Browsing by Author "Alwasel, Saleh H."

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Analysis of Phenolic Compounds by Lc-Hrms and Determination of Antioxidant and Enzyme Inhibitory Properties of Verbascum Speciousum Schrad
(Acg Publications, 2023) Kiziltas, Hatice; Bingol, Zeynebe; Goren, Ahmet C.; Alwasel, Saleh H.; Gulcin, Ilhami
Studies have shown an inverse correlation between age-related illnesses like coronary heart disease and cancer and fruit and vegetable intake. Given the probable health benefits of natural antioxidants from plants, research on them has increased. Verbascum L is a large genus of Scrophulariaceae family and 323 species distributed worldwide. Since Verbascum L. species are plants that are grown in many regions of Turkiye and are used in folk medicine, it is important to evaluate the biological activity of these species. In this study antioxidant properties of Verbascum speciosum Schrad. were investigated. The antioxidant capacities of water and ethanol-based extracts obtained from air parts were evaluated with Fe3+ reducing, CUPRAC, FRAP, DPPH center dot, and ABTS(center dot+) scavenging antioxidant methods. Extracts were also examined to determine their AChE, alpha-glycosidase and alpha-amylase enzyme inhibitions. This investigation could be a basis for further phytochemical investigations of Verbascum speciosum Schrad.
Anticholinergic, Antidiabetic and Antioxidant Activities of Ferula Orientalis L. Determination of Its Polyphenol Contents by Lc-Hrms
(Acg Publications, 2021) Kiziltas, Hatice; Goren, Ahmet C.; Bingol, Zeynebe; Alwasel, Saleh H.; Gulcin, Ilhami
To evaluate the antioxidant activity of evaporated ethanolic extract of Ferula orientalis L. (EEFO) and lyophilized water extract of Ferula orientalis L. (WEFO) several in vitro antioxidant methods such as ABTS(center dot+) scavenging activity, DPPH. scavenging activity, Fe(3+)reduction method, cupric ions (Cu2+) reduction capacity, and metal ion (Fe2+)-binding activities using ferrozine reagent were separately performed. Also, BHT, alpha-tocopherol and ascorbic acid were used as the standard antioxidant molecules. Moreover, some phenolic compounds that are responsible for antioxidant abilities of EEFO and WEFO were determined by LC-HRMS. EEFO and WEFO demonstrated effective antioxidant abilities when compared with the standards. EEFO demonstrated IC50 values of 1.946 mu g/mL against acetylcholinesterase (AChE), 0.815 mu g/mL against alpha-glycosidase, and 0.675 mu g/mL against alpha-amylase.
Comprehensive Metabolic Profiling of Acantholimon Caryophyllaceum Using Lc-Hrms and Evaluation of Antioxidant Activities, Enzyme Inhibition Properties and Molecular Docking Studies
(Elsevier, 2022) Kiziltas, Hatice; Bingol, Zeynebe; Goren, Ahmet Ceyhan; Pinare, Sueuroleyman Mesut; Ortaakarsu, Ahmet Bugra; Alwasel, Saleh H.; Gulcin, Lhami
The Acantholimon taxon consists of thorny, perennial and subshrub flowering plants. Extraction of various Acantholimon species are traditionally applied to treat liver disease and diabetes and roots are boiled used to treat wounds and skin irritation. Here, we quantified, the radical scavenging activities of ethanol (EEAC) and water (WEAC) extracts of Acantholimon caryophyllaceum Boiss (A. caryophyllaceum) against 1,1-diphenyl-2-picryl-hydrazyl (DPPHGreek ano teleia) and 2,2-azino-bis3-ethylbenzthiazoline-6-sulfonic acid (ABTS*+) as well as their abil-ity to reduce Fe3+, Fe3+-TPTZ, and Cu2+. The antioxidant activities of both extracts were similar to those of standards in all assays. For instance, IC50 of EEAC and WEAC for scavenging DPPH were 19.8 and 69.3 mg/mL, respectively. We also assessed the inhibitory effects of EEAC and WEAC against acetylcholinesterase (AChE), a-amylase and a-glycosidase, which are associated with Alzheimer's disease and diabetes. The ethanol extract inhibited these enzymes with IC50 of 1.137, 0.172 and 0.511 mg/mL, respectively. The results of liquid chromatography-high resolution mass spectrometry (LC-HRMS) revealed that (-)-epigallocatechin was the main phenolic compound in both EEAC and WEAC. Molecular docking analysis revealed binding interactions between the main phenolic compounds (-)-epigallocatechin gallate, (-)-epigallocatechin, fumaric acid, hyperoside, and myricetin with AChE, a-amylase and a-glycosidase enzymes.(c) 2022 Published by Elsevier B.V. on behalf of SAAB.
Comprehensive Metabolite Profiling of Berdav Propolis Using Lc-ms/Ms: Determination of Antioxidant, Anticholinergic, Antiglaucoma, and Antidiabetic Effects
(Mdpi, 2023) Karagecili, Hasan; Yilmaz, Mustafa Abdullah; Erturk, Adem; Kiziltas, Hatice; Guven, Leyla; Alwasel, Saleh H.; Gulcin, Ilhami
Propolis is a complex natural compound that honeybees obtain from plants and contributes to hive safety. It is rich in phenolic and flavonoid compounds, which contain antioxidant, antimicrobial, and anticancer properties. In this study, the chemical composition and antioxidant activities of propolis were investigated; ABTS(center dot+), DPPH center dot and DMPD center dot+ were prepared using radical scavenging antioxidant methods. The phenolic and flavonoid contents of propolis were 53 mg of gallic acid equivalent (GAE)/g and 170.164 mg of quercetin equivalent (QE)/g, respectively. The ferric ion (Fe3+) reduction, CUPRAC and FRAP reduction capacities were also studied. The antioxidant and reducing capacities of propolis were compared with those of butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), alpha-tocopherol and Trolox reference standards. The half maximal inhibition concentration (IC50) values of propolis for ABTS(center dot+), DPPH center dot and DMPD center dot+ scavenging activities were found to be 8.15, 20.55 and 86.64 mu g/mL, respectively. Propolis extract demonstrated IC50 values of 3.7, 3.4 and 19.6 mu g/mL against alpha-glycosidase, acetylcholinesterase (AChE) and carbonic anhydrase II (hCA II) enzyme, respectively. These enzymes' inhibition was associated with diabetes, Alzheimer's disease (AD) and glaucoma. The reducing power, antioxidant activity and enzyme inhibition capacity of propolis extract were comparable to those demonstrated by the standards. Twenty-eight phenolic compounds, including acacetin, caffeic acid, p-coumaric acid, naringenin, chrysin, quinic acid, quercetin, and ferulic acid, were determined by LC-MS/MS to be major organic compounds in propolis. The polyphenolic antioxidant-rich content of the ethanol extract of propolis appears to be a natural product that can be used in the treatment of diabetes, AD, glaucoma, epilepsy, and cancerous diseases.
Lc-Hrms Profiling of Phytochemicals, Antidiabetic, Anticholinergic and Antioxidant Activities of Evaporated Ethanol Extract of Astragalus Brachycalyx Fischer
(Acg Publications, 2021) Kiziltas, Hatice; Bingol, Zeynebe; Goren, Ahmet C.; Pinar, Suleyman Mesut; Alwasel, Saleh H.; Gulcin, Ilhami
Astragalus is a perennial plant that has existed for about 2500-3000 years and consists of more than 250 taxonomic parts. Twenty species of Astragalus are endemic to Turkey, as well as the richest genus with 425 taxa. The roots of Asfragalus species are used in folk medicine as hepatoprotective, antioxidant, antibacterial, antihypertensive, antidiabetic and diuretic. Also, it is used to treat diabetes mellitus, leukemia, nephritis and uterine cancer. It is known that in Anatolia, Astragalus roots are traditionally used against leukemia and wound healing. For the purpose, the measuring of antioxidant activity of evaporated ethanol extract of Asfragalus brachycalyx FISCHER (EEAB), some bioanalytic methods including DPPH center dot and ABTS(center dot+) scavenging effects, ferric ions (Fe3+) and cupric ions (Cu2+) reducing abilities, and metal (Fe') chelating activity were realized. alpha-Tocopherol, ascorbic acid, and BHT were used as the standard antioxidants. On the other hand, some phenolic compounds, which responsible for antioxidant activities of EEAB was determined by liquid chromatography-high resolution mass spectrometry (LC-HRMS). At the similar concentration, EEAB exhibited efficient antioxidant effects when compared to standard compounds. Additionally, EEAB showed IC50 values of 1.985 mu g/mL toward acetylcholinesterase (AChE), 0.620 mu g/mL on alpha-glycosidase and 0.306 mu g/mL against alpha-amylase enzymes.
Rosmarinic Acid Inhibits Some Metabolic Enzymes Including Glutathione S-Transferase, Lactoperoxidase, Acetylcholinesterase, Butyrylcholinesterase and Carbonic Anhydrase Isoenzymes
(Taylor & Francis Ltd, 2016) Gulcin, Ilhami; Scozzafava, Andrea; Supuran, Claudiu T.; Koksal, Zeynep; Turkan, Fikret; Cetinkaya, Songul; Alwasel, Saleh H.
Rosmarinic acid (RA) is a natural polyphenol contained in many aromatic plants with promising biological activities. Carbonic anhydrases (CAs, EC 4.2.1.1) are widespread and intensively studied metalloenzymes present in higher vertebrates. Acetylcholinesterase (AChE, E.C. 3.1.1.7) is intimately associated with the normal neurotransmission by catalysing the hydrolysis of acetylcholine to acetate and choline and acts in combination with butyrylcholinesterase (BChE) to remove acetylcholine from the synaptic cleft. Lactoperoxidase (LPO) is an enzyme involved in fighting pathogenic microorganisms, whereas glutathione S-transferases (GSTs) are dimeric proteins present both in prokaryotic and in eukaryotic organisms and involved in cellular detoxification mechanisms. In the present study, the inhibition effects of rosmarinic acid on tumour-associated carbonic anhydrase IX and XII isoenzymes, AChE, BChE, LPO and GST enzymes were evaluated. Rosmarinic acid inhibited these enzymes with K(i)s in the range between micromolar to picomolar. The best inhibitory effect of rosmarinic acid was observed against both AChE and BChE.
Sahlep (Dactylorhiza Osmanica): Phytochemical Analyses by Lc-Hrms, Molecular Docking, Antioxidant Activity, and Enzyme Inhibition Profiles
(Mdpi, 2022) Kiziltas, Hatice; Goren, Ahmet Ceyhan; Alwasel, Saleh H.; Gulcin, Ilhami
Studies have shown an inverse correlation among age-related illnesses like coronary heart disease and cancer and intake of fruit and vegetable. Given the probable health benefits of natural antioxidants from plants, research on them has increased. Dactylorhiza osmanica is consumed as a food and traditional medicine plant in some regions of Turkey, so evaluation of the biological ability of this species is important. In this study, the amount of phenolic content (LC-HRMS), antioxidant activities and enzyme inhibitory properties of an endemic plant, D. osmanica, were investigated. The antioxidant capacities of an ethanol extract of D. osmanica aerial parts (EDOA) and roots (EDOR) were evaluated with various antioxidant methods. Additionally, the enzyme inhibitory effects of EDOA and EDOR were examined against acetylcholinesterase (AChE), alpha-glycosidase, and alpha-amylase enzymes, which are associated with common and global Alzheimer's disease and diabetes mellitus. The IC50 values of EDOA against the enzymes were found to be 1.809, 1.098, and 0.726 mg/mL, respectively; and the IC50 values of EDOR against the enzymes were found to be 2.466, 0.442, and 0.415 mg/mL, respectively. Additionally, LC-HRMS analyses revealed p-Coumaric acid as the most plentiful phenolic in both EDOA (541.49 mg/g) and EDOR (559.22 mg/g). Furthermore, the molecular docking interaction of p-coumaric acid, quercitrin, and vanillic acid, which are the most plentiful phenolic compounds in the extracts, with AChE, alpha-glucosidase, and alpha-amylase, were evaluated using AutoDock Vina software. The rich phenolic content and the effective antioxidant ability and enzyme inhibition potentials of EDOA and EDOR may support the plant's widespread food and traditional medicinal uses.
Synthesis of New Cyclic Thioureas and Evaluation of Their Metal-Chelating Activity, Acetylcholinesterase, Butyrylcholinesterase, and Carbonic Anhydrase Inhibition Profiles
(Wiley, 2017) Taslimi, Parham; Sujayev, Afsun; Garibov, Emin; Nazarov, Nazar; Huyut, Zubeyir; Alwasel, Saleh H.; Gulcin, Ilhami
In the presence of trifluoracetic acid (TFAA), an efficient method for the synthesis of tetra(hexa)hydropyrimidinethione-carboxylates has been used on the basis of three-component condensation of thiourea with its different aldehydes and -diketones. Some novel cyclic thioureas were synthesized, and their hCA I, hCA II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibitors and metal-chelating properties were evaluated. K-i values of novel synthesized compounds for AChE and BChE are in the range of 51.84-135.96 and 143.96-274.55 nM, respectively. Also, HCA I and II were effectively inhibited by these novel compounds, with K-i values in the range of 404.16-745.13 nM for hCA I and of 434.20-689.57 nM for hCA II, respectively. Additionally, acetazolamide (AZA), clinically used as a CA inhibitor, with a K-i value of 883.68 +/- 121.27 nM in hCA I and 1008.66 +/- 144.70 nM in hCA II. Also, tacrine inhibited AChE and BChE showed K-i values of 314.63 +/- 31.66 and 373.57 +/- 75.07 nM, respectively.