Substituted piperazine conjugated to quinoline-thiosemicarbazide as potent α-glucosidase inhibitors to target hyperglycemia

Scientific Reports, Год журнала: 2025, Номер 15(1)

Опубликована: Янв. 13, 2025

Diabetes mellitus, particularly type 2 diabetes, is a growing global health challenge characterized by chronic hyperglycemia due to insulin resistance. One therapeutic approach managing this condition the inhibition of α-glucosidase, an enzyme involved in carbohydrate digestion, reduce postprandial blood glucose levels. In study, series thiosemicarbazide-linked quinoline-piperazine derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity, identify new agents diabetes management. Structure-activity relationship (SAR) analysis revealed that nature position substituents on aryl ring significantly impacted potency. Among derivatives, 2,5-dimethoxy phenyl substitution (7j) exhibited most potent activity with IC50 value 50.0 µM, demonstrating 15-fold improvement compared standard drug acarbose. Kinetic studies identified compound 7j as competitive inhibitor, Ki 32 µM. Molecular docking simulations demonstrated key interactions between active site while molecular dynamics confirmed stability enzyme-ligand complex, reflected low RMSD RMSF values.

Язык: Английский

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Current Understanding and Translational Prospects of Tetrahedral Framework Nucleic Acids

JACS Au, Год журнала: 2025, Номер 5(2), С. 486 - 520

Опубликована: Фев. 10, 2025

Tetrahedral framework nucleic acids (tFNAs) represent a promising advancement in acid nanotechnology due to their unique structural properties, high biocompatibility, and multifaceted biomedical applications. Constructed through one-pot annealing method, four single-stranded DNAs self-assemble into stable, three-dimensional tetrahedral nanostructures with enhanced mechanical robustness physiological stability, resisting enzymatic degradation. Their ability permeate mammalian cells without transfection agents, coupled modifiable surfaces, positions tFNAs as versatile carriers for drug gene delivery systems. The tFNA-based platforms exhibit superior therapeutic efficacy, including antioxidative anti-inflammatory effects, alongside efficient cellular uptake tissue penetration. These features underpin role precision medicine, enabling targeted of diverse agents such synthetic compounds, peptides, acids. Additionally, demonstrate significant potential regenerative immune modulation, antibacterial strategies, oncology. By addressing challenges translational integration, stand poised accelerate the development research clinical applications, fostering novel therapies enhancing outcomes across wide spectrum diseases. This Perspective thoroughly details attributes applications critically evaluates tFNAs' potential, outlining inherent implementation exploring solutions these obstacles.

Язык: Английский

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Contributions of Gamma-Aminobutyric Acid (GABA) Produced by Lactic Acid Bacteria on Food Quality and Human Health: Current Applications and Future Prospects

Foods, Год журнала: 2024, Номер 13(15), С. 2437 - 2437

Опубликована: Авг. 1, 2024

The need to increase food safety and improve human health has led a worldwide in interest gamma-aminobutyric acid (GABA), produced by lactic bacteria (LABs). GABA, from glutamic reaction catalyzed glutamate decarboxylase (GAD), is four-carbon, non-protein amino that increasingly used the industry safety/quality of foods. In addition possible positive effects called postbiotic, on neuroprotection, improving sleep quality, alleviating depression relieving pain, various benefits GABA-enriched foods such as antidiabetic, antihypertension, anti-inflammatory are also being investigated. For all these reasons, it not surprising efforts identify LAB strains with high GABA productivity production LABs through genetic engineering yield accelerating. However, GABA's contributions have yet been fully discussed literature. Therefore, this current review highlights synthesis applications LABs, discusses its as, for example, drug withdrawal syndromes regulating obesity overeating. Still, other potential interactions (among others) remain unanswered questions be elucidated future. Hence, paves way toward further studies.

Язык: Английский

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A review on the composition, extraction and applications of phenolic compounds

Deleted Journal, Год журнала: 2024, Номер unknown

Опубликована: Окт. 1, 2024

Язык: Английский

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Insights of biopolymeric blended formulations for diabetic wound healing

International Journal of Pharmaceutics, Год журнала: 2024, Номер 656, С. 124099 - 124099

Опубликована: Апрель 16, 2024

Язык: Английский

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In vitro and in silico assessment of antidiabetic and antioxidant potencies of secondary metabolites from Gymnema sylvestre

Biomedicine & Pharmacotherapy, Год журнала: 2024, Номер 177, С. 117043 - 117043

Опубликована: Июнь 27, 2024

This study investigated the chemical constituents, antioxidant potential, and in vitro silico antidiabetic activity of Gymnema sylvestre. Column chromatography spectroscopic techniques identified twelve compounds from methanol extract, including 4 sterols (1-4), 5 triterpenoids (5-9), 3 flavonoids (10-12). The chemophenetic significance all was also investigated. capacity extract (1-4) evaluated using FRAP DPPH assays. exhibited strong free radical scavenging (IC

Язык: Английский

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The Putative Antidiabetic Effect of Hypericum perforatum on Diabetes Mellitus

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(1), С. 354 - 354

Опубликована: Янв. 3, 2025

Diabetes mellitus (DM), a global disease that significantly impacts public health, has become increasingly common over time. In this review, we aim to determine the potential benefits of St. John’s Wort (SJW) as an adjunct therapy for DM. We gathered information from studies conducted in vitro, vivo, and humans. vitro investigated concentrations SJW extracts capable inhibiting certain enzymes or factors involved inflammatory pathway, such β-signal transducer activator transcription 1, nuclear factor κB, methylglyoxal, oxidative stress (OS). The extract was found have positive effects on OS anti-inflammatory properties DM, suggesting it could serve protective agent against diabetic vascular complications, cell damage, apoptosis. According vivo research, essential components can stimulate thermogenesis adipose tissue, inhibit several key signaling pathways, delay early death pancreatic β cells, all which contribute combating obesity. may also help treat prediabetes reduce neuropathic pain. Human confirmed some these results. However, plant’s side need further investigation through clinical research before be used

Язык: Английский

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Efficacy of Low-Carbohydrate Diets Versus Low-Fat Diets in Glycemic Control Among Patients With Type 2 Diabetes: A Systematic Review

Cureus, Год журнала: 2025, Номер unknown

Опубликована: Янв. 6, 2025

This systematic review evaluates the comparative efficacy of low-carbohydrate diets (LCDs) versus low-fat (LFDs) in improving glycemic control, weight management, and lipid profiles individuals with type 2 diabetes mellitus (T2DM) or prediabetes. Seven randomized controlled trials involving diverse populations were included, dietary interventions ranging from very ketogenic (LCK) (typically <10% total caloric intake carbohydrates, higher fat moderate protein) to carbohydrate regimens (30-45% calories). LFDs, contrast, prioritized (50-60% calories), reduced (<20-30%) protein (15-20%). Across studies, LCDs consistently demonstrated greater reductions HbA1c, fasting glucose, triglycerides, alongside superior loss increased high-density lipoprotein cholesterol compared LFDs. Additionally, associated significant medication use, highlighting their potential decrease pharmacological dependency improve metabolic outcomes, including enhanced insulin sensitivity inflammation. Despite variability long-term outcomes adherence, emerged as a promising alternative traditional approaches for managing T2DM. Further research is warranted explore strategies such behavioral technological support, evaluate sustainability, effects on cardiovascular health quality life. These findings underscore transformative management highlight need personalized approaches.

Язык: Английский

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Unveiling the Cyclopropyl Appended Acyl Thiourea Derivatives as Antimicrobial, α-Amylase and Proteinase K Inhibitors: Design, Synthesis, Biological Evaluation, Molecular Docking, DFT and ADMET Studies

Archives of Biochemistry and Biophysics, Год журнала: 2025, Номер unknown, С. 110304 - 110304

Опубликована: Янв. 1, 2025

Язык: Английский

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Diabetes-related cognitive impairment: Mechanisms, symptoms, and treatments

Open Medicine, Год журнала: 2025, Номер 20(1)

Опубликована: Янв. 1, 2025

Diabetes-related cognitive impairment is increasingly recognized as a significant complication, profoundly impacting patients' quality of life. This review aims to examine the pathophysiological mechanisms, clinical manifestations, risk factors, assessment and diagnosis, management strategies, future research directions in diabetes. A comprehensive literature search was conducted using PubMed, Medline, other medical databases identify, review, evaluate published articles on The focused studies examining pathophysiology, presentations, diagnostic approaches, strategies. current revealed that chronic hyperglycemia, insulin resistance, vascular factors are major contributing deficits Clinical manifestations include impairments attention, memory, executive function, visuospatial abilities, language. Risk encompass disease duration, glycemic control, presence complications, age, education level, comorbidities. Assessment tools screening instruments, neuropsychological testing, neuroimaging techniques. Management strategies involve control optimization, lifestyle modifications, training, pharmacological interventions. highlights prevalence impact diabetes, resulting from complex metabolic disturbances. Early detection multifaceted interventions crucial for preserving function improving patient outcomes. Future should focus neuroprotective biomarker identification, personalized approaches. Collaborative efforts between clinicians researchers essential effectively address this growing healthcare challenge enhance life individuals with diabetes-related impairment.

Язык: Английский

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