scholarly journals Trypanocidal activity of the anthocyanidin delphinidin, a non-competitive inhibitor of arginine kinase

2021 ◽  
pp. 1-5
Author(s):  
Edward Valera-Vera ◽  
Chantal Reigada ◽  
Melisa Sayé ◽  
Fabio A. Digirolamo ◽  
Facundo Galceran ◽  
...  
2020 ◽  
Author(s):  
Edward Valera-Vera ◽  
Chantal Reigada ◽  
Melisa Sayé ◽  
Fabio A. Digirolamo ◽  
Facundo Galceran ◽  
...  

ABSTRACTThe enzyme arginine kinase from Trypanosoma cruzi (TcAK) catalyzes the interconversion of arginine and phosphoarginine to maintain the ATP/ADP cell balance, and is involved in the parasites energetic homeostasis and stress responses. Using virtual screening approaches, some plant-derived polyphenolic pigments such as anthocyanidins, were predicted to inhibit TcAK activity. In this work, it was demonstrated that the anthocyanidin delphinidin showed a non-competitive inhibition mechanism of TcAK in vitro (Ki arginine = 1.32 μM and Ki ATP = 500 μM). Molecular docking simulations predicted that delphinidin occupies a hydrophobic pocket close to the ATP/ADP binding site. Delphinidin also exerted trypanocidal activity over T. cruzi trypomastigotes with a calculated IC50 of 19.51 μM. Anthocyanidins are low-toxicity natural products which can be exploited for the development of trypanocidal drugs with less secondary effects than those currently used for the treatment of Chagas disease.


2016 ◽  
Vol 87 ◽  
pp. 498-503 ◽  
Author(s):  
Edward A. Valera Vera ◽  
Melisa Sayé ◽  
Chantal Reigada ◽  
Flávia S. Damasceno ◽  
Ariel M. Silber ◽  
...  

Author(s):  
M. Locke ◽  
J. T. McMahon

The fat body of insects has always been compared functionally to the liver of vertebrates. Both synthesize and store glycogen and lipid and are concerned with the formation of blood proteins. The comparison becomes even more apt with the discovery of microbodies and the localization of urate oxidase and catalase in insect fat body.The microbodies are oval to spherical bodies about 1μ across with a depression and dense core on one side. The core is made of coiled tubules together with dense material close to the depressed membrane. The tubules may appear loose or densely packed but always intertwined like liquid crystals, never straight as in solid crystals (Fig. 1). When fat body is reacted with diaminobenzidine free base and H2O2 at pH 9.0 to determine the distribution of catalase, electron microscopy shows the enzyme in the matrix of the microbodies (Fig. 2). The reaction is abolished by 3-amino-1, 2, 4-triazole, a competitive inhibitor of catalase. The fat body is the only tissue which consistantly reacts positively for urate oxidase. The reaction product is sharply localized in granules of about the same size and distribution as the microbodies. The reaction is inhibited by 2, 6, 8-trichloropurine, a competitive inhibitor of urate oxidase.


Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
WR Cunha ◽  
FM Dos Santos ◽  
JA Peixoto ◽  
RCS Veneziani ◽  
AEM Crotti ◽  
...  

1968 ◽  
Vol 19 (03/04) ◽  
pp. 364-367 ◽  
Author(s):  
H. C Hemker ◽  
P. W Hemker

SummaryThe enzyme kinetics of competitive inhibition under conditions prevailing in clotting tests are developed and a method is given to measure relative amounts of a competitive inhibitor by means of the t — D plot.


2015 ◽  
Vol 12 (1) ◽  
pp. 1 ◽  
Author(s):  
Rosmilah Misnan ◽  
Nurul Izzah Abdul Rahman ◽  
Zailatul Hani Mohd Yadzir ◽  
Noormalin Abdullah ◽  
Mohd Faizal Bakhtiar ◽  
...  

Crab meat is widely consumed in several countries around the world. However, when consumed, crab meats are frequent cause of allergic reactions throughout the world. Scylla serrata is among the most common mud crab in Malaysia. In a previous study two major allergens of mud crab at 36 and 41 kDa was identified. Thus, the aim of this study is to further identify these major allergens by a proteomic approach. Protein extract was prepared and resolved by 2-dimensional electrophoresis (2-DE). Immunoblotting was then performed using reactive sera from patients with crab allergy. Major allergenic spots were then excised from the 2-DE gel and analysed by mass spectrometry. The 2-DE profile of the extract revealed approximately >100 protein spots between pH of 4.00 to 8.00. Mass spectrometry analysis has identified the 36 and 41 kDa proteins as tropomyosin and arginine kinase, respectively. Our findings indicated that tropomyosin and arginine kinase play a major role in allergic reaction to mud crab meat among local patients with crab meat allergy, and should be included in diagnostics and therapeutic strategies of this allergy.


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