Current Enzyme Inhibition最新文献

{"title":"Evaluation of the Pharmacological Properties of Piscine Venoms from both Lionfish (Pterois) and Stonefish (Synanceja)","authors":"K. Ramalingam","doi":"10.2174/1573408016999201231204746","DOIUrl":"https://doi.org/10.2174/1573408016999201231204746","url":null,"abstract":"\u0000\u0000 For the past 70 years, the focus of research is on the search for poisons and toxins\u0000found in venomous and poisonous organisms, purely directed towards the pharmacological properties\u0000of the toxins. In the research of finding novel compounds in pharmaceutical research, the identified\u0000source was the piscine venom.\u0000\u0000\u0000\u0000The Scorpaenidae family was considered the most venomous of all. The toxins isolated from\u0000stonefish and lionfish are responsible for the effects caused in cardiovascular and neuromuscular systems\u0000and also for causing cytolytic activities. The main objective of the review is to study the mechanism of\u0000the stonefish venom and portray its benefits in the field of drug discovery.\u0000\u0000\u0000\u0000A study on the mechanism of stonefish venom was carried out by inducing cardiovascular endothelium.\u0000The release of neurotransmitter signals thus leads to the depolarisation of cell membrane by\u0000the formation of pores in the cell membrane in the neuromuscular system of rabbits, porcine artery, mice\u0000and rats. Lionfish venom in cross-reactivity with the results evolved from a stonefish venom activity. The\u0000presence of enzymatic hyaluronidases in the primary structures of lionfish has evolved from stonefish and\u0000their anticancer potential has also been demonstrated for the benefits of drug discovery as they possess\u0000biological and chemical activity.\u0000\u0000\u0000\u0000This review depicts an overview of the pharmacological activities of lionfish venom in comparison\u0000with the stonefish venom and their purpose of applications for future research in drug discovery.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41536230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Computational Study on Identification of Potential Elephantiasis Inhibitors Against UDP-Galactopyranose Mutase (UGM)","authors":"Sangavi Pandiyan, Langeswaran Kulanthaivel","doi":"10.2174/1573408016666200831171943","DOIUrl":"https://doi.org/10.2174/1573408016666200831171943","url":null,"abstract":"\u0000\u0000Lymphatic filariasis, regularly known as elephantiasis, is a dismissed tropical\u0000malady. A filarial parasite causes the disease when it is transmitted to humans through mosquitoes. The\u0000World Health Organization distinguished that this is one of the subsequent driving reasons for lasting\u0000and long haul inability. Inaccessibility of immunization and medication opposition of a large portion of\u0000the ebb and flow hostile to filarial drugs necessitate quest of novel medication that focuses on creating\u0000elective medications. UDP-galactopyranose mutase (UGM) is a flavoenzyme that catalyzes the change\u0000of UDP-galactopyranose mutase to UDP-galactofuranose, which is a focal response in galactofuranose\u0000biosynthesis. This UGM is fundamental for some pathogens however, it is missing in people, makes\u0000UGM a potential medication target.\u0000\u0000\u0000\u0000In the current investigation, UGM from the parasitic nematode Brugia malayi has been considered\u0000as an objective during in silico medicate planning of powerful filarial inhibitor.\u0000\u0000\u0000\u0000Here, we build up the homology model of UGM protein dependent on the gem structure of\u00004DSG. To break down the quality and unwavering quality of the created model, model approval was\u0000performed utilizing the SAVES server. Mixes from Specs, Enamine, and Maybridge databases were\u0000screened to recognize a potential ligand that could hinder the action of the UGM protein utilizing Glide\u0000HTVS and Glide XP.\u0000\u0000\u0000\u0000Because of the scoring boundaries, the best 6 hit mixes were chosen and exposed to ADME\u0000forecast utilizing QikProp module from Schrodinger. To check the security of docked buildings, an\u0000atomic element study was completed.\u0000\u0000\u0000\u0000The consequences of this examination give six novel lead mixes to building up an enemy\u0000of filarial medication focusing on the UGM protein.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43951506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of Achyranthes Aspera Linn. Leaves Extract on Reactive Oxygen Species (ROS) in Diabetes-induced Rats by Flow cytometry and Possible Molecular Mechanism through Molecular Docking","authors":"T. Deshpande, H. Une","doi":"10.2174/1573408016999201228193350","DOIUrl":"https://doi.org/10.2174/1573408016999201228193350","url":null,"abstract":"\u0000\u0000Oxidative stress is caused due to the overproduction of the reactive oxygen\u0000species (ROS) and the disturbance developed in the antioxidant potential of biochemical processes.\u0000ROS mostly form in the brain due to the high consumption of oxygen and the insufficiency of endogenous\u0000antioxidant resistance mechanisms. Cytochrome P450 2E1 has an excessive percentage of\u0000NADPH oxidase activity, which causes the production of ROS and increases oxidative stress.\u0000\u0000\u0000\u0000We have studied the effect of ethyl acetate extract of Achyranthes Aspera (EAAA) on ROS\u0000in the brain of diabetes-induced rats. We have also investigated the possible molecular mechanism of\u0000reduction in ROS through molecular docking.\u0000\u0000\u0000\u0000To study the oxidative stress induced by ROS in diabetic rats, we estimated the ROS in rat\u0000brain through flow cytometry. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to diabetesinduced\u0000rats. Results were articulated as mean ± standard deviation (SD). Data were analyzed using\u0000analysis of variance (ANOVA) followed by Bonferroni as a post hoc test. We performed molecular\u0000docking of flavonoids on CYP2E1 to study the inhibitory potential.\u0000\u0000\u0000\u0000The results have shown that EAAA reduces the generation of ROS in the diabetes-induced rat\u0000in a dose-dependent manner. The oral dose of EAAA 50mg/kg and 100 mg/kg was given to the rats\u0000and the ROS generation got affected accordingly. Luteolin, quercetin, and apigenin inhibited the\u0000CYP2E1 very effectively. Luteolin formed 4 hydrogen bonds with CYP2E1, which indicated its potential\u0000inhibition. Although, luteolin and apigenin showed a very good binding affinity with the enzyme.\u0000\u0000\u0000\u0000 From the present work, we have concluded that the ethyl acetate extract of achyrantesaspera\u0000can effectively inhibit the ROS generation in the diabetes-induced rats by inhibiting the activity\u0000of CYP2E1.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48263969","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Laurus nobilis Linn. Inhibits Polyol Pathway Enzymes: Strategy for Managing Diabetic Complications","authors":"H. Bankole, A. Fatai, Sulihat Motunrayo Aleshe, M. Kazeem, A. Kappo","doi":"10.2174/1573408017666210223124126","DOIUrl":"https://doi.org/10.2174/1573408017666210223124126","url":null,"abstract":"\u0000\u0000The rising incidence of diabetic complications necessitate the continuous search for safer, cheaper and effective pharmacological agents. Polyol pathway is an underlying process implicated in the pathogenesis of diabetic complications. Inhibition of enzymes in the polyol pathway is a veritable means of ameliorating diabetic complications.\u0000\u0000\u0000\u0000\u0000This study evaluated the inhibitory potential of some spicy plants on the activities of polyol pathway enzymes (aldose reductase and sorbitol dehydrogenase).\u0000\u0000\u0000\u0000\u0000Aqueous extracts of Laurus nobilis (bay), Cinnamomum zeylanicum (cinnamon), Murraya koenigii (curry), Thymus vulgaris (thyme) and Curcuma longa (turmeric) were incubated with appropriate enzymes and substrates, and percentages inhibition determined.\u0000\u0000\u0000\u0000\u0000 Results showed that bay extract had effective IC50 for inhibition of both aldose reductase (174.87 µg/mL) and sorbitol dehydrogenase (37.08 µg/mL). It also revealed that bay extract inhibited aldose reductase and sorbitol dehydrogenase in a non-competitive and competitive manner respectively.\u0000\u0000\u0000\u0000\u0000It is therefore concluded that bay extract effectively inhibited activities of polyol pathway enzymes, and may contribute to the amelioration of diabetic complications.\u0000\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43873306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"PDE3 Inhibition by Cilostazol Ameliorated Behavioral and Biochemical Deficits in Prenatal Alcohol Induced Experimental ADHD","authors":"Niti Sharma, B. Sharma, Neerupma Dhiman, L. Golani","doi":"10.2174/1573408017666210203202024","DOIUrl":"https://doi.org/10.2174/1573408017666210203202024","url":null,"abstract":"\u0000\u0000Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder with complex aetiology and phenotypes. Maternal consumption of alcohol is known to produce deleterious effects in the progeny, generating ADHD related phenotypes. Phosphodiesterase-3 (PDE3) has been shown to provide benefits in various brain conditions. \u0000\u0000\u0000\u0000To investigate the role of a selective PDE3 inhibitor, effects of cilostazol administration on core phenotypes of prenatal alcohol exposure (PAE) model of ADHD were assessed.\u0000\u0000\u0000\u0000PAE was established by exposing animals to 6/4 g.kg-1 (weekdays/weekends) ethyl alcohol from gestational day 8-20 and cilostazol (30/60 mg.kg-1 p.o.) was administered to the offspring (PND21-48) of females exposed to ethyl alcohol. To identify probable mechanisms involved, the effects on protein markers of neuronal function such as, neuronal survival-BDNF, neuronal transcription factor-pCREB, brain inflammation (IL-6, IL-10 and TNF-α) and brain oxidative stress (TBARS and GSH) were studied in frontal cortex, cerebellum, and striatum. Also, effects on behaviour such as hyperactivity, inattention and anxiety were assessed.\u0000\u0000\u0000\u0000PAE induced hyper-locomotion, inattention, and anxiety in tested animals. Administration of cilostazol to PAE group of animals resulted in amelioration of behavioural deficits. Also, cilostazol resulted in a significant increase in the levels of BDNF, pCREB, IL-10 and GSH along with significant decrease in TNF-α, IL-6 and TBARS in different brain areas of PAE group. \u0000\u0000\u0000\u0000Cilostazol, a selective PDE3 inhibitor rectified behavioural phenotypes associated with ADHD, possibly by altering protein markers associated with neuronal survival, neuronal transcription factor, brain inflammation, and brain oxidative stress.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41510481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, In-Silico Potential Enzymatic target predictions, Pharmacokinetics, Toxicity, Anti-Microbial and Anti-Inflammatory Studies of Bis-(2-methylindolyl) methane Derivatives","authors":"Dnyaneshwar T. Nagre, Suraj N. Mali, B. Thorat, S. A. Thorat, A. Chopade, M. Farooqui, B. Agrawal","doi":"10.2174/1573408017666210203203735","DOIUrl":"https://doi.org/10.2174/1573408017666210203203735","url":null,"abstract":"\u0000\u0000The bis(indolyl)methanes (BIMs) scaffold is being reported for wide varieties of pharmacological profiles including anti-bacterial, anti-proliferative, anti-cancer, cytotoxic, insecticidal, analgesic, antioxidant, and anti-inflammatory agents.\u0000\u0000\u0000\u0000A series of bis(indolyl)methanes have been synthesized using greener and new approach using the reaction of different substituted aldehydes and indole in presence of easily available and biodegradable base such as piperidine in acetic acid at room temperature and characterized with ultraviolet–visible spectrophotometry (UV–Vis or UV/Vis),Fourier-transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy(NMR),etc. The antibacterial and antifungal activities were also carried out against Staphylococcus aureus (RCMB 000106) and Bacillis subtilis (RCMB 000107), as two Gram positive bacterial strains and Salmonella typhi and Escherichia coli (RCMB 000103), as two Gram negative bacterial strains. Fungal Species such as Candida Albicans, Penicillium chrysogenum, Aspergillus niger were also used for in-vitro antifungal evaluation. All our newly synthesized 14 compounds (4a-4n) were subjected for anti-inflammatory activity in-vitro and compared with known standard drug Aceclofenac. \u0000\u0000\u0000\u0000Our newly synthesized compounds showed good to moderate antibacterial agents, in-silico ADMET and anti-inflammatory profiles. We hope that our current study would aid future developments of bis(indolyl)methanes as antibacterial and anti-inflammatory agents.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47054089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A review on pancreatic lipase inhibitors from natural sources: a potential target for obesity","authors":"B. T., M. R, Suriyaprakash Tnk, S. N.","doi":"10.2174/1573408017666210121114441","DOIUrl":"https://doi.org/10.2174/1573408017666210121114441","url":null,"abstract":"\u0000\u0000 Obesity is a worldwide lifestyle disorder and its incidence is growing at an alarming rate. Pancreatic lipase (PL) plays a key role in lipid metabolism and hence a potential target for obesity treatment. There have been reports that many bioactive compounds from natural sources are vast pool of PL inhibitors. \u0000\u0000\u0000\u0000 In search of natural pancreatic lipase inhibitors, the review summarizes the potential of natural products for their pancreatic lipase inhibitory activity.\u0000\u0000\u0000\u0000\u0000 In this review the data obtained from literature search across various electronic databases and journal article publications are reviewed.\u0000\u0000\u0000\u0000\u0000 The pancreatic lipase inhibitory activities of 61 biological sources were reviewed in this paper is backed by preclinical experimental evidence, either in vivo or in vitro.\u0000\u0000\u0000\u0000\u0000 This article can be used as a ready to use reference for therapeutic lead molecules from plants, marine and insect derived natural products with PL inhibitory activity. The research is more focused on the discovery of more ingenious pancreatic lipase inhibitors with lesser consequences.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46051343","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Molecular Docking Demonstration of the Liquorice Chemical Molecules on the Protease and ACE2 of COVID-19 Virus.","authors":"I. Koyuncu, M. Durgun, Nuri Yorulmaz, Ş. Toprak, Ataman Gonel, N. Bayraktar, Murat Çağlayan","doi":"10.2174/1573408016999201228193118","DOIUrl":"https://doi.org/10.2174/1573408016999201228193118","url":null,"abstract":"\u0000\u0000COVID-19 has spread rapidly in many countries of the world and poses a serious threat to global\u0000public health, yet no specific drug has been identified or currently available for its treatment. Since it may take years to\u0000design a drug for treatment, the shortest and most effective way now is to screen the available drugs or active substances by\u0000molecular docking methods.\u0000\u0000\u0000\u0000The aim of this study is to investigate the potential for use in COVID-19 treatment by investigating the inhibitory\u0000effects of Glycyrrhiza glabra main active ingredients on COVID-19 main protease (SARS-CoV-2,), SARS-CoV-2 - ACE2\u0000Complex and ACE-2 by molecular docking method, which are known to have antiviral effects on SARS-CoV.\u0000\u0000\u0000\u0000Molecular docking was performed by use of Autodock 4.2 to analyse the probability of docking.\u0000Several compounds that extracted from the root of the licorice plant (glycyrrhizic acid, glabridin, 6-azauridine, pyrazofurin\u0000and mycophenolic acid) was docked COVID-19 Mpro and docking results were analysed by Autodock 4.2 and Biovia\u0000Discovery Studio Visualizer 2020. The evaluation was based on the docking score (binding energies) calculated by\u0000Autodock 4.2. Nelfinavir was used as standards for comparison.\u0000\u0000\u0000\u0000As a result of the study, the compounds of Glabridin in COVID-19 main protease (6LU7), ACE-2 (1R4L) and\u0000SARS-CoV-2, - ACE2 Complex (6LZG) have very low binding energy (-8.75 to -7.64) and low potential to inhibition\u0000constant has been found to have.\u0000\u0000\u0000\u0000These results suggests that Glabridin appeared to have the best potential to act as a COVID-19 Mpro inhibitors.\u0000However, further research is necessary to investigate their potential medicinal use.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44240982","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Perspective on Acetylcholinesterase: A Potential Target for Alzheimer’s Disease Intervention","authors":"Rajesh Basnet, Sandhya Khadka, B. B. Basnet, Radheshyam Gupta","doi":"10.2174/1573408016999200801021329","DOIUrl":"https://doi.org/10.2174/1573408016999200801021329","url":null,"abstract":"\u0000\u0000Alzheimer's disease (AD) is an unexplained progressive degenerative brain\u0000disease; it accounts for 60-70% of dementia cases worldwide, has an estimated global incidence of\u000024.3 million, and is associated with deterioration of the central nervous system. Acetylcholinesterase\u0000(AChE) is an enzyme that catalyzes the breakdown of acetylcholine to acetate and choline. It is also\u0000the potential target of most of the clinically used drugs for the treatment of AD. The degeneration of\u0000cholinergic neurons and the loss of neural transmission are the main reasons for the decline of cognitive\u0000ability in AD patients.\u0000\u0000\u0000\u0000 In recent years, the development of targeted drugs in AD has made significant achievements.\u0000The global impact of AD continues to grow, and as a result, the focus of disease-modifying\u0000therapies remains elusive. The role of treatment is not limited to pharmacology but involves many\u0000factors, such as the psychological, social, and economic aspects of the patient and family. AChE is an\u0000important target in AD to consider the use of AChE inhibitors in patients with mild to moderate AD,\u0000even though the costs are high and no other direct progress has been made. Although there are many\u0000AChE inhibitors, there is no selective potent inhibitor for AChE. There is still a need to address human\u0000AChE structure, provide key insights into key protein-ligand interactions, and provide the basis\u0000for molecular modeling and structure-based drug design.\u0000\u0000\u0000\u0000In this review, we briefly introduce the clinical characteristics of AD, the development\u0000of crystal structure, and the latest research on AD. In recent years, the development of different strategies\u0000for amyloid-β, BACE1, and type-1 interferon receptor alpha-1 has attracted great attention.\u0000There is an urgent need to further characterize available instrumental compounds to explore the use\u0000of new selectivity and key protein-ligand interactions in AD. In the past few decades, great progress\u0000has been made in the treatment of AD, but AD is still one of the world's problems, and the inability\u0000to cure AD, indicates that there is an urgent need for new treatments.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46704137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Carbon Nanotubes Inhibit the Pepsin Activity at High Ionic Strength","authors":"K. M. Jasem, H. Al-Hakeim, Jawad Kadhem Al-Shams","doi":"10.2174/1573408016999200603170618","DOIUrl":"https://doi.org/10.2174/1573408016999200603170618","url":null,"abstract":"\u0000\u0000Gastroesophageal reflux disease (GERD) is a common chronic gastrointestinal\u0000disorder in adults that occurs as the stomach contents reflux and come up into the esophagus\u0000due to a dysfunction in the lower oesophageal sphincter. One approach commonly used to treat\u0000GERD is inhibition of the activity of pepsin enzyme. Carbon nanotubes (CNTs) are nanoparticles of\u0000carbon atoms that possess numerous interesting physical and chemical properties. CTNs functionalization\u0000expands the range of their properties to make them soluble in biological fluids and to confer\u0000the property of carrying drug or biological macromolecules which increase the scope of their applications\u0000in biomedical science.\u0000\u0000\u0000\u0000This study aims to utilize CNTs as a pepsin inhibitor and as a new medication for the\u0000treatment of GERD.\u0000\u0000\u0000\u0000The pepsin activity before and after the addition of an exact amount of the CNTs to the reaction\u0000mixture was measured colorimetrically.\u0000\u0000\u0000\u0000The results showed that both Vmax and Km changed after the addition of CNTs to the pepsin\u0000solution indicating a mixed inhibition of pepsin activity. This finding pointed to the ability of\u0000CNTs to bind with the pepsin molecule and pepsin-protein complex, therefore inhibiting the enzyme\u0000activity.\u0000\u0000\u0000\u0000The findings also demonstrated a complete inhibition of pepsin activity by CNTs when\u0000increasing the ionic strength of the reaction mixture. It can be inferred that using CNTs at a high concentration\u0000of NaCl at 37°C is the optimal condition for pepsin inhibition.\u0000","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-11-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45487741","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}