Cichoriin, a Biocoumarin, Mitigates Oxidative Stress and Associated Adverse Dysfunctions on High-Fat Diet-Induced Obesity in Rats DOI Creative Commons
Hany Ezzat Khalil, Miada F. Abdelwahab, Hairul-Islam Mohamed Ibrahim

et al.

Life, Journal Year: 2022, Volume and Issue: 12(11), P. 1731 - 1731

Published: Oct. 28, 2022

Metabolic dysfunctions linked to obesity carry the risk of co-morbidities such as diabetes, hepatorenal, and cardiovascular diseases. Coumarins are believed display several biological effects on diverse adverse health conditions. This study was conducted uncover impact cichoriin high-fat diet (HFD)-induced obese rats. Methods: Obesity induced in twenty rats by exposure an HFD for six weeks. The were randomly divided into five groups; group I comprised healthy considered control one. On other hand, HFD-induced following (five per each group): II (the group), groups III (cichoriin 50 mg/kg) IV 100 treatment groups, V received atorvastatin (10 (as a standard). Triglycerides (TG), total cholesterol (TC), high-density lipoprotein (HDL-C), low-density (LDL-C), alanine transaminase (ALT), aspartate (AST), creatine kinase MB (CK-MB), urea, creatinine, hepatic renal malondialdehyde (MDA) well reduced glutathione (GSH) levels assessed. Histopathological analysis heart, kidney, liver tissues investigated. mRNA protein expressions peroxisome proliferator-activated receptor gamma (PPAR-γ) estimated. Results: administration alleviated metabolic improved histopathological characteristics liver. Additionally, lipid profile functions, oxidative balance state. Cichoriin demonstrated upregulation PPAR-γ. Taken together, these findings first report beneficial role alleviating adapting it innovative management strategy.

Language: Английский

Boron-Containing Coumarins (Review) DOI

Yu. N. Las’kova,

A. A. Serdyukov,

Igor B. Sivaev

et al.

Russian Journal of Inorganic Chemistry, Journal Year: 2023, Volume and Issue: 68(6), P. 621 - 643

Published: June 1, 2023

Language: Английский

Citations

12
A Comprehensive Review of The Molecular Dynamic Study Of Chalcones, Coumarins and Chromones as Selective MAO‐B Inhibitors [2015‐Till Date] DOI

Riya Rachel Thomas,

Namitha Chandran,

Della Grace Thomas Parambi

et al.

ChemistrySelect, Journal Year: 2024, Volume and Issue: 9(27)

Published: July 16, 2024

Abstract Molecular dynamics (MD) simulation is an in silico method used the biomolecular level of research to study how protein interacts with target time. It provides a detailed information and ligand structure crucial amino acid interactions. Monoamine oxidase B (MAO−B) isoenzyme responsible for catalyses oxidative deamination various biogenic amines brain peripheral tissues. The selective inhibitors MAO−B are considered as management symptoms neurodegenerative disorders like Alzheimer's disease(AD) Parkinson disease(PD). Recently structural scaffolds containing chalcones, coumarins chromones derived candidates shown potent, selective, competitive reversible type inhibitors. similarities between above can produce almost similar interactions inhibitor binding cavity MAO−B. Numerous molecular reports were supported by mentioned fact. current review focus on last ten year report towards inhibition. also focuses software details MD requirement from each class compound recognition inhibitory activity.

Language: Английский

Citations

4
Pharmacochemical Studies of Synthesized Coumarin–Isoxazole–Pyridine Hybrids DOI Creative Commons

Matina D. Douka,

Ioanna Sigala, Catherine Gabriel

et al.

Molecules, Journal Year: 2025, Volume and Issue: 30(7), P. 1592 - 1592

Published: April 2, 2025

Several new coumarin–isoxazole–pyridine hybrids were synthesized through a 1,3-dipolar cycloaddition reaction of nitrile oxides, prepared in situ from pyridine aldehyde oximes, with propargyloxy- or propargylaminocoumarins moderate-to-good yields. Synthetic modifications applied using (diacetoxyiodo)benzene (PIDA) at room temperature, microwave irradiation, tert-butyl nitrite (TBN) under reflux. Coumarin, isoxazole, and groups selected for hybridization one molecule due to their biological impact inhibit lipid peroxidation an enzyme implicated inflammation. Preliminary vitro screening tests lipoxygenase (LOX) inhibition anti-lipid the performed. A discussion on structure–activity relationship is presented. Compounds 12b 13a found be potent LOX inhibitors IC50 5 μΜ 10 μΜ, respectively, while presented high (90.4%) peroxidation. Furthermore, exhibited moderate-to-low anticancer activities HeLa, HT-29, H1437 cancer cells.

Language: Английский

Citations

0
Synthetic Strategies and Structure Activity Relationships (SAR) of Biologically Active Coumarin‐Based Hybrids DOI
Biplab Debnath, Soumen K. Manna, Arindam Maity

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(16)

Published: April 1, 2025

Abstract Coumarin (2‐benzopyrone), a secondary plant metabolite, is considered privileged scaffold in medicinal chemistry. and its derivatives have been demonstrated to exhibit various biological activities such as antiviral, antibacterial, anticancer, anti‐inflammatory, anticonvulsant, antioxidant, antidepressant, anti‐Alzheimer, antidiabetic. Because of wide spectrum activities, it has explored extensively which resulted the development many clinically useful drug molecules. Attempts made prepare coumarin by either substituting them with variety aromatic heterocyclic rings functionalities or preparing hybrids linked through an appropriate linker obtain develop potential therapeutic agents. The inclusion natural metabolites gained importance recent past enhance activity. moieties are easily synthesized chemical methods Knoevenagel reaction, Pechmann condensation, Kostanecki–Robinson coupling Claisen rearrangement, Michel addition Witting Reformatsky Perkin so on. current review provides overview classification coumarins, details approaches used for synthesis derivatives. introduced synthetic compounds discussed structure‐activity relationship (SAR) supported their 2D molecular docking studies interaction within receptors. SAR will support chemist directing novel diverse pharmacological properties.

Language: Английский

Citations

0
Review on Contemporary Synthetic Recipes to Access Versatile Coumarin Heterocycles DOI

S. M. Basavarajaiah,

Nagesh Gunavanthrao Yernale,

Munianjinappa Punith Kumar

et al.

Polycyclic aromatic compounds, Journal Year: 2023, Volume and Issue: 44(5), P. 3576 - 3600

Published: July 21, 2023

Coumarin and its derivatives are extensively used as scaffolds in the synthesis of novel heterocyclic motifs. In literature, several approaches especially involving metal metal-free catalysts have been developed to get biological potential coumarin analogs. This review spotlights recent advancements associated molecules recounting literature articles from 2015 middle 2022. Further, this review, we focused on contents based classical non-classical methods for synthesis.

Language: Английский

Citations

9
Synthesis and in-vitro anti-proliferative with antimicrobial activity of new coumarin containing heterocycles hybrids DOI Creative Commons

Eman Abdelaziz,

Nehal M. El‐Deeb, Mervat F. Zayed

et al.

Scientific Reports, Journal Year: 2023, Volume and Issue: 13(1)

Published: Dec. 21, 2023

A series of new coumarin-N-heterocyclic hybrids, coumarin-quinolines 7a-e, coumarin-acridines 10b,c and coumarin-neocryptolepines 13b,c were synthesized evaluated for their anticancer antimicrobial activities. The structures all hybrids confirmed by FT-IR, 1H-NMR, 13C-NMR, MS spectrometry. anti-proliferative activity 10c 13c bio-evaluated using MTT-assay against colon (CaCo-2), lung (A549), breast (MDA-MB-231), hepatocellular carcinoma (HepG-2) human cancer cell lines doxorubicin as a reference drug. results demonstrated that, displayed moderate to good the lines. most active 7a-d CaCo-2 line with IC50: 57.1, 52.78, 57.29, 51.95 56.74 µM, selectivity index 1.38, 1.76, 2.6, 1.96 0.77; respectively. While, 7a,d potent A549 51.72, 54.8 µM 1.5, 0.67; Moreover, 7c showed potency MDA-MB-231 50.96 2.20. Interestingly, docking revealed that binding energy current compounds marked affinity values ranging from -6.54 -5.56 kcal interactions reported key amino acid SER 79. Furthermore, 10b,c, 13b Gram-positive Gram-negative bacterial fungal strains. 10b, 13b, 10c, exhibited broad-spectrum antibacterial E.coli, S. mutans, aureus MIC 3.2 66 this also antifungal C. albicans 0.0011 29.5 µM. In-silico investigation pharmacokinetic properties indicated tested had high GI absorption, low Blood Brain Barrier (BBB) permeability in addition membrane penetrability.

Language: Английский

Citations

9
Exploring the impact of novel thiazole-pyrazole fused benzo-coumarin derivatives on human serum albumin: Synthesis, photophysical properties, anti-cholinergic activity, and interaction studies DOI

Anindita Bhatta,

Jahnabi Upadhyaya,

Dipak Chamlagai

et al.

Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy, Journal Year: 2023, Volume and Issue: 308, P. 123669 - 123669

Published: Nov. 20, 2023

Language: Английский

Citations

8
Synthesis of phenylthiourea-based pyrazole, thiazole and/or pyran compounds: molecular modeling and biological activity DOI Creative Commons

Ahmad Fawzi Qarah,

Kahdr Alatawi,

Adel I. Alalawy

et al.

Journal of Taibah University for Science, Journal Year: 2023, Volume and Issue: 17(1)

Published: Aug. 11, 2023

The significant biological activity of phenylthiourea derivatives prompted the synthesis a new phenylthiourea-based heterocyclic ring systems (pyrazole, thiazole, and pyran), their chemical structures were elucidated by spectral data. DFT/B3LYP methodology was applied to explore configuration energetic features FMO's compounds. exhibited comparable energy gap, ranging from 2.13 2.56 eV, arranged in following order: 5 < 8 7 6 4b 4a. antitumor investigated against diverse cell lines, such as HepG2, HCT-116, MCF-7, PC3, WI38, using Doxorubicin reference drug. hybrids 5, 6, revealed strong cytotoxic HCT-116 (IC50 = 2.29 ± 0.46-9.71 0.34 µM). Furthermore, molecular docking studies compounds indicated that greatest score values, accordance activity.

Language: Английский

Citations

7
Sustainable synthesis of benzopyran derivatives catalyzed by MgO nanoparticles: Spectral, DFT and TEM analysis DOI Creative Commons
Har Lal Singh, Mamta Chahar,

Sangeeta Yadav

et al.

Results in Chemistry, Journal Year: 2023, Volume and Issue: 5, P. 100884 - 100884

Published: Jan. 1, 2023

In current work, a magnesium oxide nanocatalyst was synthesized via greener route using aloe-vera plant leaf extracts as reducing and stabilizing agent to construct MgO nanoparticle. The has been characterized by UV–visible spectroscopy, FT-IR TEM, SAED. Further, nanoparticles used catalyst for the efficient facile green synthesis of various benzopyran derivatives (4a-i) in good outstanding yields (89–94%) under microwave irradiation. This showed characteristics terms amount, recoverability, activity reusability without noticeably degrading performance.

Language: Английский

Citations

6
Microwave assisted synthesis of new quinolone and coumarin molecular hybrids: SAR, molecular modelling studies as dual antagonists and its antimicrobial evaluation targeting bacterial and fungal infections DOI
Tella Lakshmi Viveka, Gangadhara Angajala, Valmiki Aruna

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1303, P. 137482 - 137482

Published: Jan. 3, 2024

Language: Английский

Citations

2