Synthesis of Schiff Bases Containing Phenol Rings and Investigation of Their Antioxidant Capacity, Anticholinesterase, Butyrylcholinesterase, and Carbonic Anhydrase Inhibition Properties

Pharmaceutics, Journal Year: 2023, Volume and Issue: 15(3), P. 779 - 779

Published: Feb. 26, 2023

The widespread usage of Schiff bases in chemistry, industry, medicine, and pharmacy has increased interest these compounds. derivative compounds have important bioactive properties. Heterocyclic containing phenol groups their structure the potential to capture free radicals that can cause diseases. In this study, we designed synthesized eight (10-15) hydrazineylidene derivatives (16-17), which contain moieties be used as synthetic antioxidants, for first time using microwave energy. Additionally, antioxidant effects (16-17) were studied by bioanalytical methods 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) cation radical (ABTS•+) 1,1-diphenyl-2-picrylhydrazyl (DPPH•) scavenging activities, Fe3+, Cu2+, Fe3+-TPTZ complex reducing capacities. context studies on found powerful DPPH (IC50: 12.15-99.01 μg/mL) ABTS•+ 4.30-34.65 μg/mL). inhibition abilities determined towards some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), human carbonic anhydrase I II (hCAs II), are linked global disorders Alzheimer's disease (AD), epilepsy, glaucoma. enzyme inhibition, it was observed inhibited AChE, BChE, hCAs I, hCA with IC50 values ranges 16.11-57.75 nM, 19.80-53.31 26.08 ± 8.53 85.79 24.80 respectively. addition, light results obtained, hope study will useful guiding evaluation biological activities fields food, medical, pharmaceutical industries future.

Language: Английский

---

The DFT and in-silico analysis of 2,2′-((1e,1′e)-((3,3′-dimethyl-[1,1′-biphenyl]−4,4′ diyl)bis(azanylylidene))bis(methanylylidene))diphenol molecule

Colloids and Surfaces A Physicochemical and Engineering Aspects, Journal Year: 2024, Volume and Issue: 687, P. 133444 - 133444

Published: Feb. 11, 2024

Language: Английский

---

Synthesis and biological studies of pyrimidine derivatives targeting metabolic enzymes

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(8)

Published: May 21, 2024

Abstract Novel synthesized pyrimidine derivatives were investigated against carbonic anhydrase isoenzymes I and II (hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α‐glycosidase, aldose reductase (AR) enzymes associated with some common diseases such as epilepsy, glaucoma, Alzheimer's disease, diabetes, neuropathy. When the results examined, novel found to have effective inhibition abilities toward metabolic enzymes. IC 50 values K i calculated for each derivative compared positive controls. The exhibited in range of 39.16 ± 7.70–144.62 26.98 nM hCA I, 18.21 3.66–136.35 21.48 II, which is different pathological physiological processes, 33.15 4.85–52.98 19.86 on AChE, 31.96 8.24–69.57 21.27 BChE. Also, determined 17.37 1.11–253.88 39.91 α‐glycosidase 648.82 53.74–1902.58 98.90 AR Within scope study, types evaluated.

Language: Английский

---

Insights into Manganese Superoxide Dismutase and Human Diseases

International Journal of Molecular Sciences, Journal Year: 2022, Volume and Issue: 23(24), P. 15893 - 15893

Published: Dec. 14, 2022

Redox equilibria and the modulation of redox signalling play crucial roles in physiological processes. Overproduction reactive oxygen species (ROS) disrupts body's antioxidant defence, compromising homeostasis increasing oxidative stress, leading to development several diseases. Manganese superoxide dismutase (MnSOD) is a principal enzyme that protects cells from damage by converting anion radicals hydrogen peroxide mitochondria. Systematic studies have demonstrated MnSOD plays an indispensable role multiple This review focuses on preclinical evidence describes mechanisms diseases accompanied with imbalanced status, including fibrotic diseases, inflammation, diabetes, vascular neurodegenerative cancer. The potential therapeutic effects activators mimetics are also discussed. Targeting this specific radical scavenger may be clinically beneficial strategy, understanding provide positive insight into preventing treating related

Language: Английский

---

Screening of Carbonic Anhydrase, Acetylcholinesterase, Butyrylcholinesterase, and α-Glycosidase Enzyme Inhibition Effects and Antioxidant Activity of Coumestrol

Molecules, Journal Year: 2022, Volume and Issue: 27(10), P. 3091 - 3091

Published: May 11, 2022

Coumestrol (3,9-dihydroxy-6-benzofuran [3,2-c] chromenone) as a phytoestrogen and polyphenolic compound is member of the Coumestans family quite common in plants. In this study, antiglaucoma, antidiabetic, anticholinergic, antioxidant effects were evaluated compared with standards. To determine activity coumestrol, several methods—namely N,N-dimethyl-p-phenylenediamine dihydrochloride radical (DMPD•+)-scavenging activity, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) (ABTS•+)-scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH•)-scavenging potassium ferric cyanide reduction ability, cupric ion (Cu2+)-reducing activity—were performed. Butylated hydroxyanisole (BHA), Trolox, α-Tocopherol, butylated hydroxytoluene (BHT) used reference antioxidants for comparison. scavenged DPPH an IC50 value 25.95 μg/mL (r2: 0.9005) while BHA, BHT, α-Tocopherol demonstrated values 10.10, 25.95, 7.059, 11.31 μg/mL, respectively. When these results evaluated, had similar DPPH•-scavenging effect to BHT lower better than BHA α-tocopherol. addition, inhibition tested against metabolic enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), carbonic anhydrase II (CA II), α-glycosidase, which are associated some global diseases such Alzheimer’s disease (AD), glaucoma, diabetes. exhibited Ki 10.25 ± 1.94, 5.99 1.79, 25.41 1.10, 30.56 3.36 nM towards enzymes,

Language: Английский

---

Identification and characterization of anthocyanins and non-anthocyanin phenolics from Australian native fruits and their antioxidant, antidiabetic, and anti-Alzheimer potential

Food Research International, Journal Year: 2022, Volume and Issue: 162, P. 111951 - 111951

Published: Sept. 19, 2022

Polyphenols are vital bioactive constituents that have beneficial effects on human health. The aim of this study was to characterize the biologically active phenolic metabolites in Australian native commercial fruits (Kakadu plum, Davidson's quandong peach, and muntries) their antioxidant, α-glucosidase, acetylcholinesterase inhibition activities. were measured through total content (TPC), flavonoid (TFC), condensed tannin (TCT), monomeric anthocyanin (TMAC). Moreover, different in-vitro biological assays (DPPH, ABTS, FICA, OH-RSA, activities) conducted measure anti-diabetic, anti-Alzheimer's potential these selected fruits. LC-ESI-QTOF-MS/MS implied for identification quantification purposes. In study, a 307 (51 acids, 194 flavonoids, 15 tannins, 23 other polyphenols, 5 stilbenes, 12 lignans, 7 terpenoids) putatively identified. A 41 compounds quantified/semi-quantified. Kakadu plum identified with higher concentration polyphenols activities compared Davidson muntries. Molecular docking also discover actual role most abundant α-glucosidase

Language: Английский

---

Antioxidant, Antidiabetic, Anticholinergic, and Antiglaucoma Effects of Magnofluorine

Molecules, Journal Year: 2022, Volume and Issue: 27(18), P. 5902 - 5902

Published: Sept. 11, 2022

Magnofluorine, a secondary metabolite commonly found in various plants, has pharmacological potential; however, its antioxidant and enzyme inhibition effects have not been investigated. We investigated the potential of Magnofluorine using bioanalytical assays with 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS

Language: Английский

---

Enzyme inhibition, molecular docking, and density functional theory studies of new thiosemicarbazones incorporating the 4‐hydroxy‐3,5‐dimethoxy benzaldehyde motif

Archiv der Pharmazie, Journal Year: 2022, Volume and Issue: 356(4)

Published: Dec. 27, 2022

New Schiff base-bearing thiosemicarbazones (1-13) were obtained from 4-hydroxy-3,5-dimethoxy benzaldehyde and various isocyanates. The structures of the synthesized molecules elucidated in detail. Density functional theory calculations also performed to determine spectroscopic properties compounds. Moreover, enzyme inhibition activities these compounds investigated. They showed highly potent effects on acetylcholinesterase (AChE) human carbonic anhydrases (hCAs) (KI values are range 51.11 ± 6.01 278.10 40.55 nM, 60.32 9.78 300.00 77.41 64.21 9.99 307.70 61.35 nM for AChE, hCA I, II, respectively). In addition, molecular docking studies performed, confirmed by binding affinities most derivatives.

Language: Английский

---

Assessment of hypolipidemic and anti‐inflammatory properties of walnut (Juglans regia) seed coat extract and modulates some metabolic enzymes activity in triton WR‐1339‐induced hyperlipidemia in rat kidney, liver, and heart

Journal of Molecular Recognition, Journal Year: 2022, Volume and Issue: 36(3)

Published: Dec. 20, 2022

Atherosclerosis and cognitive impairment are both influenced by hyperlipidemia. Due to their high margin of safety low cost, natural chemicals have recently attracted particular attention in the context treatment disease. Hence, purpose this study was investigate possible amendatory impact ethanol extract walnut (Juglans regia) seed coat (E-WSC) on some metabolic enzymes (glutathione reductase (GR), paraoxonase-1 (PON1), aldose (AR), sorbitol dehydrogenase (SDH), acetylcholinesterase (AChE), glutathione S-transferase (GST), butyrylcholinesterase (BChE)) activity liver, kidney, heart rats with Triton WR-1339-induced Rats were divided into five groups: control group, HL-Control group (Triton WR-1339 400 mg/kg, i.p administered group), E- WSC + 150 (150 mg/kg,o.d given 300 (E- o.d group) HL+ E-WSC (Group receiving 30 min prior administration i.p). In HL-Control, AR, SDH, BChE enzyme significantly increased all tissues compared control, while other studied decreased. The effects hyperlipidemia balance improved alterations investigated prevented E-WSC. As a result, promising compounds that can be used as adjuvant therapy disorders may found powder.

Language: Английский

---

Structural characterization and biological evaluation of uracil-appended benzylic amines as acetylcholinesterase and carbonic anhydrase I and II inhibitors

Journal of Molecular Structure, Journal Year: 2023, Volume and Issue: 1280, P. 135047 - 135047

Published: Jan. 28, 2023

Language: Английский

---