Synthesis, Characterization, and Antioxidant Activity Evaluation of New N-Methyl Substituted Thiazole-Derived Polyphenolic Compounds

Molecules, Год журнала: 2025, Номер 30(6), С. 1345 - 1345

Опубликована: Март 17, 2025

Reactive oxygen species play a significant role in various pathological conditions, driving the need for novel, potent antioxidants. While polyphenols are known their antioxidant properties, limited stability and bioavailability present challenges therapeutic applications. To address these limitations, series of novel thiazolyl-polyphenolic compounds was synthesized via multi-step synthetic route incorporating Hantzsch heterocyclization final step. The 7a–k were structurally characterized using spectroscopic techniques, including NMR, MS, IR. In silico thermodynamic calculations, HOMO–LUMO gap bond dissociation enthalpy (BDE) revealed promising profile indicated that substitution position 2 thiazole ring does not substantially influence activity conferred by catechol moiety 4. capacity experimentally validated panel six distinct assays: two radical scavenging assays (ABTS DPPH) four electron transfer-based (RP, TAC, FRAP, CUPRAC). vitro evaluation demonstrated 7j 7k exhibited significantly enhanced compared to established standards, ascorbic acid Trolox. These findings suggest strategic modifications scaffold represent direction future research aimed at developing agents with properties. study is based on N-methyl substituted scaffold, but studies can include such as changing substituent nitrogen, hydrazone linker or possible insertion substituents 5 electronic physico-chemical

Язык: Английский

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Norfloxacin affects inorganic nitrogen compound transformation in tailwater containing Corbicula fluminea

Journal of Hazardous Materials, Год журнала: 2024, Номер 476, С. 135116 - 135116

Опубликована: Июль 6, 2024

Язык: Английский

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Alleviation of hyperglycaemia and oxidative stress by fruit extracts of different cultivars of the cornelian cherry (Cornus mas L. and Cornus mas × Cornus officinalis) in rats with diabetes mellitus

Food & Function, Год журнала: 2025, Номер unknown

Опубликована: Янв. 1, 2025

Biological effects of fruit extracts from the different cultivars cornelian cherry in rats with streptozotocin-induced diabetes mellitus.

Язык: Английский

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Assessing water quality of River Mahananda, Malda, India using Cirrhinus reba as a bioindicator: Oxidative stress biomarkers and histopathological fingerprints

Environmental Monitoring and Assessment, Год журнала: 2025, Номер 197(5)

Опубликована: Апрель 9, 2025

Язык: Английский

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A Systematic Review of Endothelial Dysfunction in Chronic Venous Disease—Inflammation, Oxidative Stress, and Shear Stress

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(8), С. 3660 - 3660

Опубликована: Апрель 12, 2025

Chronic venous disease (CVD) is among the most common diseases in industrialized countries and has a significant socioeconomic impact. The diversity of clinical symptoms manifestations CVD pose major challenges routine diagnosis treatment. Despite high prevalence huge number surgical interventions performed every day, substantial proportion etiopathogenesis remains unclear. There are several widely advocated generally valid theories “peri-capillary fibrin cuffs” “white cell trapping hypothesis”, which consider role reflux/obstruction, inflammation, vascular remodeling, hemodynamic changes, genetic social risk factors. specific provoking factors for development reflux: incompetence valve system, inflammation wall, hypertension. Over past few years, increasing scientific data demonstrated link between oxidative stress, endothelial dysfunction, inflammation. High levels oxidants persistent can cause cumulative changes hemodynamics, resulting permanent irreversible damage to microcirculation cells. Production reactive oxygen species expression inflammatory cytokines adhesion molecules involved vicious cycle wall remodeling. interaction ROS, particular, superoxide anion radical, with nitric oxide leads decrease NO bioavailability, followed by initiation prolonged vasoconstriction hypoxia impairment tone. This review addresses ED, oxidative, stress mediation. Based on predefined inclusion exclusion criteria, we conducted systematic published articles using PubMed, PMC Europe, Scopus, WoS, MEDLINE, Google Scholar databases interval from 24 April 2002 1 2025. current included studies (n = 197) articles, including new reviews, updates, grey literature, were evaluated according eligibility criteria. selection process was standardized form PRISMA rules, manual search databases, double-check ensure transparent complete reporting reviews. Studies had report quantitative assessments relationship shear chronic disease.

Язык: Английский

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Diisononyl phthalate down-regulates the expression of antioxidant genes NFE2L2 , TXN , and TXNRD2 , while Diethyl-hexyl terephthalate up-regulates their expression including SOD-1

Xenobiotica, Год журнала: 2025, Номер unknown, С. 1 - 18

Опубликована: Апрель 16, 2025

Phthalates, widely utilized as plasticisers to enhance the flexibility of rigid materials like polyvinyl chloride, are known for their endocrine-disrupting properties and cytotoxic effects. This study investigated impact Diisononyl phthalate (DINP) Diethyl-hexyl terephthalate (DEHT) on human endothelial cells (EA.hy926). The assessment focused cell viability, reactive oxygen species (ROS) production, antioxidant-responsive genes expression (NFE2L2, SOD1, TXN, TXNRD2) following exposure varying 1, 10, 100 µg/mL DINP or DEHT. Cell viability was determined using MTT lactate dehydrogenase (LDH) release assays. ROS were measured DCFDA assay. Gene analysis conducted via qRT-PCR after 48 h exposure. Results revealed that significantly reduced at 11 17% 72 h, respectively; whereas increased LDH by 69% 48h. levels also rose 19-30%, accompanied down-regulation NFE2L2, TXNRD2. Conversely, DEHT had no adverse effect but elevated production (11-14%) induced up-regulation antioxidant genes, including SOD1. findings indicate could negatively affect cellular response, leads without detrimental effects viability.

Язык: Английский

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Potential treatment of glutathione in bullfrogs with abnormal hepatic lipid metabolism revealed by hepatic lipid metabolism and serum metabolomics analysis

Frontiers in Cellular and Infection Microbiology, Год журнала: 2024, Номер 14

Опубликована: Авг. 13, 2024

Introduction With the continuous growth of bullfrog supply, it has become an important aquaculture species. Due to lack actionable industry standards and regulation, misuse anti-disease drugs abnormal liver lipid metabolism in bullfrogs have a major obstacle development industry. Glutathione is natural tripeptide that can be synthesized intracellularly, its physiological functions mainly include treatment diseases, antioxidant, detoxification, anti-tumor, enhancement immunity, delaying aging. Methods In this study, therapeutic effect glutathione on with was revealed from hepatic serum metabolomics analysis. The survival rate, histomorphology, antioxidant enzyme activity, lipase activity metabolomics, were studied analyzed by feeding for 20 days NC, FI GSH groups. Results results study showed able repair improve rate metabolism; SOD enzymes significantly increased; activities ACP AKP decreased; HDL-C T-CHO LDL-C, TBA, TG decreased liver; contents metabolites, such as PC, PS, PE up-regulated, levels up-regulated Autophagy - other, Necroptosis ErbB signaling pathway, down-regulated Sphingolipid metabolism, D-Amino acid metabolic some extent pathways alleviate disorders glycerophospholipid amino certain extent, thus alleviating abnormalities metabolism. Discussion could effectively treat disorder bullfrogs, promote function, reduce inflammation, healthy green

Язык: Английский

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Cardioprotective Effects of an Aqueous Extract of Solanum tuberosum (Irish Potato Peels) on the Heart of Streptozotocin-Induced Diabetic Wistar Rats

Asian Journal of Biological Sciences, Год журнала: 2024, Номер 18(1), С. 179 - 194

Опубликована: Дек. 10, 2024

Язык: Английский

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Investigation of Impact of Oxidative Stress on Human Periodontal Ligament Cells Exposed to Static Compression

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(24), С. 13513 - 13513

Опубликована: Дек. 17, 2024

Oxidative stress (OS) is a common feature of many inflammatory diseases, oral pathologies, and aging processes. The impact OS on periodontal ligament cells (PDLCs) in relation to including has been investigated different studies. However, its orthodontic tooth movement (OTM) remains poorly understood. This study used an vitro model with human PDLCs previously exposed H2O2 investigate the effects under static compressive force which simulated conditions OTM. Human were treated varying concentrations identify sub-lethal doses that affected viability minimally. To mimic compromised resembling OTM OS, pretreated selected for 24 h. Using loading model, (2 g/cm2) was applied additional cell viability, proliferation, cytotoxicity evaluated using live/dead resazurin assays. Apoptosis induction assessed based caspase-3/7 activity. gene expression related bone remodeling (RUNX2, TNFRSF11B/OPG, BGLAP), inflammation (IL6, CXCL8/IL8, PTGS2/COX2), apoptosis (CASP3, CASP8), autophagy (MAP1LC3A/LC3, BECN1) analyzed RT-qPCR. suggests altering effect previous exposure static-compression-related mechanosensing. Further research needed fully elucidate these mechanisms.

Язык: Английский

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Design, synthesis and evaluation of imidazo[1,2-a]pyrazin-8(7H)-one derivatives as acetylcholinesterase inhibitors and antioxidants

Research Square (Research Square), Год журнала: 2024, Номер unknown

Опубликована: Июнь 24, 2024

A series of 8-(piperazin-1-yl)imidazo[1,2-a]pyrazine derivatives were designed and synthesized as acetylcholinesterase inhibitors (AChEIs) antioxidants for the treatment Alzheimer's disease (AD). Moreover, biological evaluation results demonstrated that these compounds exhibited moderate inhibitory activities toward (AChE) radical scavenging activities. Among them, compound 14r was most potent AChE inhibitor with an IC₅₀ value 0.47 µM activity against butyrylcholinesterase (BuChE) (IC₅₀ = 11.02 µM). Meanwhile had best selectivity index (SI) values 23.45. Compound has better well compared to reference drug galantamine (AChE 5.01 µM, BuChE 18.46 SI 3.68). 14o antioxidant 89.33 which lower than ascorbic acid 25.70 µM) control drug. Furthermore, molecular docking studies indicated could simultaneously bind both catalytic active site peripheral anionic AChE, consistent mixed inhibition pattern shown by enzyme kinetic studies. The interaction’s stability 14r-AChE/BuChE also assessed using a conventional atomistic 100 ns dynamics simulation study, revealed conformational representative in cavity AChE. In addition, properties all predicted online through SwissADME, matched orally administered drugs. Based on properties, AChEI valuable further development.

Язык: Английский

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