scholarly journals Computational and Investigative Study of Flavonoids Active against Trypanosoma cruzi and Leishmania spp

2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Frederico F. Ribeiro ◽  
Francisco J.B.M. Junior ◽  
Marcelo S. da Silva ◽  
Marcus Tullius Scotti ◽  
Luciana Scotti
Keyword(s):  
Antioxidant Activity ◽  
Trypanosoma Cruzi ◽  
Dimethyl Ether ◽  
Leishmania Species ◽  
Dihydroorotate Dehydrogenase ◽  
In Silico Docking ◽  
Leishmania Spp ◽  
Parasitic Activity ◽  
Molecular Maps ◽  
Quantum Parameters

Flavonoid compounds active against Trypanosoma cruzi and Leishmania species were submitted to several methodologies in silico: docking with the enzymes cruzain and trypanothione reductase (from T. cruzi), and N-myristoyltransferase, dihydroorotate dehydrogenase, and trypanothiona reductase (from Leishmania spp). Molecular maps of the complexes and the ligands were calculated. In order to compare and evaluate the antioxidant activity of the flavonoids with their antiprotozoal activity, quantum parameters were calculated. Considering the energies, interactions, and hydrophobic surfaces calculated, the flavonoids chrysin dimethyl ether against T. cruzi, and ladanein against Leishmania sp. presented the best results. The antioxidant activity did not show any correlation with anti-parasitic activity; only chrysin and its dimethyl ether showed favorable anti-parasitic results. This study hopes to contribute to existing research on these natural products against these tropical parasites.

scholarly journals Multi-Anti-Parasitic Activity of Arylidene Ketones and Thiazolidene Hydrazines against Trypanosoma cruzi and Leishmania spp.

Molecules ◽  
2017 ◽  
Vol 22 (5) ◽  
pp. 709 ◽  
Author(s):  
Guzmán Álvarez ◽  
Cintya Perdomo ◽  
Cathia Coronel ◽  
Elena Aguilera ◽  
Javier Varela ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Leishmania Spp ◽  
Parasitic Activity

Naphthoquinones and derivatives for chemotherapy: perspectives and limitations of their anti-trypanosomatids activities

2020 ◽  
Vol 26 ◽  
Author(s):  
Luíza Dantas-Pereira ◽  
Edézio F. Cunha-Junior ◽  
Valter V. Andrade-Neto ◽  
John F. Bower ◽  
Guilherme A. M. Jardim ◽  
...  
Keyword(s):  
Large Scale ◽  
Neglected Tropical Diseases ◽  
Folk Medicine ◽  
Leishmania Species ◽  
Parasitic Infections ◽  
Mechanistic Analysis ◽  
Leishmania Spp ◽  
Nanomolar Range

: Chagas disease, Sleeping sickness and Leishmaniasis, caused by trypanosomatids Trypanosoma cruzi, Trypanosoma brucei and Leishmania spp., respectively, are considered neglected tropical diseases, and they especially affect impoverished populations in the developing world. The available chemotherapies are very limited and a search for alternatives is still necessary. In folk medicine, natural naphthoquinones have been employed for the treatment of a great variety of illnesses, including parasitic infections. This review is focused on the anti-trypanosomatid activity and mechanistic analysis of naphthoquinones and derivatives. Among all the series of derivatives tested in vitro, naphthoquinone-derived 1,2,3-triazoles were very active on T. cruzi infective forms in blood bank conditions, as well as in amastigotes of Leishmania spp. naphthoquinones containing a CF3 on a phenyl amine ring inhibited T. brucei proliferation in the nanomolar range, and naphthopterocarpanquinones stood out for their activity on a range of Leishmania species. Some of these compounds showed a promising selectivity index (SI) (30 to 1900), supporting further analysis in animal models. Indeed, high toxicity to the host and inactivation by blood components are crucial obstacles to be overcome to use naphthoquinones and/or their derivatives for chemotherapy. Multidisciplinary initiatives embracing medicinal chemistry, bioinformatics, biochemistry, and molecular and cellular biology need to be encouraged to allow the optimization of these compounds. Large scale automated tests are pivotal for the efficiency of the screening step, and subsequent evaluation of both the mechanism of action in vitro and pharmacokinetics in vivo are essential for the development of a novel, specific and safe derivative, minimizing adverse effects.

The Widespread Anti-Protozoal Action of HIV Aspartic Peptidase Inhibitors: Focus on Plasmodium spp., Leishmania spp. and Trypanosoma cruzi

2017 ◽  
Vol 17 (11) ◽  
pp. 1303-1317 ◽  
Author(s):  
Marta Branquinha ◽  
Leandro Sangenito ◽  
Catia Sodre ◽  
Lucimar Kneipp ◽  
Claudia d'Avila-Levy ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Peptidase Inhibitors ◽  
Aspartic Peptidase ◽  
Leishmania Spp

scholarly journals Leishmania spp. parasite isolation through inoculation of patient biopsy macerates in interferon gamma knockout mice

2010 ◽  
Vol 52 (2) ◽  
pp. 83-88 ◽  
Author(s):  
Milton Adriano Pelli de Oliveira ◽  
Alause da Silva Pires ◽  
Rosidete Pereira de Bastos ◽  
Glória Maria Collet de Araujo Lima ◽  
Sebastião Alves Pinto ◽  
...  
Keyword(s):  
Species Identification ◽  
Interferon Gamma ◽  
Knockout Mice ◽  
New World ◽  
Clinical Signs ◽  
Leishmania Species ◽  
Mouse Strains ◽  
Preliminary Results ◽  
Immunohistochemical Assay ◽  
Leishmania Spp

Isolation of Leishmania parasite and species identification are important for confirmation and to help define the epidemiology of the leishmaniasis. Mice are often used to isolate pathogens, but the most common mouse strains are resistant to infection with parasites from the Leishmania (Viannia) subgenus. In this study we tested the inoculation of interferon gamma knockout (IFNγ KO) mice with biopsy macerates from Leishmania-infected patients to increase the possibility of isolating parasites. Biopsies from twenty five patients with clinical signs of leishmaniasis were taken and tested for the presence of parasites. Immunohistochemical assay (IHC) and conventional histopathology detected the parasite in 88% and 83% of the patients, respectively. Leishmania sp. were isolated in biopsy macerates from 52% of the patients by culture in Grace's insect medium, but 13% of isolates were lost due to contamination. Inoculation of macerates in IFNγ KO mice provides isolation of parasites in 31.8% of the biopsies. Most isolates belong to L. (Viannia) subgenus, as confirmed by PCR, except one that belongs to L. (Leishmania) subgenus. Our preliminary results support the use of IFNγ KO mice to improve the possibility to isolate New World Leishmania species.

Strategies for overcoming tropical disease by ruthenium complexes with purine analog: Application against Leishmania spp. and Trypanosoma cruzi

2017 ◽  
Vol 176 ◽  
pp. 144-155 ◽  
Author(s):  
Marzena Fandzloch ◽  
José Manuel Méndez Arriaga ◽  
Manuel Sánchez-Moreno ◽  
Andrzej Wojtczak ◽  
Julia Jezierska ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Ruthenium Complexes ◽  
Tropical Disease ◽  
Purine Analog ◽  
Leishmania Spp

Molecular diagnosis of Trypanosoma cruzi/Leishmania spp. coinfection in domestic, peridomestic and wild mammals of Venezuelan co-endemic areas

2018 ◽  
Vol 14 ◽  
pp. 123-130 ◽  
Author(s):  
Mercedes Viettri ◽  
Leidi Herrera ◽  
Cruz M. Aguilar ◽  
Antonio Morocoima ◽  
Jesús Reyes ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Molecular Diagnosis ◽  
Wild Mammals ◽  
Leishmania Spp ◽  
Endemic Areas
Sign in / Sign up

Export Citation Format

Share Document