Synthesis, Enzyme Inhibition, and Acid Dissociation Constant of 1,4-Naphthoquinone Thiazole Hybrid DOI
Yahya Nural, Yeliz Demir

Hacettepe University Journal of the Faculty of Pharmacy, Journal Year: 2024, Volume and Issue: 44(3), P. 234 - 243

Published: Aug. 9, 2024

In this study, N-((Z)-4-((3r,5r,7r)-adamantan-1-yl)-3-(3-amino-1,4-dioxo-1,4-dihydronaphthalen-2yl)thiazol-2(3H)-ylidene)-2,6-difluorobenzamide 3 was synthesized as a new 1,4-naphthoquinone thiazole hybrid compound by reaction of naphthoquinone acyl thiourea 2 with 1-((3r,5r,7r)-adamantan-1-yl)-2-bromoethan-1-one in 74% yield and its molecular structure characterized various analytical techniques such 1H/13C NMR, FT-IR, HRMS. The inhibition effect the on butyrylcholinesterase (BChE), acetylcholinesterase (AChE), human carbonic anhydrase isoenzymes (hCA I hCA II) investigated. product showed varying degrees 89.92 ± 10.47 nM (against I), 51.60 5.37 II), 68.11 6.58 AChE), 126.90 10.99 BChE). Although significant enzyme activity against enzymes tested, it higher AChE than standard drug Tacrine. Three acid dissociation constants (pKa) values (pKa1= 2.75±0.02, pKa2= 6.79±0.02, pKa3= 10.85±0.02) were determined potentiometrically 0.1 M NaCl ionic strength at 25.0±0.1 ºC 25% (v/v) DMSO:water hydro organic medium.

Language: Английский

A multidimensional study for design of phytochemical profiling, antioxidant potential, and enzyme inhibition effects of ışgın (Rheum telianum) as an edible plant DOI Creative Commons
Ahmet Zafer Tel, Kübra Aslan, Mustafa Abdullah Yılmaz

et al.

Food Chemistry X, Journal Year: 2025, Volume and Issue: 25, P. 102125 - 102125

Published: Jan. 1, 2025

The present study reveals in vitro antioxidant properties and the phytochemical content of a novel Rheum species (Rheum telianum), which grows Southeastern Anatolia. To perform analysis, dried leaves seeds plants were ground extracted with ethanol to obtain plant secondary metabolites activity. Then, extracts subjected DPPH scavenging Cupric reducing (CUPRAC), Fe3+, Ferric power (FRAP). In addition capacity assays, quantitative phenolic, flavonoid, metabolite determined through spectrophotometric LC-MS/MS chromatographic methods. IC50 values showed that both R. telianum have high inhibitory over radicals 20.79 5.67 μg/mL, respectively. samples' dominant evaluated analysis results. inhibition effects on acetylcholinesterase butyrylcholinesterase, α-glycosidase human carbonic anhydrases II isoenzyme enzymes, associated some global diseases including Alzheimer's disease, type-2 diabetes mellitus glaucoma determined. conclusion, extracts' contents functional relationship plants' possible usage food, medicine, cosmetic industries was revealed.

Language: Английский

Citations

1

Sage ( Salvia macrochlamys ): LC-HRMS for phytochemical analysis, cytotoxicity, enzyme inhibition, antioxidant activity, molecular docking and molecular dynamics simulations DOI
Hatice Kızıltaş, Ahmet Buğra Ortaakarsu, Zeynebe Bingöl

et al.

Plant Biosystems - An International Journal Dealing with all Aspects of Plant Biology, Journal Year: 2024, Volume and Issue: 158(5), P. 1057 - 1075

Published: Aug. 5, 2024

This study primarily aims to evaluate the phenolic content and biological activity of Salvia macrochlamys both in vitro silico. The antioxidant activities were assessed using various methods. Additionally, cytotoxic effects α-amylase, α-glucosidase, acetylcholinesterase (AChE) enzyme inhibitory abilities ethanolic extract aerial parts (EESM) evaluated. Then, molecular docking interactions dynamic calculations EESM against α-glycosidase, AChE enzymes carried out. High was determined ethanol water extracts. IC50 values (EC 3.1.1.7), α-glycosidase (E.C.3.2.1.20), α-amylase (E.C.3.2.1.1) as 1.622 μg/mL, 0.530 1.320 respectively. enzyme-inhibiting properties also Rosmarinic acid identified one most abundant compounds (WESM) (3919.65 mg/kg 10520.77 mg/kg, respectively). Their high level flavonoids phenolics, well potent enzyme-inhibitory displayed by extracts, may contribute broadening use traditional modern therapeutic applications.

Language: Английский

Citations

4

Phytochemical profile and bioactive properties of sage ( Salvia fruticosa ) and thyme ( Thymus vulgaris ) extracts DOI Creative Commons
Kübra Aslan, Emre Erden,

Kader Kelle

et al.

International Journal of Food Properties, Journal Year: 2025, Volume and Issue: 28(1)

Published: March 19, 2025

We examined the phytochemical content, antioxidant, antimicrobial, anticholinergic, antidiabetic, and antiglaucoma properties of ethanol water extracts from Salvia fruticosa (SF) Thymus vulgaris (TV). Extracts were analyzed using four antioxidant assays, while enzyme inhibition was tested against α-amylase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), human carbonic anhydrase II (hCA II). Antimicrobial activity evaluated pan-resistant bacterial strains. LC-MS/MS identified rosmarinic acid as major compound (27.61 34.35 mg/L in TV SF, respectively). Ethanolic had higher phenolic content (181.0 ± 7.86 107.0 5.78 µg GAE/mg for SF TV, showed stronger metal-reducing capacity, superior radical scavenging ability, judging by IC50 values (13.68 1.18 μg/mL), defined concentration that reduces 50% activity. The highest observed hCA (SF ethanolic extract, 14.51 4.07 AChE aqueous 16.51 3.77 BChE (TV 10.60 4.93 μg/mL). extract inhibited growth Staphylococcus aureus Enterococcus faecalis (11 mm at 60 These findings highlight potential sources natural antioxidants, inhibitors, antimicrobials pharmaceutical food formulations.

Language: Английский

Citations

0

Phytochemical Analysis, Antioxidant, Anticholinergic, Antidiabetic, and Antiglaucoma Potentials of Sage (Salvia adiyamanensis) DOI
Ahmet Zafer Tel, Kübra Aslan, İlhami Gülçın

et al.

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: April 10, 2025

Abstract In this study, the antioxidant effect of ethanolic extracts were prepared from aerial part Salvia adiyamanensis was investigated through five methods, including DPPH⋅, ABTS, and Fe3+, Cu2+, Fe3+-TPTZ reducing assays. The IC50 values extract determined as 35.40 ± 8.35 29.50 5.12 µg/mL for DPPH ABTS radicals scavenging enzyme inhibition property against α-glycosidase, acetylcholinesterase, butyrylcholinesterase, human carbonic anhydrase I, II, a result, IC50 30.78, 191.3, 8.02, 32.68 54.82 µg/mL, respectively. LC-MS/MS revealed that S. compromised characteristic phenolics rosmarinic acid, chlorogenic luteolin, quercetin, apigenin, caffeic acid Salvia genus. These findings strongly suggest has potential to be natural medicine treatment metabolic diseases such diabetes, Alzheimer’s disease, or glaucoma.

Language: Английский

Citations

0

Antioxidants: a comprehensive review DOI Creative Commons
İlhami Gülçın

Archives of Toxicology, Journal Year: 2025, Volume and Issue: unknown

Published: April 15, 2025

Language: Английский

Citations

0

Exploring of biological activity and diverse metabolites in hemp (Cannabis sativa) seed oil by GC/MS, GC–FID, and LC–HRMS chromatographies DOI Creative Commons
İlhami Gülçın,

Eda Mehtap Özden,

Muzaffer Mutlu

et al.

Future Journal of Pharmaceutical Sciences, Journal Year: 2024, Volume and Issue: 10(1)

Published: Sept. 19, 2024

Abstract Background This study investigated the antidiabetic and antioxidant properties of hemp seed oil using various bioanalytical methods. Furthermore, this determined suppressive on α-amylase, acetylcholinesterase carbonic anhydrase II that purified by sepharose-4B-L-Tyrosine-sulfanilamide affinity chromatoghraphy, all which are related to different metabolic diseases. Moreover, phenolic concentration in essential was quantified through LC–HRMS chromatography. Thirteen distinct compounds were detected oil. Additionally, both chemical components quantity oils within assessed GC–FID GC/MS analyses. Results The predominant included linoleoyl chloride (34.62%), linoleic acid (33.21%), 2-4-di-tert-butylphenol (5.79%). Hemp oil's ability scavenge radicals studied use 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) 1,1-diphenyl-2-picrylhydrazil radical scavenging results unveiled its potent radical-scavenging properties, with an 46.20 μg/mL for IC 50 9.76 radicals. investigation also extended explore reducing capabilities Fe 3+ -2,4,6-tri(2-pyridyl)-S-triazine, copper (Cu 2+ ), iron (Fe ). demonstrated notable inhibitory effect against α-amylase (IC : 545.66 μg/mL), achethylcholinesterase 28.00 322.62 μg/mL). Conclusions interdisciplinary research will prove valuable set stage future investigations into characteristics enzyme inhibition patterns plants hold medical industrial significance.

Language: Английский

Citations

2

Hamamelitannin’s Antioxidant Effect and Its Inhibition Capability on α-Glycosidase, Carbonic Anhydrase, Acetylcholinesterase, and Butyrylcholinesterase Enzymes DOI Open Access
Lokman Durmaz, Hasan Karageçili, Adem Ertürk

et al.

Processes, Journal Year: 2024, Volume and Issue: 12(11), P. 2341 - 2341

Published: Oct. 25, 2024

Hamamelitannin (2′,5-di-O-galloyl-hamamelose) bears two-gallate moieties in its structure, and is a natural phenolic product the leaves bark of Hamamelis virginiana. The antioxidant capacity hamamelitannin was evaluated by range methods, with following findings: ability to reduce potassium ferric cyanide; scavenging N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD•+); 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) (ABTS•+); 1,1-diphenyl-2-picrylhydrazyl (DPPH•); cupric ions (Cu2+). Additionally, reference antioxidants α-Tocopherol, butylated hydroxyanisole (BHA), Trolox, hydroxytoluene (BHT) were used for comparison. For DPPH scavenging, had an IC50 value 19.31 μg/mL, while values BHA, BHT, α-Tocopherol 10.10, 25.95, 7.05, 11.31 respectively. study found that functioned similarly α-tocopherol, Trolox terms DPPH• but better than BHT. as polyphenolic secondary metabolite, inhibition capability several metabolic enzymes demonstrated, including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase I (CA I), II II) α-glycosidase. Ki exhibited 7.40, 1.99, 10.18, 18.26, 25.79 nM toward AChE, BChE, hCA I, II, α-glycosidase,

Language: Английский

Citations

2

Understanding chemical properties, formation mechanism, and cation-π interaction of dibenzocines from DFT calculations DOI
Hamid Saeidian, Zohreh Mirjafary,

Azadeh Bakhtiari

et al.

Journal of Organometallic Chemistry, Journal Year: 2024, Volume and Issue: 1017, P. 123285 - 123285

Published: July 24, 2024

Language: Английский

Citations

1

Optimization of bioactivities of solvent extracts of bark and heartwood of Pterocarpus marsupium and exploration of neuroprotective effect linking to the major Phytoconstituents DOI
Sandeep Kumar Swain,

Bikash Kisan,

Neelam Meher

et al.

Industrial Crops and Products, Journal Year: 2024, Volume and Issue: 221, P. 119416 - 119416

Published: Aug. 14, 2024

Language: Английский

Citations

1

Employing soil isolated fungi for production of bioactive phenolic compounds: a fermentative approach DOI
Rathnaprabha Dharavath,

A. Srividya

Preparative Biochemistry & Biotechnology, Journal Year: 2024, Volume and Issue: 54(9), P. 1121 - 1131

Published: March 13, 2024

An efficient method of solid-state fermentation (SSF) is reported for producing bioactive phenolic compounds using soil-isolated fungi. Antioxidant activity a rapid DPPH (1,1-diphenyl-2-picryl hydrazyl), was employed to screen the 120 fungal isolates from soil. Aspergillus terreus 1, fumigatus, 2, Penicillium citrinum, wentii1, wentii expansum and granulatum were chosen, concerning their antioxidant total content. These strains applied on agro residues viz. sugarcane bagasse, corn cob, rice straw, pea pod wheat evaluate release compounds. The fermented extracts various agro-residues showed good against DPPH, ferric ion, nitric oxide radicals. highest observed in followed by pod. Additionally, content positively correlated with potential. This study highlights significant potential solid substrate fungi produce potent properties. utilization SSF extraction natural sources not only offers clean sustainable approach but also contributes valorization agro-industrial residues.

Language: Английский

Citations

0