Alpha-glucosidase Inhibitor Research Articles

Advancements in Anti-Diabetic Therapy: A Review of Enhanced Efficacy and Bioavailability of Voglibose Nanoformulations

The global incidence of type 2 diabetes mellitus (T2DM) is escalating, with projections indicating that 440 million individuals will be affected by 2030. T2DM accounts for 85-95% of all diabetes cases in affluent nations and an even higher proportion in less developed countries. This widespread disease is influenced by numerous factors including cultural shifts, aging populations, urbanization, dietary changes, reduced physical activity, and other unhealthy lifestyle behaviors. Pathophysiologically, T2DM is characterized by insulin resistance, β-cell dysfunction, increased hepatic glucose production, and decreased glucagon-like peptide 1 (GLP-1) levels. Management challenges such as suboptimal medication regimens, poor patient adherence, and inadequate treatment strategies contribute to the prevalence of diabetes-related complications. Alpha-glucosidase inhibitors (α-GIs) like acarbose, voglibose, and miglitol, which primarily act in the gastrointestinal tract to reduce postprandial hyperglycaemia, have been identified as beneficial in managing these issues. Particularly, voglibose has shown superior efficacy and tolerance compared to other α- GIs. Despite their effectiveness, α-GIs are sometimes limited by gastrointestinal side effects, affecting long-term treatment adherence. Recent advancements in nanotechnology offer promising enhancements in the delivery and efficacy of these medications. Nano-formulations, ranging from 10 to 100 nm, can protect drugs from environmental degradation and improve bioavailability by optimizing the dissolution rate and increasing the saturation solubility of poorly soluble drugs. The development of nanoparticle formulations is emerging as a critical strategy to enhance the oral bioavailability of α-GIs, potentially revolutionizing T2DM management by improving drug absorption and minimizing side effects.

Antioxidative and Anticancer Potential of Luteolin: A Comprehensive Approach Against Wide Range of Human Malignancies.

Luteolin is widely distributed phytochemical, a flavonoid, in kingdom plantae. Luteolin with potential antioxidant activity prevent ROS-induced damages and reduce oxidative stress which is mainly responsible in pathogenesis of many diseases. Several chemo preventive activities and therapeutic benefits are associated with luteolin. Luteolin prevents cancer via modulation of numerous pathways, that is, by inactivating proteins; such as procaspase-9, CDC2 and cyclin B or upregulation of caspase-9 and caspase-3, cytochrome C, cyclin A, CDK2, and APAF-1, in turn inducing cell cycle arrest as well as apoptosis. It also enhances phosphorylation of p53 and expression level of p53-targeted downstream gene. By Increasing BAX protein expression; decreasing VEGF and Bcl-2 expression it can initiate cell cycle arrest and apoptosis. Luteolin can stimulate mitochondrial-modulated functions to cause cellular death. It can also reduce expression levels of p-Akt, p-EGFR, p-Erk1/2, and p-STAT3. Luteolin plays positive role against cardiovascular disorders by improving cardiac function, decreasing the release of inflammatory cytokines and cardiac enzymes, prevention of cardiac fibrosis and hypertrophy; enhances level of CTGF, TGFβ1, ANP, Nox2, Nox4 gene expressions. Meanwhile suppresses TGFβ1 expression and phosphorylation of JNK. Luteolin helps fight diabetes via inhibition of alpha-glucosidase and ChE activity. It can reduce activity levels of catalase, superoxide dismutase, and GS4. It can improve blood glucose, insulin, HOMA-IR, and HbA1c levels. This review is an attempt to elaborate molecular targets of luteolin and its role in modulating irregularities in cellular pathways to overcome severe outcomes during diseases including cancer, cardiovascular disorders, diabetes, obesity, inflammation, Alzheimer's disease, Parkinson's disease, hepatic disorders, renal disorders, brain injury, and asthma. As luteolin has enormous therapeutic benefits, it could be a potential candidate in future drug development strategies.

Isolation, characterization, and in vitro inhibitory activity of a new alpha-glucosidase inhibitor from Schleichera oleosa (Lour.) Oken leaves

Isolation, characterization, and in vitro inhibitory activity of a new alpha-glucosidase inhibitor from Schleichera oleosa (Lour.) Oken leaves

Isolation and Characterization of Lactic Acid Bacteria From "Trites" Having the Ability to Produce α-Glucosidase Inhibitors.

Alpha-glucosidase inhibitors are one of the therapies used for treating type 2 diabetes by inhibiting the absorption of carbohydrates in the gastrointestinal tract. In addition to antimicrobial activity, some probiotic species show α-glucosidase inhibitor activity, making them potential alternative therapies for type 2 diabetes. This study aimed to characterize probiotics from "trites," a traditional food from North Sumatra, Indonesia, that exhibit α-glucosidase inhibition, potentially useful for type 2 diabetes treatment. The probiotic potential of the isolates was evaluated through antagonistic activity, acid tolerance, bile tolerance, and susceptibility to antimicrobial agents. α-Glucosidase inhibition was tested with acarbose as a control. The best-performing isolate, LBSU8, was identified as Pediococcus acidilactici through 16S rRNA gene sequencing. Gene analysis using genome sequencing for LBSU8 revealed antimicrobial secondary metabolites, including RiPPs, polyketide, and NRP, while capsular polysaccharide might contribute to its antidiabetic activity. Though no specific α-glucosidase inhibitory secondary metabolites were identified, enzymes like dTDP-glucose 4,6-dehydratase, transketolase, and glucose-1-phosphate thymidylyltransferase may contribute to this activity. P. acidilactici LBSU8 shows potential as an alternative diabetes therapy in the food and drug industries. Further studies are needed to elucidate the exact mechanism behind its α-glucosidase inhibitory activity and to explore its efficacy in clinical settings.

Unveiling the Bioactive Potential of Colaconema formosanum: An in Silico Exploration of Novel Peptides from Phycobiliproteins

Colaconema formosanum, new Rhodophyta in Taiwan. However, currently, there is little documented research on the protein bioactivity of this species. The objectives of this study were to conduct an in silico assessment of C. formosanum proteins as possible sources of bioactive peptides. Six proteins from C. formosanum, phycobiliproteins group, were selected based on LC-MS/MS analysis and these proteins were verified using the Mascot database. Subsequently, in silico analysis was started by checking the protein's physicochemical properties, followed by the bioactive peptide activities in the BIOPEP-UWMTM database. Additional parameters, including the theoretical degree of hydrolysis, value and relative frequency were also assessed. The peptides were ranked using PeptideRanker to screen for novel promising bioactive, and subsequently, an evaluation of the proteins' allergenicity and toxicity was conducted. Various bioactive activities, such as an inhibitor of ACE, DPP-IV, DPP-III, alpha-glucosidase, glutamate-carboxypeptidase, leucyltransferase, antioxidant, anti-inflammatory, and other activities were generated using in silico proteolysis of phycobiliproteins employing five proteases. In silico results indicated that phycobiliproteins from C. formosanum possess significant potential as a valuable reservoir of bioactive peptides. No previous reports have been made about the in silico analysis of this species. These discoveries present novel prospects for utilizing these bioactive peptides in the pharmaceutical and biotechnology industry.

Development of marker-based quantification methods for Diospyros Montana Roxb using DoE approach and in-silico anti-diabetic screening of selected phytoconstituents of the Diospyros genus

Diabetes mellitus is a rising global health issue, necessitating effective and affordable treatments. This study aimed to develop marker-based quantification methods for Diospyros montana Roxb using a DoE approach and conduct in-silico anti-diabetic screening of its phytoconstituents. Methanolic extracts of the plant underwent fractionation, with the chloroform fraction used for simultaneous HPLC quantification of Plumbagin and Juglone. The in-vitro anti-diabetic effects were evaluated through alpha-amylase and alpha-glucosidase inhibition assays. Cytoscape 3.7.2 was used to construct networks linking phytoconstituents to Type-2 diabetes targets and pathways, while docking studies involved proteins 1SO2, 3H1V, and 5DXU. A validated HPLC method quantified Plumbagin (Rt: 4.618) and Juglone (Rt: 3.998). The chloroform fraction showed significant enzyme inhibition with IC50 values of 36.775 and 33.124. Gene network analysis highlighted 8-hydroxyisodiospyrin, and docking revealed Astragalin’s strong binding to 3H1V (score: −10.537). This study underscores Diospyros montana Roxb potential in diabetes management, warranting further research.

Antidiabetic potency of glimepiride and naringin: an in silico and in vitro investigation

Glimepiride (GLM) is one of the potential antidiabetic drugs used in clinics for a long time. It is currently used in combination with metformin along with other drugs, but has shown various complications in patients from long-term use. Thus, the hypothesis is to use a lower dose of GLM with a non-toxic class of flavonoid, naringin (NARN), for better therapy with minimal side-effects. Initially, we assessed the binding efficacy of GLM and NARN against nine putative target enzymes using AutoDock 4.2 software. We also analysed the drug chemistry, drug-ability, and cytotoxicity, as well as performed molecular dynamic (MD) simulation at 100 ns with individual and combination states using GROMACS-2022 software. Both candidates showed higher binding efficacy, especially against the AKT-serine/threonine kinase-1 (AKT1) target enzyme (−11.85 kcal/mol), and demonstrated higher stability and compatibility with AKT1 from MD-simulation (based on RMSD, Rg, RMSF, and H-bond plots) in combination than individual form. The in vitro cytotoxicity with human embryonic kidney (HEK-293) cells suggested 100 µg/mL (observed 80% of the cell viability) as a non-toxic dose for further study. Alpha-amylase, alpha-glucosidase, and DPP-IV inhibition assays revealed that both GLM and NARN inhibited up to 60% at 100 µg/mL in a concentration-dependent manner. At the end, selecting a lower dose of GLM and a higher dose of NARN (2:8 v/v ratio) showed up to 87% inhibition at 100 µg/mL. Both in silico and in vitro studies suggest that the investigated formulation could be a potential and non-toxic dose for diabetics.

Exploring Hyaluronidase and Alpha-Glucosidase Inhibition Activities of the Hydrothermal Extract of Coffee Silverskin Obtained from a Central Composite Design

Coffee silverskin (CS), the main by-product of coffee roasting production, contains various valuable bioactive compounds in its chemical compositions. Hydrothermal water extraction (HDTE) is one of the promising techniques for valorizing the organic fraction of CS into functional bioactive ingredients, which can be further exploited in various applications. This study aimed to evaluate the hyaluronidase and α-glucosidase inhibition activities of the CS extracts obtained under optimized water extraction conditions. Process optimization was performed using central composite design response surface methodology (CCD-RSM) with a broader range of extraction temperatures (25, 137.5, and 250 °C), reaction times (5, 38.5, and 72 min), and solid-to-liquid ratios (1:10, 1:80, and 1:150). The highest yield of 39.62% was obtained at 137.5 °C, with a reaction time of 72 min and an S/L ratio of 1:80. The total caffeoylquinic acid contents (T-CQA) were quantified based on the sum of three major isomers, including 3-CQA, 4-CQA, and 5-CQA. The results revealed that the highest T-CQA (2.76 ± 0.20 mg/g CS) was significantly obtained (p < 0.05) by subcritical water extraction (SWE) at 143.2 °C with an S/L ratio of 1:10 and an extraction time of 10.41 min. At such conditions, the total phenolic content (TPC), antioxidant properties (AP), and caffeine were 96.13 mg gallic acid equivalence per gram (GAE/g) CS, 20.85 ± 0.17 mg Trolox equivalence per gram (TE/g) CS, and 10.84 ± 1.25 mg/g CS, respectively. The 50% inhibition capacity (IC50) of hyaluronidase and α-glucosidase inhibition of the CS extracted were 5.00 mg/mL and 9.00 mg/mL, respectively. Our results supported the potential direct or indirect applications of CS, such as hydrothermal CS extract (HDT-CSE), in functional food or drinks. Repurposing CS residue to manufacture new products can efficiently reduce the amount of organic waste in landfills, thus conserving resources and energy and contributing to a lower overall carbon footprint in coffee production.

In silico study of Sambiloto (Andrographis paniculata) compounds from GC-MS and LC-MS/MS as alpha-glucosidase and DPP-4 enzyme inhibitor

Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia, impaired insulin secretion, and insulin action. To overcome this disease, some people treat it with natural ingredients. Sambiloto (Andrographis paniculata) is reported to have a wide range of pharmacological activities, one of which is anti-diabetic. Sambiloto showed activity in lowering blood glucose which has the potential as an antidiabetic. Computational methods, such as molecular docking, can increase the effectiveness and reduce the cost of searching for new active compounds. The purpose of this study was to determine the component compounds contained in the ethanol extract of Sambiloto and obtain the potential compounds to inhibit the alpha-glucosidase and DPP-4 enzymes as anti-diabetics with molecular docking method. Sambiloto leaves were macerated for 3 x 24 hours using ethanol 96% as a solvent and concentrated with an evaporator. Sambiloto extract was analyzed using LC-MS, and GC-MS. In-silico analysis includes geometry optimization and molecular docking methods. Preparation of the test ligands was carried out by the ChemBioDraw Ultra and ChemBio3D applications, then optimization by Gaussian 09 application. The crystal structures of the target proteins used were those with PDB ID 5NN8 for alpha-glucosidase and 2QOE for DPP-4. Molecular docking was performed using Autodock 4.2.3 application. From analysis with LC- MS/MS and GC-MS methods, 18 compounds were identified. Molecular docking was performed on the identified compounds. The results of molecular docking showed that the compound S17 (11-(P- Bromoanilino)-5H-Dibenzo [B,E] [1,4] Diazepine), S1 (andrographolide) and S2 (andrographanin) have the potential to inhibit the activity of alpha-glucosidase enzyme; on the other hand S17 (11-(P-Bromoanilino)-5H-Dibenzo [B,E][1,4]Diazepine) and S5 (andrographolactone) have the potential to inhibit the activity of DPP-4 enzyme. These compounds have the potential to inhibit alpha- glucosidase and DPP-4 enzymes which act as antidiabetics.

IN VITRO ASSESSMENT OF ETHANOLIC EXTRACT OF CUCUMIS MADERASPATANUS LEAVES AS AN α-AMYLASE AND α-GLUCOSIDASE INHIBITOR

Objective: The current study was planned to study the phytochemicals, Antioxidant, and inhibitor activity of alpha-glucosidase and alpha-amylase from leaf extract of Cucumis maderaspatanus. Methods: Extract was extracted using a soxhlet apparatus using solvents, such as n-hexane, chloroform, ethyl acetate, ethanol, and aqueous. The extracts were evaporated using a rotary evaporator. The phytochemicals were measured qualitatively and quantitatively and the antioxidant activity was done and the IC50 value was calculated. Result: The qualitative analysis of the ethnolic leaf extract of C. maderaspatanus shows the presence of carbohydrates, terpenoids, phenol compounds, tannins, saponins, flavonoids, alkaloids, anthocyanins, betacyanins, quinones, glycosides, sterol, and coumarins. Quantitative analysis of ethanolic leaf extract of C. maderaspatanus showed that the presence of phenols (98.63±0.03), flavonoids (80.35±0.78), saponin (16.56±0.04), alkaloids (12.56±0.05), and total antioxidant (130.18±2.45). The IC50 value of various parameters such as DPPH (IC50=265), Nitric oxide (IC50=213), Hydrogen peroxide (IC50=355), Hydroxyl (IC50=290), Superoxide (IC50=145), alpha-amylase activity (IC50=48), and alpha-glucosidase activity (IC50=76). Conclusion: From the study, it was concluded that the ethanolic leaf extracts of C. maderaspatanus have good antioxidant capacity, alpha-amylase, and alpha-glucosidase inhibitor activity due to phytochemicals present in it.

Treatment Patterns and Glycaemic Control Between 2015 and 2019 in Tianjin, China: A Real-World Study of Adults with Type 2 Diabetes.

Diabetes is associated with a high economic burden in China; therefore, strategies to prevent diabetes, improve glycaemic control, delay disease-related complications and maintain quality of life are essential. This study was conducted to evaluate trends in treatment patterns and glycaemic control in people with type 2 diabetes (T2D) in real-world clinical practice in Tianjin, China. This retrospective, cross-sectional, multicentre study analysed data from adults with T2D living in Tianjin, China between 2015 and 2019, based on information obtained from a regional electronic medical record database. Temporal trends in treatment patterns and glycaemic control were assessed using linear regression (continuous variables), and Cochran-Armitage (two categories) or Cochran-Mantel-Haenszel (≥ 3 categories) tests. Between 2015 and 2019, data from 312,203 individuals treated at 75 hospitals were included. Over this period, there was an upward trend in the prevalence of hypertension, hyperlipidaemia, obesity, cardiovascular disease, stroke and retinopathy each year (all P < 0.001). The use of metformin or dipeptidyl peptidase-4 inhibitors increased, while thiazolidinedione, alpha-glucosidase inhibitor and glinide use decreased; the use of basal insulin (BI), glucagon-like peptide-1 receptor agonists (GLP-1 RAs), GLP-1 RAs + BI, bolus insulin and BI + bolus insulin increased, whereas the use of premixed insulin showed a downward trend (all P < 0.001). From 2015 to 2019, an increased proportion of individuals achieved glycated haemoglobin (HbA1c) < 7% (< 53 mmol/mol; 28.1-33.7%), fasting plasma glucose (FPG) < 7 mmol/l (21.7-26.9%) and postprandial glucose (PPG) < 10 mmol/l (22.0-48.2%; all P < 0.001). There was no change in the proportion of individuals with an FPG ≥ 7 mmol/l and a PPG ≥ 10 mmol/l, while the prevalence of residual hyperglycaemia increased (P < 0.001). Glycaemic control improved between 2015 and 2019 in people with T2D in Tianjin, China; however, there is an unmet need for more effective glycaemic control.

Pharmacophore-based 3D-QSAR modeling, virtual screening, docking, molecular dynamics and biological evaluation studies for identification of potential inhibitors of alpha-glucosidase.

Alpha-glucosidase enzyme is considered an important therapeutic target for controlling hyperglycemia associated with type 2 diabetes. Novel scaffolds identified as potential alpha-glucosidase inhibitors from the Maybridge library utilizing pharmacophore modeling, molecular docking and biological evaluation are reported in this manuscript. A total of 51 xanthone series scaffolds previously reported as alpha-glucosidase inhibitors were collected and used as training and test sets. These sets were employed to develop and validate a pharmacophore-based 3D-QSAR model with statistically meaningful results using Schrodinger software. The model showed a high F value (F, 80.1) at five component partial least square factors, a high cross-validation coefficient (Q2, 0.66) and a good correlation coefficient (R2, 0.95). Pearson correlation coefficient (r) of 0.8400 indicated a greater degree of confidence in the model. Subsequently, virtual screening was performed with PHASE module of Schrodinger software using the above model to identify novel alpha-glucosidase inhibitors, and mapped compounds were evaluated for their interactions with the protein. The X-ray co-crystallised structure of the alpha-glucosidase protein in complex with acarbose (PDB Code: 5NN8) was used for molecular docking analysis using GLIDE module and a total of eight compounds were further selected for biological evaluation. Molecular dynamics analysis using GROMACS software was performed in the active site of alpha-glucosidase protein to gain insights into binding mechanism of the four active compounds which were finally found to exhibit inhibitory activity in the biological assay.

Exploring cutting-edge approaches in diabetes care: from nanotechnology to personalized therapeutics.

Diabetes mellitus (DM) is a persistent condition characterized by high levels of glucose in the blood due to irregularities in the secretion of insulin, its action, or both. The disease was believed to be incurable until insulin was extracted, refined, and produced for sale. In DM, insulin delivery devices and insulin analogs have improved glycemic management even further. Sulfonylureas, biguanides, alpha-glucosidase inhibitors, and thiazolidinediones are examples of newer-generation medications having high efficacy in decreasing hyperglycemia as a result of scientific and technological advancements. Incretin mimetics, dual glucose-dependent insulinotropic polypeptide, GLP-1 agonists, PPARs, dipeptidyl peptidase-4 inhibitors, anti-CD3 mAbs, glucokinase activators, and glimins as targets have all performed well in recent clinical studies. Considerable focus was placed on free FA receptor 1 agonist, protein tyrosine phosphatase-1B inhibitors, and Sparc-related modular calcium-binding protein 1 which are still being studied. Theranostics, stem cell therapy, gene therapy, siRNA, and nanotechnology are some of the new therapeutic techniques. Traditional Chinese medicinal plants will also be discussed. This study seeks to present a comprehensive analysis of the latest research advancements, the emerging trends in medication therapy, and the utilization of delivery systems in treating DM. The objective is to provide valuable insights into the application of different pharmaceuticals in the field of diabetes mellitus treatment. Also, the therapeutic approach for diabetic patients infected with COVID-19 will be highlighted. Recent clinical and experimental studies evidence the Egyptian experience. Finally, as per the knowledge of the state of the art, our conclusion and future perspective will be declared.

Insights into Catechin-Copper Complex Structure and Biologic Activity Modulation.

Compounds of natural origin found in varying quantities in plant-based products constitute a highly significant category, possessing structural significance as well as the capacity to regulate oxidative processes. The activity of these compounds may be modulated by the composition of the biological environment in which they operate, the pH of the environment, or the presence of metal cations in plants or plant extracts. A successful complexation reaction was mainly confirmed by FT-IR, observing the shift from the original transmittance of catechin bonds, especially O-H ones. This work shows the synthetic methodology and the optimization process that took place to synthesize a catechin-copper complex, which demonstrated antioxidant activity. It was tested for iron chelation ability, hydroxyl radicals, and the inhibition of lipoxygenase (15-LOX). An antidiabetic assay was performed by determining the inhibition of alpha-amylase and alpha-glucosidase, finding that the synthesized complex had similar inhibitory potential as pure catechin. The antibacterial tests showed results against Staphylococcus aureus and the antifungal properties of the complex against Candida albicans.

In vitro Anti-oxidant, Alpha-Amylase, and Alpha-Glucosidase Inhibition Studies of Physica aipolia (Ehrh.ex Humb.) Furnr

Background: Diabetes prevalence is progressively rising everywhere, particularly in developing countries. Lichens have evolved into a rich source of innovative bioactive chemicals with their anti-oxidant capabilities, widening the scope of well-documented and effective diabetes treatment. Objective: The main objectives of this study were to perform in vitro alpha-amylase, alphaglucosidase inhibition analysis, and anti-oxidant of lichen Physica aipolia. Method: Folin Ciocalteu’s reagent was used to determine the total phenolic content for biological activities. The Aluminum trichloride method was used to determine total flavonoid content, and the free radical assay method was used to determine the antioxidant activity of P. aipolia using 2,2- diphenyl-1-picrylhydrazyl (DPPH). Moreover, substrate 2-Chloro-4-nitrophenyl-α-D-maltotrioside (CNPG3) and substrate-nitrophenyl-α-D-glucopyranose (p-NPG) were used for the determination of alpha-amylase and alpha-glucosidase inhibition activities respectively, and molecular docking was performed by Auto Dock Vina. Results: Total phenolic and flavonoid contents present in P. aipolia were 37.41 ± 2.87 mg GAE/g and 5.53 ± 0.95 mg QE/g, respectively. For anti-oxidant inhibition activity, crude extract of methanol showed an IC50 value of 15.324 ± 0.80 μg/mL. Furthermore, a methanolic crude extract showed significant inhibition activities against alpha-amylase (IC50 = 178.50 ± 1.10 μg/mL) and alphaglucosidase (IC50 = 76.10 ± 0.91 μg/mL). During in silico analysis, zeorin showed an effective binding affinity with -7.9 kcal/mol, and Atranorin showed -7.4 kcal/mol in the orthosteric site of the protein. Conclusion: Physica aipolia exhibits the potential to impact biological functions, demonstrating antidiabetic properties, as confirmed by molecular docking analysis in silico.

Stevia By-product Fraction has Antioxidant Capacity and has been Evaluated for its Antihyperglycemic and Antilipid Potential

Introduction/Objective: The ethanolic pretreatment of stevia leaves is considered ecologically favorable and increases its yield, purity level, and sensory profile of sweeteners. We investigated the by-product generated so that we can provide a viable and applicable destination to effectively contribute to the production and industrial chain of stevia sweeteners. Recently, an antioxidant and antidiabetic fraction was obtained through stevia methanolic extraction. However, this process is costly, has a low yield, and is non-green. In this study, we got an antioxidant fraction of stevia from its pretreatment by-product, the ethanolic extract, characterized its bioactive compounds – mainly phenolic acids and flavonoids – and evaluated its antidiabetic and antilipid capacity. Methods: The ethanolic extract was fractionated, then the ethyl acetate fraction was microencapsulated. Physicochemical, Mass Spectrometry (UHPLC/MS-MS), scanning electron microscopy, microencapsulation efficiency, and antioxidant capacity analyses were carried out. The antioxidant capacity was evaluated. Antihyperglycemic capacity was assessed by inhibition of α-glucosidase and α-amylase. For antilipid potential, inhibition of pancreatic lipase was measured. Results: Antioxidant potential was observed mainly in the fraction. Microencapsulation improved the stability of the fraction. Mass spectrometry allowed comparison with phenolic and flavonoid compounds from the methanolic and ethanolic fractions of the by-product. Many compounds were coincident, which may explain the similar antioxidant capacity found. The samples showed more than 90% inhibition of alpha-glucosidase, which may indicate potential antidiabetic activity. All samples showed inhibition of the pancreatic lipase enzyme higher than 80%, reaching 91.05% for the free fraction. Conclusion: This study represented the recovery of a by-product and showed that this antioxidant fraction deserves further investigation for its bioactive potential, especially antioxidant, antidiabetic, and anti-lipid.

Biological characterization of marine algae and its potent in vitro antioxidant, antimicrobial and larvicidal activity: a focus on Ulva lactuca Linnaeus 1753: 1163.

This study evaluated the biological characteristics of seaweeds Turbinaria ornata, Ulva lactuca, and Gracilaria crassa. Among the seaweeds tested, ethyl acetate extract of Ulva lactuca exhibited the highest antibacterialactivity against Salmonella enterica, Staphylococcus aureus, and Pseudomonas aeruginosa. The phytochemical analysis of ULME and ULEA showed the presence of most of the tested phytochemicals, whereas only amino acids, tannins, glycosides, and carbohydrates were detected by ULHE. The DPPH scavenging property of U. lactuca exerted the maximum antioxidant property of 62.54% (ULME), 75.64% (ULEA), and 39.55% (ULHE), whereas the alpha amylase inhibitory property (µg/mL) of ULME, ULEA, and ULHE was, respectively, 80.99, 51.15, and 49.23. ULME, ULEA, and ULHE exhibited the greatest alpha-glucosidase inhibition, with IC50 values (g/mL) of 116.12, 45.59, and 170.10 correspondingly. ULEA also showed potent mosquito-larvicidal effects against Aedes aegypti larvae with the maximum lethal concentration values with LC50 and LC90 values (mg/mL) being 11.55 and 65.97, respectively. FTIR analysis of ULME, ULHE, and ULEA were found to have various functional groups, including alkanes, carboxylic acids, alkenes, alkynes, aldehydes, amides and alkanes, ketones, and aromatics, while HPLC revealed a strong peak at 4.760 retention time. In conclusion, Ulva lactuca, particularly its ethyl acetate extract, demonstrates significant antibacterial, antioxidant, and enzyme-inhibitory properties, highlighting its therapeutic and biotechnological potential. Its diverse phytochemicals and effective mosquito-larvicidal activity further support its broad application prospects.

Review on the role of nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3) inflammasome pathway in diabetes: mechanistic insights and therapeutic implications.

This review explores the pivotal role of the nucleotide-binding oligomerization domain (NOD)-like receptor protein 3 (NLRP3) inflammasome in the pathogenesis of diabetes and its complications, highlighting the therapeutic potential of various oral hypoglycemic drugs targeting this pathway. NLRP3 inflammasome activation, triggered by metabolic stressors like hyperglycemia, hyperlipidemia, and free fatty acids (FFAs), leads to the release of pro-inflammatory cytokines interleukin-1β and interleukin-18, driving insulin resistance, pancreatic β-cell dysfunction, and systemic inflammation. These processes contribute to diabetic complications such as nephropathy, neuropathy, retinopathy, and cardiovascular diseases (CVD). Here we discuss the various transcriptional, epigenetic, and gut microbiome mediated regulation of NLRP3 activation in diabetes. Different classes of oral hypoglycemic drugs modulate NLRP3 inflammasome activity through various mechanisms: sulfonylureas inhibit NLRP3 activation and reduce inflammatory cytokine levels; sodium-glucose co-transporter 2 inhibitors (SGLT2i) suppress inflammasome activity by reducing oxidative stress and modulating intracellular signaling pathways; dipeptidyl peptidase-4 inhibitors mitigate inflammasome activation, protecting against renal and vascular complications; glucagon-like peptide-1 receptor agonists attenuate NLRP3 activity, reducing inflammation and improving metabolic outcomes; alpha-glucosidase inhibitors and thiazolidinediones exhibit anti-inflammatory properties by directly inhibiting NLRP3 activation. Agents that specifically target NLRP3 and inhibit their activation have been identified recently such as MCC950, Anakinra, CY-09, and many more. Targeting the NLRP3 inflammasome, thus, presents a promising strategy for managing diabetes and its complications, with oral hypoglycemic drugs offering dual benefits of glycemic control and inflammation reduction. Further research into the specific mechanisms and long-term effects of these drugs on NLRP3 inflammasome activity is warranted.

Unveiling the Therapeutic Potential of Basella alba: A Comprehensive Investigation into Its Anti-arthritic Properties, Phytochemical Profile, and Molecular Docking Insights.

Polyherbal antidiabetic tablets were formulated, evaluated and compressed by combining the powder extract of Nigella sativa, Trigonella foenum, and Glycyrrhiza Glabra. A number of tests were carried out, including a uniformity weight test, an assessment of the tablets’ hardness and friability, an ash value, moisture content, an extractive value that is soluble in water or alcohol, density (bulk and tapped), repose angle, Carr’s index, disintegration time with preliminary phytochemical screening. The tablet also had ex-vivo antidiabetic performance to enzymes alpha-amylase as well as glucosidase. To ensure the presence of active ingredients, thin-layer chromatography was performed. Column chromatography as performed using silica gel G as a stationary phase. The column of material was created using acetic acid, toluene, and ethyl acetate. As follows: (5.0:4.2:0.8) for 10 ml. The mobile phase of the sample, which contains toluene, ethyl acetate, acetic acid (50:42:8) and fractions, was isolated, collected and sent to IIT Bombay for GCHRMS analysis. In GCHRMS, the chemical constituent was found to be 2 H-Pyran-2-one, tetrahydro-4-hydroxy-4-methyl-, Tetrahydro [2 , 2’] bifuranyl-5-one, 1H-Benzimidazole, 2-(1-methylethyl)-, Bifenthrin, Propionamide, 2,2-diphenyl-N-(2-pyridinyl)-, Dihydromyristicin, 2-Dodecanone, di-p-Tolyl sulfone. The tablets showed promising results for alpha-amylase and alpha-glucosidase inhibition activities.

Bioguided Fractionation and Isolation of Natural Antidiabetic Agents from Polyherbal Tablet.

Polyherbal antidiabetic tablets were formulated, evaluated and compressed by combining the powder extract of Nigella sativa, Trigonella foenum, and Glycyrrhiza Glabra. A number of tests were carried out, including a uniformity weight test, an assessment of the tablets’ hardness and friability, an ash value, moisture content, an extractive value that is soluble in water or alcohol, density (bulk and tapped), repose angle, Carr’s index, disintegration time with preliminary phytochemical screening. The tablet also had ex-vivo antidiabetic performance to enzymes alpha-amylase as well as glucosidase. To ensure the presence of active ingredients, thin-layer chromatography was performed. Column chromatography as performed using silica gel G as a stationary phase. The column of material was created using acetic acid, toluene, and ethyl acetate. As follows: (5.0:4.2:0.8) for 10 ml. The mobile phase of the sample, which contains toluene, ethyl acetate, acetic acid (50:42:8) and fractions, was isolated, collected and sent to IIT Bombay for GCHRMS analysis. In GCHRMS, the chemical constituent was found to be 2 H-Pyran-2-one, tetrahydro-4-hydroxy-4-methyl-, Tetrahydro [2 , 2’] bifuranyl-5-one, 1H-Benzimidazole, 2-(1-methylethyl)-, Bifenthrin, Propionamide, 2,2-diphenyl-N-(2-pyridinyl)-, Dihydromyristicin, 2-Dodecanone, di-p-Tolyl sulfone. The tablets showed promising results for alpha-amylase and alpha-glucosidase inhibition activities.