Current Enzyme Inhibition - Volume 14, Issue 2, 2018

Introduction: 3-(3-thioxo-3H-1,2-dithiol-5-yl)phenyl 4-[(1E)-3-oxo-3-phenylprop-1-en-1- yl]benzoate and their analogues were synthesized on the basis of Claisen-Schmidt condensation reaction wherein chalcone intermediates were synthesized by the reaction of substituted aldehydes and acetophenones. Final products were synthesized by reacting chalcone intermediates with 5-(4- hydroxyphenyl)-3H-1,2-dithiole-3-thione. Read More

Background: In this study, we investigate the inhibitory effects of phenolic and saponins extracts of Cupressus sempervirens cones and seeds. Objective: The ethyl acetate and butanolic extracts of Cupressus sempervirens (L) cones and seeds, collected from Laghouat (Algeria) were analyzed for their saponins and phenolic content. We also studied the in vitro antidiabetic activity of C. sempervirens using α-amylase di Read More

Background: There has been a great interest in the discovery of alternative medicines from medicinal herbs for type 2 diabetes, specifically screening for phytochemicals which are able to inhibit or delay glucose absorption. Introduction: The aim of this study was to evaluate the inhibition of crude extract and rosmarinic acid rich fractions from Orthosiphon stamineus on α-amylase and α-glucosidase activities. Methods: The Read More

Background: Inhibition of aromatase enzyme presents the key in Breast cancer treatment actually an important number of synthetics and natural inhibitors of this enzyme were studied. However, steroidal synthetic inhibitors were identified as the most efficient ones, indeed, the most commercialized treatment of breast cancer is steroidal. On the other hand, natural inhibitors have also provided good activities via the a Read More

Background: Obesity is an important risk factor for nonalcoholic fatty liver disease which varies from hepatic steatosis to liver cirrhosis. Interventions in weight and metabolic control are important in reducing steatosis risk. Aims: The aim of the present study was to investigate the role of celecoxib in hepatic triacylglycerol deposition in non-alcoholic fatty liver disease exploring the signaling involved in obese mice lip Read More

Introduction: Peptidoglycan, key constituent of bacterial cell wall, presents a novel target for broad spectrum antibiotics and extensive research is being conducted to synthesize inhibitors of its biosynthesis. A majority of bacteria need either lysine, or meso-DAP, as component of peptidoglycan. Background: Present compound has been designed as per structure activity relationship (SAR) of reported analogues and enzyme active Read More

Background: Based on the sequences of their catalytic domains, the astacins can be grouped into several major subfamilies such as digestive and hatching enzymes, meprin cluster and BMP1/ Tolloid like Proteases (BTP). Ethylene Diamine Tetra-Acetate (EDTA) was used to dock into the active site cleft of the astacins to know the interaction network and to identify the important residues for binding. Introduction: Comparative an Read More

Introduction: Pseudomonas aeruginosa is an opportunistic pathogen leading to severe, acute and chronic infections in burn patients. In the process of wound healing, a significant delay in the closure of excisional wound sites is due to the bacterial skin infection, so anti-infection is important in wound healing. Objective: Abuse of antibiotics leads to the development of multi drug resistance of P. aeruginosa strains which requires Read More

Background: It has been considered that Helicobacter pylori, a bacterium associated with a number of important upper gastrointestinal conditions cannot always effectively eradicated by the traditional approaches; however, there some alternative therapies have been presented. Honey has been used as a medicine since ancient times in many countries for its elevated antioxidant activity, as well as expressive antimicrobial a Read More

Background: Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive molecular target for the development of small-molecular inhibito Read More