Aldose reductase (AR) inhibitors have vital importance in the treatment and prevention of diabetic complications. In this study, rat kidney AR was purified 19.34-fold with a yield of 3.49% and a specific activity of 0.88 U/mg using DE-52 Cellulose anion exchange chromatography, gel filtration chromatography and 2′5′ ADP Sepharose-4B affinity chromatography, respectively. After purification, the in vitro inhibition effects of some phenolic acids (tannic acid, chlorogenic acid, sinapic acid, protocatechuic acid, 4-hydroxybenzoic acid, p-coumaric acid, ferulic acid, vanillic acid, syringic acid, α-resorcylic acid, 3-hydroxybenzoic acid and gallic acid) were investigated on purified enzyme. We determined IC50, Ki values and inhibition types of these phenolic acids. As a result, tannic and chlorogenic acid had a strong inhibition effect. On the other hand, gallic acid had a weak inhibition effect. In this study, all phenolic acids except for chlorogenic acid and p-coumaric acid showed non-competitive inhibition effects on rat kidney AR.

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Carbonic anhydrases (CAs) are known as a drug-target enzymes. The inhibitors of the enzyme are important compounds for discovering new therapeutic agents and understanding in detail protein-drug interactions at the molecular level. For this purpose, the in vitro effects of some anti-inflammatory agents such as tenoxicam, fluorometholone acetate, and dexamethasone were investigated on esterase activity of human erythrocyte CA-I and CA-II in this study. hCA-I and hCA-II were purified by affinity chromatography with a yield of 47.25% and 87%, and a specific activity of 642.8 EU/mg proteins and 5576.9 EU/mg proteins, respectively. SDS-PAGE was performed to determine the purity of the enzymes. Inhibitory effects of the drugs on hCA-I and hCA-II were determined by spectrophotometric method. IC50 values for hCA-I and hCA-II were 0.198, 2.18, 11.7, 0.11, 17.5 and 14 μm using tenoxicam, fluorometholone acetate, and dexamethasone, respectively. For fluorometholone acetate and dexamethasone, Ki values from Lineweaver-Burk plots were obtained as 1.044 and 21.2 μm (noncompetitive) for hCA-I and 9.98 and 8.66 μm (non-competitive) for hCA-II. In conclusion, tenoxicam, fluorometholone acetate, and dexamethasone showed potent inhibitory effects on esterase activity of hCA-I and hCA-II isozymes under in vitro conditions.

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Aldose reductase (AR) inhibitors play a vital importance as a potential therapeutic and preventive medicine when it comes to hyperglycemia associated diabetic complications. Additionally, capsaicin is used as a food additive and a drug in a number of diverse clinical trials. The aim of this study is to determine the in vitro inhibition behavior of capsaicin on AR enzyme activity, which was obtained from different rat tissues (heart, kidney, liver, and brain). We showed that AR was inhibited by capsaicin in the micromolar range and noncompetitive manner in all of the tissues. K values of capsaicin were found to be 8.87, 264, 535, and 597, respectively, in heart AR, kidney AR, liver AR, and brain AR. In conclusion, capsaicin may be an effective molecule when used in low concentrations to prevent diabetic complications associated with the polyol pathway.

Dyes used during various industrial activities in the production of the essential consumer goods, of modern life's, especially such as textiles, leather, cosmetics, food and beverage, paper and pulp mill cause the most important inevitable environmental pollution problems of the contemporary world's, and also threatens the ecological balance. Especially, as a result of the textile wastewaters that contain high amounts of synthetic dyes, light transmission is reduce and the photosynthetic activity of aquatic life is adversely affected, so this situation causes a highly toxic effect on living communities. Although physical and chemical methods are used for the removal of these dyes, alternative methods such as biological systems are needed due to disadvantages like high costly, acting on a limited number of dyes types and disposal of concentrated sludge in large quantities. Biosorption method with low-cost, high metal binding capacity and its feature as microorganisms taking the main role drawn the attention of the scientific world as an alternative method for the removal of industrial waste. Studies in recent year has drawn the attention to the existence of organism which have the ability to remove many types of dyes from wastewater. Bacteria, fungi (mold-yeast and filamentous fungi), algae and seaweeds are group of organisms can be used in this regard. Trametes versicolor (white rot fungus) which is a filamentous fungus is a species of belonging to Basidiomycetes class, tested in numerous researches as a dyes remover. Rhizopus arrhizus belonging to Zygomycetes class is another fungal species tested as dyes remover. The species that belong Cladophora genus from green algs and bacteria that belong to Bacillus and Pseudomonas genus are between microorganisms group that can be used as biosorbent. This study is aimed to provide an overview to the microorganism used in biosorption method and collect latest information about the subject. The first economic feasibility studies on applicability of biosorption technology show that this process provides significantly cost savings and that the recovery of heavy metals reduces additional cost.Copy Right, IJAR, 2017,. All rights reserved.

A series of novel dopamine analogs incorporating urea and sulfonamide functional groups was synthesized from 3,4‐dimethoxyphenethylamine. The reaction of 3,4‐dimethoxyphenethylamine with N,N‐dimethylcarbamoyl chloride, followed by the sulfonyl chlorination of the urea derivative, gave benzene‐1‐sulfonyl chloride 9, which was reacted with NH3 (aq) or N‐alkyl amines to give related sulfonamides. The O‐demethylation reaction of the subsequent compounds with BBr3 afforded four novel phenolic dopamine analogs including sulfonamide and urea in the same structure. The anticholinergic and antioxidant effects of the synthesized compounds were examined. Compound 13 exhibited inhibition at the micromolar level for both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The IC50 value of 13 was calculated as 298 ± 43 µM for AChE and 321 ± 29 µM for BChE. The antioxidant and antiradical effects of the molecules were investigated by five different methods. Among the synthesized compounds 10–18, the best antioxidant and antiradical activities belong to the phenolic compounds 15–18. Compounds 16 and 18 have a higher reducing power than the standards used, that is, butylated hydroxytoluene, butylated hydroxyanisole, Trolox, and α‐tocopherol, for Fe3+–Fe2+ and Cu2+–Cu+ reducing activities. For the DPPH• radical scavenging method, compounds 16–18 have a much better scavenging power than the standard molecules. In addition, it has been determined by the induced‐fit docking method that compound 13 is well‐fitted in the active site of the enzymes. ADME studies reveal that the pharmacokinetic and physicochemical properties of all synthesized compounds are within an acceptable range.

Background: The 2019 novel coronavirus disease (COVID-19) has caused a global health catastrophe by affecting the whole human population around the globe. Unfortunately, there is no specific medication or treatment for COVID-19 currently available. Objective: It’s extremely necessary to apply effective drug treatment in order to end the pandemic period and return daily life to normal. In terms of the urgency of treatment, rather than focusing on the discovery of novel compounds, it is critical to explore the effects of existing herbal agents with proven antiviral properties on the virus. Method: Molecular docking studies were carried out with three different methods, Glide extra precision (XP) docking, Induced Fit docking (IFD), and Molecular Mechanics/Generalized Born Surface Area (MM/GBSA), to determine the potential effects of 58 phytochemicals in the content of Rosmarinus officinalis, Thymbra spicata, Satureja thymbra, and Stachys lavandulifolia plants -have antiviral and antibacterial effects- against Main Protease (Mpro) and Angiotensin Converting Enzyme 2 (ACE2) enzymes. Results: 7 compounds stand out among all molecules by showing very high binding affinities. According to our findings, the substances chlorogenic acid, rosmarinic acid, and rosmanol exhibit extremely significant binding affinities for both Mpro and ACE2 enzymes. Furthermore, it was discovered that carnosic acid and alpha-cadinol showed potential anti-Mpro activity, whereas caffeic acid and carvacrol had promising anti-ACE2 activity. Conclusion: Chlorogenic acid, rosmarinic acid, rosmanol, carnosic acid, alpha-cadinol, caffeic acid, and carvacrol compounds have been shown to be powerful anti-SARS-COV-2 agents in docking simulations against Mpro and ACE2 enzymes, as well as ADME investigations.