Urease Inhibitory Kinetic Studies of Various Extracts and Pure Compounds from Cinnamomum Genus.

Manoj Kumar,Sunita Dalal,Monika Bhardwaj,Neha Sikri,Poonam Yadav,Sudhir Kumar Kataria,Pooja Kadyan,Divya Vashishth,Sulekha Chahal,Bhavna Sharma,Jitender Sharma

doi:10.3390/molecules26133803

Manoj Kumar, Sunita Dalal + Show 9 more

Open Access

https://doi.org/10.3390/molecules26133803

Copy DOI

Abstract

Urease is an enzyme that plays a significant role in the hydrolysis of urea into carbonic acid and ammonia via the carbamic acid formation. The resultant increase in pH leads to the onset of various pathologies such as gastric cancer, urolithiasis, hepatic coma, hepatic encephalopathy, duodenal ulcers and peptic ulcers. Urease inhibitors can reduce the urea hydrolysis rate and development of various diseases. The Cinnamomum genus is used in a large number of traditional medicines. It is well established that stem bark of Cinnamomum cassia exhibits antiulcerogenic potential. The present study evaluated the inhibitory effect of seven extracts of Cinnamomum camphora, Cinnamomum verum and two pure compounds Camphene and Cuminaldehyde on urease enzyme. Kinetic studies of potential inhibitors were carried out. Methanol extract (IC50 980 µg/mL) of C. camphora and a monoterpene Camphene (IC50 0.147 µg/mL) possess significant inhibitory activity. The Lineweaver Burk plot analysis suggested the competitive inhibition by methanol extract, hexane fraction and Camphene. The Gas Chromatography-Mass Spectroscopy (GC–MS) analysis of hexane fraction revealed the contribution of various terpenes. The present study targets terpenes as a new class of inhibitors that have potential therapeutic value for further development as novel drugs.

Highlights

Enzyme inhibition studies are a significant area of research in pharmaceutical studies, as they result in the discovery of drugs for the treatment of various physiological conditions
The enhanced activity of urease leads to various conditions such as pathological changes in humans infected with Helicobacter pylori, Proteus mirabilis, Ureoplasma urealyticum, Klebsiella pneumonia, Staphylococcus and Salmonella species
H. pylori infection leads to gastric inflammation, duodenal and gastric ulcers, gastric adenocarcinoma and gastric lymphoma

Summary

Introduction

Enzyme inhibition studies are a significant area of research in pharmaceutical studies, as they result in the discovery of drugs for the treatment of various physiological conditions. The enhanced activity of urease leads to various conditions such as pathological changes in humans infected with Helicobacter pylori, Proteus mirabilis, Ureoplasma urealyticum, Klebsiella pneumonia, Staphylococcus and Salmonella species. H. pylori prevails in 50% of the global population, with or without disease symptoms. The urease enzyme in cytoplasm and/or on the surface of H. pylori is a major virulence factor and is implicated for its high prevalence in the human population [3]. The ureolytic activity of P. mirabilis, U. urealyticum, K. pneumoniae, Staphylococcus and Salmonella species is a major virulence prevalence in the human population [3]. The ureolytic activity of P. mirabilis, U. urealyticum, K. pneumoniae, Staphylococcus and Salmonella species is a major virulence factor responsible in the pathogenesis of many oth eofr1c0linical conditions such as hepatic coma, pyelonephritis and urinary stones [4,5]

Methods

Results

Conclusion