Α-amylase Inhibition Assay Research Articles

Antioxidant, Hypoglycemic, Antilipidemic, and Protective Effect of Polyherbal Emulsion (F6-SMONSECCE) on Alloxan-Induced Diabetic Rats.

The current study focused on the antioxidant potential, α-amylase inhibitory activity, and hypoglycemic, hypolipidemic, and histoprotective (pancreas and kidney) effects of polyherbal emulsion on the alloxan-induced diabetic rats. Polyherbal formulations were prepared from extracts and oils of Nigella sativa (N. sativa), Citrullus colocynthis (C. colocynthis), and Silybum marianum (S. marianum). Out of nine stable formulations, one formulation named F6-SMONSECCE was found to be the best after its evaluation using antioxidant and in vitro α-amylase inhibition assay. The prepared herbal formulations showed significant (p < 0.05) antioxidant activity in terms of radical scavenging as 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric-reducing antioxidant power (FRAP) assays and also revealed the presence of a significant amount of total phenolic and flavonoid contents. "F6- SMONSECCE" (prepared with composition; Silybum marianum oil (SMO) + Nigella sativa extract (NSE) + Citrullus colocynthis extract CCE) was selected for an in vivo trial to ascertain its antidiabetic potential. The treatment dose was determined by using an acute toxicity trial on rats. Administration of alloxan (150 mg/kg b.w., i.p.) significantly (P < 0.05) augmented the blood glucose levels and lipid contents as total cholesterol (TC), triglycerides (TG), low-density lipoproteins (LDL-c), and very-low-density lipoproteins (VLDL-c). However, the levels of insulin and high-density lipoproteins (HDL-c) were found to be decreased, and the histopathological alterations were also found in the pancreas and kidney. The administration of the polyherbal formulation (F6-SMONSECCE) significantly attenuated the blood glucose levels (22.94%), TC (29.10%), TG (38.15%), LDL-c (27.58%), and VLDL-c (71.52%), whereas on the other side, the insulin (-149.15%) and HDL-c levels (-22.22%) were significantly increased. A significant histopathological normalization was observed in the pancreas and kidney tissues of the F6-SMONSECCE-treated rats. The current findings proposed that the prepared polyherbal formulation "F6-SMONSECCE" exhibited significant antioxidant, antilipidemic, and hypoglycemic potential and hence might be suggested as a remedy against diabetes or as a coadjuvant to synthetic medicines to maintain normal physiology.

Green Synthesis and Characterizations of Chromium Oxide Nanoparticles (Cr&lt;sub&gt;2&lt;/sub&gt;O&lt;sub&gt;3&lt;/sub&gt; NPs) Derived from Pomegranate Husk and its α-Amylase Inhibitory and Antioxidant Properties

A disease of imbalanced control of blood glucose levels due to impairment of insulin secretion or acceptance is known as diabetes mellitus. It could be induced by the high intake of sugar in diets, or by genetic background, or both. The antioxidant, which plays a role in neutralising free radicals, is crucial as the free radical could increase the chances of getting diabetes through several pathways. Injection of insulin and anti-diabetic drugs are common approaches to treating diabetes, but unfortunately, many side effects have been reported. Green synthesis of metal oxide nanoparticle, which is one of the applications of nanotechnology, could be a promising method in combating diabetes as it is biocompatible, less toxic, and has large surface to volume ratio. In this study, green synthesis and characterization of Cr2O3 NPs were carried out. The Cr2O3 NPs were shown to be spherical in shape, with an average size that falls within 100 nm. The EDX spectrum indicated that only chromium (Cr) and oxygen (O) were present in the sample. Other characterization techniques such as FTIR and UV-VIS spectroscopy were conducted. For ABTS and DPPH assays, Cr2O3 NPs exhibited highest free radical scavenging properties at 74.57% and 84.12% at 30 minutes and 60 minutes at the concentrations of 5 mg/mL and 1 mg/mL, respectively. Lastly, Cr2O3 NPs showed 95.28 % at the concentration of 0.25 mg/mL in α-amylase inhibition assay.

COMPARISON OF SOME BIOLOGICAL ACTIVITIES AND CATECHIN TANNIN CONTENTS OF TWO JUNIPERUS AND PRUNUS SPECIES

Objective: Qualitative and quantitative determination of catechin in fruits of J. communis var. saxatilis, J. oxycedrus subsp. oxycedrus, P. spinosa, and P. cerasifera was analyzed by LC-MS/MS using standards. Antidiabetic, antimicrobial, and antioxidant activities of fruit and cone extracts of these plants were evaluated. Qualitative analysis of secondary metabolites was also done. Material and Method: Antimicrobial activity was done with MIC. ABTS·+ and DPPH• scavenging activies were used antioxidant activity. α-Amylase and α-glucosidase inhibition assays were done for antidiabetic activity. Result and Discussion: JCS (IC50 = 578 ± 20 μg/ml), JOO (IC50 = 3706 ± 52 μg/ml), and PS (IC50 = 313 ± 7 μg/ml) extracts were observed to show a higher activity than acarbose (IC50 = 4061 ± 146 μg/ml). J. communis var. saxatilis fruit extract was observed with MIC values between (312.5 -2500 µg/ml) against all microorganisms. JCS extract has the highest phenolic composition and JOO has the lowest phenolic composition (µg GAE/ mg extract). JCS extract indicated the highest antioxidant activity. It was determined that plant containing the highest catechin (1173.3±5.77 ng/ml) and epigallocatechin (208±7.21 ng/ml) was JCS. In this research, it can be said that JCS with the highest tannin content shows the highest effects.

Screening of Syzygium cumini (L.) Seed Ethanol and Hexane Extracts for Phytochemicals, Antioxidant, and Anti-Diabetic Efficacy: An In-vitro Study

Many medicinal plant extracts have been known since ancient times to possess antioxidant activity to scavenge free radicals and anti-diabetic activity to control diabetes. In this study, seeds of Syzygium cumini were extracted in ethanol and hexane solvents. Primary and secondary metabolites were quantified. DPPH assay, nitric oxide scavenging (NOS) assay and ferric reducing antioxidant power (FRAP) assays were employed to study antioxidant activity. α-amylase inhibitory assay (AAI), yeast glucose uptake assay (YGU) and haemoglobin glycosylation inhibitory (HGI) assays were adapted to determine anti-diabetic properties. The results from the assays and the IC50 values (18.35 µg/ml in DPPH, 943.8 µg/ml in NOS, 871.3 µg/ml in FRAP, 886 µg/ml in AAI, 764 µg/ml in YGU, and 1495.1 µg/ml in HGI assay) indicate that S. cumini seed ethanol extract has higher antioxidant and anti-diabetic efficiency than the hexane extract. Our findings suggest that the rich phytochemical content of S. cumini seeds and its good antioxidant and anti-diabetic activity may be responsible for its popularity and wide traditional use and can be exploited to develop antioxidant and anti-diabetic drugs.

Biochemical, structural characterization and in-vitro evaluation of antioxidant, antibacterial, cytotoxic, and antidiabetic activities of nanosuspensions of Cinnamomum zeylanicum bark extract.

Cinnamomum zeylanicum is a traditional medicinal plant known for its anti-inflammatory, antidiabetic, antimicrobial, anticancer, and antioxidant properties. Its therapeutic efficacy using nanosuspensions is still unclear for treating infectious diseases. This study was designed to evaluate the bioactivities, biochemical characterization, and bioavailability of freshly prepared nanosuspensions of C. zeylanicum. Structural and biochemical characterization of C. zeylanicum and its biological activities, such as antioxidants, antimicrobials, antiglycation, α-amylase inhibition, and cytotoxicity was performed using Fourier-transform infrared (FTIR) spectroscopy and High-Performance Liquid Chromatography (HPLC). C. zeylanicum extract and nanosuspensions showed TPCs values of 341.88 and 39.51mg GAE/100g while showing TFCs as 429.19 and 239.26mg CE/100g, respectively. DPPH inhibition potential of C. zeylanicum extract and nanosuspension was 27.3% and 10.6%, respectively. Biofilm inhibition activity revealed that bark extract and nanosuspension showed excessive growth restraint against Escherichia coli, reaching 67.11% and 66.09%, respectively. The α-amylase inhibition assay of extract and nanosuspension was 39.3% and 6.3%, while the antiglycation activity of nanosuspension and extract was 42.14% and 53.76%, respectively. Extracts and nanosuspensions showed maximum hemolysis at 54.78% and 19.89%, respectively. Results indicated that nanosuspensions possessed antidiabetic, antimicrobial, anticancer, and antioxidant properties. Further study, however, is needed to assess the clinical studies for the therapeutic use of nanosuspensions.

Determination of Phytochemicals, Minerals, and Evaluation of Antioxidant, Antidiabetic Activities of Young Fronds of &lt;i&gt;Diplazium esculent&lt;/i&gt;um: A Vegetable of Tripura, India

Diplazium esculentum belongs to the family Athyriaceae, an edible fern rich in micronutrients, beta-carotene, folic acid, and minerals like calcium, iron, and phosphorus. The present study aims to determine secondary metabolites and minerals content and evaluate the antioxidant and antidiabetic activities of young fronds of Diplazium esculentum. The plant extract was prepared by the Soxhlet apparatus method. Total alkaloids and total tannin content were determined by the titrimetric method. Folin and Ciocalteu's colorimetric method used gallic acid as a standard drug to determine total phenols. The antioxidant activity of plant extract was evaluated by DPPH free radical scavenging and hydrogen peroxide scavenging assay. α-amylase inhibition assay was performed for evaluation of the antidiabetic activity of plant extract. Fronds of Diplazium esculentum contain a significant number of total alkaloids (145.54±1.49), phenols (174.2±0.95), and tannins (263.96±1.32) mg/g of dry extract. Fronds of Diplazium esculentum also contain a significant amount of minerals. Diplazium esculentum shows significant antioxidant activity compared to the standard drug ascorbic acid and antidiabetic activity compared to the standard drug metformin. Based on these findings, young fronds of Diplazium esculentum can be recommended as a good source of phytochemicals and minerals. It also shows significant antioxidant and antidiabetic activities.

Evaluation of In-vitro Anti-oxidant and α-amylase inhibition activity of Allium tuberosom and its Phytochemical analysis

Allium tuberosom, a species native to Chinese province of Shanxi and also found in the North-eastern states of India especially Manipur, is well known for its medicinal properties such as antibacterial, cardiac, stimulant, anti-cancer, etc. Fresh samples of Allium tuberosum were collected from Manipur and assayed for the presence of potent phytochemicals. Moreover, the extracts of the sample were also investigated for their anti-oxidant and anti-diabetic activities. Two solvents of varied polarity were used for soxhlet extraction and standard protocols were employed throughout the study. Presence of various phytochemicals such as alkaloids, flavonoids, saponins, etc. was reported. Upon evaluation of anti-oxidant activity by DPPH method, it was recorded that more the concentration of the sample more was its anti-oxidant activity for both the extracts (hexane and methanol), i.e. upto 63.1% for hexane extract and 67.4% for methanol extract. Anti-diabetic activity by α-amylase inhibition assay was also dependent on its concentration. 64.19% for hexane extract and 62.7% for methanol extract of α-amylase inhibiting activity was recorded. The results of the current study prove the potentiality of the species to be further considered as a valuable asset for clinical trials so as to be explored in pharmaceutical purposes.

Thymus linearis Extracts Ameliorate Indices of Metabolic Syndrome in Sprague Dawley Rats.

The extract library (n-hexane (NH), ethyl acetate (EA), methanol (M), distilled water (DW), and combined extract (CE)) was standardized using in vitro phytochemical, antioxidant, and α-amylase inhibition assays, after which the protective effect of selected "hit," i.e., CE against metabolic syndrome, was determined in vivo, using rats fed a high-fat diet supplemented with additional cholesterol administration. CE was administered to Sprague Dawley rats in high dose as 100 mg/kg in carboxymethyl cellulose (CMC) (1 ml; 0.75% in DW) and low-dose group as 50 mg/kg in CMC (0.5 ml; 0.75% in DW). After 10 weeks, the effects of CE on insulin resistance, lipid metabolism, nonalcoholic fatty liver disease (NAFLD), oxidative stress, and genotoxicity were assessed through histological, biochemical, and hematological investigations. Phytochemical analysis including RP-HPLC analysis of the extracts showed that flavonoids and phenolics (myricetin, kaempferol, and apigenin), previously known to be effective against obesity and diabetes, are present in the extracts. Antioxidant studies revealed that the plant possesses a highly significant (p < 0.05) concentration of antioxidants. Satisfactory α-amylase inhibitory activity was also observed in in vitro experiments. In vivo studies showed that CE-administered animals had significantly (p < 0.05) lower weight gain and smaller adipocytes than the control group. Moreover, CE resisted any significant (p < 0.05) change in the organ weights. Analogous to findings from its traditional use, the plant extract had a positive modulatory effect on insulin resistance and hyperglycemia. The study also indicated that CE resisted high-fat diet-induced disturbance in lipid profile and countered any pathological changes in liver enzymes caused by fat-infused diet. Furthermore, a study on endogenous antioxidant levels indicated that CE was effective in maintaining catalase and peroxidase levels within the normal range and resisted the effects of lipid peroxidation of thiobarbituric acid reactive substances. In principle, the current study's findings scientifically validate the implication of T. linearis in metabolic syndrome and recommend further studies on molecular insights of the observed therapeutic activity.

Study of Phytochemical Constituent and Biological Activities of Methanolic Extract of Rhizomes of Neopicrorhiza scrophulariiflora and Roots of Rheum australe collected from the Alpine Region of Nepal

Rhizomes of Neopicrorhiza scrophularii flora and roots of Rheum australe were collected from the alpine regions of the Jumla district of Nepal. The phytochemical analysis of the methanolic extract of these plants revealed the presence of polyphenols, flavonoids, quinones, saponins, and tannins. The total phenolic and flavonoid content in the extracts of N. scrophulariiflora were estimated to be 141.27±1.414 mg GAE/gm and 43.48±5.476 QE/gm respectively and that in the extracts of R. austral were estimated to be 101.54±4.061 mg GAE/gm and 24.97±2.857 mg QE/gm respectively. A brine shrimp lethality test was performed with the extracts of N. scrophulariiflora and R. austral against brine shrimp nauplii and results revealed high toxicity of the extracts towards nauplii with LC50 values 173.78μg/mL and 257.03μg/mL respectively. N. scrophulariiflora showed the strongest DPPH radical scavenging activity with IC50 value of 57.49 μg/mL in comparison to R. austral whose IC50 was determined to be 68.91μg/mL, ascorbic acid taken as standard with IC50 value 49.05μg/ml. In α-amylase inhibition assay, N. scrophulariiflora extract exhibited strong activity with IC50 value 140.67μg/mL while that of R. austral extract showed mild activity with IC50 value 192.88μg/mL. All the biological studies revealed that N. scrophulariiflora extract is more active than that R. austral extract. Column chromatography of the extract of N. scrophulariiflora was performed and 50 % methanolic fraction was further subjected to FTIR and GC-MS analysis. The GC-MS analysis showed various compounds and among them, 13 major compounds were identified.

Green Synthesis of ZnO and V-Doped ZnO Nanoparticles Using Vinca rosea Plant Leaf for Biomedical Applications.

The present work focused on the synthesis of Vinca rosea leaf extract derived ZnO and vanadium-doped ZnO nanoparticles (V-ZnO NPs). The chemical composition, structural, and morphology of ZnO and vanadium-doped ZnO NPs were examined by FTIR, XRD, and SEM-EDX. The FTIR confirmed the presence of functional groups corresponding to ZnO and vanadium-doped ZnO NPs. SEM-EDX clearly indicated the morphology of synthesised NPs; the hexagonal crystal of NPs was confirmed from XRD. In addition, the cytotoxic effect of ZnO and V-ZnO NPs was estimated against the breast cancer (MCF-7) cell line. From the assay, Vinca rosea (V. rosea) capped ZnO NPs have shown improved cytotoxic activity than that of Vinca rosea capped V-ZnO NPs. ZnO and vanadium-doped ZnO NPs showed the strongest antibacterial activity against Enterococcus, Escherichia coli, Candidaalbicans, and Aspergillus niger. The α-amylase inhibition assays demonstrated antidiabetic activity of synthesised NPs. From the assay test, results obtained Vinca rosea capped ZnO nanoparticles prepared using the green approach showed high effective antioxidant, antidiabetic activity, and anticancer activity than vanadium-doped ZnO NPs.

In-silico and In-vitro Evaluation of the Anti-diabetic Potential of p-Propoxybenzoic Acid

Background: p-propoxybenzoic acid (p-PBA) is reported as an active chemical constituent of medicinal plants that possess anti-diabetic activity. It is termed a Multiple-Designed Ligand (MDL) having the ability to block more than one enzyme. A molecular docking study justifies the binding ability of p-PBA with acarbose and NaVO4 which were considered standard compounds having the ability to block target enzymes. α-amylase inhibition assay was used as an in-vitro screening model to evaluate the activity of p-PBA against diabetes on an initial basis. Methods: For the molecular docking study, a PDB file of p-PBA was prepared and PDB files of α-amylase (1C8Q), α-glucosidase (5KZW) and PTP1B (5K9W) were procured. p-PBA was docked against the enzymes using the blind docking method. The binding score of p-PBA and standard with enzymes was obtained and compared. The percentage inhibition of an α-amylase enzyme by p-PBA was measured by using a DNS-modified α-amylase inhibition assay and half-maximal inhibitory concentration (IC50) was calculated. Results: p-PBA has a significant inhibitory effect against α-amylase, α-glucosidase, and PTP1B with docking scores of 8.43 ± 0.44 kcal/mol, 9.19 ± 0.49 kcal/mol, and 9.40 ± 0.47 kcal/mol respectively. IC50calculated from the results of α-amylase inhibition assay p-PBA was 56.59 μg/mL. Conclusion: A combination of in-silico and in-vitro methods assessed p-PBA’s anti-diabetic potential on an initial basis. A molecular docking study involving p-PBA concluded the affinity of p-PBA to α-amylase, α-glucosidase, and PTP1B was significantly correlated with the affinity of acarbose and NaVO4. In-vitro α-amylase assay validated the compound’s inhibitory action against the enzyme.

Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives.

In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, 1H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity, ranging from moderate to high depending upon their structures and concentrations and compared to the standard drug acarbose. Both in silico and in vitro analysis indicated that the synthesized triazole molecules are potent for DM type-II. Out of all the compounds, compound K-1 showed the maximum antidiabetic activity with 87.01% and 99.17% inhibition at 800 µg/mL in the α-amylase and α-glucosidase inhibition assays, respectively. Therefore these triazoles may be further used as promising molecules for development of antidiabetic compounds.

Single crystal structure of nitro terminated Azo Schiff base: DNA binding, antioxidant, enzyme inhibitory and photo-isomerization investigation

Novel azo schiff base compound, namely, 2‑hydroxy-5-[(E)-phenyldiazenyl] benzaldehyde (AzNP) was synthesized by reacting 2‑hydroxy-5-[(E)-phenyldiazenyl]benzaldehyde and 4-(4-nitrophenoxy)benzenamine under inert conditions. The synthesized compound AzNP was characterized by Fourier transform (FT-IR), Nuclear magnetic resonance (NMR) and Ultraviolet-visible (UV–vis) spectroscopy. The solid state structure was elucidated by single-crystal X-ray crystallography. The compound was crystallized in the Monoclinic system with P 1 21/c1 space group, having a = 6.4859(3 Å, b = 15.6673(7) Å, c = 19.7908(9) Å, β = 90.945(2), and Z = 4, showing only one intermolecular C21-H21...N2 interaction, with donor and acceptor distance of 3.5774(16) Å, responsible for the elegant 3D network of the structure. DFT calculations were performed for structure-property relationship information of AzNP. In order to comprehend the selectivity behavior of the compound, binding interaction with CT-DNA was examined using standard optical spectroscopy. The observed hypochromism in the binding studies indicated that ligand substantially interact via the groove binding mode (Kb =9.91×103 mol−1dm3) with the DNA. Further assessment of binding mode of AzNP with DNA was made through hydrodynamic measurement and molecular docking analysis which confirmed the major groove binding mode of the ligand. Additionally, the DPPH (2,2-diphenyl-1-picrylhydrazyl), the ferric reducing power, and the α-amylase inhibition assays were used to evaluate the biological significance. Analysis of Cis-Trans conformational changes was also done to investigate photoisomerization properties of synthesized compound AzNP.

Chromatography analysis, in light of vitro antioxidant, antidiabetic, antiobesity, anti-inflammatory, antimicrobial, anticancer, and three-dimensional cancer spheroids’ formation blocking activities of Laurus nobilis aromatic oil from Palestine

Laurus nobilis (LN) has been used throughout the years as a food flavoring and in traditional medicine. The LN leaves have various biological activities, such as antioxidant, wound healing, antibacterial, analgesic, and anti-inflammatory activities. However, oxidative stress, cancer, diabetes, microbial infections, and inflammatory diseases are closely linked. The objective of this research is to characterize Laurus nobilis (LN) aromatic oil (AO) and evaluate its antioxidant, antidiabetic, antiobesity, antimicrobial, and antimutagenic bioactivities. The AO constituents were characterized using gas chromatography–mass spectrometry (GC–MS). The antimicrobial activity was performed using a microdilution assay against six common microbial species. Free radicals, a porcine pancreatic lipase, α-amylase, and α-glucosidase inhibitory assays were conducted utilizing reference biomedical methods. The cytotoxic effect of LNAO was established on a variety of cancer and normal cell lines using the MTS assay. The anti-inflammatory activity of LNAO was evaluated using the Cayman COX activity kit. The results indicate about 99% of the total oil is composed of 36 compounds, the characterized AO metabolites showed content of many oxygenated terpenoids with 1,8-Cineole and Terpinyl acetate as a major component with a percentage of (40.39 and 15.07, respectively. The plant AO showed potent antioxidant activity (IC50 = 2.2 ± 1.38) and has moderate anti-amylase (IC50 = 60.25 ± 1.25), anti-glucosidase (IC50 = 131.82 ± 0.1), and antilipase (IC50 = 83.17 ± 0.06) activities. Moreover, LNAO showed potent antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, Proteus vulgaris (MICs = 1.56 µg/mL), methicillin-resistant Staphylococcus aureus (MRSA) (MIC = 3.125 µg/mL) and Candida albicans (MIC = 0.195 µg/mL). The cytotoxicity results demonstrated that at a concentration of 1 mg/mL, LNAO has potent breast cancer (MCF-7), and hepatocellular carcinoma (Hep 3B) cancer cells inhibitory activities of 98% and 95%, respectively. Importantly, we are the first to show that LNAO significantly hinders hepatocellular carcinoma spheroids’ formation capacity in a 3D model. These results show that LNAO is a promising natural source with powerful antioxidant, antidiabetic, anticancer, and antimicrobial activities that could be exploited in the future to treat a variety of diseases.Graphical

Valorization of Adhatoda vasica leaves: Extraction, in vitro analyses and in silico approaches.

Adhatoda vasica (also called Vasaka) is a traditional medicinal herb used traditionally for the relief of cough, asthma, nasal congestion, bronchial inflammation, upper respiratory infections, bleeding disorders, skin diseases, leprosy, tuberculosis, diabetes, allergic conditions, rheumatism, tumor, and many more diseases. The present study aims to investigate the biological activities of vasicine, a potent alkaloid from A. vasica with different biological/ pharmacological assays and in silico techniques. Vasicine showed antimicrobial activity as evidenced fromthe colony-forming unit assay. It showed antioxidant activity in ABTS scavenging assay (IC50 = 11.5 μg/ml), ferric reducing power assay (IC50 = 15 μg/ml), DPPH radical scavenging assay (IC50 = 18.2 μg/ml), hydroxyl radical scavenging assay (IC50 = 22 μg/ml), and hydrogen peroxide assay (IC50 = 27.8 μg/ml). It also showed anti-inflammatory activity in proteinase inhibitory assay (IC50 = 76 μg/ml), BSA method (IC50 = 51.7 μg/ml), egg albumin method (IC50 = 53.2 μg/ml), and lipooxygenase inhibition assay (IC50 = 76 μg/ml). Vasicine showed antidiabetic activity in α-amylase inhibition assay (IC50 = 47.6 μg/ml), α-glucosidase inhibition assay (IC50 = 49.68 μg/ml), and non-enzymatic glycosylation of hemoglobin assay. It showed antiviral activity against HIV-protease (IC50 = 38.5 μg/ml). Vasicine also showed anticancer activity against lung cancer cells (IC50 = 46.5 μg/ml) and human fibroblast cells (IC50 = 82.5 μg/ml). In silico studies revealed that similar to the native ligands, vasicine also showed a low binding energy, i.e., good binding affinity for the active binding sites and interacted with α-amylase (-6.7 kcal/mol), α-glucosidase (-7.6 kcal/mol), cyclooxygenase (-7.4 kcal/mol), epidermal growth factor receptor (-6.4 kcal/mol), lipooxygenase (-6.9 kcal/mol), and HIV-protease (-6.4 kcal/mol). The present study ascertains the potential of vasicine as a bioactive compound isolated from A. vasica having therapeutic usefulness in many human diseases.

Evaluation of Anti-diabetic Potential of Anti-microbial Carbon Quantum Dots from Vitis vinifera Seeds

Carbon quantum dots (CQDs) have a size of 10 nm (or less), with lots of biomedical advantages, creating huge excitement in different research fields. The aim of this study includes an eco-friendly synthesis of biogenic CQDs from grape (<i>Vitis vinifera</i>) seeds, identifying the characteristics and assessing its anti-diabetic as well as anti-microbial activity. CQDs are prepared by the pyrolysis method. Synthesized CQDs were confirmed by ultraviolet (UV)–visible (Vis) spectrophotometer, and the characterization study was done by X-ray diffractometer, photoluminescence spectroscopy, Fourier transform infra-red spectroscopy, and transmission electron microscopy with selected area electron diffraction (SAED). Anti-diabetic activity of CQDs was analyzed by <i>in vitro</i> α-glycosidase, α-amylase inhibition assays, and glucose uptake studies. The anti-bacterial activity of CQDs was analyzed by anti-microbial assay technique against <i>Escherichia coli, Pseudomonas aeruginosa</i>, <i>Staphylococcus aureus,</i> and <i>Streptococcus mutans</i>. The results showed that the CQDs synthesized from a natural source like grape seeds, were amorphous in nature, the average particle size was 4 nm, and they contain functional groups like carboxyl and hydroxyl. Subsequently, it showed that the sp2 domains also produce green fluorescence. The anti-diabetic experimental method revealed that the CQDs enhance glucose uptake and inhibit carbohydrate hydrolyzing enzymes. CQDs also exhibit anti-bacterial properties against both Gram-positive and Gram-negative bacteria, according to their antimicrobial impact. Due to their small size and higher activity, CQDs will become strong anti-diabetic agents as well as anti-bacterial ones.

Design, synthesis, spectroscopic characterization, single crystal X-ray analysis, in vitro α-amylase inhibition assay, DPPH free radical evaluation and computational studies of naphtho[2,3-d]imidazole-4,9-dione appended 1,2,3-triazoles

In our quest to design and develop N/O-containing inhibitors of α-amylase, we have tried to synergize the inhibitory action of 1,4-naphthoquinone, imidazole and 1,2,3-triazole motifs by incorporating these structures into a single matrix. For this, a series of novel naphtho[2,3-d]imidazole-4,9-dione appended 1,2,3-triazoles is synthesized by a sequential approach involving [3 + 2] cycloaddition of 2-aryl-1-(prop-2-yn-1-yl)-1H-naphtho[2,3-d]imidazole-4,9-diones with substituted azides. The chemical structures of all the compounds are established with the help of 1D-NMR, 2D-NMR, IR, mass and X-ray studies. The developed molecular hybrids are screened for their inhibitory action on the α-amylase enzyme using the reference drug, acarbose. Different substituents present on the attached aryl part of the target compounds show amazing variations in inhibitory action against the α-amylase enzyme. Based on the type of substituents and their respective positions, it is observed that compounds containing –OCH3 and –NO2 groups show more inhibition potential than others. All the tested derivatives display α-amylase inhibitory activity with IC50 values in the range of 17.83 ± 0.14 to 26.00 ± 0.17 μg/mL. Compound 2-(2,3,4-trimethoxyphenyl)-1-{[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl]methyl}-1H-naphtho[2,3-d]imidazole-4,9-dione (10y) show maximum inhibition of amylase activity with IC50 value 17.83 ± 0.14 μg/mL as compared to reference drug acarbose (18.81 ± 0.05 μg/mL). A molecular docking study of the most active derivative (10y) is performed with A. oryzae α-amylase (PDB ID: 7TAA) and it unveils favourable binding interactions within the active site of the receptor molecule. The dynamic studies reveal that the receptor-ligand complex is stable as the RMSD of less than 2 is observed in 100 ns molecular dynamic simulation. Also, the designed derivatives are assayed for their DPPH free radical scavenging ability and all of them exhibit comparable radical scavenging activity with the standard, BHT. Further, to assess their drug-likeness properties, ADME properties are also evaluated and all of them demonstrate worthy in silico ADME results.

"Ficus johannis Boiss. leaves ethanolic extract ameliorate streptozotocin-induced diabetes in rats by upregulating the expressions of GCK, GLUT4, and IGF and downregulating G6P".

The leaves of Ficus johannis Boiss (F. johannis), commonly known as Fig tree, Anjir, and Teen, are used by the folk medicinal practitioners in Iran for controlling hyperglycemia in diabetic patients. This study investigated the pharmacological basis for antidiabetic effect of the ethanolic extract of F. johannis leaves using in vitro and in vivo experimental models. Qualitative screening of phytochemicals, estimation of total phenolic and flavonoid contents, and in vitro antioxidant and α-amylase inhibition assays were performed. Moreover, the High-performance liquid chromatography (HPLC) quantification, acute toxicity, glucose tolerance, and in vivo antidiabetic effect along with the evaluation of gene expressions involved in diabetes mellitus were carried out. Significant quantities of phenolic (71.208 ± 2.89 mgg-1 GAE) and flavonoid (26.38 ± 3.53 mgg-1 QE) were present. Inhibitory concentration (IC50) of the plant extract exhibited an excellent in vitro antioxidant (IC50 = 33.81µg/mL) and α-amylase (IC50 = 12.18µg/mL) inhibitory potential. The HPLC analysis confirmed the gallic acid (257.79 mgg-1) as main constituent of the extract followed by kaempferol (22.86 mgg-1), myricetin (0.16 mgg-1), and quercetin (3.22 mgg-1). Ethanolic extract displayed glucose tolerance in normo-glycemic rats. Streptozotocin-induced hyperglycemia declined dose dependently in the extract treated rats with improvement in lipid profile and liver and renal function biomarkers. The F. johannis-treated groups showed an increase in mRNA expressions of glucose transporter 4 (GLUT-4), glucokinase, insulin growth like factor 1 and peroxisomal proliferator activating receptor gamma in pancreas. However, the Glucose-6-phosphatase was downregulated. Present study suggests that the ethanolic extract of F. johannis leaves demonstrates a good anti-diabetic profile by improving insulin sensitivity, GLUT-4 translocation, and carbohydrate metabolism while inhibiting lipogenesis.

TLC-bioautography-MS-based Identification of Antioxidant, α-Amylase and α-Glucosidase Inhibitory Compounds in a Polyherbal Formulation “Sugreen-120”

Background Sugreen-120 is one of the famous Indian polyherbal formulations used for the treatment of diabetes. Due to a lack of scientific evidence, the present study is aimed at investigating the phytopharmacology of Sugreen-120 concerning its antioxidant and antidiabetic characteristics. Materials and Methods Total phenols and flavonoid content followed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity was estimated in Sugreen-120. α-Amylase and α-glucosidase inhibitory action of Sugreen-120 was estimated to evaluate its antidiabetic potential. Thin layer chromatography (TLC)-bioautography-MS analysis was performed to determine DPPH free radical, α-amylase and α-glucosidase inhibitory phytoconstituents in Sugreen-120. High performance thin layer chromatography (HPTLC)-based quantitative analysis of Sugreen-120 was performed for the simultaneous separation of caffeic acid and kaempferol. In silico docking analysis was performed to determine the effect of Sugreen-120 metabolites against α-amylase and α-glucosidase enzymes. Results The results showed that Sugreen-120 is enriched in total phenols and flavonoids and even has good potential to scavenge DPPH free radicals with an inhibitory concentration (IC50) value of 414.59 ± 4.925 µg/mL. In α-amylase and α-glucosidase inhibitory assays, the efficacy of Sugreen-120 was found in a dose-dependent manner and the IC50 values were found as 220.106 ± 1.375 and 441.44 ± 1.992 µg/mL, respectively. TLC-bioautographic analysis showed that 06 constituents were found active against DPPH free radical, 04 constituents active against α-amylase and 03 constituents active against α-glucosidase. A HPTLC quantitative study revealed the content of caffeic acid and kaempferol to be 5.233 ± 0.026 and 16.959 ± 0.036 µg/mg, respectively. In silico docking analysis showed that out of 5 identified metabolites, myricetin, ellagic acid, and kaempferol were found with significant interaction with α-amylase and α-glucosidase proteins. Hence, it can be concluded that Sugreen-120 exhibits not only an antidiabetic effect but also antioxidant potential. It can be a palliative choice and an alternative that can be used for the treatment of diabetes.

Discovery of Novel Thiazolidinedione-Derivatives with Multi-Modal Antidiabetic Activities In Vitro and In Silico.

Diabetes mellitus (DM) and related complications continue to exert a significant burden on health care systems globally. Although conventional pharmacological therapies are beneficial in the management of this metabolic condition, it is still necessary to seek novel potential molecules for its management. On this basis, we have synthesised and evaluated the anti-diabetic properties of four novel thiazolidinedione (TZD)-derivatives. The TZD derivatives were synthesised through the pharmacophore hybridisation strategy based on N-arylpyrrole and TZD. The resultant derivatives at different concentrations were screened against key enzymes of glucose metabolism and glucose utilisation in the liver (HEP-G2) cell line. Additionally, peroxisome proliferator-activated receptor-γ activation was performed through docking studies. Docking of these molecules against PPAR-γ predicted strong binding, similar to that of rosiglitazone. Hence, TZDD2 was able to increase glucose uptake in the liver cells as compared to the control. The enzymatic inhibition assays showed a relative inhibition activity; with all four derivatives exhibiting ≥ 50% inhibition activity in the α-amylase inhibition assay and a concentration dependent activity in the α-glucosidase inhibition assay. All four derivatives exhibited ≥30% inhibition in the aldose reductase inhibition assay, except TZDD1 at 10 µg/mL. Interestingly, TZDD3 showed a decreasing inhibition activity. In the dipeptidyl peptidase-4 inhibition assay, TZDD2 and TZDD4 exhibited ≥20% inhibition activity.