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- Volume 18, Issue 3, 2022
Current Enzyme Inhibition - Volume 18, Issue 3, 2022
Volume 18, Issue 3, 2022
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In Vitro Investigation of Potential Pepsin Inhibitors: New Perspectives for the Treatment of Gastroesophageal Reflux
Authors: Luca Leoni, Valerio Damiani and Riccardo SalvioBackground: In patients with Gastroesophageal Reflux Desease (GERD), the digestive enzyme pepsin can reach the esophagus and extraesophageal sites and cause damage with inflammation and other tedious symptoms. Methods: In this work, a number of biocompatible, non-toxic, and hypoallergenic compounds were tested in vitro as pepsin inhibitors. The residual enzyme activity in the presence of the investi Read More
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Antioxidant Activity and Inhibitory Effect of Curcumin on Some Enzymes Involved in Several Diseases: Acetylcholinesterase, Butyrylcholinesterase, α-glucosidase and Tyrosinase
Authors: Seghira Bisset, Widad Sobhi, Chawki Bensouici and Abdelhalim khenchoucheAim: This study investigates the potential effect of pure curcumin on the inhibition of different enzymes involved in several diseases. Background: Several chronic diseases such as Alzheimer’s, diabetes, and Parkinson’s are related to oxidative stress and enzyme activity. Today, various plant origin products are beneficial against several chronic diseases with secondary metabolites such as phenolic compounds. Curcumin, a pol Read More
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Synthesis, Characterization and Evaluation of 5α, 6β-Dihalo Androsterone Derivatives as 5α-Reductase Inhibitors
Authors: Akansha Sharma, Priyanka Rana, Poonam Arora, Tanzeer Kaur and Neelima DhingraBackground and Objective: Testosterone under the influence of 5α-reductase enzyme gets converted to dihydrotestosterone and high levels are found to be causative for androgen dependent diseases like benign prostatic hyperplasia. Thus, 5α-reductase has been recognised as an important target for discovering new drugs against Benign Prostatic Hyperplasia and Prostate Cancer. Methods: In the present study, a series of 5α Read More
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Effects of p-Hydroxybenzaldehyde, Vanillin, and Syringaldehyde on Protein Tyrosine Phosphatase 1B Activity
Authors: Joy A. Peter, Ahmed Olatunde, Suleiman Aminu, Ismaila Alhaji Umar and Aminu MohammedBackground: The protein tyrosine phosphatases phosphatase 1B (PTP 1B) is a negative regulator of insulin signal transduction, and hence, serves as a therapeutic target in the treatment of diabetes. Objective: The present study investigated the inhibitory effects of p-hydroxybenzaldehyde, vanillin, and syringaldehyde on the activity of protein tyrosine phosphatases phosphatase 1B (PTP 1B) in vitro. Methods: The PTP 1B inhi Read More
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Antidiabetic Potential of Ruthenium(III) Hydroxamate Complexes: Spectrophotometric Investigations
Authors: Raj Kaushal and Mandeep KaurBackground: The potential antidiabetic and antioxidant properties of four ruthenium(III) hydroxamate complexes [RuCl(H2O)(LI-III)2] (1-3) and [RuCl3(H2O)(HLIV)2] (4) were investigated on α- cell enzymes (α-amylase and α-glucosidase). Methods: In the instance of α-amylase inhibition investigations, the antidiabetic studies of the complexes revealed that they are more active than even the Acarbose as standard, with c Read More
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In Silico Design, Synthesis and Evaluation of Hydroxyxanthone Derivatives as Potential Anti-diabetic Agents Targeting α-glucosidase
Authors: Riya Saikia, Aparoop Das, Kalyani Pathak, Neelutpal Gogoi, Tirna Paul, Jon J. Sahariah and Himangshu SarmaBackground: Glucosidase is a catalytic enzyme that catalyzes, specifically hydrolyses, the carbohydrates to free glucose units in blood in the last step of carbohydrate metabolism. So far, many compounds with α-glucosidase inhibitory activity, for example, acarbose, voglibose etc., have been accounted and commercialized for diabetes therapy. However, xanthones are recognized as efficient glucosidase inhibitors because of t Read More
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3D-QSAR, Molecular Docking and Pharmacokinetic Studies: In-Silico Approach to Search Novel Inhibitors of 5-Alpha Reductase for Treatment of Benign Prostatic Hyperplasia
Authors: Harnoor Kaur, Neelima Dhingra, Alka Kumari, Priyanka Rana and Tanzeer KaurAim: This study aims to identify novel steroidal 5-alpha reductase (5AR) inhibitors using computational approaches. Objectives: The objective of this study is to exploit the steroidal nuclei for possible modifications by creating a library of 17-oximino-5-androsten-3-carboxamide derivatives and identify potent 5AR inhibitors based on docking and pharmacokinetic parameters. Background: Benign prostatic hyperplasia (BPH) is a c Read More
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Volumes & issues
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Volume 20 (2024)
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Volume 19 (2023)
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Volume 18 (2022)
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Volume 17 (2021)
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Volume 16 (2020)
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Volume 15 (2019)
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Volume 14 (2018)
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Volume 13 (2017)
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Volume 12 (2016)
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Volume 11 (2015)
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Volume 10 (2014)
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Volume 9 (2013)
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Volume 8 (2012)
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Volume 7 (2011)
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Volume 6 (2010)
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Volume 5 (2009)
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Volume 4 (2008)
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Volume 3 (2007)
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Volume 2 (2006)
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Volume 1 (2005)
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