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A biochemistry-oriented drug design: synthesis, anticancer activity, enzymes inhibition, molecular docking studies of novel 1,2,4-triazole derivatives
(Taylor & Francis Inc, 2024) Yuriy, Karpenko; Kusdemir, Gulnur; Volodymyr, Parchenko; Tuzun, Burak; Taslimi, Parham; Karatas, Omer Faruk; Anastasia, Khilkovets
In this study, we researched the reactions of 5-(5-bromofuran-2-yl)-4-methyl-1,2,4-triazole-3-thiol and 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols with some halogen-containing compounds, a number of new compounds were synthesized (1.1-1.5 and 2.1-2.8). These compounds showed excellent to good inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. For obtaining the effects of these compounds on AChE and BChE enzymes were determined spectrophotometrically according to Ellman. IC50 values of these enzymes were ranging between 1.63 and 17.68 nM for AChE and 8.71 and 84.02 nM for BChE. After, prostate cancer is the second leading cause of cancer-related mortality for men over the age of 65 in developed countries. Current treatment options remain limited in the treatment of advanced-stage prostate cancer leading to biochemical recurrence in almost 40% of the patients. Therefore, there is an urgent need for development of novel therapeutic tools for treatment of prostate cancer patients. In this study, we aimed at analyzing the potential of all compounds against prostate cancer cells. We found that, of the tested compounds, 2.1, 2.2 and 2.3 showed significant cytotoxic activities against PC3 prostate cancer cells, although their effect on the viability of normal prostate cells was limited. These findings suggest their selective targeting potential for prostate cancer cells and offer them as candidate therapeutic agents against prostate cancer. The inhibitory activities of some chemical compounds, such as (1.1-1.5 and 2.1-2.8) were assessed by performing the molecular docking study in the presence of AChE, BChE and prostate cancer protein. MM/GBSA methods are calculated binding free energy. Finally, ADME/T analysis was performed to examine the drug properties of the 13 studied molecules.Communicated by Ramaswamy H. Sarma
A Simple and Efficient Procedure Toward 2-Thioxoquinazolin-4(1H)-One Derivatives
(Jihad Daneshgahi, 2024) Shourkaei, Fateme Ahmadi; Ranjbar, Parviz Rashidi; Mahdavi, Mohammad; Tuzun, Burak; Taslimi, Parham
A facile synthetic route for constructing 2-thioxoquinazolin-4(1H)-one derivative through cyclization reactions using readily available starting materials 2-aminobenzoic acids, alkyl/aryl amines, and carbon disulfide is described. These reactions occur under mild conditions, producing the desired products with good to high yields. Molecular docking was conducted to assess the activities of the 2-thioxoquinazolin-4(1H)-one derivative against breast cancer protein (PDB ID: 1JNX), liver cancer protein (PDB ID: 2H80), and colon cancer protein (PDB ID: 4UYA). Furthermore, an ADME/T analysis was performed to evaluate the impact of these compounds on human metabolism.
Alzheimer's Disease Drug Design by Synthesis, Characterization, Enzyme Inhibition, In Silico, SAR Analysis and MM-GBSA Analysis of Schiff Bases Derivatives
(Korean Institute Chemical Engineers, 2025) Karatas, Halis; Kul, Ilayda Bersu; Aydin, Meltem; Tuzun, Burak; Taslimi, Parham; Kokbudak, Zuelbiye
Schiff bases, azomethine group containing compounds, form a significant class in pharmaceutical and medicinal chemistry with biologic applications. In this study, two new Schiff base molecules (7 and 9) were synthesized from the condensation reaction of 1-amino-5-(4-methylbenzoyl)-4-p-tolylpyrimidin-2(1H)-one (Z1) with 3-chlorobenzaldehyde and 3-fluorobenzaldehydes in good yields (76-75%). The synthesized Schiff bases were completely characterized by IR, NMR and LC-MS. Moreover, both synthesized compounds were evaluated against acetylcholinesterase and butyrylcholinesterase as two important targets in the treatment of Alzheimer's disease. Approximately, both new compounds were more potent than positive control tacrine against these studied enzymes. Cholinesterase enzyme inhibition is a widely used treatment approach for a variety of mental illnesses. Through the inhibition of the acetylcholinesterase enzyme, which hydrolyzes acetylcholine, cholinesterase inhibitors directly improve cholinergic transmission. Using the SAR (structure-activity relationship) approach to connect different functional groups, the influence of this synthesized molecule on the activity was examined. The investigated compounds were then structurally characterized at the levels of B3LYP, HF, and M062X/6-31+G(d,p). Using maps of molecular electrostatic potential (MEP), the active sites of the compounds under study were identified. In the end, our focus was on evaluating the drug's potential as an inhibitor against the Alzheimer's disease, specifically targeting the Alzheimer's disease protein, that are Acetylcholinesterase (AChE) (PDB ID: 1OCE, 1QTI, and 4M0E) and Butyrylcholinesterase (BChE) (PDB ID: 6R6V and 2WSL). The binding free energy is computed using MM/GBSA techniques. ADME/T characteristics were investigated to see whether these compounds could be potential drugs.
Aminopyrazole-substituted metallophthalocyanines: Preparation, aggregation behavior, and investigation of metabolic enzymes inhibition properties
(WILEY-V C H VERLAG GMBH, 2019) Guzel, Emre; Kocyigit, Umit M.; Arslan, Baris S.; Atas, Mehmet; Taslimi, Parham; Gokalp, Faik; Nebioglu, Mehmet; Sisman, Ilkay; Gulcin, Ilhami
The synthesis, characterization, aggregation behavior, theoretical studies, and investigation of antimicrobial, antidiabetic, and anticholinergic properties of 4-(2-(5-amino-4-(4-bromophenyl)-3-methyl-1H-pyrazol-1-yl)ethoxy)phthalonitrile (2) and its soluble aminopyrazole-substituted peripheral metallo (Mn, Co, and Ni)-phthalocyanine complexes (3-5) are reported for the first time. The synthesized compounds and phthalocyanine complexes were characterized spectroscopically. The new phthalonitrile derivative (2) and its peripheral metallophthalocyanine complexes (3-5) were found to be effective inhibitors of alpha-glycosidase, acetylcholinesterase (AChE), human carbonic anhydrase I and II isoforms (hCA I and II), and butyrylcholinesterase (BChE) with K-i values in the range of 1.55 +/- 0.47 to 10.85 +/- 3.43 nM for alpha-glycosidase, 8.44 +/- 0.32 to 21.31 +/- 7.91 nM for hCA I, 11.73 +/- 2.82 to 31.03 +/- 4.81 nM for hCA II, 101.62 +/- 26.58 to 326.54 +/- 89.67 nM for AChE, and 68.68 +/- 11.15 to 109.53 +/- 19.55 nM for BChE. This is the first study of peripherally substituted phthalocyanines containing an aminopyrazole group as potential carbonic anhydrase enzyme inhibitor. Also, the antimicrobial activities of the synthesized compounds were evaluated against six microorganisms (four bacteria and two Candida species) using the broth microdilution method. The gram-positive bacteria were detected to be more sensitive than gram-negative bacteria and yeasts in the synthesized compounds.
Bioactivity and molecular docking studies of some nickel complexes: New analogues for the treatment of Alzheimer, glaucoma and epileptic diseases
(Academic Press Inc Elsevier Science, 2020) Kisa, Dursun; Korkmaz, Nesrin; Taslimi, Parham; Tuzun, Burak; Tekin, Saban; Karadag, Ahmet; Sen, Fatih
The interaction of the coordination compounds with biological molecules resulted in the investigation of the drug potential of these molecules. In this study, enzyme inhibition of DSA (1-3) coordination compounds that were previously investigated for their anticancer and antibacterial properties was investigated. Also, DSA (1-3) had Ki values of 635.30 + 152.62, 184.01 + 90.05, and 163.03 +/- 60.01 mu M against human carbonic anhydrase I, 352.23 +/- 143.09, 46.2 +/- 15.47, and 54.117 +/- 18.80 mu M against AChE, 310.64 +/- 97.35, 35.54 +/- 7.01, and 101.51 +/- 15.314 mu M against BChE, respectively. The biological activity values of these compounds against enzymes whose name are AChE, BChE, and hCAI were compared. Ellman and Verporte methods were used for the study of these enzymes. Cholinesterase inhibitors, also known as anti-cholinesterase and cholinesterase blocking drugs, are chemicals that prevent the breakdown of the neurotransmitter acetylcholine or butyr-ylcholine. They may be used as drugs for Alzheimer's and myasthenia gravis. It is a common method for com-paring biological activity values of nickel complexes with molecular docking calculations. Nickel complexes were studied against enzymes that are human carbonic anhydrase isozyme I for ID 2CAB (hCA I), butyr-ylcholinesterase for ID 1P0I (BChE), and acetylcholinesterase for ID 1EEA (AChE), respectively.
Biological Activity and Molecular Docking Study of Some Bicyclic Structures: Antidiabetic and Anticholinergic Potentials
(Taylor & Francis Ltd, 2022) Taslimi, Parham; Akhundova, Fidan; Kurbanova, Malahat; Turkan, Fikret; Tuzun, Burak; Sujayev, Afsun; Sadeghian, Nastaran
Bicyclic structures were synthesized by LACASA-DA cycloaddition reaction using (S)-BINOL as a chiral inductor. The N-2 pyridazine position was protected; the hydroxyl group was carbonylated to form the new bicyclic structure. The protective group was removed, the double bond dehydroxylated leading to the target compound. Removing of the protective group was performed using newly found ecofriendly catalyst for N-Boc deprotection. The obtained features from the model against AChE enzyme suggest that a lower the size of the ring, number of -NH-NH- groups, number of secondary aromatic amines, number of aromatic ketone groups may contribute to the inhibitory activity. The features obtained from the model against BChE enzyme suggest that the sum of topological distances between two nitrogen atoms, number of secondary aromatic amides, may be more favorable for inhibition. The features obtained from selectivity-based model suggest that the number of aromatic ethers, unsaturation content related to their molecular size and molecular shape may be more specific for the inhibition of the AChE enzyme in comparison to the BChE enzyme. Similarly, these aromatic structures inhibited the alpha-glucosidase enzyme at the micromolar level due to its structural feature. Inhibition values were found to be statistically significant, especially for cholinesterase enzymes. Molecular docking method was used to compare the biological activities of molecules against enzymes. The enzymes used in this study are alpha-glycosidase, butyrylcholinesterase, acetylcholinesterase, respectively. ADME/T analysis was performed to use some bicyclic molecules as drugs in the future.
Chalcone-based schiff bases: Design, synthesis, structural characterization and biological effects
(Elsevier, 2025) Yalazan, Halise; Koc, Damla; Kose, Fadime Aydin; Akgul, Muhammed Ismail; Fandakli, Seda; Tuzun, Burak; Taslimi, Parham
The presented work describes the synthesis, characterization, and biological effects of three new Schiff base compounds (SOH-F/Cl/Br) and their phthalonitrile derivatives (SCN-F/Cl/Br). The structures of all synthesized compounds were elucidated by NMR, FT-IR, and mass spectroscopic methods. Enzyme results were obtained at the nanomolar level. Cytotoxic activity of novel compounds was evaluated against neuroblastoma (SH-SY5Y) and mouse fibroblast (NIH-3T3) cell lines using MTT. It has been determined that all tested molecules have a powerful cytotoxic effect; IC50 values were under 10 mu M against SH-SY5Y cells. Among all compounds, the lowest IC50 value was observed in SCN-Br (1.798 +/- 0.036 mu M). Moreover, the IC50 concentration of SCN-Br (12.79 +/- 0.33 mu M) in healthy NIH-3T3 cells was significantly higher than in cancerous cells. The activity comparison of the studied six molecules was made with both DFT calculations and molecular docking calculations. Various proteins that are hCA I protein (PDB ID: 2CAB), hCA II protein (PDB ID: 5AML), and SH-SY5Y protein (PDB ID: 7LQZ, 5WIV, and 2F37) were used in molecular docking calculations. After this comparison, ADME/T calculations were used to analyze the molecules to be used as drugs.
Characterization and inhibition effects of some metal ions on carbonic anhydrase enzyme from Kangal Akkaraman sheep
(WILEY, 2018) Kocyigit, Umit M.; Taslimi, Parham; Gulcin, Ilhami
In this work, the carbonic anhydrase (CA) enzyme was purified from Kangal Akkaraman sheep in Sivas, Turkey with specific activity value of 6681.57 EU/mg and yield of 14.90% with using affinity column chromatography. For designating the subunit molecular mass and enzyme purity. sodium dodecyl sulfate polyacrylamide gel electrophoresis method was used and single band for this procedure was obtained. The molecular mass of CA enzyme was found as 28.89 kDa. In this study, the optimum temperature and optimum pH were obtained from 30 and 7.5. V-max and K(m )values for p-nitrophenylacetate substrate of the CA were determined from Lineweaver-Burk graphs. Additionally, the inhibitory results of diverse heavy metal ions (He+, Fe2+, pb(2+), co(2+), A(g+), and Cu2+) on sheep were studied. Indeed, CA enzyme activities of Kangal sheep were investigated with using esterase procedure under in vitro conditions. The heavy metal concentrations inhibiting 50% of enzyme activity (IC50) and K-i values were obtained.
Co and Zn Metal Phthalocyanines with Bulky Substituents: Anticancer, Antibacterial Activities and Their Inhibitory Effects on Some Metabolic Enzymes with Molecular Docking Studies
(Taylor & Francis Ltd, 2022) Turkan, Fikret; Taslimi, Parham; Cabir, Beyza; Agirtas, Mehmet Salih; Erden, Yavuz; Celebioglu, Hasan Ufuk; Tuzun, Burak
In this study, we reported the synthesis of new cobalt and zinc phthalocyanine compounds with ((ethylenediamine-N,N',N'-triacetic acid-N-2-ethyl)oxy) (ETAEO) substituted groups. Characterization studies and anticancer properties of both synthesized compounds were determined as well. The inhibitory effects of these complexes on some metabolic enzymes were examined and it was observed that the enzymes inhibited by complex molecules at the micromolar levels. In addition, the active sites of the enzymes were determined by molecular modeling programme for screening the enzyme-inhibitor interactions. The molecular docking method was used to calculate the interactions of molecules with enzymes. Also, human prostate and breast cancer cell lines (PC-3 and MCF-7) were used to determine the anticancer properties of the complexes. All doses of the tetrakis (ETAEO) phthalocyaninato Cobalt II (1) did not show any significant changes in PC-3 cell viability, but significantly reduced in MCF-7 cell viability. Similarly, all doses of the tetrakis (ETAEO) phthalocyaninato zinc II (2) significantly reduced MCF-7 cell viability compared to the control and solvent control groups. According to the enzyme inhibition studies, both complexes showed the best inhibition effects for alpha-Glycosidase enzyme with 125.85 +/- 30.35 mu M and 165.30 +/- 27.18 mu M Ki values.
Composition characterization and biological activity study of Thymbra spicata l. var. spicata essential oil
(2021) Eruygur, Nuraniye; Kocyıgıt, Umit M.; Atas, Mehmet; Cevık, Ozge; Gökalp, Faik; Taslimi, Parham; Gulcın, İlhami
The current research aimed to determine and report in vitro antioxidant, antimicrobial, antibiofilm, cytotoxic, anti-cholinesterase, and anti-diabetic properties and the stability of the major component of basic oil of Thymbra spicata var. spicata through different phases as theoretically. Essential oil exhibits potential biological activities because of the multiple components it contains.In the current research, the evaluation of Thymbra spicata essential oil antioxidant properties was conducted utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2- azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) radical scavenging activity.Antimicrobial activity was assessed from minimum inhibition concentration (MIC) using the technique of microdilution and cytotoxicity activity was evaluated by MTT assay through MCF-7 and PC3 human cancer cell lines.Consequently, Cytotoxic activity was evaluated by means of MTT assay utilized. The essential oil was detected to have 340 ?g/mL inhibiting influence on the growth of PC3 prostate cancer cells with IC50 value. Also, the T. spicata plant was observed to significantly repress the enzymes, namely acetylcholinesterase (AChE), butyrylcholinesterase (BChE), ?-glycosidase. IC50 values of enzymes were obtained 0.23 ?g/mL for AChE, 1.64 ?g/mL for BChE, 7.78 ?g/mL for ?-glycosidase. It was concluded that this plant may be used for Alzheimer's and diabetes disease.
Cytotoxic effects, carbonic anhydrase isoenzymes, ?-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives
(Taylor & Francis Inc, 2021) Celebioglu, Hasan Ufuk; Erden, Yavuz; Hamurcu, Fatma; Taslimi, Parham; Senturk, Ozan Sanli; Ozmen, Ummuhan Ozdemir; Tuzun, Burak
Today, interest in studies on the search for new drugs to be used in diseases such as cancer, cardiovascular diseases, neurodegenerative diseases and diabetes, as well as prevention of microbial inflammation is increasing day by day. Emerging biological and pharmacological effects of sulfonyl hydrazone derivative compounds reveal their importance. In the present study, heteroatom-containing sulfonyl hydrazone derivatives have been studied for their anticancer and antimicrobial properties, as well as their effects on enzymes that could play roles in Alzheimer's dissease and diabetes. High doses of the tested compounds significantly decreased the cell viabilities of breast cancer (MCF-7) and prostate cancer (PC-3) cell lines. Furthermore, all compounds possessed antimicrobial activities against very common bacteriaE. coliandS. aureus. These compounds were good inhibitors of the alpha-glycosidase, human carbonic anhydrase I and II isoforms and acetylcholinesterase enzyme withK(i)values in the range of 1.14 +/- 0.14-3.63 +/- 0.26 nM for alpha-glycosidase, 66.05 +/- 9.21-125.45 +/- 11.54 nM for hCA I, 89.14 +/- 10.43-170.22 +/- 26.05 nM for hCA II and 754.03 +/- 73.22-943.92 +/- 58.15 nM for AChE, respectively. Molecular docking method was used to theoretically compare biological activities of sulfonyl hydrazone derivatives against enzymes. The theoretical results were compared with the experimental results. Thus, these compounds have strong biological activities. Communicated by Ramaswamy H. Sarma
Determination of anticancer properties and inhibitory effects of some metabolic enzymes including acetylcholinesterase, butyrylcholinesterase, alpha-glycosidase of some compounds with molecular docking study
(Taylor & Francis Inc, 2021) Turkan, Fikret; Taslimi, Parham; Abdalrazaq, Sakar Mubarak; Aras, Abdulmelik; Erden, Yavuz; Celebioglu, Hasan Ufuk; Tuzun, Burak
Inhibitory effect of the complexes on some metabolic enzyme demonstrated that the enzymes inhibited by ligand and it's complex molecules at the micromolar level. The best inhibition effect for alpha-glycosidase (alpha-Gly) enzyme against cobalt complex with Ki value of 3.77 +/- 0.58 mu M. For achethylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes against SM-Co complex, Ki values of 74.23 +/- 5.02 mu M and 101.21 +/- 12.84 mu M Ki were observed, respectively. Molecular docking studies were performed to compare the biological activities of ligands and ligand complexes against enzymes whose names are AChE for ID 4M0E, BChE for ID 5NN0, alpha-Gly for ID 1XSI respectively. Also, anticancer properties of the complexes studied. The doses of all compounds caused significant reductions in MCF-7 cell viability. Zr compound showed the best cytotoxic activity against the MCF-7 cell. SM ligand administered to PC-3 cells exhibited a more pronounced cytotoxic effect than the SM-Co and Zr compounds. Communicated by Ramaswamy H. Sarma
Determination of the inhibition profiles of pyrazolyl-thiazole derivatives against aldose reductase and ?-glycosidase and molecular docking studies
(Wiley-V C H Verlag Gmbh, 2020) Demir, Yeliz; Taslimi, Parham; Kocyigit, Umit M.; Akkus, Musa; Ozaslan, Muhammet Serhat; Duran, Hatice Esra; Budak, Yakup
Aldose reductase (AR) is the first and rate-limiting enzyme of the polyol pathway, which converts glucose to sorbitol in an NADPH-dependent reaction. alpha-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 from sheep liver using simple chromatographic methods. The inhibitory effects of pyrazolyl-thiazoles ((3aR,4S,7R,7aS)-2-(4-{1-[4-(4-bromophenyl)thiazol-2-yl]-5-(aryl)-4,5-dihydro-1H-pyrazol-3-yl}phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives;3a-i) on AR and alpha-glycosidase enzymes were investigated. All compounds showed a good inhibitory action against AR and alpha-glycosidase. Among these compounds, compound3dexhibited the best inhibition profiles against AR, with aK(i)value of 7.09 +/- 0.19 mu M, whereas compound3eshowed the lowest inhibition effects, with aK(i)value of 21.89 +/- 1.87 mu M. Also, all compounds showed efficient inhibition profiles against alpha-glycosidase, withK(i)values in the range of 0.43 +/- 0.06 to 2.30 +/- 0.48 mu M, whereas theK(i)value of acarbose was 12.60 +/- 0.78 mu M. Lastly, molecular modeling approaches were implemented to predict the binding affinities of compounds against AR and alpha-glycosidase. In addition, the ADME analysis of the molecules was performed.
The effects of wireless electromagnetic fields on the activities of carbonic anhydrase and acetylcholinesterase enzymes in various tissues of rats
(WILEY, 2018) Kocyigit, Umit Muhammet; Taslimi, Parham; Gurses, Fatih; Soylu, Sinan; Dastan, Sevgi Durna; Gulcin, Ilhami
The purpose of our study is to assist in understanding the effects of wireless electromagnetic waves on carbonic anhydrase (CA) and acetylcholinesterase (AChE) enzymes activities in the different tissues of the rats. For this purpose, two different groups each of which contains eight rats (n=8) were formed as being control group and wireless electromagnetic wave-administered group. The rats were necropsied after 60min from the injection of chemicals into the rats intraperitoneally. The different tissues of the rats were extracted. CA and AChE enzymes activities were measured for each tissue. All the experimental results were provided in mean +/- S.D. Statistical significance was identified to be P<0.05. It was observed that there were significant changes of enzyme activities in wireless-administered group in salivary gland, stomach, colon, liver, and striated muscle tissues.
Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes
(WILEY, 2017) Kocyigit, Umit M.; Taslimi, Parham; Gezegen, Hayreddin; Gulcin, Ilhami; Ceylan, Mustafa
Carbonic anhydrase (CA; EC 4.2.1.1) is used for remedial purposes for several years, as there is significant focus on expanding more new activators (CAAs) and high affinity inhibitors. Alzheimers disease and other similar ailments such as dementia and vascular dementia with Lewy bodies reduce cholinergic activity in the important areas involved in cognition and memory. Prevalent drugs for the symptomatic therapy of dementia are significant in increasing the associated cholinergic deficiency by inhibiting acetylcholinesterase (AChE). These six-membered carbocycles showed nice inhibitory action against AChE and human carbonic anhydrase (hCA) II and I isoforms. The hCA I, II, and AChE were efficiently inhibited by these molecules, with K-i values in the range of 6.70-35.85nM for hCA I, 18.77-60.84nM for hCA II, and 0.74-4.60 for AChE, respectively.
Evaluation of Anticholinergic, Antidiabetic and Antioxidant Activity of Astragalus dumanii, an Endemic Plant
(Kahramanmaras Sutcu Imam Univ Rektorlugu, 2022) Kocyigit, Umit Muhammet; Eruygur, Nuraniye; Atas, Mehmet; Tekin, Mehmet; Taslimi, Parham; Gokalp, Faik; Gulcin, Ilhami
The research was conducted to separately evaluate and detect the possible in vitro antioxidant, antimicrobial activity of ethanol extracts prepared from aerial parts and roots of Astragalus dumanii and anti-cholinesterase and alpha-glucosidase inhibitory activity from only aerial parts of its The antioxidant capacity was tested by scavenging of DPPH and ABTS free radicals. Compared with the standard antioxidant compound gallic acid; Root and aerial part extract showed lower DPPH radical scavenging activity, however aerial part extract demonstrated higher ABTS radical scavenging activity. The phenolic contents were detected as 5.31 +/- 0.03 and 13.23 +/- 0.05 mg gallic acid equivalent g-1 extract, flavonoid contents were found as 8.26 +/- 0.004 and 7.93 +/- 0.005 mg Qercetin equivalent g-1 extract. In addition, the effects of the extracts obtained from aerial parts of the plant on acetylcholinesterase, butyrylcholinesterase and a-glycosidase enzymes were investigated in vitro and IC50 values were obtained as 1.47, 0.83 and 0.48 mu g mL-1, respectively. When these values were compared with standard substances, it was seen that Astragalus dumanii could be a good enzyme inhibitory agent. Antimicrobial activity of the plant extracts were determined using the microdilution method and the extracts was not observed to have any antimicrobial activities..
In vitro cytotoxic and in vivo antitumoral activities of some aminomethyl derivatives of 2,4-dihydro-3H-1,2,4-triazole-3-thiones-Evaluation of their acetylcholinesterase and carbonic anhydrase enzymes inhibition profiles
(WILEY, 2019) Timur, Irfan; Kocyigit, Umit M.; Dastan, Taner; Sandal, Suleyman; Ceribasi, Ali Osman; Taslimi, Parham; Gulcin, Ilhami; Koparir, Metin; Karatepe, Mustafa; Ciftci, Mehmet
The 1,2,4-triazole and its derivatives were reported to exhibit various pharmacological activities such as antimicrobial, analgesic, anti-inflammatory, antitumoural, cytotoxic, and antioxidant properties. In this study, a series of triazole compounds (M1-M10) were evaluated for some biological activities. In vitro qualifications of these compounds on acetylcholinesterase (AChE) and human carbonic anhydrase enzyme activities were performed. Also, their antitumoral activities in human colon cancer (HT29) cell line cultures were examined. In addition, colon cancer experimentation was induced in rats by an in vivo method, and the in vivo anticancer effects of triazole derivatives were investigated. Also, the effects of these derivatives in levels of antioxidant vitamin A, vitamin E, and MDA were studied in rat liver and blood samples. Most of the compounds were found to exhibit significant antioxidant and antitumoral activities. All the compounds had cytotoxic activities on HT29 cell lines with their IC50 values lower than 10 mu M concentrations. The low IC50 values of the compounds are M1 (3.88 mu M), M2 (2.18 mu M), M3 (4.2 mu M), M4 (2.58 mu M), M5 (2.88 mu M), M6 (2.37 mu M), M7 (3.49 mu M), M8 (4.01 mu M), M9 (8.90 mu M), and M10 (3.12 mu M).
Inhibitory effects of oxytocin and oxytocin receptor antagonist atosiban on the activities of carbonic anhydrase and acetylcholinesterase enzymes in the liver and kidney tissues of rats
(WILEY, 2017) Kocyigit, Umit M.; Taskiran, Ahmet Sevki; Taslimi, Parham; Yokus, Ahmet; Temel, Yusuf; Gulcin, Ilhami
The aim of this study was to investigate the effects of oxytocin (OT), atosiban, which is an OT receptor antagonist, and OT-atosiban chemicals injected to rats on the activities of carbonic anhydrase (CA) and acetylcholinesterase (AChE) enzymes in liver and kidney tissues of rats. For this purpose, four different groups, each consisting of six rats (n=6), were formed (control group, OT administered group, atosiban administered group, and both OT and atosiban administered group). The rats were necropsied 60min after intraperitoneal injection of chemicals into the rats. Liver tissues of rats were extracted. CA and AChE enzyme activities were measured for each tissue by using hydratase, esterase, and acetylcholiniodide methods. Activity values for each enzyme obtained were statistically calculated.
Inhibitory effects of some drugs on carbonic anhydrase enzyme purified from Kangal Akkaraman sheep in Sivas, Turkey
(WILEY, 2018) Kocyigit, Umit M.; Dastan, Sevgi Durna; Taslimi, Parham; Dastan, Taner; Gulcin, Ilhami
In this study, carbonic anhydrase (CA) enzyme was purified and characterized from blood samples of Kangal Akkaraman sheep and inhibitory properties on certain antibiotics were examined. CA purification was composed of preparation of the hemolysate and conducting the Sepharose-4B-tyrosine-sulfanilamide affinity gel chromatography in having specific activity of 11626EUmg(-1), yield of 14.40%, and 242.76-fold purification. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis was performed to assess the enzyme purity and a single band was observed. Some antibiotics were exhibited in vitro inhibition on the CA activity. IC50 values of these inhibitors were calculated by plotting activity percentage. IC50 values of certain drugs (dexamethasone; caffeine; metamizole sodium; tetramisol; ceftiofur HCl; ivermectin; tavilin 50; penokain G; neosym; and sulfamezathine) were found as 0.38, 8.24, 285.53, 114.77, 5.33, 2.76, 27.58, 213.50, 208.28, and 36.60M, respectively. K-i values of different drugs on Kangal Akkaraman sheep blood CA activity were found in the range of 0.21 +/- 0.038-266.64 +/- 37.11 mu M.
Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast cancer
(WILEY, 2017) Dastan, Taner; Kocyigit, Umit M.; Dastan, Sevgi Durna; Kilickaya, Pakize Canturk; Taslimi, Parham; Cevik, Ozge; Koparir, Metin; Orek, Cahit; Gulcin, Ilhami; Cetin, Ahmet
The aim of this study was to evaluate biologically active novel molecules having potentials to be drugs by their antitumor properties and by activities of apoptotic caspase and topoisomerase. Following syntheses of novel eight bis(-aminoalkyl)phosphinic acid derivatives (4a-h) as a result of array of reactions, compounds were evaluated by cytotoxic effects in vitro on human breast cancer (MCF-7) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF-7 and HUVEC lines, while 4c, 4e, and 4f compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. Also, some of the bis(-aminoalkyl)phosphinic acid derivatives (4a, 4e-h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.

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