Gümüşhane ÜniversitesiGümüşhane ÜniversitesiAçık Erişim Arşivi · RDL Open

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Yeniden eskiyeEskiden yeniye
  • MakaleYalnız künye2026
    Phytochemical profiling, biological activities, and molecular docking analysis of Dorycnium pentaphyllum subsp. haussknechtii

    Ayna, Adnan; Hakan, Oguzhan; Yapıcı, İsmail; İzol, Ebubekir; Yılmaz, Mustafa Abdullah; Necip, Adem; Yapar, Yakup

    BACKGROUND: In the current study, the biological activity fingerprint of Dorycnium pentaphyllum subsp. haussknechtii was investigated by an interdisciplinary approach through analysis of its phytochemical content, antioxidant capacity, enzyme inhibitory potential and molecular docking. RESULTS: The analysis of the phytochemical content by liquid chromatography–tandem mass spectrometry was characterized by the presence of flavan-3-ols, such as epicatechin, epigallocatechin, and catechin, as well as quercetin-derived flavonoids such as isoquercitrin. Analysis of the antioxidant capacity by 2,2-diphenyl-1-picrylhydrazyl, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), ferric reducing antioxidant power, Fe3+–Fe2+ reducing and cupric reducing antioxidant capacity methods indicated the strong antioxidant capacity of the plant extract. In addition, the plant extract was able to modulate biological enzyme activity effectively, with IC50 values of 111.78 μg mL−1 for acetylcholinesterase, 22.07 μg mL−1 for butyrylcholinesterase, 1.39 μg mL−1 for α-glucosidase, 7.34 μg mL−1 for carbonic anhydrase I, and 17.41 μg mL−1 for carbonic anhydrase II. To have a better understanding of the molecular mechanism for the plant extract's properties, the major phenolic compounds present in the plant extract were investigated for molecular docking with their respective enzymes. As such, the results revealed a strong binding affinity and conformational stability, with strong hydrogen bonding and π–π interactions. CONCLUSION: Generally, the properties revealed by the plant extract indicate that the phenolic content, strong antioxidant properties, and enzyme inhibition activity of D. pentaphyllum subsp. haussknechtii have shown great potential for being a useful natural source for therapeutic lead compounds.

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  • MakaleAçık Erişim2026
    Synthesis, Characterization, Biological Properties, and Sensor Applications of Novel Thiosemicarbazone Derivatives

    Gezegen, Hayreddin; Özbek, Oguz; Topal, Meryem; Şahin, Hatice; Koçyiğit, Ümit M.

    In this study, novel thiosemicarbazone derivative molecules (5a–j) were synthesized. The characterization of the synthesized molecules was carried out using 1H–, 13C–NMR, FT–IR, and Q–TOF spectroscopic techniques. Then, the inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The hCA I II, and AChE were efficiently inhibited by synthesized thiosemicarbazone derivatives, with Ki values in the range of 0.293–1.666 µM for hCA I, 0.298–1.332 µM for hCA II, and 52.51–138.63 µM for AChE, respectively. Finally, the sensor properties of the synthesized thiosemicarbazone derivatives were investigated. The newly synthesized thiosemicarbazone derivative molecules exhibited high selectivity towards Pb2+ ions. The sensor prepared with 5a from these molecules had a Nernstian behavior of 28.8 ± 1.5 mV/decade and a low detection limit of 2.86 × 10−6 M in a wide concentration range of 1.0 × 10−1–1.0 × 10−5 M. The newly proposed sensor also had a wide pH working range (5.0–10.0), a very fast response time (5 s), and good reproducibility. The newly fabricated sensors were used as indicator electrodes for the potentiometric titration of Pb2+ ions with ethylenediaminetetraacetic acid (EDTA) and were successfully applied for the determination of Pb2+ ion content in different water samples.

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  • MakaleAçık Erişim2026
    Investigation of the enzyme-inhibitory, antibacterial, and anticancer properties of metal phthalocyanines

    Topal, Meryem; Topal, Fevzi; Yilmaz, Fırat; Bulut Atalay, Esra; Koçyiğit, Ümit Muhammet; Güzel, Emre

    In this study, the enzyme inhibitory, antibacterial, and anticancer activities of a phthalonitrile derivative and its metal phthalocyanines (Pcs; indium, zinc, copper, cobalt, and manganese; 1–6) were investigated. The cobalt and manganese Pcs were synthesized for the first time in this study. The inhibitory activities of the symmetric Pcs, which were expected to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) via their 4-(isopropylbenzyl)oxy substituents through host–guest interactions, were investigated. More selective inhibition of AChE than BChE was observed for these compounds. For AChE, CoPc was identified as the most potent inhibitor (IC50 = 14.81 nM), whereas for BChE, InPc was identified as the most potent inhibitor (IC50 = 56.35 nM). The Ki values indicated that most compounds exhibited competitive inhibition; copper phthalocyanine (CuPc) showed particularly strong inhibition against AChE (Ki = 3.08 nM ± 1.12), whereas the lowest Ki value against BChE was observed for MnPc (Ki = 25.98 ± 1.97 nM). Most compounds exhibited competitive inhibition; however, CuPc showed competitive inhibition toward AChE but a noncompetitive inhibition pattern toward BChE. Dual inhibition of AChE and BChE by these compounds may be promising for addressing cholinergic deficits associated with Alzheimer’s disease. In addition, the acceptability of compounds 1–6 with respect to pharmacological drug-likeness criteria was assessed based on predicted absorption, distribution, metabolism, excretion (ADME) outcomes. In antibacterial tests, varying levels of inhibition were observed against selected bacterial strains. In anticancer assays, all compounds exhibited high cytotoxicity against the MCF-7 breast cancer cell line. Higher antiproliferative activity was observed for CuPc than for the other compounds. Morphological changes were induced in cancer cells by CuPc and MnPc. Overall, these compounds may have potential as enzyme inhibitors and as antibacterial and anticancer agents.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleYalnız künye2025
    Phytochemical Profile, Antioxidant Capacity, Acetylcholinesterase, and Butyrylcholinesterase Enzyme Inhibition Properties of Myosotis amoena Boiss

    Yapici, Ismail; Kayaoglu, Esma; Izol, Ebubekir; Yilmaz, Mustafa Abdullah; Behçet, Lutfi; Cakir, Oguz; Gülçin, Ilhami

    Myosotis amoena Boiss. (Turkish name: Ho & scedil; boncukotu) is a perennial herbaceous plant that produces blue flowers during the spring. Phytochemicals, which are secondary metabolites distributed across plants, fungi, microorganisms, and even animal tissues, play crucial roles in health through their antioxidant and bioactive properties. Their antioxidant capacity largely arises from hydroxyl groups and aromatic ring structures that stabilize free radicals via electron delocalization. Enzyme inhibition is a therapeutic strategy in several diseases, including Alzheimer's disease (AD), where acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors are employed to manage symptoms. This study investigated the phytochemical composition (via LC-MS/MS), total phenolic content, antioxidant capacity, and AChE/BChE inhibitory effects of the ethanol extract of M. amoena using four in vitro methods. The CUPRAC assay demonstrated that M. amoena (1.070) exhibited higher antioxidant activity than Trolox (0.894), although its activity in FRAP, ABTS, and Fe3+ reduction assays was lower compared to standard antioxidants. The extract contained 53.03 mg GAE/g extract of total phenolics, with rosmarinic acid being the predominant compound (15.27 mg/g). Furthermore, the extract strongly inhibited AChE and BChE, with IC50 values of 3.9 and 19.8 mu g/mL, respectively. These findings highlight, for the first time, the significant bioactive potential of M. amoena as a natural source of antioxidants and cholinesterase inhibitors, supporting its prospective use in the prevention or management of neurodegenerative conditions.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2025
    Novel Sulfonylhydrazones With Sulfonate Ester Framework: Promising Dual Inhibitors of AChE and hCAs

    Öztürk, Cansu; Balci, Neslihan; Aslan, Osman Nuri; Kalay, Erbay

    Alzheimer's disease (AD) is a progressive neurodegenerative disorder that affects millions of individuals worldwide. Treatment strategies for AD vary depending on cognitive and behavioral symptoms, with cholinergic replacement therapy using acetylcholinesterase (AChE) inhibitors being one of the primary approaches. Recent studies have also identified human carbonic anhydrases (hCAs) as significant therapeutic targets for AD, offering new opportunities for the development of innovative treatments. Carbonic anhydrase inhibitors have been shown to prevent early mitochondrial damage and inhibit H2O2 production, thereby reducing amyloid plaque formation. Building on the promising potential of hydrazones particularly sulfonyl hydrazones as anticholinesterase agents, we synthesized 12 novel chlorine-substituted sulfonyl hydrazone compounds containing aryl sulfonate ester groups. These compounds were evaluated for their inhibitory effects on AChE, hCA I, and hCA II enzymes. The synthesized compounds exhibited low nanomolar inhibitory activity, with Ki values ranging from 9.58 ± 2.22 to 104.04 ± 23.82 nM for AChE, 9.12 ± 2.21 to 477.63 ± 218.52 nM for hCA I, and 17.54 ± 7.74 to 564.62 ± 213.98 nM for hCA II. Notably, compound 6 showed strong inhibitory activity against hCA I (Ki = 9.12 ± 2.21 nM; acetazolamide (AZA) = 26.54 ± 3.11 nM) and hCA II (Ki = 17.54 ± 7.74 nM; AZA = 21.73 ± 2.42 nM), whereas compound 4 exhibited superior AChE inhibition (Ki = 9.58 ± 2.22 nM; TAC = 23.12 ± 2.05 nM). The chemical structures of the synthesized compounds were characterized using advanced spectroscopic techniques, including FT-IR, 1H-NMR, and 13C-NMR spectroscopy.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2025
    Inhibition Effect of Diosmin Flavanoid on Some Metabolic Enzymes and Investigation of Antioxidant Properties

    Balci, Neslihan

    Diosmin is a natural flavonoid obtained by dehydrating flavanone glycoside hesperidin. This study evaluated the inhibition effects of diosmin flavonoid on human carbonic anhydrases (hCA I and hCA II) and acetylcholinesterase (AChE) enzymes, which are linked to various health issues, and compared the results with standard drugs. The antioxidant potential was assessed using five assays, namely DPPH, ABTS, FRAP, CUPRAC and Fe3+ reducing assays. The results determined that diosmin didn’t exhibit strong antioxidant activity. Additionally, the inhibition effects of diosmin on hCA I, hCA II, and AChE enzymes were examined. It effectively inhibited hCA I and hCA II enzymes with Ki values of 3.84±0.63 nM and 15.64±1.90 nM, respectively (Table 1). For comparison, the Ki values of the standard drug AZA were 1.44 ± 0.32 nM for hCA I and 3.66 ± 0.25 nM for hCA II. On the other hand, diosmin effectively inhibited AChE enzymes with Ki values of 9.31±2.40 nM. The Ki values of the standard drug Tacrine was 6.22±1.95 nM for AChE. These findings suggest that diosmin may serve as a selective enzyme inhibitor, particularly for hCA I, but has limited antioxidant capacity. Diosmin exhibited relatively weak antioxidant activity compared to standard antioxidants.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleYalnız künye2024
    Assessment of Anticholinergic and Antidiabetic Properties of Some Natural and Synthetic Molecules: An In Vitro and In Silico Approach

    Çomaklı, Veysel; Aygül, İmdat; Sağlamtaş, Rüya; Kuzu, Müslüm; Demirdağ, Ramazan; Akincioğlu, Hülya; Adem, Şevki; Gülçin, İlhami

    Introduction: This study aimed to determine the in vitro and in silico effects of some natural and synthetic molecules on acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and α-glucosidase enzymes. Background: Alzheimer's disease (AD) and Type II diabetes mellitus (T2DM) are considered the most important diseases of today’s world. However, the side effects of therapeutic agents used in both diseases limit their use. Therefore, developing drugs with high therapeutic efficacy and better pharmacological profile is important. Objectives: This study sets out to determine the related enzyme inhibitors used in treating AD and T2DM, considered amongst the most important diseases of today’s world. Methods: In the current study, the in vitro and in silico effects of dienestrol, hesperetin, L-thyroxine, 3,3',5-Triiodo-L-thyronine (T3) and dobutamine molecules on AChE, BChE and α-glycosidase enzyme activities were investigated. Results: All the molecules showed an inhibitory effect on the enzymes. The IC50 and Ki values of the L-Thyroxine molecule, which showed the strongest inhibition effect for the AChE enzyme, were determined as 1.71 µM and 0.83 ± 0.195 µM, respectively. In addition, dienestrol, T3, and dobutamine molecules showed a more substantial inhibition effect than tacrine. The dobutamine molecule showed the most substantial inhibition effect for the BChE enzyme, and IC50 and Ki values were determined as 1.83 µM and 0.845 ± 0.143 µM, respectively. The IC50 and Ki values for the hesperetin molecule, which showed the strongest inhibition for the α-glycosidase enzyme, were determined as 13.57 µM and 12.33 ± 2.57 µM, respectively. Conclusion: According to the results obtained, the molecules used in the study may be considered potential inhibitor candidates for AChE, BChE and α-glycosidase.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2023
    Schiff Base Synthesis with a New Reliable Method and Investigation of Their Inhibition Effects on Glutathione S-Transferase and Cholinesterase Enzymes

    Balcı, Neslihan; Çelik, Hülya; Türkan, Fikret; Çelebioğlu, Neslihan; Çelik, Tuba; Bursal, Ercan

    The principle purpose of this study is to synthesize some Schiff base derivatives with a new microwave irradiation technique and investigate their enzyme inhibition effects. Related Schiff base compounds (1 a–1 h) were synthesized from 4-fluoro aniline and some substituted benzaldehyde derivatives (3 a–3 h). The chemical structures of Schiff bases were elucidated by various spectroscopic methods (1H NMR, 13C NMR). The inhibitory effects of the synthesized compounds against acetylcholinesterase, butyrylcholinesterase and glutathione S-transferase were investigated. The in vitro enzyme study determined the best enzyme inhibitors for AChE, BChE, and GST enzymes as 3 h, 3 b, and 3 e compounds, respectively. The results were compared with the standard drugs tacrine for cholinesterase and ethacrynic acid for GST enzymes. Molecular docking results demonstrated the low binding energy values between −5.8 kcal/mol and −8.7 kcal/mol with hydrogen bonding, hydrophilic, and hydrophobic interactions at the active catalytic sites of the enzymes.

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  • MakaleAçık Erişim2022
    Evaluation of the in vitro antioxidant, antidiabetic and anticholinergic properties of rosmarinic acid from rosemary (Rosmarinus officinalis L.)

    Topal, Meryem; Gulcin, İlhami

    In this study, antidiabetic, anticholinergic, and antioxidant abilities of rosmarinic acid were evaluated and compared to standards. To determine its antioxidant activity different in vitro bioanalytical methods, including total antioxidant activity (TAA), ABTS•+ scavenging activity, O2•- scavenging activity, DPPH· scavenging activity, DMPD•+ scavenging activity, potassium ferric cyanide reduction ability, cupric ion (Cu2+) reduction capacity, H2O2 scavenging activity, and ferrous ions (Fe2+) binding activities were separately performed. Also, butylated hydroxyanisole (BHA), Trolox, α-tocopherol, and butylated hydroxytoluene (BHT) were used as the reference antioxidants. Rosmarinic acid inhibited the linoleic acid emulsion peroxidation by 89.2% while BHA, BHT, Trolox and α-tocopherol inhibited as 87.3, 97.6, 90.3 and 75.3%, respectively, at the same concentration (30 μg/mL). When these results are evaluated, rosmarinic acid had effective TAA than BHA and α-tocopherol and close to BHT and Trolox. In addition, rosmarinic acid exhibited Kİ values of 9.67 ± 0.81 nM towards acetylcholinesterase (AChE) and 33.56 ± 2.96 nM against α-glycosidase enzymes.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2021
    LC-HRMS Profiling and Antidiabetic, Anticholinergic, and Antioxidant Activities of Aerial Parts of Kinkor (Ferulago stellata)

    Kiziltas, Hatice; Bingol, Zeynebe; Gören, Ahmet Ceyhan; Kose, Leyla Polat; Durmaz, Lokman; Topal, Fevzi; Alwasel, Saleh H.; Gulcin, Ilhami

    Kinkor (Ferulago stellata) is Turkish medicinal plant species and used in folk medicine against some diseases. As far as we know, the data are not available on the biological activities and chemical composition of this medicinal plant. In this study, the phytochemical composition; some metabolic enzyme inhibition; and antidiabetic, anticholinergic, and antioxidant activities of this plant were assessed. In order to evaluate the antioxidant activity of evaporated ethanolic extract (EEFS) and lyophilized water extract (WEFS) of kinkor (Ferulago stellata), some putative antioxidant methods such as DPPHGreek ano teleia scavenging activity, ABTS(center dot+) scavenging activity, ferric ions (Fe3+) reduction method, cupric ions (Cu2+) reducing capacity, and ferrous ions (Fe2+)-binding activities were separately performed. Furthermore, ascorbic acid, BHT, and alpha-tocopherol were used as the standard compounds. Additionally, the main phenolic compounds that are responsible for antioxidant abilities of ethanol and water extracts of kinkor (Ferulago stellata) were determined by liquid chromatography-high-resolution mass spectrometry (LC-HRMS). Ethanol and water extracts of kinkor (Ferulago stellata) demonstrated effective antioxidant abilities when compared to standards. Moreover, ethanol extract of kinkor (Ferulago stellata) demonstrated IC50 values of 1.772 mu g/mL against acetylcholinesterase (AChE), 33.56 +/- 2.96 mu g/mL against alpha-glycosidase, and 0.639 mu g/mL against alpha-amylase enzyme respectively.

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  • MakaleAçık Erişim2019
    Secondary metabolites of ethanol extracts of pinus sylvestris cones from eastern anatolia and their antioxidant, cholinesterase and α-glucosidase activities

    Topal, Meryem

    Scots pine (Pinus sylvestris) is the most widely distributed tree species among pine species. Antiradical, antioxidant properties and inhibition properties on butyrylcholinesterase (BChE), acetylcholinesterase (AChE) and α-glycosidase activities of ethanol extracts of P. sylvestris were reported from Sarikamis (Kars), Gumushane and Erzurum provinces of Turkey. The cones of P. Sylvestris from Gumushane showed the highest IC50 values in both DPPH. (14.75 µg/mL) and ABTS.+ (12.56 µg/mL) radical scavenging activities. An LC-HRMS method developed and the secondary metabolite composition of extracts were identified. The major compounds are determined as (+)-trans taxifolin, quercitrin, fumaric acid, (-) epicatechin, and nepetin-7-O-glucoside, apigenin-7-O-glucoside in P. sylvestris cones.

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  • MakaleAçık Erişim2019
    Anticholinergic and antidiabetic effects of isoeugenol from clove (Eugenia caryophylata) oil

    Topal, Fevzi

    Isoeugenol (2-methoxy-4-(prop-1-en-1-yl)phenol), a component of from clove (Eugenia caryophylata) oil, is a starting material for both the biotechnological and synthetic production of vanillin and vanillic acid. In this article, the isoeugenol showed excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes, α-glycosidase, and α-amylase. Isoeugenol has the IC50 values of 411.5 for α-amylase, 19.25 nM for α-glycosidase and 77.00 nM for AChE. Ki values of isoeugenol were found as 21 ± 9 nM and 16 ± 3 nM against α-glycosidase and AChE, respectively. On the other hand, tacrine as standard AChE inhibitor exhibited IC50 value of 20.38 nM. α-Glycosidase inhibitors, commonly referred to as starch blockers, are anti-diabetic drugs that help reduce edible blood glucose levels. AChE inhibitors are used for the treatment of some neurologic degenerational diseases, which involve Alzheimer’s disease. Also, there is a growing interest and the need to search for newer effective and safe AChE, α-amylase, and α-glycosidase inhibitors for the treatment of some metabolic disorder.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2019
    The inhibition profile of sesamol against α-glycosidase and acetylcholinesterase enzymes

    Topal, Meryem

    Sesamol (1,3-benzodioxol-5-ol) is found in the oilseed product, sesame. In our study, the inhibitory effects of sesamol compound on acetylcholinesterase and α-glycosidase enzymes were evaluated. Another aim of this study was to compare the inhibitory effects of sesamol to acarbose for α-glycosidase enzyme and tacrine for acetylcholinesterase (AChE). Sesamol exhibited non-competitive inhibition for both metabolic enzymes. IC50 values for AChE and α-glycosidase enzymes were calculated as 86.63 nM and 99.00 nM, respectively. On the other hand, Ki values were calculated as 46.68 nM and 75.33 nM for AChE and α-glycosidase enzymes, respectively. According to the obtained results showed effective inhibition at low concentrations.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleYalnız künye2019
    Inhibition profiles of Voriconazole against acetylcholinesterase, α-glycosidase, and human carbonic anhydrase I and II isoenzymes

    Topal, Fevzi

    In this work, the inhibitory activity of Voriconazole was measured against some metabolic enzymes, including human carbonic anhydrase (hCA) I and II isoenzymes, acetylcholinesterase (AChE), and α-glycosidase; the results were compared with standard compounds including acetazolamide, tacrine, and acarbose. Half maximal inhibition concentration (IC50) values were obtained from the enzyme activity (%)-[Voriconazole] graphs, whereas Ki values were calculated from the Lineweaver-Burk graphs. According to the results, the IC50 value of Voriconazole was 40.77 nM for α-glycosidase, while the mean inhibition constant (Ki) value was 17.47 ± 1.51 nM for α-glycosidase. The results make an important contribution to drug design and have pharmacological applications. In addition, the Voriconazole compound demonstrated excellent inhibitory effects against AChE and hCA isoforms I and II. Voriconazole had Ki values of 29.13 ± 3.57 nM against hCA I, 15.92 ± 1.90 nM against hCA II, and 10.50 ± 2.46 nM against AChE.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2017
    Novel eugenol derivatives: Potent acetylcholinesterase and carbonic anhydrase inhibitors

    Topal, Fevzi; Gulcin, Ilhami; Dastan, Arif; Guney, Murat

    Eugenol was used as starting material to obtain some phenolic compounds. The synthesis of these phenolic compounds was performed in a two-step procedure. The structures of the formed products (novel eugenol derivatives 1–6) have been determined on the basis of NMR spectroscopy and other spectroscopic methods. The compounds were tested in terms of carbonic anhydrase (CA) inhibition potency. Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes, which catalyse the reaction between carbon dioxide (CO2) and water (H2O), to generate bicarbonate (HCO3−) and protons (H+). CO2, HCO3− and H+ are essential molecules and ions for many important physiologic processes occurring in all living organisms. Acetylcholinesterase (AChE, E.C.3.1.1.7) is found in high concentrations in the red blood cells and brain. Novel eugenol derivatives (1–6) were tested for the inhibition of two cytosolic CA isoforms I, and II (hCA I, and II) and AChE. These compounds demonstrated effective inhibitory profiles with Ki values in ranging of 113.48-738.69 nM against hCA I, 92.35-530.81 nM against hCA II, and 90.10-379.57 nM against AChE, respectively. On the other hand, acetazolamide clinically used as CA inhibitor, shoed Ki value of 594.11 nM against hCA I, and 120.68 nM against hCA II, respectively. Also, AChE was inhibited by tacrine as an AChE inhibitor at the 71.18 nM level.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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  • MakaleAçık Erişim2016
    Acetylcholinesterase and carbonic anhydrase isoenzymes I and II inhibition profiles of taxifolin

    Gocer, Hulya; Topal, Fevzi; Topal, Meryem; Küçük, Murat; Teke, Dilek; Gülçin, Ilhami; Alwasel, Saleh H.; Supuran, Claudiu T.

    Taxifolin, also known as dihydroquercetin, is a flavonoid commonly found in plants. Carbonic anhydrase (CA, EC 4.2.1.1) plays an important role in many critical physiological events including carbon dioxide (CO2)/bicarbonate (HCO3-) respiration and pH regulation. There are 16 known CA isoforms in humans, of which human hCA isoenzymes I and II (hCA I and II) are ubiquitous cytosolic isoforms. In this study, the inhibition properties of taxifolin against the slow cytosolic isoenzyme hCA I, and the ubiquitous and dominant rapid cytosolic isoenzyme hCA II were studied. Taxifolin, as a naturally bioactive flavonoid, has a K-i of 29.2nM against hCA I, and 24.2nM against hCA II. For acetylcholinesterase enzyme (AChE) inhibition, K-i parameter of taxifolin was determined to be 16.7nM. These results clearly show that taxifolin inhibited both CA isoenzymes and AChE at the nM levels.

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  • MakaleAçık Erişim2015
    Acethylcholinesterase inhibitory potential and antioxidant properties of pyrogallol

    Ozturk Sarikaya, S. Beyza

    Pyrogallol is found naturally in crops and fruits of many plants. It is also an active ingredient of many pharmaceuticals. For this reason, we employed different in vitro antioxidant assays such as cupric ion Cu2+ reducing power, Fe3+ reducing power, total antioxidant activity by ferric thiocyanate method, ABTS radical scavenging, DMPD radical scavenging, DPPH • scavenging, Fe2+ chelating, O2•- scavenging and H2O2 scavenging activities of pyrogallol. Pyrogallol inhibited 77.95% lipid peroxidation of linoleic acid emulsion at 30 μg/mL concentration. BHA, BHT, α-tocopherol and trolox exhibited inhibitions of 89.88, 89.97, 83.82 and 91.85% against peroxidation of linoleic acid emulsion at the same concentration, respectively. In addition, pyrogallol was an effective of all the scavenging and reducing power results. In this study, pyrogallol was also evaluated as potential inhibitor for acethycholinesterse enzyme. The results showed that pyrogallol exhibited potent acetylcholinesteras inhibitory activity with IC50 and Ki values 10.2 and 8.6 μM, respectively.

    • SDG 3 · Sağlık ve Kaliteli Yaşam
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