Synthesis and Biological Activity of Some Bromophenols and Their Derivatives Including Natural Products DOI
Çetin Bayrak, Parham Taslımı, Namık Kılınç

et al.

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(8)

Published: July 11, 2023

In addition to the first synthesis of natural bromophenol butyl 2-(3,5-dibromo-4-hydroxyphenyl)acetate (1), indene derivatives 34 and 35 were synthesized from 3-phenylpropenal in BBr3 medium. Five known bromophenols some by methods. Cholinesterase (ChEs) inhibitors reduce breakdown acetylcholine are used treatment Alzheimer's disease (AD) dementia symptoms. The inhibition effects all obtained compounds examined towards acetylcholinesterase (AChE), butyrylcholinesterase (BChE) α-glycosidase enzymes. All demonstrated strong against both cholinergic For determination Ki values novel Lineweaver-Burk graphs obtained. found ranging 0.13-14.74 nM for AChE, 5.11-23.95 BChE, 63.96-206.78 α-glycosidase, respectively. their exhibit effective profile when compared positive controls.

Language: Английский

DPPH Radical Scavenging Assay DOI Open Access
İlhami Gülçın, Saleh Alwasel

Processes, Journal Year: 2023, Volume and Issue: 11(8), P. 2248 - 2248

Published: July 26, 2023

Today, there is an increasing interest in antioxidants, especially to prevent the known harmful effects of free radicals human metabolism and their deterioration during processing storage fatty foods. In both cases, natural-source antioxidants are preferred over synthetic antioxidants. So, has been a parallel increase use assays estimate antioxidant efficacy food systems. many bioanalytical methods that measure effect. Of these, 1,1-diphenyl-2-picrylhydrazil (DPPH) removing assay most putative, popular, commonly used method determine ability. this review, general approach DPPH radical scavenging taken. context, studies, including attempts adapt different analytes, search for highest activity values, optimize measurement, have previously performed. Therefore, it highly important introduce measures aimed at standardizing conditions activity, various reaction media suitable assay. For aim, chemical basic principles defined discussed outline. addition, study describes defines sections biological Additionally, some chemical, critical, technical details removal given. This simple which prospective compounds or herbal extracts mixed with solution absorbance measured after certain period. However, despite rapid advances instrumental techniques analysis, not undergone extreme modification. presents detailed information about in-depth review developments.

Language: Английский

Citations

385

Comprehensive Phytochemical Content by LC/MS/MS and Anticholinergic, Antiglaucoma, Antiepilepsy, and Antioxidant Activity of Apilarnil (Drone Larvae) DOI
Hakan İNCİ, Ebubekir İzol, Mustafa Abdullah Yılmaz

et al.

Chemistry & Biodiversity, Journal Year: 2023, Volume and Issue: 20(10)

Published: Aug. 23, 2023

Apilarnil is 3-7 days old drone larvae. It an organic bee product known to be rich in protein. In this study, the biological activities of were determined by its antioxidant and enzyme inhibition effects. Antioxidant Fe3+ , Cu2+ -TPTZ ((2,4,6-tris(2-pyridyl)-s-triazine), reducing ability 1,1-diphenyl-2-picrylhydrazyl (DPPH⋅) scavenging assays. Also, effects tested against carbonic anhydrase I II isoenzymes (hCA I, hCA II), acetylcholinesterase (AChE) butyrylcholinesterase (BChE) enzymes. activity was generally lower than standard molecules applied methods. DPPH⋅ radical assay, exhibited higher some standards. Enzyme results towards (IC50 : 14.2 μg/mL), II: 11.5 AChE 22.1 BChE 16.1 μg/mL) calculated. addition, quantity 53 different phytochemical compounds a validated method LC/MS/MS. Compounds with highest concentrations (mg analyte/g dry extract) as quinic acid (1091.045), fumaric (48.714), aconitic (47.218), kaempferol (39.946), quercetin (27.508). As result, it that had effective profile when compared antioxidants.

Language: Английский

Citations

33

Isofraxidin: Antioxidant, Anti‐carbonic Anhydrase, Anti‐cholinesterase, Anti‐diabetic, and in Silico Properties DOI Creative Commons
Lokman Durmaz, İlhami Gülçın, Parham Taslımı

et al.

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(34)

Published: Sept. 7, 2023

Abstract The development of innovative pharmacological formulations for the treatment and prevention various major diseases, including cancer, diabetes, glaucoma, has been facilitated by some natural compounds. This study tested inhibitory effects isofraxidin on acetylcholinesterase, α‐glycosidase, butyrylcholinesterase enzymes, as well human carbonic anhydrase I II (hCA II) isoenzymes. Esterase activity was used to gauge Isofraxidin's ability inhibit CA (in vitro). For isoenzymes hCA II, half maximal concentration (IC 50 ) values were determined be 67.61 52.42 nM, respectively. At same manner, inhibition constant (K i 12.58±0.50 4.41±0.35 Then, IC value compound acetylcholinesterase (AChE) (BChE) calculated 18.50 10.75 On other hand, K α‐glycosidase 55.16 56.81±2.30 Additionally, antioxidant properties investigated using techniques like 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS), 1,1‐Diphenyl‐2‐picrylhydrazyl (DPPH), N,N‐dimethyl‐ρ‐phenylenediamine (DMPD), cupric ions (Cu 2+ reducing capacity (CUPRAC), iron reduction procedures. Following graphing results, determined. As a result, phenolic molecule showed strong profiles profile. We therefore think that these findings may pave way novel therapeutic management illnesses. Several plant‐based substances extracts have gained attention in recent years potential inhibitors enzyme. activities Isofraxidin with enzyme proteins compared. Finally, ADME/T analysis performed predict movements molecules metabolism.

Language: Английский

Citations

28

Antioxidant, antidiabetic, antiglaucoma, and anticholinergic effects of Tayfi grape (Vitis vinifera): A phytochemical screening by LC-MS/MS analysis DOI Creative Commons
Hasan Karageçili, Ebubekir İzol, Ekrem Kıreçcı

et al.

Open Chemistry, Journal Year: 2023, Volume and Issue: 21(1)

Published: Jan. 1, 2023

Abstract Grapes ( Vitis vinifera ), grape extracts, and products are known to possess beneficial effects. Antioxidant activity enzyme inhibition activities of Tayfi ) extracts were studied compared standards. The IC 50 values the ethanol extract grape’s scavenging abilities for ABTS˙ + DPPH˙ radicals found be 5.9 16.1 μg/mL, respectively, higher than those positive controls. Also, phenolic flavonoid ingredients seed measured 82.8 mg GAE/g 91 QE/g. water exhibited 5.3 5.8 μg/mL toward α-glycosidase, respectively; 385.2 567.6 α-amylase; 27.1 13.8 acetylcholinesterase (AChE); 54.7 12.6 CA II. Twenty-two biomolecules detected by LC-MS/MS. four types conventional antibiotics utilized hospitals proved ineffective against Staphylococcus aureus Escherichia coli bacteria. had high AChE, II inhibitions in addition having antioxidant activity. use pharmacological purposes individuals with diseases mentioned above can sustained clinical pharmacology studies.

Language: Английский

Citations

26

Bioactive compounds and biological activity in edible insects: A review DOI Creative Commons

María de la Luz Sánchez-Estrada,

Humberto Aguirre-Becerra,

Ana Angélica Feregrino‐Pérez

et al.

Heliyon, Journal Year: 2024, Volume and Issue: 10(2), P. e24045 - e24045

Published: Jan. 1, 2024

New strategies to combat hunger are a current and urgent demand. The increase in population has generated high demand for products services that affect food production, cultivation areas, climate. Viable sustainable alternative sources have been sought meet quality requirements. In this context, edible insects good source of macro-nutrients, bioactive compounds confer biological properties improve their nutritional aspects benefit human health. This review aims present the benefits contributions from point view contribution macronutrients, compounds, as well consider some anti-nutritional reported insects. It was found possess most macronutrients necessary life rich commonly plants. These can vary significantly depending on developmental stage, diet, species However, they also contain phytochemicals which anti-nutrients predominate, adversely humans with allergenic reactions or reduced nutrient viability when consumed amounts prolonged periods. Hydrocyanide, oxalates, soluble oxalate, phytate studied anti-nutrients. doses at occur far below limits foods. addition, anti-nutrient levels decrease processing, such oven-drying defatting methods. there few studies, so more trials needed avoid generalizing. Therefore, be considered complete food.

Language: Английский

Citations

13

Comprehensive metabolic profiling of Thymus canoviridis (endemic) and Thymus pubescens var. pubescens using UPLC-MS/MS and evaluation of their antioxidant activities, enzyme inhibition abilities, and molecular docking studies DOI
Leyla Güven, Hasan Can, Adem Ertürk

et al.

South African Journal of Botany, Journal Year: 2024, Volume and Issue: 165, P. 478 - 493

Published: Jan. 10, 2024

Language: Английский

Citations

11

Anti-Cholinergic Effects of the Phenolic Extract from the Astragalus crenatus Plant: A Computational and Network Pharmacology Study DOI Creative Commons
Sabrina Lekmine, Ouided Benslama, Hichem Tahraoui

et al.

Pharmaceuticals, Journal Year: 2024, Volume and Issue: 17(3), P. 348 - 348

Published: March 7, 2024

Investigations into cholinesterase inhibition have received attention from researchers in recent years for the treatment of Alzheimer’s disease. Cholinesterase enzymes, namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), hold pivotal significance disease (AD) treatment. In this study, we utilized ethanolic extract Astragalus crenatus followed by liquid chromatography–electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) to separate identify at least 21 compounds extract. Rosmarinic acid exhibited highest concentration (96.675 ± 1.3 mg/g extract), succeeded hesperidin (79.613 1.2 hesperetin (75.102 1.4 rutin (68.156 1.6 chlorogenic (67.645 1.5 fisetin (66.647 2.3 hyperoside (63.173 extract). A. efficiently inhibited both AChE BChE activities a dosage-dependent manner. Molecular docking was employed scrutinize anticholinesterase mechanisms identified phytocompounds. Notably, network pharmacology analysis executed most efficacious compound. Based on binding energies, emerged as potent inhibitor against BChE, exhibiting scores −10.5 Kcal/mol −9.8 Kcal/mol, respectively. Due its dual activities, holds promise development novel therapeutics aimed neurological disorders, particularly AD.

Language: Английский

Citations

10

Effects of sinapic acid on lead acetate‐induced oxidative stress, apoptosis and inflammation in testicular tissue DOI Open Access
Sibel Çiğdem Tuncer, Serkan Ali Akarsu, Sefa Küçükler

et al.

Environmental Toxicology, Journal Year: 2023, Volume and Issue: 38(11), P. 2656 - 2667

Published: July 20, 2023

In this study, the effect of lead acetate (PbAc) and sinapic acid (SNP) administration on oxidative stress, apoptosis, inflammation, sperm quality histopathology in testicular tissue rats was tried to be determined. PbAc administered at a dose 30 mg/kg/bw for 7 days induce toxicity rats. Oral doses 5 10 SNP were after administration. According our findings, while increased MDA content rats, it decreased GPx, SOD, CAT activity GSH content. NF-kB, IL-1β, TNF-α, COX-2, which are among inflammation parameters that due PbAc, with SNP. Nrf2, HO-1, NQO1 mRNA transcript levels but treatments these dose-dependent manner. RAGE NLRP3 gene expression upregulated treated MAPK14, MAPK15, JNK relative treatment While apoptosis markers Bax, Caspase-3, Apaf-1 level Bcl-2 decreased, inhibited markers. caused histopathological deterioration testis negatively affected spermatogenesis. When examined, decrease motility spermatozoon density by increase ratio dead abnormal spermatozoa As result, inducing stress testicles, changes quality.

Language: Английский

Citations

20

Potential antioxidant, anticholinergic, antidiabetic and antiglaucoma activities and molecular docking of spiraeoside as a secondary metabolite of onion (Allium cepa) DOI Creative Commons
Lokman Durmaz, Hatice Kızıltaş, Hasan Karageçili

et al.

Saudi Pharmaceutical Journal, Journal Year: 2023, Volume and Issue: 31(10), P. 101760 - 101760

Published: Aug. 23, 2023

Onion contains many dietary and bioactive components including phenolics flavonoids. Spiraeoside (quercetin-4-O-β-D-glucoside) is one of the most putative flavonoids in onion. Several antioxidant techniques were used this investigation to assess capabilities spiraeoside, 1,1-diphenyl-2-picrylhydrazyl radical (DPPH·) scavenging, N,N-dimethyl-p-phenylenediamine (DMPD•+) 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonate) (ABTS•+) scavenging activities, cupric ions (Cu2+) reducing potassium ferric cyanide reduction abilities. In contrast, water-soluble α-tocopherol analogue trolox conventional antioxidants butylated hydroxytoluene (BHT), hydroxyanisole (BHA), utilized as standards for evaluation. scavenged DPPH radicals an IC50 28.51 μg/mL (r2: 0.9705) meanwhile BHA, BHT, trolox, displayed 10.10 0.9015), 25.95 0.9221), 7.059 0.9614) 11.31 0.9642), accordingly. The results exhibited that spiraeoside had effects similar but less potent than α-tocopherol, BHA. Also, inhibitory evaluated toward some metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II) α-glycosidase, which are related a number illnesses, such Alzheimer's disease (AD), diabetes mellitus glaucoma disorder. values 4.44 nM 0.9610), 7.88 0.9784), 19.42 0.9673) 29.17 mM 0.9209), respectively against these enzymes. Enzyme inhibition abilities compared clinical inhibitors acetazolamide (for CA II), tacrine AChE BChE) acarbose α-glycosidase). demonstrated effective antioxidant, anticholinergic, antidiabetic antiglaucoma activities. With properties, it has shown potential be medicine diseases.

Language: Английский

Citations

16

Phenolic Content Analysis of Two Species Belonging to the Lamiaceae Family: Antioxidant, Anticholinergic, and Antibacterial Activities DOI Creative Commons
A.R. Ndhlala, Mesut Işık, Arzu Kavaz Yüksel

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(2), P. 480 - 480

Published: Jan. 18, 2024

The Lamiaceae family are utilized as ornamental, medicinal, and food supplements throughout the world. current study focuses on a comparative analysis of phenolic compositions bioactivities (including antioxidant, anticholinergic, antibacterial activities) ethanolic extracts derived from aerial parts two species (Lavandula stoechas L. Thymus sipyleus Boiss). presence compounds phytochemicals in plant was identified using LC-MS/MS technique. revealed that vanillic acid (125,596.66 µg/L) most abundant phytochemical stoechas. Kaempferol (8550.52 substance sipyleus. assessment antioxidant efficacy conducted DPPH (2.2-diphenyl-1-picryl-hydrazyl-hydrate), ABTS (2.2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid)), Fe3+–Fe2+ reducing, CUPRAC (Cu2+–Cu+ reducing) assays. anticholinergic activity samples determined acetylcholinesterase (AChE) inhibition assay. results were higher T. than ethanol extracts. exhibited radical scavenging ranging 15 to 18%, while had effects 34% 38%. AChE potential for IC50 values 0.221 ± 0.01 mg/mL 0.067 0.02 mg/mL, respectively. these against pathogenic bacteria isolates MIC (minimal inhibitory concentration) method. These findings indicated possess be natural antioxidants realm preservation. Additionally, their antimicrobial properties suggest therapeutic utility management certain diseases.

Language: Английский

Citations

7