Α-amylase Inhibition Assay Research Articles

A comparative study of Ghanaian propolis extracts: Chemometric analysis of the chromatographic profile, antioxidant, and hypoglycemic potential and identification of active constituents

Diabetes is a disease characterized by high post-prandial glucose levels, which lead to other complications such as peripheral end organ damage. The use of enzyme inhibitors in the management of Type-2 diabetes ensure the control of blood glucose levels via the control of carbohydrate metabolism. The use of standard agents such as acarbose is associated with unwanted side effects hence the need to investigate other sources of antihyperglycemic agents. Propolis, a natural substance from bees, possesses diverse biological activities including antioxidant, antimicrobial and antidiabetic properties. However, the phytochemical content of propolis and its extracts may vary depending on the geographical area, the solvent of extraction and type of bees. This study represents the first attempt to compare different extracts of propolis from the same source in sub-Saharan Africa. In this study, the effect of solvent and source of Ghanaian propolis on parameters such as the total phenolic and flavonoid contents, chromatographic profile, antioxidant and α-amylase inhibitory effects were investigated with the aim of identifying and characterizing the most promising extract, which could be of direct or indirect benefit in the management of Type-2 diabetes.Combinations of water, ethanol-water and ethanol extracts were prepared from propolis from three regions. Phytochemical screening was performed on the extracts after which the Folin Ciocalteu method and aluminum chloride colorimetric assay were used to estimate the total phenolic and flavonoid contents respectively. Antioxidant potential of extracts was estimated using DPPH and phosphomolybdenum assays. In-vitro α-amylase inhibition assay was used to investigate hypoglycemic effect of the extracts. Statistical tools such as ANOVA, principal component analysis, hierarchical cluster analysis employed to determine sources of variations within the data obtained, to classify the extracts based on activity and to predict the most effective extract. This extract was then subjected to UHPLC-Q-TOF MS/MS and GC–MS techniques to characterize the constituents.Chemometric analysis of the data obtained showed that the variations in the data could be explained by both propolis source and extraction solvent. Though ethanol extracts generally contained more constituents, the more notable activities were in the ethanol-water extracts. The ethanol-water extract of Bono East propolis (EWBE) was the most potent DPPH radical scavenger (IC50 of 149.37 ± 2.90 µg/mL as compared to 116.60 ± 0.93 µg/mL GAE standard). It was also one of the three extracts which were more potent than acarbose (369.89 µg/mL) in the α-amylase inhibition assay. The predominant constituents from the LC-MS dereplication of EWBE were caffeic acid and flavonoid derivatives whilst 5,5-dimethyl-1-oxa-5 silacyclononanone-9 was the most significant active constituent identified through the GC–MS analysis. The identified constituents are known to have strong antioxidant and antidiabetic properties.The effects of source and solvent of extraction on the biological and physicochemical properties of propolis in Ghana have been quantified using statistical tools. The combined biological effects of propolis suggest a possible role in their usage in the management of type-2-diabetes and its related complications. Ethanol-water extracts were the most promising with EWBE showing the strongest antihyperglycemic activity. Such extracts represent leads towards further research into toxicity and formulation in order to develop safe and useful products for the management of type-2 diabetes.

Hypoglycemic activity of Syzygium cumini (L.) Skeels seed extracts: an approach to in vitro, in vivo, and in silico studies

This research is carried out to explore the hypoglycemic activity of Syzygium cumini seed extracts by in vitro, in vivo, and in silico methods. For in vitro studies the α-amylase and α-glucosidase enzyme inhibition assays were employed. For in vivo studies 30 alloxan induced Wistar rats were used. They were orally administered with glibenclamide and low/high dose of the extracts and were monitored regularly for the change in blood glucose levels for about 28 days. The in silico molecular docking was conducted to evaluate the binding interaction of 1,2,3-Benzenetriol with human pancreatic α-amylase and α-glucosidase. It was found that all the extracts were able to inhibit the α-amylase and α-glucosidase enzymes. Among which the acetone extract showed greater inhibition with 72.52 ± 0.51% and 63.02 ± 0.73% for both the enzymes, respectively. There was significant (p < 0.05) reduction in blood glucose levels in the rats administered with glibenclamide and extracts. In silico docking results revealed that the compound 1,2,3-Benzenetriol exhibited the highest binding affinity for human pancreatic α-amylase with binding energy −7.7 kcal/mol. Thus suggesting the utilization of S. cumini seeds in the management of diabetes mellitus. Communicated by Ramaswamy H. Sarma

Study of Pharmacological Profile of Chloroform Leaf Extract of Ludwigia perennis - A Wetland Plant

Aim: The main objective of this study was to find out various therapeutic properties of chloroform leaf extract of the wetland plant Ludwigia perennis.&#x0D; Place and Duration of Study: Department of Biotechnology, Sree Narayana Guru College, Coimbatore, Tamilnadu, Scigen Research and Innovation in Thanjavur, Tamil Nadu; and the Sri Lakshmi Narayana Institute of Medical Sciences in Osudu, Pondicherry between April 2023 and August 2023.&#x0D; Methodology: Chloroform leaf extract of Ludwigia perennis was employed for evaluating the antioxidant, antidiabetic, anti-nutritional, anticancer, anti-inflammatory, and antipyretic properties, respectively.&#x0D; Results: The DPPH assay found that the IC50 for the leaf extract was 48.78µg/mL, while the IC50 for the standard was 49.74µg/mL. The IC50 for the phosphomolybdenum test was 32.31µg/mL for the leaf extract and 33.73µg/mL for the standard. The IC50 values for the hydroxyl radical scavenging experiment were 55.6µg/mL for the standard and 47.54µg/mL for the leaf extract. The IC50 of the standard in the α-amylase inhibitory assay is 394.48µg/mL, and the extract's IC50 is 330.38µg/mL, respectively. The IC50 of the standard in the α-glucosidase inhibitory assay was 394.06µg/mL, and the extract's IC50 was 335.45µg/mL, respectively. Antinutrient content such as alkaloids was 21.4%, oxalate was 6.6%, phytate was 4.18%, and saponin was 30%, respectively. The IC50 of HeLa cells treated with leaf extract was 180µg/mL. After 4hours of treatment with chloroform leaf extract, the inhibition was 51.75% when 50mg/kg was used and 58.74% when 250mg/kg was used. Here, the inhibitory percentage of indomethacin is 59.45%. This means that the leaf extract has anti-inflammatory activity. Chloroform leaf extracts produced significant antipyretic effects in 250 and 500mg/kg doses.&#x0D; Conclusion: Therefore, the chloroform leaf extract of Ludwigia perennis has shown to have anti-oxidant, anti-diabetic, anti-nutrient, anti-cancer, anti-inflammatory, and anti-pyretic activities. These evidences suggest the plant is a potential source for developing new drugs.

Moxifloxacin and hydrazine mix ligand metal complexes of Cd(II), Cu(II), Co(II), and Zn(II); synthesis, characterization, and pharmacological activities, with molecular docking studies

In the current study, four new mixed ligand metal complexes of Cd(II), Cu(II), Co(II), and Zn(II) with moxifloxacin (used as a primary ligand) and hydrazine (as an ancillary ligand) were synthesized. The newly prepared organometallic compounds were characterized by using conventional spectroscopic (UV–Vis, Atomic absorption, FTIR, and powder XRD), microscopic (SEM), elemental (CHN), and thermal (TGA) techniques. The synthesized chelates were evaluated for cytotoxicity (by hemolytic activity) and antimicrobial activity against different bacterial (S. aureus, B. subtilis, E. coli, and P. multocidia) and viral (A. flavus, A. niger, R. solani, and A. alternata) strains. The prepared metal complexes were also in vitro assayed for antidiabetic potential through α-amylase inhibition assay, and the results were further verified through molecular docking studies. This study demonstrates that half of the new metal complexes are good antibacterial agents, and complex 2 was significantly active against all four assayed bacterial strains. All the synthesized mixed ligand metal complexes proved to have significant fungicidal activity. Complex 3 has proved to be potentially active (24.3%) against Aspergillus flavus with a higher activity as compared to the reference standard, i.e., fluconazole (23.5%). The hemolytic values of 6.07%, 4.94%, and 12.05% for metal complexes 2, 3, and 4, respectively, were in acceptable range and comparable to moxifloxacin, while higher (19.05%) for complex 1. Present work reveals that all the bi-ligand complexes are significant antidiabetic agents, where complexes 3 and 4, with 62.45% and 54.25% α-amylase inhibition, have a similar effect as that of the standard drug, i.e., Acarbose having 64.12% α-amylase inhibition. The molecular docking studies correspondingly prove these two compounds as potent α-amylase inhibitors.

In-vitro and ex-vivo antidiabetic, and antioxidant activities of Box-Behnken design optimized Solanum xanthocarpum extract loaded niosomes

One of the most prevalent lifestyle diseases, diabetes mellitus (DM) is brought on by an endocrine issue. DM is frequently accompanied by hyperglycemia, a disease that typically results in an excess of free radicals that stress tissues. The medical community is currently concentrating on creating therapeutic medications with roots in nature to lessen the damage associated with hyperglycemia. Solanum xanthocarpum has a number of medicinal benefits. The investigation aimed to produce and analyze niosomal formulations containing S. xanthocarpum extract (SXE). Niosomes were made by implementing the solvent evaporation process, which was further optimized using Box-Behnken design. Drug release, DPPH assessments, α-amylase inhibition assay, α-glucosidase inhibition assay, and confocal laser scanning microscopy (CLSM) investigation were all performed on the developed formulation (SXE-Ns-Opt). SXE-Ns-Opt displayed a 253.6 nm vesicle size, a PDI of 0.108, 62.4% entrapment efficiency, and 84.01% drug release in 24 h. The rat's intestinal CLSM image indicated that the rhodamine red B-loaded SXE-Ns-Opts had more intestinal penetration than the control. Additionally, the antioxidant effect of the obtained formulation was demonstrated as 89.46% as compared to SXE (78.10%). Additionally, acarbose, SXE, and SXE-Ns-Opt each inhibited the activity of α-amylase by 95.11%, 85.88%, and 89.87%, and also suppressed the enzyme of α-glucosidase by 88.47%, 81.07%, and 85.78%, respectively. To summarise, the establishment of the SXE-Ns-Opt formulation and its characterization demonstrated the legitimacy of the foundation. A promising candidate for the treatment of diabetes mellitus has been shown as in vitro studies, antioxidant against oxidative stress, CLSM of rat's intestine and a high degree of penetration of formulation.

Application of Box–Behnken design for the optimization of Plumbago zeylanica extract-loaded niosomes: preparation, characterization and in vitro antidiabetic and antioxidant activity

This study aimed to develop and evaluate a niosomal formulation loaded with Plumbago zeylanica extract (PZE). The solvent evaporation method was used to prepare niosomes and optimized using the Box–Behnken design. The optimized formulation (PZE-Ns-Opt) was characterized for drug release, DPPH assay, α-amylase inhibition assay, α-glucosidase inhibition assay, and confocal laser scanning microscopy (CLSM) study. PZE-Ns-Opt showed a vesicle size of 253.6 nm, PDI of 0.108, entrapment efficiency of 62.4%, and drug release of 84.01%. The CLSM image of the rat’s intestine suggested that the rhodamine red B-loaded PZE-Ns-Opts showed superior penetration compared to the control. Further, the antioxidant activity of the prepared formulation was exhibited as 89.46%±0.016 as compared to PZE (78.10%±0.005). In addition to this, α- amylase activity was inhibited by 95.11%±4.62, 85.88%±2.56, and 89.87%±3.65 by acarbose, PZE, and PZE-Ns-Opt, respectively. In comparison, the α-glucosidase activity was inhibited by 88.47%±1.04, 81.07%±0.50 and 85.78%±0.71 by acarbose, PZE, and PZE-Ns-Opt, respectively. To conclude, the development of PZE-Ns-Opt formulation and its characterization showed the establishment’s authenticity. The in vitro antidiabetic, antioxidant studies expressed the protective effect from oxidative stress, CLSM of rat’s intestine ability to penetrate to great extent and could be a promising candidate for the management of diabetes mellitus.

Hypoglycemic, anti-inflammatory, and anti-aging potential of Canthium coromandelicum (Burm.f.) Alston leaf extracts: In vitro and in silico ADMET studies

The present study focused on the hypoglycemic, anti-inflammatory and anti-aging effects of Canthium coromandelicum (Burm.f.) Alston leaf extract by in vitro and in silico analyses. In vitro antidiabetic activities were studied by α-amylase and α-glucosidase enzyme inhibition assays. The anti-inflammatory activity was analysed by bovine serum albumin denaturation assay and anti-aging activity by the inhibition of tyrosinase enzyme. The molecular docking study was undertaken to examine the binding mode and interactions of reported compounds of the hydroalcoholic extract of C. coromandelicum leaf with 7TAA, 3WY1, 2Y9X, and 4COX proteins. The plant exhibited promising antidiabetic effects with an inhibition of 86.09% against α-amylase and 83.53% against α-glucosidase enzymes. The extract had a notable anti-inflammatory activity with an inhibition range of 50.23 to 73.17%. The anti-aging activity showed 50.31 to 76.78% of inhibition in anti-tyrosinase assay with a potential effect in hyperpigmentation. In molecular docking analysis, the compounds like linoleic acid, phytol, methyl linoleate, palmitic acid and ethyl octa-decanoate had potent inhibitory activities against 7TAA, 3WY1, 2Y9X and 4COX proteins (6.90 to -4.42 kcal/mol) especially linoleic acid was found to be highly effective (-6.11 kcal/mol) antidiabetic effect with notable binding scores. The obtained results suggest that phytoconstituents identified from the plant have the potential in controlling diabetes by inhibiting α-amylase and α-glucosidase enzymes with promising anti-inflammatory and anti-aging properties. However, further research is required to ascertain its potential effect in experimental animals and isolation of bioactive compounds.

Development of nanofunctionalized oxovanadium(IV) complex and its anticancer, antidiabetic, DNA cleavage and cell imaging studies

VO(IV) complex is little toxic and highly effective than vanadium salts. A vanadyl metal complex from 8-formyl-7-hydroxy-4-methyl coumarin derivative has been synthesized and functionalized with copper nanoparticles. The Spectrochemical studies such as UV, FTIR, 1NMR and ESR spectra were recorded to characterize the ligand(CUAP), Vanadyl complex[VO(CUAP)SO4] and nano Cu-VO(IV)complex efficiently. The structural studies of vanadyl complex confirmed that the ligand coordinate with metal through nitrogen atom of azomethine, carbonyl oxygen and phenolic oxygen. ESR spectrum of vanadyl complex revealed the covalent nature. XRD pattern of nano Cu-VO(IV) complex indicated the crystalline nature and the average particle size was 20.91 nm. SEM image of nano Cu-VO(IV) complex showed that the nano particles accumulated to form spherical shaped particles. The particle size obtained from Transmission Electron Microscopy of nano functionalized metal complex is ∼ 20 nm. It is closely matched to the particle size calculated from XRD results. Fluorescence of vanadyl complex and nano Cu-VO(IV) complex exhibit the emission from 270 to 900 nm range with significant fluorescence at ∼ 750 nm. The DNA cleavage of all the compounds was evaluated using Agarose gel electrophoresis technique and showed greater cleavage of vanadyl complex. The anticancer activity of compounds was carried out against two cancer cell lines viz Human Breast Cancer Cell line (MCF-7) and Human Leukemia Cancer Cell Line(K-562). Oxovanadium complex exhibited good anticancer activities than ligand and nano-functionalized complex. The antidiabetic activities of vanadyl and nano functionalized complexes were studied against α-Amylase and β-Glucosidase inhibition assay. In this study vanadyl complex showed higher inhibition activity on α-Amylase compared with standard Acarbose. The bioimaging of nano-functionalized metal complex showed high fluorescent properties. The molecular docking study of ligand and vanadyl complex showed greater docking results with CDK2 receptor.

Exploring the Multifaceted Potential of a Peptide Fraction Derived from Saccharomyces cerevisiae Metabolism: Antimicrobial, Antioxidant, Antidiabetic, and Anti-Inflammatory Properties.

The rising demand for minimally processed, natural, and healthier food products has led to the search for alternative and multifunctional bioactive food components. Therefore, the present study focuses on the functional proprieties of a peptide fraction derived from Saccharomyces cerevisiae metabolism. The antimicrobial activity of the peptide fraction is evaluated against various foodborne pathogens, including Candida albicans, Candida krusei, Escherichia coli, Listeria monocytogenes, and Salmonella sp. The peptide fraction antioxidant properties are assessed using FRAP and DPPH scavenging capacity assays. Furthermore, the peptide fraction's cytotoxicity is evaluated in colorectal carcinoma and normal colon epithelial cells while its potential as an antidiabetic agent is investigated through α-amylase and α-glucosidase inhibitory assays. The results demonstrate that the 2-10 kDa peptide fraction exhibits antimicrobial effects against all tested microorganisms, except C. krusei. The minimal inhibitory concentration for E. coli, L. monocytogenes, and Salmonella sp. remains consistently low, at 0.25 mg/mL, while C. albicans requires a higher concentration of 1.0 mg/mL. Furthermore, the peptide fraction displays antioxidant activity, as evidenced by DPPH radical scavenging activity of 81.03%, and FRAP values of 1042.50 ± 32.5 µM TE/mL at 1.0 mg/mL. The peptide fraction exhibits no cytotoxicity in both tumor and non-tumoral human cells at a concentration up to 0.3 mg/mL. Moreover, the peptide fraction presents anti-inflammatory activity, significantly reducing the expression of the TNFα gene by more than 29.7% in non-stimulated colon cells and by 50% in lipopolysaccharide-stimulated colon cells. It also inhibits the activity of the carbohydrate digestive enzymes α-amylase (IC50 of 199.3 ± 0.9 µg/mL) and α-glucosidase (IC20 of 270.6 ± 6.0 µg/mL). Overall, the findings showed that the peptide fraction exhibits antibacterial, antioxidant, anti-inflammatory, and antidiabetic activity. This study represents a step forward in the evaluation of the functional biological properties of S. cerevisiae bioactive peptides.

HYPOGLYCEMIC POTENTIAL OF HIBISCUS ROSA-SINENSIS AND MANGIFERA INDICA LEAVES BY IN VITRO METHODS

Objective: The objective of the present study was to provide in vitro evidence for the potential inhibitory activity of extracts of Mangifera indica (MI) and Hibiscus rosa-sinensis on α-amylase and α-glucosidase enzymes. Methods: The plant extracts were prepared with methanol by maceration. Different concentrations (10, 20, 40, 80, and 100 μg/mL) of both the extracts were made using distilled water, and the extracts were subjected to α-amylase and α-glucosidase inhibitory assay. The absorbance was measured at 540 nm and 405 nm using spectrophotometer. Using this method, the percentage of α-amylase and α-glucosidase inhibitory activity and IC50 values of each extract were calculated. Results: The methanolic extracts of MI and H. rosa-sinensis exhibited significant α-amylase and α-glucosidase inhibitory activity. The inhibitory effect of α-amylase inhibitory assay was observed up to 89% and 90% at a concentration of 100 μg/mL in MI and H. rosa-sinensis, respectively. The inhibitory effect of α-glucosidase inhibitory assay was observed up to 89% and 91% at a concentration of 100 μg/mL in MI and H. rosa-sinensis, respectively, and is comparable to the standard acarbose (94% at 100 μg/mL). The IC50 values of α-amylase inhibitory assay of MI and H. rosa-sinensis are 35.33 and 30.97, respectively. The IC50 values of α-glucosidase inhibitory assay of MI and H. rosa-sinensis are 31.67 and 25.86, respectively. The IC50 value of acarbose is 6.94. Conclusion: The results obtained support that MI and H. rosa-sinensis extracts exhibit considerable α-amylase and α-glucosidase inhibitory activity which can be attributed to the phytochemical constituents present in them. Further, this study supports its usage in ethno medicines for the management of diabetes.

Antidiabetic effects of polyherbal mixture made of Centaurium erythraea, Cichorium intybus and Potentilla erecta

Ethnopharmacological relevanceThe polyherbal mixture made of Centaurium erythraea aerial parts and Cichorium intybus roots and Potentilla erecta rhizomes has been used for centuries to treat both the primary and secondary complications of diabetes. Aim of the studyAs a continuation of our search for the most effective herbal mixture used as an ethnopharmacological remedy for diabetes, this study aimed to compare the in vitro biological activities of this polyherbal mixture and its individual ingredients, and, most importantly, to validate the ethnopharmacological value of the herbal mixture through evaluation of its phytochemical composition, its potential in vivo toxicity and its effect on diabetes complications. Materials and methodsPhytochemical analysis was performed using HPLC-UV. Antioxidant activity was estimated via the DPPH test. Potential cytotoxicity/anticytotoxicity was assessed using an in vitro RBCs antihemolytic assay and an in vivo sub-chronic oral toxicity method. Antidiabetic activity was evaluated using an in vitro α-amylase inhibition assay and in vivo using a chemically induced diabetic rat model. ResultsThe HPLC-UV analysis revealed the presence of p-hydroxybenzoic acid, p-hydroxybenzoic acid derivative, catechin, five catechin derivatives, epicatechin, isoquercetin, hyperoside, rutin, four quercetin derivatives, caffeic acid, and four caffeic acid derivatives in the polyherbal mixture decoction. Treatment with the decoction has shown no toxic effects. The antioxidant and cytoprotective activities of the polyherbal mixture were higher than the reference's ones. Its antidiabetic activity was high in both in vitro and in vivo studies. Fourteen days of treatment with the decoction (15 g/kg) completely normalized blood glucose levels of diabetic animals, while treatments with insulin and glimepiride only slightly lowered glycemic values. In addition, lipid status of treated animals as well as levels of serum AST, ALT, ALP, creatinine, urea and MDA were completely normalized. In addition, the polyherbal mixture completely restored the histopathological changes of the liver, kidneys and all four Cornu ammonis regions of the hippocampus. ConclusionsThe polyherbal mixture was effective in the prevention of both primary and secondary diabetic complications such as hyperlipidemia, increased lipid peroxidation, non-alcoholic fatty liver disease, nephropathy and neurodegeneration.

Anti-Obesity Effect of a Tea Mixture Nano-Formulation on Rats Occurs via the Upregulation of AMP-Activated Protein Kinase/Sirtuin-1/Glucose Transporter Type 4 and Peroxisome Proliferator-Activated Receptor Gamma Pathways.

White, green, and oolong teas are produced from the tea plant (Camellia sinensis (L.) Kuntze) and are reported to have anti-obesity and hypolipidemic effects. The current study aims to investigate the anti-obesity effects of a tea mixture nano-formulation by targeting the AMPK/Sirt-1/GLUT-4 axis in rats. In vitro lipase and α-amylase inhibition assays were used to determine the active sample, which was then incorporated into a nanoparticle formulation subjected to in vivo anti-obesity testing in rats by measuring the expression level of different genes implicated in adipogenesis and inflammation using qRT-PCR. Moreover, metabolomic analysis was performed for each tea extract using LC/ESI MS/MS coupled to chemometrics in an attempt to find a correlation between the constituents of the extracts and their biological activity. The in vitro pancreatic lipase and α-amylase inhibition assays demonstrated more effective activity in the tea mixture than the standards, orlistat and acarbose, respectively, and each tea alone. Thus, the herbal tea mixture and its nanoparticle formulation were evaluated for their in vivo anti-obesity activity. Intriguingly, the tea mixture significantly decreased the serum levels of glucose and triglycerides and increased the mRNA expression of GLUT-4, P-AMPK, Sirt-1, and PPAR-γ, which induce lipolysis while also decreasing the mRNA expression of TNF-α and ADD1/SREBP-1c, thereby inhibiting the inflammation associated with obesity. Our study suggests that the tea mixture nano-formulation is a promising therapeutic agent in the treatment of obesity and may also be beneficial in other metabolic disorders by targeting the AMPK/Sirt-1/Glut-4 pathway.

Novel benzotriazole-benzimidazole metal complexes: structure-activity relationship, synthesis, characterization, and antidiabetic activity

To investigate the relationship between structure and antidiabetic activity, four novel metal complexes [Cu2(ebmb)2Cl4] (1), [Zn2(ebmb)Cl4] (2), [Cu(ebmb)SO4]n (3) and [Cu(mbmb)SO4]n (4) have been synthesized by 1-[(2-ethyl-1H-benzimidazole- 1-yl)methyl]-1H-benzotriazole (ebmb) and 1-[(2-methyl-1H-benzimidazole-1-yl) methyl]-1H-benzotriazole (mbmb), and the antidiabetic activities of them have been evaluated. The X-ray single crystal diffraction analysis reveals that complexes 1-2 are binuclear complexes and isostructural expect the different central metal. Complexes 3-4 possess the same central metal but different ligands, and they have very similar structure and they both possess one-dimensional chain structure. We assessed the in vitro antidiabetic activities of the complexes. The results of the α-amylase and α-glucosidase inhibition assays showed that complexes 1 and 4 possessed strongest inhibitory activities with the IC50 values of 1.29mM±0.04 (1) and 4.69mM±0.43 (4) for α-amylase, 0.75±0.04μM (1) and 1.63±0.11μM (4) for α-glucosidase. Finally, we evaluated the effect of complexes 1 and 4 on the glucose consumption of insulin resistant (IR) HepG2 cells, the results showed that both two complexes can improve the IR state of HepG2 cells, the glucose consumption of complex 1-treated IR-HepG2 cells and complex 4-treated IR-HepG2 cells were 1.3 times and 1.18 times as much as the model group, respectively. What's more, the structure-function relationship of complexes had also been discussed in this paper.

Ultrasonic-Assisted Synthesis of Heterocyclic Curcumin Analogs as Antidiabetic, Antibacterial, and Antioxidant Agents Combined with in vitro and in silico Studies.

Heterocyclic analogs of curcumin have a wide range of therapeutic potential and the ability to control the activity of a variety of metabolic enzymes. 1H-NMR and 13C-NMR spectroscopic techniques were used to determine the structures of synthesized compounds. The agar disc diffusion method and α-amylase inhibition assay were used to examine the antibacterial and anti-diabetic potential of the compounds against α-amylase enzyme inhibitory activity, respectively. DPPH-free radical scavenging and lipid peroxidation inhibition assays were used to assess the in vitro antioxidant potential. In this work, nine heterocyclic analogs derived from curcumin precursors under ultrasonic irradiation were synthesized in excellent yields (81.4-93.7%) with improved reaction time. Results of antibacterial activities revealed that compounds 8, and 11 displayed mean inhibition zone of 13.00±0.57, and 19.66±00 mm, respectively, compared to amoxicillin (12.87±1.41 mm) at 500 μg/mL against E. coli, while compounds 8, 11 and 16 displayed mean inhibition zone of 17.67±0.57, 14.33±0.57 and 23.33±00 mm, respectively, compared to amoxicillin (13.75±1.83 mm) at 500 μg/mL against P. aeruginosa. Compound 11 displayed a mean inhibition zone of 11.33±0.57 mm compared to amoxicillin (10.75±1.83 mm) at 500 μg/mL against S. aureus. Compound 11 displayed higher binding affinities of -7.5 and -8.3 Kcal/mol with penicillin-binding proteins (PBPs) and β-lactamases producing bacterial strains, compared to amoxicillin (-7.2 and -7.9 Kcal/mol, respectively), these results are in good agreement with the in vitro antibacterial activities. In vitro antidiabetic potential on α-amylase enzyme revealed that compounds 11 (IC50=7.59 µg/mL) and 16 (IC50=4.08 µg/mL) have higher inhibitory activities than acarbose (IC50=8.0 µg/mL). Compound 8 showed promising antioxidant inhibition efficacy of DPPH (IC50 = 2.44 g/mL) compared to ascorbic acid (IC50=1.24 g/mL), while compound 16 revealed 89.9±20.42% inhibition of peroxide generation showing its potential in reducing the development of lipid peroxides. In silico molecular docking analysis, results are in good agreement with in vitro biological activity. In silico ADMET profiles suggested the adequate oral drug-likeness potential of the compounds without adverse effects. According to our findings, both biological activities and in silico computational studies results demonstrated that compounds 8, 11, and 16 are promising α-amylase inhibitors and antibacterial agents against E. coli, P. aeruginosa, and S. aureus, whereas compound 8 was found to be a promising antioxidant agent.

Synthesis of hydrazinylthiazole carboxylates: a mechanistic approach for treatment of diabetes and its complications.

Aim: The deaths of thousands of people and millions affected by diabetes mellitus triggered us to look for alternative possible solutions to cure diabetes and its complications. Materials & methods: A series of hydrazinylthiazole carboxylates (3a-n) was prepared by cyclocondensation reaction of thiosemicarbazones with ethyl 2-chloroacetoacetate. These compounds were screened for antidiabetic potential through α-amylase inhibition, antiglycation and antioxidant assays. Results & conclusion: Most of the compounds exhibited a promising antidiabetic property. Compounds 3e and 3h showed excellent α-amylase and glycation inhibition properties. The hemolytic assay indicated that all compounds are biocompatible. Docking studies carried out on α-amylase target showed correlation between in vitro inhibition and binding energy.

Prospects of silver nanoparticles (AgNPs) synthesized by Justicia secunda aqueous extracts on diabetes and its related complications

The wide range of secondary metabolites in medicinal plant extracts are used to treat and manage various diseases worldwide but more recently plant-mediated bio-nanotechnology is rapidly generating great research interest. Herein, the in-vitro study of the antidiabetic, anti-inflammatory, antiglycation, and antioxidant potentials of silver nanoparticles (AgNPs) synthesized by Justicia secunda aqueous extracts was evaluated. The synthesized AgNPs was characterized by UV-visible spectrophotometer, Fourier transform infrared spectroscopy (FT-IR) and Scanning electron microscopy (SEM). The antioxidant activity was evaluated via reducing power, 2,2-diphenyl-1-picrylhydrazyl (DPPH), total antioxidant capacity (TAC) and nitric oxide scavenging assays; antidiabetic activity was evaluated with α-glucosidase and α-amylase inhibitory assays; antiglycation activity was evaluated using fructosamine inhibitory assay, and anti-inflammatory activity was performed using trypsin inhibitory and albumin denaturation assays. The AgNPs from all the plant parts showed good biological potentials investigated compared to the plant extracts however, the synthesized AgNPs using the leaf aqueous extract (AgNPs-JsL) showed a better antioxidant, antidiabetic, antiglycation, and anti-inflammatory potentials with an essential quality absorption band in the ultraviolet region of 410 nm and average size distribution of 50.47nm. In conclusion, all the parts of J. secunda showed substantial antidiabetic, antioxidant, antiglycation and anti-inflammatory potentials with high yield of various bioactive metabolites, however, the AgNPs-JsL was more potent followed by the flower, stem and roots extracts, respectively.

Synthesis of Silver Nanoparticles by Leaf Extract of Cucumis melo L. and Their In Vitro Antidiabetic and Anticoccidial Activities.

In this study, silver nanoparticles were synthesized using Cucumis melo L. leaf extract via a green synthesis approach and their potential against diabetes and coccidiosis was tested under in vitro conditions. The phytochemical components in the leaf extract reacted with silver nitrate in solution and yielded C. melo-silver nanoparticles (Cm-AgNPs). The synthesis of AgNPs was confirmed via UV-visible spectroscopy by obtaining a peak at 440 nm. The nanoparticles were characterized by their morphology, crystallinity, and the presence of functional groups. In vitro α-amylase and α-glucosidase inhibition assays were carried out at different concentrations in the range of 20 to 100 μg/mL of Cm-AgNPs. The Cm-AgNPs exhibited enzyme inhibitory activity in a concentration-dependent manner. As the concentration of Cm-AgNPs increased the inhibitory activities were also increased linearly and the highest inhibition was observed at 100 μg/mL. The effectiveness of Cm-AgNPs against Eimeria tenalla was assessed by an in vitro 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay using Madin-Darby bovine kidney (MDBK) cell lines. The results revealed that the viability of the oocysts and further sporulation were decreased with the increased concentration of Cm-AgNPs. The AgNPs synthesized from the C. melo leaf extract have shown promising potential against diabetes and coccidiosis, and they could be used in biomedical applications.

An investigation on photocatalytic and α-amylase inhibitory activities of Co(II) and Zn(II) phthalocyanines

Metallophthalocyanines have broad range of photocatalytic and biological applications, so they have been investigated widely by the scientific community. In this study, P4P-1 and P4P-2 phthalocyanines and their water soluble derivatives (QP4P-1 and QP4P-2) were synthesized and characterized by different spectral data. Photocatalytic performance of QP4P-1 and QP4P-2 were tested on photodegradation of 4-nitrophenol (4-NP). QP4P-1 shows remarkable photocatalytic activity with 90 % product conversion (TON:1500) in aqueous solution of 4-nitrophenol. α-amylase inhibition assay is performed in order to find out the enzyme inhibitory potential of water soluble phthalocyanine QP4P-2. QP4P-2 inhibited α-amylase 64.2 ± 0.8 % at 300 µM concentration and the IC50values ​​of the molecule was calculated as 128.2 ± 1.5 µM. QP4P-2 reflects the potential α-amylase inhibitory activity as compared to others.

A polysaccharide NAP-3 from Naematelia aurantialba: Structural characterization and adjunctive hypoglycemic activity

A novel polysaccharide (NAP-3) was isolated and purified from Naematelia aurantialba after water extraction. The structure of NAP-3, which was determined by FT-IR, HPLC, GC–MS, and NMR, indicated that NAP-3 was a homogeneous polysaccharide with the molecular weight of 428 kDa, mainly consisted of β-1, 3-D-Manp, β-1, 2, 3-D-Manp, β-D-Xylp, β-1, 4-D-Glcp, β-1, 4-D-Rhap in a molar ratio of 6.49: 1.11: 2.4: 0.13: 0.83. In vitro α-glucosidase and α-amylase inhibitory assay showed that NAP-3 had a low IC50 value, which exhibited similar enzyme inhibitory activity as acarbose. NAP-3 was evaluated as an adjuvant with metformin for antidiabetic therapy in HFD/STZ-induced diabetic mice and insulin resistance HepG2 cells. The combination of NAP-3 and metformin in diabetic mice exhibited significant hypoglycemic activity, reducing body weight, serum insulin levels, glucose tolerance, insulin tolerance, and increasing antioxidant levels compared to metformin alone. The combination of NAP-3 and metformin improved oxidative stress by increasing ROS clearance, thereby enhancing glucose uptake in HepG2 cells. This study provided new data for the study of Naematelia aurantialba polysaccharides and offers a new adjuvant therapy for the treatment of diabetes.

In Vitro, In Silico, and In Vivo Studies of Cardamine hirsuta Linn as a Potential Antidiabetic Agent in a Rat Model.

Diabetes mellitus (T2DM) is a multifaceted metabolic disorder with no definite treatment. In silico characterization can help to explain the interaction between molecules and predict 3D structures. The aim of the present study was to evaluate the hypoglycemic activities of the hydro-methanolic extract of Cardamine hirsuta in a rat model. In vitro antioxidant and α-amylase inhibitory assays were evaluated in the present study. Phyto-constituents were quantified using RP-UHPLC-MS analysis. Molecular docking of compounds into the binding site of different molecular targets, i.e., tumor necrosis factor (TNF-α), glycogen synthase kinase 3 β (GSK-3β), and AKT, was carried out. Acute toxicity model, in vivo antidiabetic effect, and the influence on biochemical and oxidative stress parameters were also investigated. T2DM was induced in adult male rats by streptozotocin using a high-fat diet model. Three different doses (125, 250, and 500 mg/kg BW) were orally gavaged for 30 days. Mulberrofuran-M and quercetin3-(6″caffeoylsophoroside) have demonstrated remarkable binding affinity toward TNF-α and GSK-3β, respectively. 2,2-Diphenyl-1-picrylhydrazyl and α-amylase inhibition assay exhibited IC50 values of 75.96 and 73.66 μg/mL, respectively. In vivo findings exhibited that 500 mg/kg body weight (BW) dose of the extract significantly decreased the blood glucose level, improved biochemical parameters as well as oxidative stress by reduction of lipid peroxidation, and increased high-density lipoproteins. Moreover, activities of glutathione-s-transferase, reduced glutathione, superoxide dismutase were enhanced, and cellular architecture in the histopathological examination was restored in treatment groups. The present study affirmed the antidiabetic activities of mulberrofuran-M and quercetin3-(6″caffeoylsophoroside) present in the hydro-methanolic extract of C. hirsuta, possibly due to the reduction in oxidative stress and α-amylase inhibition.