Α-glucosidase Inhibitors Research Articles

Identification of natural curcumins as potential dual inhibitors of PTP1B and α-glucosidase through experimental and computational study

Curcuma longa is a rich source of curcumin (1) and its major analogs, demethoxycurcumin (2), and bisdemethoxycurcumin (3), among the Curcuma species. In this study, curcumins (1–3) were purified from C. longa, and their inhibitory effects against protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase enzymes were assayed. These compounds potential inhibited PTP1B and α-glucosidase activities with IC50 values ranging from 37.8 to 72.6 μM, and 78.2–90.6 μM, respectively. In addition, density functional theory (DFT) accompanied by molecular docking (MD) were employed to analyze the ligand stability and the interaction of curcumins 1–3 with PTP1B and glucoside hydrolase proteins. The assay-based results and MD data obtained showed a high correlation, suggesting that the deterioration of enzyme activity caused by the distortion of the structural conformation of PTP1B and glucoside hydrolase may be related to the arrangement of amino acids in the protein structure. Our findings reveal the significant role of methoxylation in the variation of inhibitory effects of these curcumins against PTP1B and α-glucosidase. These in vitro and in silico activities of curcumins (1–3) against PTP1B and glucoside hydrolase have been examined and reported for the first time.

UHPLC-Q-TOF-MS/MS identification of metabolites in cereal beverage ‘Borde’ and its anti-obesity efficacy in Caenorhabditis elegans model

This research explores the remarkable impact of fermented cereals such as sorghum, maize, and wheat with Pediococcus acidilactici WS07, a strain isolated from Ethiopia's traditional borde beverage. The fermented cereal extracts were thoroughly evaluated for antioxidant activity, inhibition of pancreatic lipase and α-glucosidase, metabolite identification through UHPLC-Q-TOF-MS/MS, and in vivo efficacy using the C. elegans model. The results revealed significant enhancements in the bioactive compounds of fermented cereals, demonstrating promising directions for obesity prevention strategies. Notably, the fermented sorghum extracts improved lipase (88.23 %) and α-glucosidase (85.62 %) inhibitory activities compared to its unfermented counterparts. The antioxidant properties of all fermented samples were confirmed through improved DPPH (67.77–71.86 %) and ABTS (59.91–65.49 %) scavenging activities. Fermentation also led to a notable increase in polyphenols and flavonoids, with detailed metabolite analysis revealing a dynamic shift in the composition of these bioactive compounds. Additionally, C. elegans indicates that fermented extracts extend lifespan, reduce lipid accumulation, and lower triglycerides, highlighting their potential as functional foods for health enhancement and obesity management. This study not only underscores the efficacy of P. acidilactici WS07 fermentation in transforming cereals into nutrient-rich functional foods but also provides insight into how microbial fermentation can unlock the health-promoting potential of traditional diets.

Synthesis, in vitro and in silico study of novel 1,3-diphenylurea derived Schiff bases as competitive α-glucosidase inhibitors.

Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized and their anti-diabetic activity was evaluated by targeting α-glucosidase. The compounds exhibited an overwhelming inhibitory potential for α-glucosidase with higher potency ranging from 2.49-37.16 μM. The most effective compound, 5h, showed competitive inhibition of α-glucosidase (K i = 3.96 ± 0.0048 μM) in the kinetic analysis and strong binding interactions with key residues α-glucosidase in docking analysis, indicating its potential for better glycemic control in diabetes patients.

Synthesis of furo[2,3-c]carbazoles as potent α-glucosidase and α-amylase inhibitors

The carbazole-3-carbaldehyde 2, produced by N-ethyl carbazole via Vilsmeier-Haack reaction, was subjected to Dakin type oxidation with H2O2 and H2SO4 in methanol to produce the carbazole-3-ol 3. The reaction of 3 with a range of commercially available α-haloketones 4a–f in the presence of Al2O3 as catalyst in xylene led to their regio-selective cyclization to afford the furo[2,3-c]carbazoles 5a–f. Identification of the furo[2,3-c]carbazoles 5a–f were performed through 1H NMR,13C NMR, FT-IR and high resolution mass spectrometry. Single crystal X-ray diffraction analysis was employed to further confirm the structures of the some of the targeted compounds. In vitro antidiabetic activities of the newly synthesized furocarbazoles 5a–e were investigated utilizing α-glucosidase and α-amylase enzymes. The biological evaluation revealed the obvious efficiencies of the targeted molecules toward the α-glucosidase enzyme inhibition with the potent IC50 values compared to the standard acarbose. In the case of α-glucosidase inhibition, the furo[2,3-c]carbazoles chloro substituted 5c and nitro substituted 5f were found to be more potent than acarbose with the values of 215.0 and 162.70 μM, respectively. On the other hand, the compound 5f was found to be only promising candidate for α-amylase enzyme but not as effective as the standard acarbose.

Inhibitory Mechanism of Camellianin A against α-Glucosidase: In Vitro and Molecular Simulation Studies.

α-Glucosidase is an important target for type II diabetes treatment, and the search for natural α-glucosidase inhibitors is currently a hot topic in functional food research. Camellianin A is the main flavonoid in the leaves of Adinandra nitida, but research on its inhibition of α-glucosidase is rarely reported. In view of this, the present study systematically investigated the inhibitory impact of camellianin A on α-glucosidase, combining the fluorescence method and molecular docking to explore their interaction, aiming to reveal the relevant inhibitory mechanism. The results indicated that camellianin A possessed excellent α-glucosidase inhibitory activity (IC50, 27.57 ± 0.59 μg/mL), and van der Waals force and hydrogen bonding dominated the binding process between camellianin A and α-glucosidase, with a binding-site number of 1. A molecular docking experiment suggested that camellianin A formed hydrogen bonding with Glu771, Trp391, Trp710, Gly566, Asp568, and Phe444 of α-glucosidase, consistent with the thermodynamic result. Our result can provide a reference for the development of natural α-glucosidase inhibitors.

Access to Isoxazoles via Photo-oxygenation of Furan Tethered α-Azidoketones.

Photocatalyst-free visible light-enabled direct oxygenation of furan-tethered α-azidoketones was studied. The reaction yielded various products depending on the substituents, with isoxazoles forming as the major products. The findings suggest that singlet oxygen was generated during the reaction and reacted with α-azidoketones in a [4 + 2] fashion to yield endoperoxides, which rearranged in multiple ways to generate isoxazoles. Some of the synthesized isoxazoles were evaluated as α-glucosidase inhibitors, and three of them 5bi, 5bj, and 5bl exhibited good activity with IC50 values of 454.57 ± 29.34, 147.84 ± 2.28, and 272.58 ± 42.06 μM, respectively, when compared with the standard drug acarbose (IC50 = 1224.33 ± 126.72 μM).

Upgrading the Bioactive Potential of Hazelnut Oil Cake by Aspergillus oryzae under Solid-State Fermentation.

Hazelnut oil cake (HOC) has the potential to be bioactive component source. Therefore, HOC was processed with a solid-state fermentation (SSF) by Aspergillus oryzae with two steps optimization: Plackett-Burman and Box-Behnken design. The variables were the initial moisture content (X1: 30-50%), incubation temperature (X2: 26-37 °C), and time (X3: 3-5 days), and the response was total peptide content (TPC). The fermented HOC (FHOC) was darker with higher protein, oil, and ash but lower carbohydrate content than HOC. The FHOC had 6.1% more essential amino acid and benzaldehyde comprised 48.8% of determined volatile compounds. Fermentation provided 14 times higher TPC (462.37 mg tryptone/g) and higher phenolic content as 3.5, 48, and 7 times in aqueous, methanolic, and 80% aqueous methanolic extract in FHOC, respectively. FHOC showed higher antioxidant as ABTS+ (75.61 µmol Trolox/g), DPPH (14.09 µmol Trolox/g), and OH (265 mg ascorbic acid/g) radical scavenging, and α-glucosidase inhibition, whereas HOC had more angiotensin converting enzyme inhibition. HOC showed better water absorption while FHOC had better oil absorption activity. Both cakes had similar foaming and emulsifying activity; however, FHOC produced more stable foams and emulsions. SSF at lab-scale yielded more bioactive component with better functionality in FHOC.

Molecular hybridization, synthesis, in vitro α-glucosidase inhibition, in vivo antidiabetic activity and computational studies of isatin based compounds

In the pursuit of novel antidiabetic agents, a series of isatin-thiazole derivatives (7a-7j) were synthesized and characterized using a range of spectroscopic techniques. The enzyme inhibitory activities of the target analogues were assessed using both in vitro and in vivo assays. The tested compounds 7a-7j demonstrated In vitro inhibitory potential against α-glucosidase, as indicated by their IC50 values ranging from 28.47 to 46.61 µg/ml as compared to standard drug acarbose IC50 value of 27.22 ± 2.30 µg/ml. Additionally, compounds 7d and 7i were chosen for in vivo evaluation of their antidiabetic efficacy in streptozotocin-induced diabetic Wistar rats. These compounds exhibited significant antidiabetic activity both in vitro and in vivo, compound 7d produces therapeutic effects compared to standard pioglitazone by decreasing glycaemia and triglyceride levels in diabetic animals. Furthermore, a molecular docking study was conducted to elucidate the binding interactions of the compounds within the α-glucosidase enzyme binding pocket (PDB ID 3A47) and stability was confirmed by dynamics simulation trajectories. Thus, from the above findings, it may demonstrate that isatin-thiazole hybrids constitute promising candidates in the pursuit of developing newer oral antidiabetic agents.

Isolation and Characterization of Novel Pueroside B Isomers and Other Bioactive Compounds from Pueraria lobata Roots: Structure Elucidation, α-Glucosidase, and α-Amylase Inhibition Studies.

Pueraria lobata (Willd.) Ohwi is a traditional medicinal herb that has been extensively used in Chinese medicine for various therapeutic purposes. In this study, twelve chemical constituents were isolated from the roots of P. lobata, comprising three puerosides (compounds 1-3), six alkaloids (compounds 4-9), and three additional compounds (compounds 10-12). Notably, compound 1 (4R-pueroside B) was identified as a novel compound. The structures of all compounds were elucidated using a range of spectroscopic techniques, including CD spectroscopy for the first-time determination of the absolute configurations of pueroside B isomers (compounds 1 and 2). Enzyme inhibition assays revealed that, with the exception of compound 2, all isolated compounds exhibited varying degrees of α-glucosidase and α-amylase inhibitory activity. Remarkably, compound 12 demonstrated IC50 values of 23.25 μM for α-glucosidase inhibition and 27.05 μM for α-amylase inhibition, which are superior to those of the positive control, acarbose (27.05 μM and 36.68 μM, respectively). Additionally, compound 11 exhibited inhibitory activity against α-glucosidase and α-amylase comparable to the positive control, acarbose. Molecular docking studies indicated that compound 12 interacts with the active sites of the enzymes via hydrogen bonds, van der Waals forces, and hydrophobic interactions, which likely contribute to their inhibitory effects. These findings suggest that the chemical constituents of P. lobata could be potential natural sources of α-amylase and α-glucosidase inhibitors, with compound 12 being particularly promising for further investigation.

Clinical application of cluster analysis in patients with newly diagnosed type 2 diabetes.

Early prevention and treatment of type 2 diabetes mellitus (T2DM) is still a huge challenge for patients and clinicians. Recently, a novel cluster-based diabetes classification was proposed which may offer the possibility to solve this problem. In this study, we report our performance of cluster analysis of individuals newly diagnosed with T2DM, our exploration of each subtype's clinical characteristics and medication treatment, and the comparison carried out concerning the risk for diabetes complications and comorbidities among subtypes by adjusting for influencing factors. We hope to promote the further application of cluster analysis in individuals with early-stage T2DM. In this study, a k-means cluster algorithm was applied based on five indicators, namely, age, body mass index (BMI), glycosylated hemoglobin (HbA1c), homeostasis model assessment-2 insulin resistance (HOMA2-IR), and homeostasis model assessment-2 β-cell function (HOMA2-β), in order to perform the cluster analysis among 567 newly diagnosed participants with T2DM. The clinical characteristics and medication of each subtype were analyzed. The risk for diabetes complications and comorbidities in each subtype was compared by logistic regression analysis. The 567 patients were clustered into four subtypes, as follows: severe insulin-deficient diabetes (SIDD, 24.46%), age-related diabetes (MARD, 30.86%), mild obesity-related diabetes (MOD, 25.57%), and severe insulin-resistant diabetes (SIRD, 20.11%). According to the results of the oral glucose tolerance test (OGTT) and biochemical indices, fasting blood glucose (FBG), 2-hour postprandial blood glucose (2hBG), HbA1c, total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and triglyceride-glucose index (TyG) were higher in SIDD and SIRD than in MARD and MOD. MOD had the highest fasting C-peptide (FCP), 2-hour postprandial C-peptide (2hCP), fasting insulin (FINS), 2-hour postprandial insulin (2hINS), serum creatinine (SCr), and uric acid (UA), while SIRD had the highest triglycerides (TGs) and TyG-BMI. Albumin transaminase (ALT) and albumin transaminase (AST) were higher in MOD and SIRD. As concerms medications, compared to the other subtypes, SIDD had a lower rate of metformin use (39.1%) and a higher rate of α-glucosidase inhibitor (AGI, 61.7%) and insulin (74.4%) use. SIRD showed the highest frequency of use of sodium-glucose cotransporter-2 inhibitors (SGLT-2i, 36.0%) and glucagon-like peptide-1 receptor agonists (GLP-1RA, 19.3%). Concerning diabetic complications and comorbidities, the prevalence of diabetic kidney disease (DKD), cardiovascular disease (CVD), non-alcoholic fatty liver disease (NAFLD), dyslipidemia, and hypertension differed significantly among subtypes. Employing logistic regression analysis, after adjusting for unmodifiable (sex and age) and modifiable related influences (e.g., BMI, HbA1c, and smoking), it was found that SIRD had the highest risk of developing DKD (odds ratio, OR = 2.001, 95% confidence interval (CI): 1.125-3.559) and dyslipidemia (OR = 3.550, 95% CI: 1.534-8.215). MOD was more likely to suffer from NAFLD (OR = 3.301, 95%CI: 1.586-6.870). Patients with newly diagnosed T2DM can be successfully clustered into four subtypes with different clinical characteristics, medication treatment, and risks for diabetes-related complications and comorbidities, the cluster-based diabetes classification possibly being beneficial both for prevention of secondary diabetes and for establishment of a theoretical basis for precision medicine.

In Vitro Alpha-Glucosidase Inhibitory Effect of Etlingera Elatior Ethanol Extract Growing in Gayo Highland, Aceh Province, Indonesia.

The prevalence of diabetes mellitus (DM) is increasing overtime, potentially leading to various severe health complications and mortality. Despite therapeutic agents have currently been developed, unexpected adverse effects are inevitable. Hence, safe and effective medications such as those of plant origin are critical to prevent unexpected complication in DM sufferers. Etlingera elatior has been widely used as spice and traditional medicine to treat diabetes in Aceh Province, Indonesia. However, study regarding α-glucosidase inhibitory effect of E. elatior growing in Gayo highlands, Aceh, Indonesia, is completely lacking. The aim of this study was to evaluate in vitro α-glucosidase inhibitory effect of E. elatior ethanol extracts (EEEE) growing in Gayo highlands, Aceh Province, Indonesia. Antioxidant activity was determined using DPPH procedure, whereas α-glucosidase inhibition assay was carried out using spectrophotometric method. Data analysis was performed using One-Way Analysis of Variance (ANOVA), followed by Duncan's multiple range test at α=0.05. Phytochemical analysis revealed the presence of total phenolic (TPC), total flavonoid (TFC), and total tannin (TTC) content in all E. elatior plant parts, in which the highest TPC was found in the stem (158.38 GAE/g), whereas the highest TFC and TTC was obtained in the rhizome extracts. The extract of fruit showed the strongest antioxidant activities, followed by the stem and leaf, with IC 50 of 2.381 μg/mL, 6.966 μg/mL, and 19.365 μg/mL, respectively. All E. elatior extracts revealed a significant inhibitory activity against α-glucosidase at the concentration of 500 μg/mL, in which the stem extract showed the most effective α-glucosidase inhibitory effect with IC 50 value of 5.15 μg/mL, suggesting its promising potential as antidiabetic agent. This study highlights E. elatior potency as a novel source of antioxidant and natural antidiabetic compounds that are useful for the prevention and treatment of diabetes.

Lipophilic derivatives of EGCG as potent α-amylase and α-glucosidase inhibitors ameliorating oxidative stress and inflammation

Uncontrolled hyperglycemia leads to increased oxidative stress, chronic inflammation, and insulin resistance, rendering diabetes management harder to accomplish. To tackle these myriads of challenges, researchers strive to explore innovative multifaceted treatment strategies, including inhibiting carbohydrate hydrolases. Herein, we report alkyl-ether EGCG derivatives as potent α-amylase and α-glucosidase inhibitors that could simultaneously ameliorate oxidative stress and inflammation. 4″-C18 EGCG, the most promising compound, showed multifold improvement in glycaemic management compared to acarbose, with 230-fold greater inhibition (competitive) of α-glucosidase (IC50 0.81 µM) and 3-fold better inhibition of α-amylase (IC50 3.74 µM). All derivatives showed stronger antioxidant activity (IC50 6.16–15.76 µM) than vitamin C, while acarbose showed none. 4″-C18 EGCG also downregulated pro-inflammatory cytokines and showed no significant cytotoxicity up to 50 µM in primary human peripheral blood mononuclear cells (PBMC), non-cancerous cell line, 3T3-L1 and HEK 293. The in silico binding affinity analysis of 4″-C18 EGCG with α-amylase and α-glucosidase was found to exhibit a good extent of interaction as compared to acarbose. In comparison to EGCG, 4″-Cn EGCG derivatives were found to remain stable in the physiological conditions even after 24 h. Together, the reported molecules demonstrated multifaceted antidiabetic potential inhibiting carbohydrate hydrolases, reducing oxidative stress, and inflammation, which are known to aggravate diabetes.

The Roadmap of Plant Antimicrobial Peptides Under Environmental Stress: From Farm to Bedside.

Antimicrobial peptides (AMPs) are the most favorable alternatives in overcoming multidrug resistance, alone or synergistically with conventional antibiotics. Plant-derived AMPs, as cysteine-rich peptides, widely compensate the pharmacokinetic drawbacks of peptide therapeutics. Compared to the putative genes encrypted in the genome, AMPs that are produced under stress are active forms with the ability to combat resistant microbial species. Within this study, plant-derived AMPs, namely, defensins, nodule-specific cysteine-rich peptides, snakins, lipid transfer proteins, hevein-like proteins, α-hairpinins, and aracins, expressed under biotic and abiotic stresses, are classified. We could observe that while α-hairpinins and snakins display a helix-turn-helix structure, conserved motif patterns such as β1αβ2β3 and β1β2β3 exist in plant defensins and hevein-like proteins, respectively. According to the co-expression data, several plant AMPs are expressed together to trigger synergistic effects with membrane disruption mechanisms such as toroidalpore, barrel-stave, and carpet models. The application of AMPs as an eco-friendly strategy in maintaining agricultural productivity through the development of transgenes and bio-pesticides is discussed. These AMPs can be consumed in packaging material, wound-dressing products, coating catheters, implants, and allergology. AMPs with cell-penetrating properties are verified for the clearance of intracellular pathogens. Finally, the dominant pharmacological activities of bioactive peptides derived from the gastrointestinal digestion of plant AMPs, namely, inhibitors of renin and angiotensin-converting enzymes, dipeptidyl peptidase IV and α-glucosidase inhibitors, antioxidants, anti-inflammatory, immunomodulating, and hypolipidemic peptides, are analyzed. Conclusively, as phytopathogens and human pathogens can be affected by plant-derived AMPs, they provide a bright perspective in agriculture, breeding, food, cosmetics, and pharmaceutical industries, translated as farm to bedside.

In vitro and in vivo evaluation of hypoglycemic potential and acute toxicity of microencapsulated turmeric instant powder

BackgroundCurcuma longa L. (turmeric), traditionally used to treat various ailments including diabetes, has demonstrated beneficial health effects. However, its potential in food formulations requires further investigation. PurposeThis study examined the hypoglycemic effects of an instant powder containing microencapsulated turmeric oleoresin both in vitro and in vivo, alongside an acute toxicity assessment in Holtzman rats. MethodsThis study encompassed both in vitro and in vivo evaluations. In vitro, the α-glucosidase (a digestive enzyme) inhibition assay was employed to determine the powder's effectiveness. In vivo assessments included: (1) evaluation of the hypoglycemic effect in mice; (2) conducted safety testing following international guidelines, administering a 2000 mg/kg dose to rats with subsequent monitoring of biochemical parameters; and (3) histological examination of liver, kidney, and spleen tissues for potential harmful effects. ResultsThe instant powder with turmeric oleoresin microencapsulation demonstrated significant α-glucosidase inhibition in vitro and hypoglycemic effects in vivo. The acute toxicity test at 2000 mg/kg showed no mortality but revealed significant alterations in erythrocyte parameters and hemoglobin percentage. Histological examinations of liver, kidney, and spleen tissues did not differ from those of the control group, though pancreatic tissue was not evaluated in this study. ConclusionAccording to this study, the microencapsulated turmeric oleoresin instant powder exhibited antidiabetic effects without signs of overt toxicity at doses up to 2000 mg/kg in rats.

Comparative analysis of phenolic compounds in different thinned unripe kiwifruits and their biological functions

Thinned unripe kiwifruits (TUK) are considered the major agro by-products in kiwifruit production. To promote their potential applications, polyphenols and biological effects of unripe fruits from nine commercial kiwifruit cultivars were compared. Our findings showed that TUK were rich in bioactive polyphenols, which varied greatly by different cultivars. Indeed, catechin, epicatechin, procyanidin PB1, procyanidin B2, protocatechuic acid, neochlorogenic acid, and gallic acid were measured as the major phenolic components in most TUK, with the highest levels observed in ‘Hongao’ and ‘Cuiyu’ cultivars. Furthermore, TUK exerted strong in vitro antioxidant capacities, inhibitory effects on digestive enzymes, and anti-inflammatory activities. Particularly, their stronger antioxidant effects and inhibitory effects on digestive enzymes were probably attributed to their higher contents of phenolic compounds, especially procyanidin B2. Collectively, our findings reveal that TUK are potential resources of valuable polyphenols, which can be exploited as natural antioxidants and natural inhibitors of α-glucosidase and α-amylase.

Proteins make tea polyphenol EGCG not always develop satisfactory α-glucosidase inhibition: The influences of three proteins on α-glucosidase inhibitory activity of EGCG

Tea polyphenol epigallocatechin-3-gallate (EGCG) has been previously explored as an effective inhibitor of carbohydrate hydrolyzing α-glucosidase for regulating postprandial blood glucose level. Proteins act as one common dietary component, the influence of which on α-glucosidase inhibition of EGCG remains unknown. In this study, bovine serum albumin (BSA) and isolated whey protein (IWP) were found to significantly weaken the competitive inhibitory activity of EGCG against α-glucosidase by the effect order of BSA > IWP, while egg albumin (EA) hardly influenced the enzyme inhibition. Through the analyses of kinetics, spectroscopy, thermodynamics and simulated docking, a protein-EGCG-enzyme ternary complex was suggested to generate in the interaction system, in which there existed competition between proteins (BSA and IWP) and α-glucosidase regarding formation of hydrogen bondings with polyphenolic groups (especially galloyl moiety). This weakened the EGCG-enzyme binding interactions at α-glucosidase active site, and thus reduced the enzyme inhibition in vitro and in vivo. However, there existed a co-existing relationship between proteins and α-glucosidase regarding π-stackings of EGCG benzene ring with aromatic residues of both macromolecules, which remained the fluorescence quenching ability of EGCG against the enzyme. Conclusively, dietary proteins should be considered as a potential influence factor when developing natural products as inhibitors of carbohydrate hydrolyzing enzymes.

Promising Influences of Moringa oleifera in Functional Foods against Metabolic Syndrome: A Comprehensive and Mechanistic Review.

Metabolic syndrome (MetS) is now considered a global issue with a growing financial and health impact. Numerous herbal alternatives have been examined and researched due to the ever-increasing demand for new medications to treat metabolic syndrome disorders. People have empirically employed Moringa oleifera (MO), a native plant to several Asian nations, for a variety of diseases. We sought to examine recent research on MO in MetS and its potential mechanism of action in the current review. Four databases, including PubMed, Scopus, Web of Sciences, and Google Scholar, were thoroughly searched, and the data were then compiled. In total, 146 papers covering nonclinical and clinical MO investigations in metabolic syndromerelated disorders are included in this study. Numerous research confirmed MO's positive impact on the control of blood glucose, blood pressure, hyperlipidemia, and obesity. Many molecular processes have been investigated, including increasing glucose transporter type 4 (GLUT4) expression, inhibition of β-Hydroxy-β-methylglutaryl-coenzyme A (HMG-CoA), α-glucosidase inhibiting, AMP-activated protein kinase (AMPK) activation, and other suggested mechanisms. The current review established much data favoring MO's potential advantages in metabolic syndrome. However, further research involving human studies is required in this area to determine whether Moringa can effectively treat metabolic syndrome.

Exploring the anti-diabetic activity of benzimidazole containing Schiff base derivatives: In vitro α-amylase, α-glucosidase inhibitions and in silico studies

The current study explores the anti-diabetic potential of some Schiff bases containing benzimidazole scaffold. These derivative were synthesized by refluxing sodium metabisulfite with ethyl 2-(2-ethoxy-6-formylphenoxy)acetate followed by the addition of ortho phenylene diamine in DMF solvent to get the benzimidazole which was further refluxed in hydrazine hydrate to obtain the hydrazide. Finally various substituted benzaldehydes were treated with the desired hydrazide using a catalytic quantity of acetic acid to obtain the hydrazone Schiff bases. These compounds were evaluated for their ability to inhibit α-amylase and α-glucosidase inhibitory potentials. Among them, six derivatives including 2g, 2h, 2q, 2p, 2i, and 2m displayed noteworthy inhibitory activities against α-amylase (IC50 = 2.15 ± 0.17 µM to 15.18 ± 3.29 µM ) and α-glucosidase (IC50 = 4.21 ± 0.78 to 16.10 ± 0.52 µM) superior than the standard acarbose, while the remaining compounds showed significant to less inhibitory activities. By clarifying the mechanisms of interaction between the chemicals and amino acid residues, the molecular docking analysis attempted to shed light on the binding modalities of these molecules. The reactivity indices of these compounds were calculated using the Density Functional Theory (TD-DFT) approach, employing the B3LYP-d energy function and lacvp**(d,p) basis set for calculations. Schiff base derivatives based on benzimidazole, especially compounds 2h and 2g, exhibited lower electrophilicity and higher bioactivity compared to their counterparts 2i and 2m.

Potential Antihyperglycemic Effects of Adzuki (Vigna angularis) Polyphenols on Mice and Caco-2 Cells

Background/Purpose Some health-beneficial foods, including adzuki beans ( Vigna angularis), can show antihyperglycemic effects. Adzuki bean-derived polyphenols, such as (+)-catechin 7- O- β-d-glucopyranoside (C7G) and (+)-epicatechin 7- O- β-d-glucopyranoside (E7G), could be potential inhibitors of α-amylase and α-glucosidase, however, few studies of the activity of adzuki polyphenols have been performed in vivo. Thus, we evaluated the antihyperglycemic effects of crude adzuki bean extract containing polyphenols (ABP), and purified C7G or E7G using mice and Caco-2 cells. Methods Six-week-old male ICR mice were orally administered ABP (100 or 250 mg/kg), C7G or E7G (15 or 40 mg/kg), and sucrose (2 g/kg). Blood samples were taken from the lateral tail vein to measure the blood glucose levels at various times over 0–120 min. Cultured caco-2 cells, an intestinal model, were treated with ABP, C7G, or E7G. The glucose concentration in the medium was measured to examine the activity of α-glucosidase. Results Administration of adzuki polyphenols decreased blood glucose levels, especially E7G administration significantly showed antihyperglycemic effects in vivo. In Caco-2 cells, α-glucosidase activity was significantly decreased by ABP, C7G, or E7G addition in a dose-dependent manner without cytotoxicity. Conclusion These results suggest that C7G and E7G in adzuki bean extract inhibited sucrose-degrading enzymes to elicit antihyperglycemic effects in vivo, which supports the results of previous studies using adzuki beans, and may contribute to health promotion.

Combining chemical profiles and biological abilities of different extracts from Tanacetum nitens(Boiss. & Noë)Grierson using network pharmacology.

Tanacetum nitens(Boiss. & Noë)Grierson is an aromatic perennial herb used in Turkish traditional medicine to treat headache, fever, and skin diseases. This study aimed to investigate the chemical composition, antioxidant, enzyme inhibition, and cytotoxic properties of T. nitens aerial parts. Organic solvent extracts were prepared by sequential maceration in hexane, dichloromethane, ethyl acetate, and methanol while aqueous extracts were obtained by maceration or infusion. Nuclear magnetic resonance (NMR) and LC-DAD-MS analysis allowed the identification and quantification of different phytoconstituents including parthenolide, tanacetol B, tatridin B, quinic acid derivatives, β-sitosterol, and glycoside derivatives of quercetin and luteolin. The type and amount of these phytochemicals recovered by each solvent were variable and significant enough to impact the biological activities of the plant. Methanolic and aqueous extracts displayed the highest scavenging and ions-reducing properties while the dichloromethane and ethyl acetate extracts exerted the best total antioxidant activity and metal chelating power. Results of enzyme inhibition activity showed that the hexane, ethyl acetate, and dichloromethane extracts had comparable anti-acetylcholinesterase activity and the latter extract revealed the highest anti-butyrylcholinesterase activity. The best α-amylase and α-glucosidase inhibition activities were obtained from the hexane extract. The dichloromethane and ethyl acetate extracts exhibited the highest cytotoxic effect against the prostate carcinoma DU-145 cells. In conclusion, these findings indicated that T. nitens can be a promising source of biomolecules with potential therapeutic applications.