals Repurposing human PDE4 inhibitors for neglected tropical diseases: Design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors

2014 ◽  
Vol 24 (17) ◽  
pp. 4084-4089 ◽  
Author(s):  
Emanuele Amata ◽  
Nicholas D. Bland ◽  
Charles T. Hoyt ◽  
Luca Settimo ◽  
Robert K. Campbell ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Design Synthesis

scholarly journals VLP-Based Vaccines as a Suitable Technology to Target Trypanosomatid Diseases

Vaccines ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 220
Author(s):  
Aline Maria Vasconcelos Queiroz ◽  
Johny Wysllas de Freitas Oliveira ◽  
Cláudia Jassica Moreno ◽  
Diego M. A. Guérin ◽  
Marcelo Sousa Silva
Keyword(s):  
Trypanosoma Brucei ◽  
Neglected Tropical Diseases ◽  
Tropical Diseases ◽  
Vaccine Adjuvants ◽  
Host Interaction ◽  
Virus Like Particle ◽  
Leishmania Spp ◽  
Potential Use ◽  
A Current ◽  
New Vaccines

Research on vaccines against trypanosomatids, a family of protozoa that cause neglected tropical diseases, such as Chagas disease, leishmaniasis, and sleeping sickness, is a current need. Today, according to modern vaccinology, virus-like particle (VLP) technology is involved in many vaccines, including those undergoing studies related to COVID-19. The potential use of VLPs as vaccine adjuvants opens an opportunity for the use of protozoan antigens for the development of vaccines against diseases caused by Trypanosoma cruzi, Leishmania spp., and Trypanosoma brucei. In this context, it is important to consider the evasion mechanisms of these protozoa in the host and the antigens involved in the mechanisms of the parasite–host interaction. Thus, the immunostimulatory properties of VLPs can be part of an important strategy for the development and evaluation of new vaccines. This work aims to highlight the potential of VLPs as vaccine adjuvants for the development of immunity in complex diseases, specifically in the context of tropical diseases caused by trypanosomatids.

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