Meryem Topal

Bio: Meryem Topal is an academic researcher from Gümüşhane University. The author has contributed to research in topics: Carbonic anhydrase & DPPH. The author has an hindex of 11, co-authored 14 publications receiving 911 citations. Previous affiliations of Meryem Topal include Atatürk University.

Synthesis and carbonic anhydrase isoenzymes I, II, IX, and XII inhibitory effects of dimethoxybromophenol derivatives incorporating cyclopropane moieties.

Abstract: Cyclopropylcarboxylic acids and esters and cyclopropylmethanols incorporating bromophenol moieties were investigated as inhibitors of the carbonic anhydrase enzyme (CA; EC 4.2.1.1). The cis- and trans-esters 5 and 6 were obtained from the reaction of 4-allyl-1,2-dimethoxybenzene (4) with ethyl diazoacetate, which after bromination with Br2 gave two isomeric monobromides (11 and 15), four isomeric dibromides (12, 13, 16, and 17), and two isomeric tribromides (14 and 18). The carboxylic acids 7, 8, and 19–26 were thereafter obtained by hydrolysis of the synthesized esters. All these bromophenol derivatives were tested against human (h) CA isoenzymes I and II (cytosolic, ubiquitous isoforms) and hCA IX and XII (transmembrane, tumor-associated enzymes). All tested bromophenols exhibited excellent inhibitory effects, in the low nanomolar range, with Ki values in the range of 0.54–59 nM against hCA I and in the range of 0.97–12.14 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and...

Rosmarinic acid: a potent carbonic anhydrase isoenzymes inhibitor

Abstract: Rosmarinic acid is a water-soluble ester of caffeic acid and 3,4-dihydroxyphenyllactic acids, and is mainly found in plant species including Boraginaceae and Lamiaceae. In this research, we determined the inhibition property of rosmarinic acid on carbonic anhydrase isoenzymes I and II (hCA I and II) purified from human erythrocytes by using Sepharose-4B affinity column chromatography. hCA I and II isoenzymes were obtained with a yield of 57.9% and 67.2% and 76.5- and 509.3-fold purification of each isoenzyme, respectively. In order to show the purity of the isoenzymes, SDS-PAGE was performed and one band was observed. In vitro inhibition of both hCA I and II isoenzymes by rosmarinic acid using CO2-esterase activity gave Ki values of 86.0 m M and 57.0 m M, respectively.

Antioxidant, antiradical, and anticholinergic properties of cynarin purified from the Illyrian thistle (Onopordum illyricum L.).

Abstract: Cynarin is a derivative of hydroxycinnamic acid and it has biologically active functional groups constituent of some plants and food. We elucidated the antioxidant activity of cynarin by using different in vitro condition bioanalytical antioxidant assays like DMPD•+, ABTS•+, , DPPH• and H2O2 scavenging effects, the total antioxidant influence, reducing capabilities, Fe2+ chelating and anticholinergic activities. Cynarin demonstrated 87.72% inhibition of linoleic acid lipid peroxidation at 30 µg/mL concentration. Conversely, some standard antioxidants like trolox, α-tocopherol, butylated hydroxytoluene (BHT), and butylated hydroxyanisole (BHA) exhibited inhibitions of 90.32, 75.26, 97.61, 87.30%, and opponent peroxidation of linoleic acid emulsion at the identical concentration, seriatim. Also, cynarin exhibited effective DMPD•+, ABTS•+, , DPPH•, and H2O2 scavenging effects, reducing capabilities and Fe2+ chelating effects. On the contrary, IC50 and Ki parameters of cynarin for acetylcholinesterase...

Acetylcholinesterase and carbonic anhydrase isoenzymes I and II inhibition profiles of taxifolin

Abstract: 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 () 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 Ki of 29.2 nM against hCA I, and 24.2 nM against hCA II. For acetylcholinesterase enzyme (AChE) inhibition, Ki parameter of taxifolin was determined to be 16.7 nM. These results clearly show that taxifolin inhibited both CA isoenzymes and AChE at the nM levels.

Antioxidants and antioxidant methods: an updated overview

Abstract: Antioxidants had a growing interest owing to their protective roles in food and pharmaceutical products against oxidative deterioration and in the body and against oxidative stress-mediated pathological processes. Screening of antioxidant properties of plants and plant-derived compounds requires appropriate methods, which address the mechanism of antioxidant activity and focus on the kinetics of the reactions including the antioxidants. Many studies evaluating the antioxidant activity of various samples of research interest using different methods in food and human health have been conducted. These methods are classified, described, and discussed in this review. Methods based on inhibited autoxidation are the most suited for termination-enhancing antioxidants and for chain-breaking antioxidants, while different specific studies are needed for preventive antioxidants. For this purpose, the most common methods used in vitro determination of antioxidant capacity of food constituents were examined. Also, a selection of chemical testing methods was critically reviewed and highlighted. In addition, their advantages, disadvantages, limitations and usefulness were discussed and investigated for pure molecules and raw extracts. The effect and influence of the reaction medium on the performance of antioxidants are also addressed. Hence, this overview provides a basis and rationale for developing standardized antioxidant methods for the food, nutraceuticals, and dietary supplement industries. In addition, the most important advantages and shortcomings of each method were detected and highlighted. The chemical principles of these methods are outlined and critically discussed. The chemical principles of methods of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) radical (ABTS·+) scavenging, 1,1-diphenyl-2-picrylhydrazyl (DPPH·) radical scavenging, Fe3+-Fe2+ transformation assay, ferric reducing antioxidant power (FRAP) assay, cupric ions (Cu2+) reducing power assay (Cuprac), Folin-Ciocalteu reducing capacity (FCR assay), peroxyl radical (ROO·), superoxide radical anion (O2·-), hydrogen peroxide (H2O2) scavenging assay, hydroxyl radical (OH·) scavenging assay, singlet oxygen (1O2) quenching assay, nitric oxide radical (NO·) scavenging assay and chemiluminescence assay are outlined and critically discussed. Also, the general antioxidant aspects of main food components were discussed by a number of methods, which are currently used for the detection of antioxidant properties of food components. This review consists of two main sections. The first section is devoted to the main components in the food and pharmaceutical applications. The second general section comprises some definitions of the main antioxidant methods commonly used for the determination of the antioxidant activity of components. In addition, some chemical, mechanistic and kinetic basis, and technical details of the used methods are given.

Advances in structure-based drug discovery of carbonic anhydrase inhibitors.

Abstract: Introduction: The enzyme carbonic anhydrase (CA, EC 4211) is found in numerous organisms across the tree of life, with seven distinct classes known to date CA inhibition can be exploited for th

Antioxidant activity and phenolic compounds of ginger (Zingiber officinale Rosc.) determined by HPLC-MS/MS

Abstract: Oxidative stress related diseases often arise from over production of free radicals and reactive oxygen/nitrogen species. The prevention of these diseases could be possible with the use of natural antioxidant plants that could be promising as therapeutic candidates. Since antioxidant properties of a species could be stem from phenolic compounds, it is, therefore, important to evaluate antioxidant and total/individual phenolic and flavonoid content. For this purpose, we evaluated antioxidant properties of ginger (Zingiber officinale Rosc.) based on three parameters: the antioxidant capacity, total phenolic and flavonoid content as well as identification of phenolic acids of water extract (WEG) and ethanol extract (EEG) of ginger. For antioxidant capacity, we performed FRAP, CUPRAC assay, Fe2+ chelating ability, DPPH and DMPD radical scavenging activities. Also, total phenolic and flavonoid contents in both extracts were also measured via Folin Ciocalteu’s method. For identification of phenolic acids, HPLC-MS/MS method was performed. The results showed that EEG had generally better antioxidant activity than WEG in all assays. HPLC-MS/MS analysis showed that there are at least eight different phenolic acids found in ginger, among which pyrogallol p-hydroxybenzoic acid, ferulic acid and p-coumaric acid were more abundant in both extracts. This study clearly showed that ginger extracts demonstrated effective antioxidant properties and their consumption may reduce or delay the progression of diseases that oxidative stress take place due to lack of antioxidant supplementation.

Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: Three for the price of one.

Abstract: Human carbonic anhydrase (CA) IX is a tumor-associated protein, since it is scarcely present in normal tissues, but highly overexpressed in a large number of solid tumors, where it actively contributes to survival and metastatic spread of tumor cells. Due to these features, the characterization of its biochemical, structural, and functional features for drug design purposes has been extensively carried out, with consequent development of several highly selective small molecule inhibitors and monoclonal antibodies to be used for different purposes. Aim of this review is to provide a comprehensive state-of-the-art of studies performed on this enzyme, regarding structural, functional, and biomedical aspects, as well as the development of molecules with diagnostic and therapeutic applications for cancer treatment. A brief description of additional pharmacologic applications for CA IX inhibition in other diseases, such as arthritis and ischemia, is also provided.