Şükrü Beydemir

• PhD
• Professor at Anadolu University

The phenolic composition, antioxidant capacity, and enzyme inhibition activities of Mangifera indica L. leaf (MLs) ethanol extract were comprehensively evaluated to explore its therapeutic and industrial applications. Quantitative profiling of 21 phenolic compounds was performed using the LC–MS/MS method, with vanillic acid (1242.47 μg/L), gallic a...

Algae have become the center of attention due to their strong antioxidants and enzyme-inhibitory activities. In this study, green algae (Enteromorpha linza) extracts obtained using acetone, hexane and methanol were investigated. In the study, antioxidant properties, anti-acetylcholinesterase (AChE) potential, ADME estimations and molecular docking...

Introduction Laurus nobilis (LN), has traditional medicinal uses, and this study investigates its therapeutic potential by focusing on its phenolic content and bioactivities such as antioxidant, antidiabetic, and anticholinergic properties. Phenolic compounds play key roles in reducing oxidative stress and modulating enzymatic activities, relevant...

In this study, hydrazine clubbed thiazole derivatives ( 3a – 3j ) were obtained by Hantzsch thiazole synthesis and characterized by MS, ¹ H NMR, and ¹³ C NMR. The inhibitory potentials of the derivatives against diabetes‐related enzymes such as aldose reductase (AR), α‐glycosidase (α‐GLY), and α‐amylase (α‐AMY) were experimentally determined, and t...

Sulfonate derivatives are an essential class of compounds with diverse pharmacological applications. This study presents the synthesis and detailed characterization of six novel Schiff base sulfonate derivatives ( L ¹ –L ⁶ ) through spectroscopic techniques (FT‐IR and NMR). Their inhibitory potential was evaluated against human carbonic anhydrase i...

Inhibition ofaldose reductase (AR), α-glycosidase (α-GLY), and α-amylase (α-AMY) are some of the essential targets in diabetes mellitus (DM). Here, a series of imidazo[1,2-a]pyridine-based 1,3,4-thiadiazole derivatives (8a–k) were successfully synthesized and characterized using ¹H NMR, ¹³C NMR, and HRMS spectroscopic techniques. The inhibition eff...

Inhibition of the cholinesterases (AChE and BChE) plays a pivotal role in the symptomatic treatment of Alzheimer’s disease. The present study reports the synthesis and anticholinesterase activity of five novel thiadiazole analogs in search of anti-Alzheimer agents. The structures of the newly synthesized compounds were characterized using 1H NMR, 1...

The identification of novel acetylcholinesterase inhibitors holds significant relevance in the treatment of Alzheimer's disease (AD), the prevailing form of dementia. The exploration of alternative inhibitors to the conventional acetylcholinesterase inhibitors is steadily gaining prominence. Quinones, categorized as plant metabolites, represent a s...

Doxorubicin (DOX) is widely used in cancer treatment but the dose‐related toxicity of DOX on organs including the liver limit its use. Therefore, there is great interest in combining DOX with natural compounds with antioxidant properties to reduce toxicity and increase drug efficacy. Esculetin is a natural coumarin derivative with biological proper...

Various carbonic anhydrase (CA) enzyme isoforms are known today. In addition to the use of CA inhibitors as diuretics, antiepileptics and antiglaucoma agents, the inhibition of other specific isoforms of CA was reported to have clinical benefits in cancers. In this study, two groups of 1,3,4-thiadiazole derivatives were designed and synthesized to...

Investigating innovative frameworks for addressing Alzheimer's disease is a challenging goal. In this specific scenario, a selection of asymmetric biscarbothioamide derivatives (3a–l) with different substitutions has been carefully formulated and successfully synthesized.

The present study focused on the synthesis and characterization of novel pyrazole carboxamide derivatives (SA1‐12). The inhibitory effect of the compounds on cholinesterases (ChEs; AChE and BChE) and carbonic anhydrases (hCAs; hCA I and hCA II) isoenzymes were screened as in vitro. These series compounds have been identified as potential inhibitors...

This study presents the first findings regarding extraction, isolation, enzyme inhibition, and antioxidant activity. The oral mucosal wound‐healing process was investigated using propolis water extract (PWE) incubation with gingival fibroblast cells and concluded that propolis was effective on the oral mucosal wound‐healing pattern compared to untr...

In this study, the mechanisms by which the enzymes glucose‐6‐phosphate dehydrogenase (G6PD), 6‐phosphogluconate dehydrogenase (6PGD), glutathione reductase (GR), glutathione‐S‐transferase (GST), and thioredoxin reductase (TrxR) are inhibited by methotrexate (MTX) were investigated, as well as whether the antioxidant morin can mitigate or prevent th...

It is known that oxidative stress originating from reactive oxygen species plays a role in the pathogenesis of Alzheimer's disease. In this study, the role of antioxidant status associated with oxidative stress in Alzheimer's disease was investigated. Peripheral blood samples were obtained from 28 healthy individuals (as control) and 28 Alzheimer's...

Eleven new thiosemicarbazone derivatives (1‐11) were designed from nine different biologically and pharmacologically important isothiocyanate derivatives containing functional groups such as fluorine, chlorine, methoxy, methyl, and nitro at various positions of the phenyl ring, in addition to the benzyl unit in the molecular skeletal structure. Fir...

In this study, a library of twelve beta-lactam-substituted benzenesulfonamides (5a-l) was synthesized using the tail-approach method. The compounds were characterized using IR, 1H NMR, 13C NMR and elemental analysis techniques. These newly synthesized compounds were tested for their ability to inhibit the activity of two carbonic anhydrases (hCA) i...

Sulfonamide compounds known as human carbonic anhydrase (hCA) inhibitors are used in the treatment of many diseases such as epilepsy, antibacterial glaucoma, various diseases. 1,3-diaryl-substituted triazenes are used for therapeutic purposes in many drug structures. Based on these two groups, the synthesis of new compounds is important. In the pre...

Sulfonamide compounds known as human carbonic anhydrase ( h CA) inhibitors are used in the treatment of many diseases such as epilepsy, antibacterial glaucoma, various diseases. 1,3-diaryl-substituted triazenes and sulfaguanidine are used for therapeutic purposes in many drug structures. Based on these two groups, the synthesis of new compounds is...

Sulfonamides are among the most promising potential inhibitors for carbonic anhydrases (CAs), which are pharmaceutically relevant targets for treating several disease conditions. Herein, a series of benzenesulfonamides bearing 1,2,3-triazole moiety as inhibitors of human (h) α-CAs (hCAs) were designed using the tail approach. The design method comb...

Aldose reductase (AR, ALR2; EC 1.1.1.21), an enzyme that converts glucose to fructose on the polyol pathway, is an important member of the Aldo‐keto reductase superfamily. ALR2 is part of the rate‐limiting step, which is associated with diabetic complications in this process, and plays a role in regulating reactive oxygen species induced by growth...

In the search for small-molecule aldose reductase (AR) inhibitors, new tetrazole-hydrazone hybrids (1-15) were designed. An efficient procedure was employed for the synthesis of compounds 1-15. All hydrazones were subjected to an in vitro assay to assess their AR inhibitory profiles. Compounds 1-15 caused AR inhibition with Ki values ranging betwee...

Aldose reductase (AR) is a crucial enzyme of the polyol pathway through which glucose is metabolized under conditions of hyperglycemia related to diabetes. A series of novel acetic acid derivatives containing quinazolin-4(3H)-one ring (1-22) was synthesized and tested for in vitro AR inhibitory effect. All the target compounds exhibited nanomolar a...

Carbonic Anhydrases (CAs) are an important family of metalloenzymes that contain zinc (Zn²⁺) ions in their active site and catalyze the conversion of carbon dioxide to bicarbonate and proton and found in all living organisms. Sulfonamides are well-known inhibitors of CAs isoenzymes. In this study, a series of benzenesulfonamide derivatives (9a–h) c...

Polyol pathway enzymes, aldose reductase (EC 1.1.1.21; AR, ALR2), and sorbitol dehydrogenase (EC 1.1.1.14; SDH, SORD) have been widely investigated as the enzymes crucially involved in the pathogenesis of several chronic complications, including nephropathy, neuropathy, retinopathy, and cataracts associated with diabetes mellitus. Although phenolic...

Cancer is a serious problem affecting the health of all human societies. Chemotherapy refers to the use of drugs to kill cancer or the origin of cancer. In the past three decades, researchers have studied about proteins and their roles in the production of cancer cells. Glutathione S‐transferases (GSTs) are a superfamily of enzymes that play a key...

New Schiff base‐bearing thiosemicarbazones (1–13) were obtained from 4‐hydroxy‐3,5‐dimethoxy benzaldehyde and various isocyanates. The structures of the synthesized molecules were elucidated in detail. Density functional theory calculations were also performed to determine the spectroscopic properties of the compounds. Moreover, the enzyme inhibiti...

Aldose reductase (AR) and sorbitol dehydrogenase (SDH) are important enzymes of the polyol pathway. In the current study, inhibitory effects of vulpinic acid (VA) carnosic acid (CA) and usnic acid (UA) on purified AR and SDH enzymes were determined. These enzymes inhibition could be essential to prevent diabetic complications. AR and SDH enzymes we...

A novel series of 1,2,3-triazole benzenesulfonamide substituted 1,3-dioxoisoindolin-5-carboxylate (7a-l) inhibitors of human α-carbonic anhydrase (hCA) was designed using a tail approach. The design method relies on the hybridization of a benzenesulfonamide moiety with a tail of 1,3-dioxoisoindoline-5-carboxylate and a zinc-binding group on a 1,2,3...

To discover alternative substances to compounds used to treat many diseases, especially treating Alzheimer’s disease (AD) and Parkinson’s disease targeting carbonic anhydrase (hCA) and acetylcholinesterase (AChE) enzymes, is important. For this purpose, a series of novel bis-ureido-substituted sulfaguanidine (SG1–4) and sulfisoxazole (SO1–4) deriva...

Aldose reductase (AR, AKR1B1; EC 1.1.1.21) is an Aldo‐keto reductase that has been widely investigated as an enzyme crucially involved in the pathogenesis of several chronic complications, including nephropathy, neuropathy, retinopathy, and cataracts associated with diabetes mellitus. Although sulfonamides have been reported to possess many other b...

Introduction: Presenilin 1 (PSEN1), catalase (CAT), glutathione-S-transferase (GST) and paraoxonase 1 (PON1) play a vital role in prediction, diagnosis and therapy of metabolic disorders. Methods: Metabolic enzyme activities and lipid peroxidation in serum of cerebrovascular diseases (CVD) and coronary artery diseases were measured by spectropho...

Serum paraoxonase 1 (PON1) is found in all mammalian species and is a calcium-dependent hydrolytic enzyme. PON1 hydrolyze several substrates, including carbonates, esters, and organophosphates. In the current study, we aimed to investigate the effect of the presynthesized benzohydrazide derivatives (1-9) on PON1 activity. Benzohydrazide compounds m...

The effects of some antibiotics and metals on goat (Capra aegagrus hircus) kidney aldose reductase (AR) and sorbitol dehydrogenase (SDH) activities were examined. For drugs and metals that exhibit inhibitory effect, Ki constants were calculated and inhibition types were determined by using Lineweaver-Burk curves. In our study, the highest inhibitio...

Paraoxonase 1 (PON1) can metabolize some compounds such as aromatic carboxylic acid and unsaturated aliphatic esters, arylesters, cyclic carbonate, plucuronide drugs, some carbamate insecticide classes, nerve gases, and lactone compounds. Methyl benzoate has recently been shown to display potent toxicity against several insect species. In the curre...

Carbonic anhydrase (CA) enzymes are involved in many physiological events. These enzymes, which contain Zn2+ in their structure, can be easily inhibited by dithiocarbamate compounds. In addition, CA enzyme inhibitory activities are known in groups such as sulfonamide and methylsulfonyl. For this purpose, in this study, a series of 23 new dithiocarb...

Human carbonic anhydrase VII (hCA VII), a cytosolic enzyme, defends against oxidative stress by preventing reactive oxygen species from forming. In our study, firstly, hCA VII was cloned into E.coli (One Shot® Mach1™‐T1R) strain by using cDNA of the human brain and successfully expressed. The integrity of the plasmid generated by colony PCR was che...

The acetylcholinesterase and carbonic anhydrase inhibitors (AChEIs and hCAIs) remain key therapeutic agents for many bioactivities such as anti-Alzheimer and antiobesity antiepileptic, anticancer, antiinfective, antiglaucoma, and diuretic effects. Here, it has been attempted to discover novel multi-target AChEIs and hCAIs that are highly potent, or...

Carbonic anhydrases (CAs, EC 4.2.1.1) convert carbon dioxide to bicarbonate in metabolism and use Zn2+ ions as a cofactor for their catalytic activity. The activators or inhibitors of CA-I and CA-II, which are the most abundant CA isozymes in erythrocytes, have pharmacological applications in medicine. So, investigation of drug-protein interaction...

Biological evaluation of New Schiff Base-Ligand Complexes

Glutathione S‐transferases (EC 2.5.1.18, GSTs), consisting of at least seven subfamilies, such as alpha, kappa, mu, pi, theta, zeta, and omega, are the family of cytosolic proteins with many known functions and also are abundant in cells. Moreover, they play significant roles in influencing the efficacy and bioavailability of pharmaceutical agents...

Aldose reductase (ALR2), one of the metabolically important enzymes, catalyzes the formation of sorbitol from glucose in the polyol pathway. ALR2 inhibition is required to prevent diabetic complications. In the present study, the novel bis-hydrazone compounds bearing isovanillin moiety (GY1-12) were synthesized, and various chromatographic methods...

Recently, as a drug target in cancer treatment, the superfamily of glutathione S‐transferase (GSTs, EC 2.5.1.18) have been invited considerable interest by scientists. In particular, as they are overexpressed in many human cancer cell lines, GSTs can catalyze the conjugation of the cellular nucleophile glutathione (GSH) with a wide range of electro...

Increased activity of aldose reductase (AR) and sorbitol dehydrogenase (SDH) are the major causes of diabetic complications. Thus, inhibition of these two enzymes is vital in preventing diabetic complications. As the synthesis of new and effective AR and SDH enzyme inhibitors is quite difficult, we have investigated the inhibition effects of antibi...

A series of novel sulfonates containing quinazolin-4(3H)-one ring derivatives was designed to inhibit aldose reductase (ALR2, EC 1.1.1.21). Novel quinazolinone derivatives (1–21) were synthesized from the reaction of sulfonated aldehydes with 3-amino-2-alkylquinazolin-4(3H)-ones in glacial acetic acid with good yields (85%–94%). The structures of t...

New hybrid thiazolyl–pyrazoline derivatives (4a–k) were obtained through a facile and versatile synthetic procedure, and their inhibitory effects on the human carbonic anhydrase (hCA) isoforms I and II as well as on acetylcholinesterase (AChE) were determined. All new thiazolyl–pyrazolines showed activity at nanomolar levels as hCA I, hCA II, and A...

Schiff bases display superior features for many areas, such as significant intermediates in industrial biological, pharmacological, catalytic and optical properties, organic synthesis, and coordination chemistry. The pre‐synthesized two Schiff base ligands (HL¹ and HL²) and their bidentate metal complexes (Co(L¹)2, Cu(L¹)2, Ni(L¹)2, Co(L²)2, Cu(L²)...

Aldose reductase (AR) acts as a multi-disease target for the design and development of therapeutic agents for the management of diabetic complications as well as non-diabetic diseases. In the search for potent AR inhibitors, the microwave-assisted synthesis of twenty new compounds with a 1,3-diaryl-5-(4-fluorophenyl)-2-pyrazoline moiety as a common...

Imidazole and thiadiazole derivatives display an extensive application in pharmaceutical chemistry, and they have been investigated as bioactive molecules for medicinal chemistry purposes. Classical carbonic anhydrase (CA) inhibitors are based on sulfonamide groups, but inhibiting all CA isoforms nonspecifically, thereby causing undesired side effe...

The underlying cause of many metabolic diseases is abnormal changes in enzyme activity in metabolism. Inhibition of metabolic enzymes such as cholinesterases (ChEs; acetylcholinesterase, AChE and butyrylcholinesterase, BChE) and α-glucosidase (α-GLY) is one of the accepted approaches in the treatment of Alzheimer’s disease (AD) and diabetes mellitu...

5-(2-Hydroxy-3-methylbenzylidene)thiazolidine-2,4-dione (3) was identified as the most potent AR inhibitor in this series, exerting uncompetitive inhibition with a K i value of 0.445 ± 0.013 µM.

A series of six N ‐carbamimidoyl‐4‐(3‐substitutedphenylureido) benzenesulfonamide derivatives ( 2a‐f ) were synthesized by reaction of sulfaguanidine with aromatic isocyanates. In vitro and in silico inhibitory effects of the novel ureido‐substituted sulfaguanidine derivatives ( 2a‐f ) were investigated by spectrophotometric methods for α‐glycosida...

The aim of this study was to determine the in vitro inhibitory effects of some metal ions (silver ion (Ag+), cadmium ion (Cd2+), cobalt ion (Co2+), copper ion (Cu2+), nickel ion (Ni2+), lead ion (Pb2+) and zinc ion (Zn2+)) on glutathione reductase (GR) enzyme activities that purified from the gill, kidney and liver tissues of Capoeta umbla. For thi...

In this study, the in vitro effects of some metal ions (Ag+, Cd2+, Cu2+, Fe2+, Ni2+ and Pb2+) on freshwater fish Capoeta umbla liver and gill glucose 6-phosphate dehydrogenase (G6PD) have been investigated. For this purpose, C. umbla liver and gill G6PD enzymes were purified, with a specific activity of 31.52 and 22.83 EU/mg protein, 3353.2 and 736...

Alzheimer's disease (AD) is a neurodegenerative disorder characterized by dementia, memory impairment, cognitive dysfunction, and speech impairment. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well documented so far. Recently, studies have also evidenced that human carbonic anhydrases (h...

It is known that free radicals, their products and reactive oxygen species (ROS) are associated with many diseases. The study focuses on both some changes in oxidative stress factors in patients with acute appendicitis (AA) and the changes of GST and PON1 enzyme activities in the metabolism. This study involved control group (n = 31) and the study...

Aldose reductase (AR) is a key enzyme, which triggers the excessive accumulation of sorbitol in insulin independent tissues leading to severe diabetes-induced microvascular complications. Substantial evidence has proven that AR inhibition is a well-established strategy to attenuate these complications. In the current work, new 2-[(4-amino-5-aryl-4H...

The amine-bis(phenolate) ligands was prepared through a Mannich reaction utilizing two equivalents of 2,4-di-tert-butylphenol or 4-tert-butylphenol, two equivalents of formaldehyde and a single equivalent of 2-aminoethyl diphenylborinate as primary amine. This work deals with the synthesis and evaluation of new (B←N) and (B-O) units containing amin...

In the present study, the phytase enzyme was purified from Lactobacillus plantarum with a 3.08% recovery, 9.57-purification fold, and with a specific activity of 278.82 EU/mg protein. Then, the effects of the 5 EU and 10 EU purified phytase was determined on the plant growth, quality, the macro-micro nutrient content of pansy (Viola x wittrockiana)...

Alzheimer's disease (AD) is a complex, predominant, and progressive form of dementia. The treatment of AD alters depending on the cognitive and behavioral symptoms. The utility of cholinergic replacement by acetylcholinesterase (AChE) inhibitors in AD treatment has been well-documented so far. Recent studies have also demonstrated that human carbon...

Carbonic anhydrases are vital class of enzymes that participate in so many essential physiological events in the organism and associated with many diseases. Inhibitors of carbonic anhydrase enzymes are used in pharmacological applications in many areas such as antiobesity, antiglaucoma, anticancer agents and anticonvulsants. So, this study focuses...

Many drugs, which are used in clinical treatments, show pharmacological effects on enzyme activity with an essential role in the pathogenesis of various diseases. Paraoxonase-I (PON1) is a member of the mammalian lactonase enzyme family, serves to the prevention of blood vessel plaque formation by protecting high-density lipoprotein and low-density...

Aldose reductase (AR) is the first and rate‐limiting enzyme of the polyol pathway, which converts glucose to sorbitol in an NADPH‐dependent reaction. α‐Glycosidase breaks down starch and disaccharides to glucose. Hence, inhibition of these enzymes can be regarded a considerable approach in the treatment of diabetic complications. AR was purified fr...

In the treatment of Alzheimer’s disease (AD), it is important to develop alternative cholinesterase inhibitors with antioxidant properties that will reduce acetylcholine deficiency and free radical formation. The aim of this study was to investigate the effect of hydroquinone, 4-hydroxybenzoic acid, 3,5-dihydroxybenzoic acid, caffeic acid, vanillic...

Sulfonamide derivatives exhibit a wide biological activity and can function as potential medical molecules in the development of a drug. Studies have reported that the compounds have an effect on many enzymes. In this study, the derivatives of amine sulfonamide (1i-11i) were prepared with reduced imine compounds (1-11) with NaBH4 in methanol. The s...

Aldose reductase (AR) catalyzes the NADPH-dependent reduction of glucose to sorbitol in the polyol pathway which plays an important role in the development of diabetic complications including cataract, retinopathy, nephropathy, and neuropathy. AR has been considered as an important target to heal these long-term diabetic complications and for this...

In the present study, a series of eleven novel 1,3‐diaryltriazene‐substituted sulfathiazole moieties (ST1 –11 ) was synthesized by the reaction of diazonium salt of sulfathiazole with substituted aromatic amines and their chemical structures were characterized by Fourier transform infrared, ¹H‐NMR (nuclear magnetic resonance), ¹³C‐NMR, and high‐res...

Some metabolic enzyme inhibitors can be used in the treatment of many diseases. Therefore, synthesis and determination of alternative inhibitors are essential. In this study, the inhibition effect of newly synthesized compounds on carbonic anhydrase (cytosolic isoforms, hCA I and hCA II), α-glycosidase (α-GLY), and acetylcholinesterase (AChE) were...

In this study, 15 novel compounds in a series of sulfonamide‐based ketenes (7a–o) were synthesized and characterized using Fourier‐transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectrometry. All compounds were tested for their ability to inhibit the human carbonic anhydrase (hCA) isoforms I and II, and acetylcho...

Carbonic anhydrases (CAs) are potent dehydration of carbonic acid and catalyst of the reversible hydration of carbon dioxide. Here, CA I and CA II was purified from human erythrocytes using the simple chromatographic method and determined the interactions between some calcium channel blockers and the enzymes. Molecular docking studies were performe...

Background In these days, most of the drugs used in clinical applications show their pharmacological influences by inhibiting or activating enzymes. Therefore, enzyme inhibitors have an essential place in the drug design for many diseases. Objective The current study aims to contribute to this growing drug design field (i.e., medicine discovery an...

Pain, as a sensible alarm signal of living organisms to avoid tissue damage, is a common and debilitating consequence of a lot of disorders and diseases. The management of chronic pain is particularly challenging. For pain treatment, many analgesic drugs are used for their therapeutic effects. In this study, some nonsteroidal anti-inflammatory drug...

Drugs show their pharmacological effects by inhibiting or activating enzymes. Therefore, enzyme inhibitors have an essential place in the drug design for numerous different sorts of diseases, i.e., cardiovascular, cancer, metabolic, and neurological. The purpose of the current study was to contribute to the growing drug discovery and development ar...

Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, ¹³C NMR, ¹H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxi...

In this study a series of pyrazole-3,4-dicarboxamide (3–10) derivatives bearing sulfonamide moiety were synthesized starting from 1-(3-nitrophenyl)-5-phenyl-1H-pyrazole-3,4-dicarboxylic acid (1). The structures of synthesized molecules were characterized by FT-IR, 1H NMR, 13C NMR, and elemental analysis methods. Human carbonic anhydrase isoenzymes...

Herein, a series of isoindole‐1,3‐dione substituted sulfonamide derivatives (3, 4 a–k) were designed, synthesized, and biologically evaluated, as inhibitors of carbonic anhydrase (CA) and acetylcholinesterase (AChE). CA and AChE inhibitory activities of newly synthesized isoindole‐1,3‐dione substituted sulfonamides compounds (3, 4 a–k) towards the...

Oxidative metabolic reactions and their by products have played a role in coronary artery disease (CAD) and Alzheimer’s disease (AD) pathogenesis. This study was carried out on 28 patients with AD, 21 patients with CAD, and 28 healthy as control. Oxidative stress biomarkers and acetylcholinesterase (AChE) activity were assayed in plasma. mRNA expre...

Sulfonamides known as inhibitors of many metabolic enzymes have been widely used as antimicrobial drugs for a long time. In the present study, we investigated in vitro inhibitory activities of benzenesulfonamide derivatives on human paraoxonase-I (hPON1). For this aim, PON1 was purified from human serum with a specific activity of 2603.57 EU/mg and...

The core purpose of the current study was to investigate the interactions of widely used broad‐spectrum antibacterial drugs developed in response to the increasing rate of antibiotic‐resistant various bacteria and to contribute to the field of drug design. Also, it is to broaden the current knowledge of paraoxonase 1 enzyme (EC: 3.1.8.1; PON1) whic...

Aldose reductase (AR) belongs to NADPH-dependent oxidoreductases and converts glucose to sorbitol in the polyol pathway. AR inhibition is essential to prevent diabetic complications. Here, AR was purified from sheep kidney using simple methods and determined the interactions between some calcium channel blockers and the enzyme. It was found that ca...

Medications show their biological effects by interaction with enzymes, which have been known to play an essential role in the pathogenesis of many diseases. Inhibition or induction of drug metabolizing enzymes has an essential place in the drug design for many kinds of diseases including cardiovascular, neurological, metabolic, and cancer. The main...

The synthesis, characterization and biological evaluation of a series of novel N-substituted phthalazine sulfonamide (5a-l) are disclosed. Phthalazines which are nitrogen-containing heterocyclic compounds are biologically preferential scaffolds, endowed with versatile pharmacological activity, such as anti-inflammatory, cardiotonic vasorelaxant, an...

Di­a­betes mel­li­tus is a chronic meta­bolic dis­ease char­ac­ter­ized by ab­nor­mal glu­cose me­tab­o­lism. Al­dose re­duc­tase (AR) is the first en­zyme in the polyol path­way and con­verts glu­cose to sor­bitol. It plays a vi­tal role as a glu­cose re­duc­ing agent and is in­volved in the patho­phys­i­ol­ogy of di­a­betic com­pli­ca­tions. In t...

Background Natural products are produced via primary and secondary metabolism in different organisms. The compounds obtained via secondary metabolism are not essential for the survival of the organism, but they can have a different value for humans. Objective The objective of this study was to examine inhibitory effects of Usnic Acid (UA), a well-...

The presented article focuses on the in vitro inhibition of plant extracts on the human carbonic anhydrase isoforms (hCA I and hCAII), and paraoxonase-1 (PON1) activities. Five different plants (Alcea rosea, Foeniculum vulgare, Elettaria cardamomum, Laurus azorica and Lavandula stoechas) were selected in this study. Methanol, ethanol, and water ext...

Aldose reductase converts glucose to sorbitol in the polyol pathway. It is an important enzyme to prevent diabetic complications. In this study, we studied the inhibitory effects of bromophenol derivatives on aldose reductase (AR), α‐glucosidase, and α‐amylase enzymes. In the bromophenols series, compound 1f showed the maximum inhibition effect aga...

Phytase (myo-inositol hexaphosphate phosphohydrolase) belongs to phosphatases. It catalyzes the hydrolysis of phytate to less-phosphorylated inorganic phosphates and phytate. Phytase is used primarily for the feeding of simple hermit animals in order to increase the usability of amino acids, minerals, phosphorus and energy. In the present study, ph...

Glutathione‐S‐transferases (GSTs) have a function in xenobiotic metabolism. They are a significant multifunctional family with a wide variety of catalytic activities. In the current study, we determined in vitro inhibition effects of 2,4‐dichlorophenoxyacetic acid dimethylamine salt (2,4‐D DMA), haloxyfop‐P‐methyl, glyphosate isopropylamine, dichlo...

Carbonic anhydrase (CA) has a key role in respiration, carbon dioxide and bicarbonate transport. Acetylcholinesterase (AChE) is a serine hydrolase and mostly abundant at neuromuscular junctions and cholinergic brain synapses. Inhibitors of these enzymes could aid in illuminating the role in disease processes. In this study, we separately purified C...