scholarly journals Estudos estruturais e de química medicinal aplicados às enzimas da via glicolítica de protozoários: enolase de Plasmodium falciparum e gliceraldeído-3-fosfato desidrogenase de Trypanosoma cruzi

Author(s):  
Fernando Vasconcelos Maluf
2021 ◽  
Author(s):  
Camila M. Clemente ◽  
Tatiana Pineda ◽  
Lina M. Yepes ◽  
Yulieth Upegui ◽  
Daniel A. Allemandi ◽  
...  

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400 ◽  
Author(s):  
Ivan Limachi ◽  
Claudia Condo ◽  
Camila Palma ◽  
Nelida Nina ◽  
Efrain Salamanca ◽  
...  

A bioassay screening against protozoa parasites of several Tacana medicinal plants gave Hyptis brevipes (Id'ene eidhue), traditionally used as decoction for intestinal parasites, as the most active extract. In this work we did a bioguided isolation of active constituents found in leaves. Structure elucidation was carried out by NMR spectroscopy and MS spectrometry analyses. Active constituents showed differentiated activity towards Giardia lamblia, Trypanosoma cruzi, several Leishmania strains, Plasmodium falciparum and cytotoxicity against HeLa cells. Brevipolide H (1) was the less cytotoxic and best antiparasitic, while the catechol derivative (2) the most active and cytotoxic.


2021 ◽  
Vol 22 (1) ◽  
pp. 469
Author(s):  
Pedro H. Scarpelli ◽  
Mateus F. Pecenin ◽  
Celia R. S. Garcia

Ca2+ signaling has been involved in controling critical cellular functions such as activation of proteases, cell death, and cell cycle control. The endoplasmatic reticulum plays a significant role in Ca2+ storage inside the cell, but mitochondria have long been recognized as a fundamental Ca2+ pool. Protozoan parasites such as Plasmodium falciparum, Toxoplasma gondii, and Trypanosoma cruzi display a Ca2+ signaling toolkit with similarities to higher eukaryotes, including the participation of mitochondria in Ca2+-dependent signaling events. This review summarizes the most recent knowledge in mitochondrial Ca2+ signaling in protozoan parasites, focusing on the mechanism involved in mitochondrial Ca2+ uptake by pathogenic protists.


2015 ◽  
Vol 30 (11) ◽  
pp. 1320-1326 ◽  
Author(s):  
Sébastien Charneau ◽  
Mariana Laundry de Mesquita ◽  
Izabela Marques Dourado Bastos ◽  
Jaime Martins Santana ◽  
José Elias de Paula ◽  
...  

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400
Author(s):  
Sergio Martínez-Luis ◽  
Lilia Cherigo ◽  
Carmenza Spadafora ◽  
Marcelino Gutiérrez

Fractionation of the ethyl acetate extract of the bacterium Pseudomonas aeruginosa led to the isolation of five compounds, cyclo –(L-Phe-L-Pro) (1), 3-heptyl-3-hydroxy-1,2,3,4-tetrahydroquinoline-2.4-dione (2), 2-heptyl-4-hydroxyquinoline (3), 2-nonyl-4-hydroxyquinoline (4), and 1-phenazinecarboxylic acid (5). The structures of compounds 1-5 were established by spectroscopic analyses. Compounds 2 4 produced inhibition on the growth of Plasmodium falciparum, with IC50 values of 3.47, 2.57 and 2.79 μg/mL, respectively. Compounds 3-4 had activity against Trypanosoma cruzi, with IC50 values of 3.66 and 3.99 μg/mL. Finally, all compounds were found inactive when tested against Leishmania donovani at 10 μg/mL.


2009 ◽  
Vol 53 (9) ◽  
pp. 3815-3821 ◽  
Author(s):  
Christophe Dardonville ◽  
Cristina Fernández-Fernández ◽  
Sarah-Louise Gibbons ◽  
Nadine Jagerovic ◽  
Lidia Nieto ◽  
...  

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.


ChemMedChem ◽  
2020 ◽  
Vol 15 (22) ◽  
pp. 2164-2175
Author(s):  
Paulo André Teixeira de Moraes Gomes ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Ignes Regina Santos ◽  
Fabiano Amaro de Sousa ◽  
Juliana Maria Conceição ◽  
...  

1988 ◽  
Vol 2 (13) ◽  
pp. 2878-2883 ◽  
Author(s):  
Jesse M. Jaynes ◽  
Catherine A. Burton ◽  
Stephen B. Barr ◽  
Gale W. Jeffers ◽  
Gordon R. Julian ◽  
...  

Author(s):  
D.J.P. Ferguson ◽  
A.R. Berendt ◽  
J. Tansey ◽  
K. Marsh ◽  
C.I. Newbold

In human malaria, the most serious clinical manifestation is cerebral malaria (CM) due to infection with Plasmodium falciparum. The pathology of CM is thought to relate to the fact that red blood cells containing mature forms of the parasite (PRBC) cytoadhere or sequester to post capillary venules of various tissues including the brain. This in vivo phenomenon has been studied in vitro by examining the cytoadherence of PRBCs to various cell types and purified proteins. To date, three Ijiost receptor molecules have been identified; CD36, ICAM-1 and thrombospondin. The specific changes in the PRBC membrane which mediate cytoadherence are less well understood, but they include the sub-membranous deposition of electron-dense material resulting in surface deformations called knobs. Knobs were thought to be essential for cytoadherence, lput recent work has shown that certain knob-negative (K-) lines can cytoadhere. In the present study, we have used electron microscopy to re-examine the interactions between K+ PRBCs and both C32 amelanotic melanoma cells and human umbilical vein endothelial cells (HUVEC).We confirm previous data demonstrating that C32 cells possess numerous microvilli which adhere to the PRBC, mainly via the knobs (Fig. 1). In contrast, the HUVEC were relatively smooth and the PRBCs appeared partially flattened onto the cell surface (Fig. 2). Furthermore, many of the PRBCs exhibited an invagination of the limiting membrane in the attachment zone, often containing a cytoplasmic process from the endothelial cell (Fig. 2).


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