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Synthesis of new fluorinated sulfonates and their Schiff bases as anti-Alzheimer drug candidates: An in vitro-in silico study
(Elsevier B.V., 2025) Çakmak, Reşit; Başaran, Eyüp; Ercan, Selami; Boğa, Mehmet; Çınar, Ercan; Topal, Giray
In this research, we designed and synthesized a series of new 3- or 4-(trifluoromethyl)- substituted sulfonate esters (1–14) linked heterocyclic Schiff base derivatives (15–28) as potential inhibitors of acetylcholinesterase and butyrylcholinesterase. The chemical structures of the target compounds were elucidated using elemental analysis and various spectral techniques. In vitro inhibitory results revealed IC50 values ranging from 12.05±0.10 to 43.08±0.20 μM against acetylcholinesterase and 0.42±0.04 to 95.52±0.00 μM against butyrylcholinesterase. Among the tested compounds, most sulfonates were found to inhibit acetylcholinesterase better than butyrylcholinesterase. In contrast, their Schiff base derivatives inhibited butyrylcholinesterase more effectively acetylcholinesterase did. Compounds 19, 20, and 21 inhibited butyrylcholinesterase better than galanthamine. The effects of trifluoromethyl group at positions 3 or 4 of the sulfonate moiety and the biosubstitutions at position R2 of the spacer moiety on the inhibitory activities were evaluated. Moreover, the antioxidant potency of these compounds was assessed by three different assays (DPPH free radical scavenging activity, ABTS cationic radical decolorization, and cupric reducing antioxidant capacity. The newly synthesized derivatives showed very low antioxidant activity (>1000 μM) in the DPPH and ABTS assays, while some of 3- trifluoromethyl substituted Schiff base derivatives (compounds 15, 20, and 21) showed activity closer to α-tocopherol in cupric reducing antioxidant capacity assay. The binding modes and binding free energies for acetylcholinesterase and butyrylcholinesterase inhibitor candidates were determined through docking studies. Taken together, we consider some inhibitor candidates to be valuable lead structures that can be used in further studies to design new anti-Alzheimer's disease drugs. © 2025 Elsevier B.V.
LC-HRMS profiling of phytochemicals with assessment of antioxidant, anticholinesterase, and antimicrobial potentials of astragalus brachystachys DC
(Wiley-V C H Verlag Gmbh, 2024) Ersoy, Ezgi; Boğa, Mehmet; Kaplan, Alevcan; Kara, Emel Mataracı; Özkan, Esra Eroğlu; Kayıran, Serpil Demirci
Astragalus species are ubiquitous in the pharmacopeia of numerous countries, signifying their widespread medicinal applications. T & uuml;rkiye is esteemed as one of the principal epicenters of diversity for this genus with 483 taxa, and many of these plants have been traditionally utilized for diseases including coughing, diabetes, cardiovascular disorders, and aches. Although there is a considerable body of chemical and biological research available on several Astragalus species, studies focusing on Astragalus brachystachys DC are exceedingly rare. In this context, This study provides the first comprehensive report on this medicinal plant the chemical constituents and biological activities of an important medicinal plant, Astragalus brachystachys DC. The aerial part samples were collected from Adana, T & uuml;rkiye, and an ethanol extract was prepared with these parts. The secondary metabolites of the extract were determined by an LC-HRMS analysis. The LC-HRMS analysis showed the presence of 39 different constituents, hyperoside (303.419 +/- 10.50 mu g/g extract), p-coumaric acid (256.975 +/- 8.51 mu g/g extract), and rutin (72.684 +/- 2.23 mu g/g extract) were determined as major compounds in the aerial parts ethanol extract. Attributed to its high total phenolic (58.53 +/- 1.30 mu g PEs/mg extract) and total flavonoid content (29.98 +/- 0.83 mu g QEs/mg extract), the extract demonstrated strong antioxidant activity according to three different assays namely DPPH free (IC50: 33.08 +/- 0.61 mu g/mL), and ABTS cation radical scavenging (IC50: 15.39 +/- 0.72 mu g/mL) and CUPRAC activity (A0.5: 36.25 +/- 0.28 mu g/mL) methods. In vitro assays showed that cholinesterase inhibitory activity results were found to be exceptional with 85.95 +/- 0.52 % inhibition on acetylcholinesterase and 66.32 +/- 1.33 % inhibition on butyrylcholinesterase at 200 mu g/mL. Regarding antimicrobial properties, Astragalus brachystachys DC extract was found to be effective against Enterococcus faecalis with a MIC value of 39.06 mu g/mL.
Phytochemical profiling by UHPLC–ESI–MS/MS, in vitro antioxidant, in vivo antidiabetic, and pro-sexual effects of salvia balansae noë ex coss. flower extract in diabetic male rats
(Wiley-V C H Verlag Gmbh, 2025) Souidi, Wadjila S.; Belhocine, Mansouria; Bouzouina, Mohamed; Yılmaz, Mustafa Abdullah; Feknous, Ines; Çakır, Oğuz; Tarhan, Abbas
Our study assessed the phytochemical composition and the effects of Salvia balansae flower aqueous extract (FAE) on sexual dysfunction in diabetic rats. Total phenolic and flavonoid content, quantification of phytochemicals by ultrahigh performance liquid chromatography (UHPLC)-electrospray ionization (ESI)-tandem mass spectrometry (MS/MS) method, and in vitro antioxidant capacity of FAE extract were elucidated. For the in vivo study, diabetes was induced by one intraperitoneal injection of streptozotocin (STZ) (40 mg/kg), and treated diabetic rats were given FAE at 200 mg/kg. Rats were subjected to a sexual incentive motivation test (SIM) and a mating behavior test, and then serum testosterone levels and sperm quality were analyzed. Our study indicates that FAE contained a large amount of phenolic compounds and flavonoids, and 13 constituents were quantified; cynaroside (3.8 mg analyte/g extract) was the main compound, followed by rosmarinic acid (3.145 mg analyte/g extract), thus confirming its high antioxidant capacity. FAE treatment significantly reduced blood glucose levels, improved sexual motivation and copulatory behavior, increased testosterone levels, and enhanced sperm quality in diabetic-treated rats compared to diabetic untreated rats. The present work demonstrates the therapeutic potential of S. balansae flowers in enhancing reproductive function in diabetic rats, potentially through its antioxidant, antihyperglycemic, and aphrodisiac properties.
Phytochemical analysis and assessment of antioxidant and enzyme inhibitory activity of alchemilla pseudocartalinica Juz.
(Wiley-V C H Verlag Gmbh, 2024) Uzunkaya, Çağla; Gökkaya, İçim; Akkaya, Didem; Soral, Michal; Seyhan, Gökçe; Barut, Burak; Yılmaz, Mustafa Abdullah
This study aimed to evaluate and compare the antioxidant capacity and enzyme inhibitory activity of extracts, sub-extracts, and fractions prepared from the aerial parts and roots of A. pseudocartalinica. The phytochemical content of the active extracts was also analyzed. According to the results, ellagic acid (38.42 mg/g) was the major compound in the aerial part methanol extract and catechin (185.30 mg/g) in the root methanol extract. The DPPH inhibition activity of all fractions was monitored, with the most active one (Fr B) reaching an IC50 value of (4.92 +/- 0.59 mu g/mL). All the fractions prepared from the aerial parts' water sub-extract showed higher a-glucosidase inhibitory activity than the positive control acarbose. In the tyrosinase assay, Fr B (58.81 +/- 7.50 mu g/mL) exhibited the highest inhibitory actions among all fractions. The structure of the major substances of the most active fraction were elucidated as quercetin 7-O-beta-glucopyranosyl-3-O-beta-glucuronopyranoside- (1), and alpha-[(2-formyl-5-hydroxymethyl)pyrrol-1-yl]aspartic acid (2).
Phenolic compounds, antioxidant and antibacterial activities of cedrus Atlantica stem barks
(Springer, 2024) Benmerache, Abbes; Kabouche, Ahmed; Kabouche, Zahia; Öztürk, Mehmet; Çakır, Cansel; Yılmaz, Mustafa Abdullah; Ertaş, Abdulselam
Stem barks of Cedrus atlantica were investigated for their antioxidant and antibacterial activities and their chemical composition. The phenolic ingredients of the extracts were studied using LC-MS/MS against twenty-seven phenolic compounds. The antioxidant activity was evaluated by DPPH, O-2-DMSO-alkaline, ABTS, beta-carotene-linoleic acid and CUPRAC assays, while the antibacterial activity was performed using the disk diffusion and MIC assays. In addition, the phenolic and flavonoid contents were determined as gallic acid and quercetin equivalents, respectively. Ethyl acetate extract exhibited the highest activity in DPPH, O-2-DMSO alkaline, ABTS, beta-carotene linoleic acid and CUPRAC assays (IC50 = 10.85 +/- 1.41, 3.36 +/- 0.40, 0.74 +/- 0.03, 10.03 +/- 0.01, A(0.50) = 23.56 +/- 1.67 mu g/mL, respectively), followed by n-butanol and hydromethanol extracts. In addition, the ethyl acetate and n-butanol extracts showed remarkable antibacterial activity against Enterobacter aerogenes and Staphylococcus aureus (ATCC 43300), respectively. The LC-MS/MS analyses of all extracts afforded high amounts of quinic acid, malic acid, rosmarinic acid, protocatechuic acid, chlorogenic acid, coumarin, vanillin, and quercetin, exhibiting antioxidant activity.
Evaluation of the antioxidant, antidiabetic and anti-alzheimer effects of Capsella bursa-pastoris-Polyphenolic Profiling by LC-MS/MS
(Acg Publications, 2024) Karageçili, Hasan; Polat, Tuğba; Yılmaz, Mustafa Abdullah; Fidan, Mehmet; Karaismailoğlu, Mehmet Cengiz; Gülçin, İIhami
Capsella bursa-pastoris species of the Capsella herb were examined in this study for sreening of antioxidant, antidiabetic and anti-Alzheimer effects. Traditionally, people consumed C. bursa-pastoris against famine and satisfy their hunger. C. bursa-pastoris species have been shown to have utility as food, medicine, and industrial materials after extensive investigation. The antioxidant properties of methanol and water extracts of C. bursa-pastoris species were assessed using; Fe3+-2,4,6-tris(2-pyridyl)-S-triazine (TPTZ), ferric (Fe3+), and cupric (Cu2+) iobs reducing assays, as well as 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid radical (ABTS(center dot+)) and N,N-dimethyl-p-phenylenediamine (DMPD) radical scavenging activities. The antioxidant and reducing capacity of C. bursa-pastoris species aerial parts water and methanol extracts were compared with standard antioxidants. The phenolic and flavonoid contents in methanol and water extracts of C. bursa-pastoris species were measured 6.86 to 12.00 mg GAE/g and 61.67 to 145.0 mg QE/g, respectively. The inhibitions of effects of water and methanol extract of C. bursa-pastoris species against alpha-amylase, and acetylcholinesterase (AChE) enzymes were investigated. The IC50 values were found as 168.6 to 238.6 mu g/mL against alpha-amylase and 19.0 to 20.9 mu g /mL against AChE. The number of fenolik compounds in both extracts of C. bursa-pastoris species were recorded using LC-MS/MS. The major phenolic and flavonoid components detected in methanol extract of C. bursa-pastoris were quinic acid (22.629 mg/g), chlorogenic acid (3.211 mg/g), rutin (1.930 mg/g), hesperidin (0.893 mg/g), and isoquercitrin (0.783 mg/g). In a similar order, quinic acid (11.356 mg/g), cyranoside (9.463 mg/g), chlorogenic acid (6.072 mg/g), hesperidin (5.912 mg/g), and isoquercitrin (5.364 mg/g) were found as plentyfull pehenolic antioxidants in methanolic extract. The results clearly demonstrated that polyphenolic antioxidants-rich ingredients of the aerial parts of C. bursa-pastoris species are biological phenolic comounds have persuasive usage in the medication of diabetes and Alzheimer's diseases.
The anti-candidal activity of salvia verticillata subsp. verticillata against several candida species
(Salahaddin University, 2024) Ibrahim, Mahdi Hashim; Surchi, Badr Qader; Azeez, Safiya A.; Alma, M. Hakkı; Kireçci, Ekrem; Yılmaz, Mustafa Abdullah; Uğuz, Metin Tansu
The examination of Salvia verticillata extract encompassed an exploration of its anti-Candida properties, phytochemical composition, antioxidant activity, and the quantification of total tannins. The use of ethanol as a solvent yielded the highest extraction efficiency at 26.1%. The plant exhibited a substantial tannin content of 6.5 mg/kg, signifying a noteworthy concentration. The inhibitory zones against Candida tropicalis reached a minimum diameter of 17.6 mm, while Candida guilliermondii displayed the most significant inhibition with a zone diameter of 21.8 mm. The minor inhibitory concentration (MIC) findings for all Candida species ranged from 6.25 to 12.5 g/ml. In the case of Candida guilliermondii, the synthetic antifungal activity FLU/25 demonstrated a maximal inhibition zone measuring 39.30 mm. Additionally, the maximum antioxidant activity, recorded at 0.3 ml, reached a value of 98.65. Phytochemical screening unveiled elevated concentrations of phenols and flavonoids, with malic acid (1901.1 g/g), hesperidin (302.4 g/g), and rosmarinic acid (30619.93 g/g) all experiencing an increase in concentration. These findings provide a comprehensive understanding of the diverse bioactive components and properties associated with Salvia verticillata extract.
Investigation of algerian crataegus monogyna jacq phenolic compounds (Using LC-ESI-MS/MS analysis, antioxidant activity, and enzyme inhibition) and their potential implications for food and nutraceutical applications
(Multidisciplinary Digital Publishing Institute (MDPI), 2024) Goudjil, Sabrina; Boussekine, Samira; Goudjil, Sarra; Goudjil, Hanane; Yılmaz, Mustafa Abdullah; Ola, Mohammad Shamsul; Ali, Ahmad; Çakır, Oğuz
Investigations into the phenolic constituents of the butanolic fraction of Crataegus monogyna were optimized using LC-ESI-MS/MS analysis, identifying and quantifying at least 23 fingerprint phytochemical compounds. The major phenolic compounds were epicatechin (99.916 ± 2.208 mg/g), isoquercetrin (53.31 ± 1.172 mg/g), chlorogenic acid (47.457 ± 1.010 mg/g), quinic acid (37.819 ± 1.406 mg/g), rutin (29.98 ± 0.740 mg/g), hesperidin (5.296 ± 0.177 mg/g, detected for the first time in the C. monogyna species), astragalin (1.774 ± 0.020 mg/g), and nicotiflorin (1.482 ± 0.016 mg/g). The antioxidant properties of the lyophilized butanolic fraction were evaluated using DPPH, GOR, ABTS, CUPRAC, and reducing power assays, all of which demonstrated that there was strong activity. Additionally, the neuroprotective effect was evaluated in vitro, showing a potent inhibitory effect on acetylcholinesterase (AChE) with an IC50 of 43.65 ± 2.10 µg/mL. The antidiabetic effect was investigated through α-amylase inhibition (IC50 = 91.19 ± 0.10 µg/mL), showing high inhibitory activity. In addition, the butanolic extract exhibited significant urease inhibition with an IC50 of 26.36 ± 0.05 µg/mL. These results suggest that Algerian C. monogyna has potential as a therapeutic agent for managing diabetes complications and as a natural source of AChE inhibitors, making it a promising subject for the treatment of urease-related conditions. Its high concentrations of natural antioxidants, such as epicatechin, isoquercetrin, chlorogenic acid, quinic acid, rutin, hesperidin, and astragalin, make it suitable for integration into medicine, pharmaceuticals, cosmetics, and the food sector.
Nizip Yaglık olive leaves (Olea europaea L.) collected at different seasons and altitudes: Enzyme inhibition, antioxidant activities and phenolic compound profiles
(Elsevier Ltd., 2024) Kaygısız, Feyza; Kaya, Elife; Yılmaz, Mustafa Abdullah
This study aimed to evaluate the antioxidant activity (DPPH, ABTS, CUPRAC, and iron-reducing power methods) phenolic component profiles (by LC-MS/MS), and cholinesterase enzyme inhibition of Nizip Yaglık olive leaf extracts. The leaves were collected from the Nizip district of Gaziantep province at three different altitudes and during four different seasons. The winter season Kocatepe location extract (W3), at a concentration of 160 μg/mL, demonstrated the highest antioxidant activity among all olive leaf extracts. The major components identified by LC-MS/MS analysis were cynaroside (luteolin-7-glucoside) and quinic acid among fifty-three components, with the highest concentration found in the summer season Kocatepe location extract (SU3, 18.986 mg/g) and the autumn season Kerzin location extract (A1, 14.147 mg/g) respectively. Fingerprint phytochemical analysis was also performed for four compounds (3-hydroxytyrosol, oleuropein, diosmin, verbascoside) on the extracts. Oleuropein and verbascoside were determined as 56.738 mg/g in the winter season Kocatepe location (W3) extract and 8.853 mg/g in the spring season Kerzin location (S1) extract, respectively. The spring season İkizce location extract (S2, IC50: 10.16 μg/mL) exhibited the strongest inhibition on the AChE enzyme, while the spring season Kocatepe location extract (S3, IC50: 7.73 μg/mL) exhibited the highest inhibition on the BChE enzyme. The study concluded that olive leaves have increased antioxidant and enzyme inhibition potential, especially when harvested in the winter and spring seasons and at higher altitudes. These findings suggested that Nizip Yaglık olive leaves could be valuable for therapeutic drug production and pharmacological research due to their rich phenolic content and high antioxidant activity.
Application of continuous wavelet transforms for simultaneous estimation of domperidone and lansoprazole in capsule formulations
(Elsevier B.V., 2025) Ertekin, Zehra Ceren; Büker, Eda; Oral, Elif Varhan; Dinç, Erdal
UV–Vis spectroscopy remains essential in pharmaceutical research and quality control due to its accessibility, simplicity, and effectiveness. However, overlapping spectra resulting from multicomponent drug formulations present challenges. Here, we describe a signal processing strategy using continuous wavelet transform (CWT) to resolve overlapping spectra of domperidone (DMP) and lansoprazole (LSP) for simultaneous quantification. Three different wavelet functions (Symlets 3, Coiflets 1, Daubechies 10), were found to be suitable for this purpose. Linear calibration curves were constructed using the CWT zero-crossing technique and the methods were validated by analyzing a set of synthetic mixtures, intra-and inter-day samples, and standard addition samples. The assay results of commercial capsule samples were compared with those obtained by derivative spectroscopy, and no significant statistical difference was observed. The proposed CWT methods demonstrated good compliance with the label claims and proved to be reliable, versatile, fast, and cost-efficient analytical methods without the need for preliminary separation procedures.
Investigation of antihyperglycemic potentials of seven Centaurea L. species through in vitro studies and characterization of possible bioactive phenolics by LC–MS/MS and molecular docking approach
(Elsevier B.V., 2025) Kahraman, Çiğdem; Aydın, Zekiye Ceren Arıtuluk; Yılmaz, Mustafa Abdullah; Çakır, Oğuz; Özenver, Nadire
The taxon Centaurea L., a natural wealth with a high endemism rate in Türkiye, has been traditionally used in treating diabetes. This study aimed to determine the diabetes-associated biological activities and phytochemical content of different solvent extracts of Centaurea benedicta (L.) L, C. cariensis Boiss. subsp. microlepis (Boiss.) Wagenitz, C. drabifolia Sm. subsp. cappadocica (DC.) Wagenitz, C. iberica Trev. ex. Sprengel, C. solstitialis L. subsp. solstitialis, C. urvillei DC. subsp. stepposa Wagenitz, and C. virgata Lam. via in vitro and in silico methods. The antihyperglycemic potentials were estimated by determining the extracts’ α-amylase, α-glucosidase, and DPP-4 enzyme inhibitory abilities. The antioxidant capacities along with the total phenolic and flavonoid contents of the plant extracts were estimated by various methods. An LC-MS/MS analysis was used for the quantitative determination of the phytochemical components of the active extracts. In silico docking approach pointed out possible substances accounting for biological activity. Evaluating the α-glucosidase inhibitory activity of the plant extracts, the methanol and ethyl acetate extracts of C. urvillei were identified as the most active plant extracts with the lowest IC50 values on α-glucosidase (17.9 and 17.6 µg/mL, respectively). None of the tested extracts inhibited α-amylase and DPP-4. The most abundant compounds in the active extracts were achieved by the LC-MS/MS method. Among those, cosmosiin and cynaroside were identified as promising antihyperglycemic agents based on molecular docking studies, suggesting their potential accounting for α-glucosidase inhibitory activity. Alcoholic and hydroalcoholic plant extracts generally exerted high antioxidant capacity. To conclude, specifically C. urvillei extracts along with cosmosiin and cynaroside were determined as potential and promising antihyperglycemic agents. The traditional usage of Centaurea species was verified, leading to the design of forthcoming projects associated with the antihyperglycemic potential of Centaurea species.
Biological activities and phytochemical investigation of some Sideritis species
(National Institute of Science Communication and Policy Research, 2024) Eruygur, Nuraniye; Kırcı, Damla; Ayaz, Fatma; Bağcı, Yavuz; Doğu, Süleyman; Yılmaz, Mustafa Abdullah
One of the most generally used plants for herbal tea is Sideritis L. species (Lamiaceae) which is commonly grown in the Mediterranean region and represented by 46 species and 53 taxa in Türkiye. Sideritis species are widely used in Türkiye due to their antispasmodic, antirheumatic, anti-inflammatory, and diuretic activities. In the present research, the effects against oxidative stress, and enzyme activitiy, as well as chemical compositions of the water and methanol extracts of seven Sideritis species (S. bilgeriana P.H. Davis), S. brevidens P.H. Davis, S. cilicica Boiss. & Balansa, S. erythrantha Boiss. & Heldr., subsp. cedretorum P. H. Davis, S. hololeuca Boiss. & Heldr., S. libanotica Labill. subsp. linearis (Benth.) Bornm., and S. libanotica Labill. subsp. violascens P. H. Davis.). Its main objective was to assess the suppression of five enzymes, tyrosinase, α-glucosidase, α-amylase, acetylcholinesterase (AChE), and butyrylcholinesterase, for the water and methanol extracts of seven different Sideritis species. The extracts were also assessed for antioxidant effects using various spectrophotometric methods involving DPPH,ABTS·+, and iron chelating, as well as the determination of total phenol and flavonoid amounts. As for the phytochemical investigation on Sideritis species, the phenolic compounds of the extracts were determined by LC-MS/MS analysis. Because of the LC-MS/MS analysis, Hierarchical Cluster Analysis was performed on four major components: quinic acid, chlorogenic acid, fumaric acid, and acacetin in the present work. As a result, our research indicates that Sideritis species, particularly S. cilicica, S. erythrantha, and S. libanotica subsp. linearis, deserve to be examined afterwards for their active secondary metabolites, which are thought to be responsible for their potential biological activities. Furthermore, the composition of extracts of Sideritis species was statistically analysed using the principal component.
Broccoli pomace: effect of drying methods and temperature on the grinding process and physicochemical properties
(Polska Akademia Nauk, 2024) Krajewska, Anna; Dziki, Dariusz; Yılmaz, Mustafa Abdullah; Özdemir, Fethi Ahmet
The objective of this study was to evaluate the impact of different drying methods and temperatures on the physicochemical properties of broccoli pomace. The broccoli juice by-product was subjected to contact-drying at temperatures of 40°C (with microwave assistance at 50 W), 60, and 80°C as well as freeze-drying at hotplate temperatures of 20, 40, and 60°C, and then ground into powders. The drying kinetics of the pomace was assessed, along with measurements of water activity, moisture content, grinding efficiency, and energy consumption of pulverizing. Additional evaluations included powder color coordinates, total polyphenol content (determined using Folin-Ciocalteu reagent), antioxidant activity (measured using DPPH and ABTS assays), and a phytochemical analysis using LC-MS/MS. The results indicated that lyophilized broccoli pomace exhibited superior grindability, compared to contact-dried broccoli pomace. The freeze-dried powders were significantly brighter and greener than those obtained through contact-drying. Contact-drying, including microwave-assisted drying, resulted in increased phenolic compound content and enhanced antiradical activity, in comparison to freeze-drying. The phytochemical analysis revealed the highest concentrations of quinic acid and fumaric acid, along with trace amounts of aconitic acid, protocatechuic acid, piceid, coumarin, and astragalin. Based on the antioxidant properties and total polyphenol content, contact drying at 80°C was identified as the optimal method for drying broccoli pomace.
Investigation of Cuckoo-Pint's (Arum maculatum) phytochemistry, in vitro antioxidant potential, enzyme inhibition, and antimicrobial activity
(John Wiley and Sons Inc., 2024) Aslan, Kübra; Kelle, Kader; Yılmaz, Mustafa Abdullah; Kopar, Emre Erden; Gülçin, İlhami
Arum maculatum, cuckoo-pint in folk linguistics, is a poisonous but medicinal plant with tremendous properties that need investigation. This study subjected cuckoo-pint's parts to in vitro antioxidant, enzyme inhibition, and antimicrobial susceptibility testing to investigate its biological activity. Further, phytochemistry was analyzed by both LC–MS/MS and total phenol, flavonoid, saponin, and reducing sugar content determination assays. Antioxidant activities were determined by Fe3+, Cu2+, Fe3+-TPTZ metal-reducing ability, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2ʹ-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging assays. According to the results, seeds and berries have remarkable metal-reducing and radical-scavenging effects as natural and synthetic analogs such as ascorbic acid, butylated hydroxyanisole, butylated hydroxytoluene, trolox, and α-tocopherol. Inhibition studies over human carbonic anhydrase II (hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-amylase were performed, and IC50 values were determined for each enzyme inhibition. According to the results, the cuckoo-pint seeds inhibited the AChE, BChE, and hCA II activity with greater IC50 values than reference inhibitors. Antimicrobial activity over pan-resistant strains was achieved for each strain with the extracts, at least 20 mm zone diameter was obtained with the lowest concentrations. LC–MS/MS results revealed 24 bioactive metabolites associated with the extracts’ biological activity. Notably, quinic acid and epicatechin correlated with cardioprotective, neuroprotective, antioxidant, and antidiabetic activity.
The anticholinesterase perspective of dimethoxyindole based benzenesulfonamides: Synthesis, biological investigation and molecular docking applications
(John Wiley and Sons Inc., 2024) Bingül, Murat; Ercan, Selami; Boǧa, Mehmet; Arslan, Zehra; Tuneğ, Muhammed; Akocak, Süleyman; Bingül, Alev Arslantürk; Şengül, İbrahim Fazıl; Şahin, Hasan
Due to the well-known biological potential of benzenesulfonamides for the inhibition of specific enzymes, here in, we propose to investigate anticholinesterase efficiencies of five newly synthesized benzenesulfonamides incorporating dimethoxyindole tails. The targeted compounds were synthesized through the C7 position of the methyl 4,6-dimethoxy-1H-indole-2-carboxylate via Schiff-base reaction. The biological study was directed to identify the acetylcholinesterase (ACh) and butyrylcholinesterase (BCh) enzyme inhibitions. The molecular docking studies were also carried out to determine the possible poses of ligands 8 a–e in binding sites of enzymes and ligand-residue interactions. Molecular dynamics simulations, RMSD and RMSF plots, hydrogen bond analysis, per-residue energy decomposition and MM-PB(GB)/SA calculations were carried out investigate the potentials of the compounds towards the designated enzymes. It is important to note that all the synthesized compounds were found to be selective towards the BChE inhibition with a range of efficiencies. In addition to that the compound 8 a exhibited more potency than the standard Galanthamine with the value of 87.75 % for the same enzyme. The results could be valuable for the determination of new targets which are highly selective for BChE inhibition. The formation of hydrogen bonds and hydrophobic interactions with the residues located on the compounds were responsible for the binding free energy scores. The stability of all the compounds proved by molecular dynamics simulations were also promising for the further directions of the study.
Environmentally friendly silver nanoparticles synthesized from Verbascum nudatum var. extract and evaluation of its versatile biological properties and dye degradation activity
(Springer, 2024) Hazman, Ömer; Khamidov, Gofur; Yılmaz, Mustafa Abdullah; Bozkurt, Mehmet Fatih; Kargıoğlu, Mustafa; Tukhtaev, Davlat; Erol, İbrahim
In the present study, green synthesis of silver nanoparticles (VNE-AgNPs) via Verbascum nudatum extract was carried out for the first time. The synthesized AgNPs were characterized by different spectral methods such as UV–vis, FTIR, XRD, TEM, and EDAX. According to TEM analyses, the average size range of AgNPs was 17–21 nm, and the dominant peaks in the 111°, 200°, 221°, and 311° planes in the XRD pattern indicated the Ag-NPs FCC crystal structure. FTIR data showed that VNE-AgNPs interacted with many reducing, capping, and stabilizing phytochemicals during green synthesis. VNE-AgNPs had higher antibacterial activity against S. aureus and E. coli bacterial strains with a maximum inhibition zone of 21 and 18 mm, respectively, than penicillin 5 IU, used as a positive control in the study. The cytotoxic effect of VNE-AgNPs appeared at a concentration of 50 µg/mL in L929 cells and 5 µg/mL in cancer (A549) cells. When the impact of VNE-AgNPs and C-AgNPs on inflammation was compared, it was found that VNE-AgNPs increased TNF-α levels (333.45 ± 67.20 ng/mg-protein) statistically (p < 0.05) more than TNF-α levels (256.92 ± 27.88 ng/mg-protein) in cells treated with C-AgNPs. VNE-Ag-NPs were found to have a degradation efficiency of 65% against methylene blue (MB) dye within 3 h. Graphical Abstract: (Figure presented.)
LC-MS /MS characterization and biological activities of Morina persica L. (Caprifoliaceae)
(Marmara University, 2024) Gözcü, Sefa; Akşit, Zeynep; Şimşek, Samed; Kandemir, Ali; Aydın, Ali; Yılmaz, Mustafa Abdullah; Akşit, Hüseyin
The study aimed to comprehensively identify the phenolic fingerprint of Morina persica L. (Caprifoliaceae) and evaluate its various biological activities. LC-MS/MS analysis of 70% Morina persica methanol extract revealed the presence of 27 phytochemicals, with quinic acid, chlorogenic acid, and rutin being the major phenolics. The antioxidant, antibacterial, antiproliferative, and cytotoxic activities were evaluated for biological screening. The results showed that the methanolic extract of M. persica has a moderate DPPH radical scavenging and ferric-reducing capacity, indicating antioxidant activity. M. persica was observed to have a sufficient antiproliferative effect against cancer cells and low cytotoxicity against normal cells. Moreover, M. persica demonstrated good antibacterial activity against Clostridium perfringens, Enterococcus faecalis, and Escherichia coli. These data suggest that the methanolic extract of M. persica could be considered both an industrial source of quinic acid and a potential biologically active ingredient for developing drug formulations.
Synthesis of furo[2,3-c]carbazoles as potent α-glucosidase and α-amylase inhibitors
(Taylor and Francis Ltd., 2024) Uçar, Tuğçe N. Uslu; Bingül, Murat; Şahin, Hasan; Kandemir, Hakan; Şengül, İbrahim Fazıl
The carbazole-3-carbaldehyde 2, produced by N-ethyl carbazole via Vilsmeier-Haack reaction, was subjected to Dakin type oxidation with H2O2 and H2SO4 in methanol to produce the carbazole-3-ol 3. The reaction of 3 with a range of commercially available α-haloketones 4a–f in the presence of Al2O3 as catalyst in xylene led to their regio-selective cyclization to afford the furo[2,3-c]carbazoles 5a–f. Identification of the furo[2,3-c]carbazoles 5a–f were performed through 1H NMR,13C NMR, FT-IR and high resolution mass spectrometry. Single crystal X-ray diffraction analysis was employed to further confirm the structures of the some of the targeted compounds. In vitro antidiabetic activities of the newly synthesized furocarbazoles 5a–e were investigated utilizing α-glucosidase and α-amylase enzymes. The biological evaluation revealed the obvious efficiencies of the targeted molecules toward the α-glucosidase enzyme inhibition with the potent IC50 values compared to the standard acarbose. In the case of α-glucosidase inhibition, the furo[2,3-c]carbazoles chloro substituted 5c and nitro substituted 5f were found to be more potent than acarbose with the values of 215.0 and 162.70 μM, respectively. On the other hand, the compound 5f was found to be only promising candidate for α-amylase enzyme but not as effective as the standard acarbose.
Xanthine oxidase inhibitory activity and uric acid dissolution power of some plant extracts: In vitro therapeutical approach for gout treatment
(Springer Science and Business Media Deutschland GmbH, 2024) Bouakkaz, Hicham; Djeridane, Amar; Mahfoudi, Reguia; Yılmaz, Mustafa Abdullah; Çakır, Oğuz; Tarhan, Abbas; Lassakeur, Zakaria; Yousfi, Mohamed
Elevated serum levels of uric acid are associated with an increased risk of hyperuricemia and gout. Recent attention has focused on the bioactive properties of plant extracts in preventing disease. Therefore, this study investigated the effects of 16 different extracts from four common plants on the inhibition of xanthine oxidase and the dissolution of uric acid, as well as the quantification of certain phytoconstituents and their haemolytic effects on human red blood cells. Results from quantitative phytochemical analysis revealed significant (p < 0.0001) intra- and inter-specific variability in total phenols, flavonoids, tannins, uric acid, sodium, potassium, and calcium depending on the studied species and the type of solvent used in extraction. A total of 19 phenolic compounds were characterized and quantified using an ultrahigh-performance liquid chromatograph coupled with an electrospray ionization source operating in both negative and positive ionization modes mass spectrometry, including phenolic acids, flavonoids and other polyphenols. The in vitro antigout activity results indicated that all extracts had the ability to express the inhibitory activity of xanthine oxidase and to dissolve uric acid at different levels. Therefore, the acetonic extracts of Cistus creticus L., Cistaceae, and Plantago ciliata Desf., Plantaginaceae, had the most significant xanthine oxidase inhibiting effect with values of 13.480 ± 0.596 and 13.020 ± 0.627 µg of allopurinol/mg of dry residue, respectively. Moreover, their aqueous extracts showed the highest dissolving properties of uric acid (solubilities > 450 mg uric acid/l). These extracts also showed no toxic effect against isolated human erythrocytes and may be able to help improve the efficacy of new therapies for gouty arthritis. Graphical Abstract: (Figure presented.)
Anti-Cataract effect of the traditional aqueouse extract of yerba mate (Ilex paraguariensis A. St.-Hil.): An in ovo perspective
(Multidisciplinary Digital Publishing Institute (MDPI), 2024) Öncü, Şeyma; Kızılkaya, Merve Becit; Bilir, Abdulkadir; Sarıtaş, Alperen; Söylemez, Evrim Suna Arıkan; Koca, Halit Buğra; Fırat, Fatma; Kaplan, Afife Büşra Uğur; Yılmaz, Mustafa Abdullah
Introduction: The therapeutic effect of different doses of the traditional aqueous extract of dried leaves of yerba mate (Ilex paraguariensis A. St.-Hil.) was investigated in an experimental cataract model in chicken embryos. Methods and Results: LC-MS/MS analysis allowed the identification and quantification of 53 metabolites. In the hydrocortisone-induced cataract model, lenses were examined morphologically after treatment and parameters related to oxidative stress (total antioxidant/oxidant status (TAS/TOS), glutathione (GSH), and malondialdehyde (MDA)) were evaluated. Antiproliferative cell nuclear antigen (PCNA) and caspase-3 H-scores were determined and crystallin alpha A (CRYAA) gene expression in the lenses was measured by RT-PCR. The degree of cataract decreased in all treatment groups. While there was no significant difference in TAS levels compared to the negative control, TOS, GSH, and MDA levels were dose-dependently regulated. Treatment groups other than the high-dose group regulated the decrease in PCNA and the increase in caspase-3. CRYAA gene expression increased significantly only at the lowest dose. Conclusion: YM, which is becoming increasingly popular as a traditional tea, showed a therapeutic effect on hydrocortisone-induced cataracts in chicken embryos at relatively low doses.

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