Abstract
Urease has attracted much attention, as it is directly involved in the formation of infection stones and contributes to the pathogenesis of urolithiasis, pyelonephritis, ammonia and hepatic encephalopathy, hepatic coma and urinary catheter encrustation. Moreover, urease is the major cause of pathologies induced by H. pylori, such as gastritis and peptic ulcer. In the present work, the new natural compound, 3-methoxydalbergione, was isolated from Viola betonicifolia. A mechanistic study of this compound as a natural urease inhibitor was performed by using enzyme kinetics and docking studies. 3-Methoxydalbergione could be considered as a lead molecule for drugs useful in the urease associated diseases.
Highlights
Viola betonicifolia Sm. (Violaceace) is a perennial herb of about 8–20 cm in height, with triangular leaves and a petiole longer than the lamina
Compound 1 was isolated as a yellow spongy mass from combined chloroform and ethyl acetate fractions of a methanolic extract of Viola betonicifolia
The compound showed urease inhibitor activity, being a competitive inhibitor. 3-Methoxydalbergione can be considered as a template drug for urease associated diseases
Summary
Viola betonicifolia Sm. (Violaceace) is a perennial herb of about 8–20 cm in height, with triangular leaves and a petiole longer than the lamina. Urease (EC 3.3.1.5) hydrolyzes urea into ammonia and carbamate. The main nitrogenous waste product of biological system urea is quickly metabolized by the action of urease present in microorganisms. The urease enzymes are present in a number of fungi, bacteria and plants. Ureases play a vital role in the nitrogen cycle, as they supply nitrogen for the growth of microorganisms by catalyzing urea degradation [11]. The high activity of ureolytic bacteria increases the amount of ammonia in the soil via fast urea degradation. During the seed germination process, urease plays a vital role in the metabolism of nitrogen, helping many soil microorganisms to obtain nitrogen for their growth [12,13]. Viola betonicifolia and studied its possible urease inhibitory activity. Kinetic and molecular modeling studies were performed to understand the mode of action of this compound
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