Integrating data augmentation and BERT-based deep learning for predicting alpha-glucosidase inhibitors derived from Black Cohosh.

Diabetes remains one of the critical health issues worldwide, and its prevalence is gaining motion due to prevailing factors such as obesity and a sedentary lifestyle. Traditional herbal medications and natural products, particularly enzyme inhibitors, such as alpha-glucosidase, serve as promising alternatives. This study attempted to identify potent alpha-glucosidase inhibitors by including data augmentation in deep-learning modeling.

Enhanced laccase production by Paramyrothecium roridum under solid-state fermentation: Application in neutral-pH delignification and valorization of acorn shells.

This study focused on isolating and characterizing a soil-borne laccase-producing fungus, Paramyrothecium roridum, and optimizing the enzyme production under submerged (SmF) and solid-state fermentation (SSF). SSF achieved a 2-fold increase in laccase production compared to SmF, yielding an activity of 50.64 U g under optimized conditions (17.

Design and synthesis of novel quinoline-piperazines fused to a phenylhydrazinecarbothioamide scaffold as promising α-glucosidase inhibitors with anti-diabetic potential.

Aims: This study focused on the design, synthesis, and dual evaluation of novel quinoline-benzoylhydrazine derivatives as α-glucosidase inhibitor for the management of hyperglycemia and type 2 diabetes mellitus.

Materials & Methods: A series of quinoline-benzoylhydrazine compounds were synthesized and evaluated as α-glucosidase inhibitors. The most active compound was subjected to the kinetic study plus molecular docking and molecular dynamics simulations to elucidate the mechanism of inhibition and stability.

Synthesis and characterization of lignin-copper nanohybrids for colorimetric acetaminophen detection: a combined physical chemistry and machine learning study.

Acetaminophen ranks among the most widely used pharmaceutical and personal care products today. Following consumption, the drug and its metabolites are excreted into sewage systems, wastewater treatment plants, and various aquatic environments, leading to significant ecological and health impacts. In this context, the study introduced novel and easily synthesized hybrid structures through the self-polymerization and coordination of lignin with copper (Cu@lignin·HSs) for the specific and sensitive detection of acetaminophen.

A novel halophilic laccase from Halomonas elongata: Purification, characterization, and application in green synthesis of salicylic acid.

This study presents the successful one-step purification and characterization of a novel laccase derived from Halomonas elongata, an extremophilic bacterium with promising applications in industrial biocatalysis. The enzyme was purified using a Cu@FeO-NH@GA hybrid affinity support, exhibiting a specific activity of 377.8 U mg and a molecular weight of ~75 kDa.

Design of novel human microbiome-derived peptides for inhibition of OXA-48 Carbapenemase: An in-silico and in-vitro approach.

Drug-resistant bacteria have become a global healthcare challenge, especially due to their acquisition of resistance to last-resort antibiotics. OXA-48 carbapenemase is one of the notorious enzymes that inactivates carbapenems through hydrolysis. The emergence of OXA-48 and OXA-48-like carbapenemases is a significant concern as they are responsible for many outbreaks of hospital-acquired infections in various countries, with limited treatment options available.

Design, synthesis, and evaluation of triazolo[1,5-a]pyridines as novel and potent α‑glucosidase inhibitors.

α-Glucosidase is a key enzyme responsible for controlling the blood glucose, making a pivotal target in the treatment of type 2 diabetes mellitus. Present work introducestriazolo[1,5-a]pyridine as a novel, potent scaffold for α-glucosidase inhibition. A diverse scope of targeted compounds was prepared through an efficient, straightforward synthetic protocol.

1-Phenyl-β-carboline-3-carboxamide-1,2,3-triazole-N-phenylacetamide hybrids as new α-glucosidase inhibitors.

In this work, 1-phenyl-β-carboline-3-carboxamide-1,2,3-triazole-N-phenylacetamide skeleton as a novel scaffold was designed based on hybridization of moieties that were found in the potent α-glucosidase inhibitors. Fourteen derivatives 14a-n of this scaffold were synthesized by the efficient chemical reactions. In vitro anti-α-glucosidase assay demonstrated that all the new fourteen derivatives with IC values ranging from 64.

Green valorization of garlic peel waste using halophilic laccase for efficient biomass delignification and biorefinery applications.

Lignocellulosic biomass, mainly composed of cellulose, hemicellulose, and lignin, is an abundant renewable resource in agricultural and forestry residues. In contrast to cellulose and hemicellulose, lignin remains underutilized due to its complex structure. In this study, a halophilic bacterium, Virgibacillus salarius was isolated, and its laccase production was optimized for delignification.

Design, synthesis, and investigation of novel 5-arylpyrazole-glucose hybrids as α-glucosidase inhibitors.

Considering the global incidence of diabetes, developing new compounds to lower blood sugar levels has become increasingly crucial. As a result, there has been a growing focus on the synthesis of α-glucosidase inhibitors in recent years. This study investigated design, synthesis, and effects of novel 5-aryl pyrazole-glucose hybrids as α-glucosidase inhibitors.

Innovative dual-contrast nanocoating for central venous catheters: prolonged infection resistance and enhanced imaging.

Central venous catheter (CVC) related bacteremia is an essential cause of hospital infections associated with morbidity, mortality, and healthcare costs. Recent advancements in catheter coatings have demonstrated an effective strategy for preventing microbial colonization and biofilm formation. In this study, CVCs coated with green and facile laccase-manganese phosphate hybrid nanostructures [(Mn(PO)·HNSs] prevented bacterial adhesion by 100%, 80%, 60%, and 58% for , , and , respectively.

Cost-reduction strategy to culture patient derived bladder tumor organoids.

Organoids as self-organized structure derived from stem cells can recapitulate the function of an organ in miniature form which have developed great potential for clinical translation, drug screening and personalized medicine. Nevertheless, the majority of patient-derived organoids (PDOs) are currently being cultured in the basement membrane matrices (BMMs), which are constrained by xenogeneic origin, batch-to-batch variability, cost, and complexity. Besides, organoid culture relies on biochemical signals provided by various growth factors in the composition of medium.

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

Diabetes mellitus, particularly type 2 diabetes, is a growing global health challenge characterized by chronic hyperglycemia due to insulin resistance. One therapeutic approach to managing this condition is the inhibition of α-glucosidase, an enzyme involved in carbohydrate digestion, to reduce postprandial blood glucose levels. In this study, a series of thiosemicarbazide-linked quinoline-piperazine derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity, to identify new agents for type 2 diabetes management.

Quinoline-thiosemicarbazone-1,2,3-triazole-acetamide derivatives as new potent α-glucosidase inhibitors.

In this work, a novel series of quinoline-thiosemicarbazone-1,2,3-triazole-aceamide derivatives 10a-n as new potent α-glucosidase inhibitors was designed, synthesized, and evaluated. All the synthesized derivatives 10a-n were more potent than acarbose (positive control). Representatively, (E)-2-(4-(((3-((2-Carbamothioylhydrazineylidene)methyl)quinolin-2-yl)thio)methyl)-1H-1,2,3-triazol-1-yl)-N-phenethylacetamide (10n), as the most potent entry, with IC = 48.

Design, synthesis, and evaluation of novel substituted imidazo[1,2-c]quinazoline derivatives as potential α-glucosidase inhibitors with bioactivity and molecular docking insights.

α-Glucosidase inhibitors are important in the treatment of type 2 diabetes by regulating blood glucose levels and reducing carbohydrate absorption. The present study focuses on identifying new inhibitors bearing imidazo[1,2-c]quinazoline backbone through multi-step synthesis. The inhibitory potencies of the novel derivatives were tested against Saccharomyces cerevisiae α-glucosidase, revealing IC values ranging from 50.

Rational design of new quinoline-benzimidazole scaffold bearing piperazine acetamide derivatives as antidiabetic agents.

In this study, a series of fifteen compounds (7a-o) based on a quinoline-benzimidazole scaffold bearing piperazine acetamide derivatives were synthesized and evaluated for their potential as α-glucosidase inhibitors, which are important therapeutic agents in the management of type 2 diabetes mellitus. Among the synthesized compounds, 7m exhibited the most potent inhibitory activity, demonstrating a 28-fold greater efficacy than the standard clinical inhibitor, acarbose. Molecular docking studies indicated strong binding interactions between 7m and the α-glucosidase active site, including hydrogen bonding, π-π stacking, and π-cation interactions.

A new route to the synthesis of 2-hydrazolyl-4-thiazolidinone hybrids, evaluation of α-glucosidase inhibitory activity and molecular modeling insights.

One of the multifactorial worldwide health syndromes is diabetes mellitus which is increasing at a disturbing rate. The inhibition of α-glucosidase, an enzyme that catalyzes starch hydrolysis in the intestine, is one helpful therapeutic approach for controlling hyperglycemia related to type-2 diabetes. To discover α-glucosidase inhibitors, some 2-hydrazolyl-4-thiazolidinone hybrids () were synthesized from new one-pot reaction procedures.

Generation of Murine Chimeric Antigen Receptor-Modified T Cells for In Vivo Studies in Syngeneic Tumor Models.

CAR-T cell therapy has emerged as a potent and effective tool in the immunotherapy of refractory cancers. However, challenges exist in their clinical application, necessitating extensive preclinical research to optimize their function. Various preclinical in vitro and in vivo models have been proposed for such purpose; among which immunocompetent mouse models serve as an invaluable tool in studying host immune interactions within a more realistic simulation of the tumor milieu.

Design of new α-glucosidase inhibitors based on the bis-4-hydroxycoumarin skeleton: Synthesis, evaluation, and in silico studies.

In this work, we have reported the design, synthesis, in vitro, and in silico enzymatic evaluation of new bis-4-hydroxycoumarin-based phenoxy-1,2,3-triazole-N-phenylacetamide derivatives 5a-m as potent α-glucosidase inhibitors. All the synthesized analogues showed high inhibition effects against α-glucosidase (IC values ranging between 6.0 ± 0.

Vahl. Leaves: Determination of Total Phenolic and Sennoside Contents of Different Fractions in Comparison with Their α- Glucosidase and Tyrosinase Inhibitory Effects.

Background: Vahl. () is a medicinal plant containing anthraquinone compounds such as sennoside. is primarily valued for its laxative properties.

Design, synthesis, in vitro, and in silico anti-α-glucosidase assays of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives as new anti-diabetic agents.

In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a-n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor.

α-Glucosidase inhibition assay of galbanic acid and it amide derivatives: New excellent semi-synthetic α-glucosidase inhibitors.

α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a-n were investigated. Galbanic acid and compounds 3a-n showed excellent anti-α-glucosidase activity with IC values ranging from 0.3 ± 0.