2-2--azino-di-(3-ethylbenzothiazoline)-6-sulfonic-acid and Diabetes-Mellitus

The strategy of utilizing nitrogen compounds in various biological applications has recently emerged as a powerful approach to exploring novel classes of therapeutics to face the challenge of diseases. A series of pyrazolo[1,5-a]pyrimidine-based compounds 3a-l and 5a-f were prepared by the direct cyclo-condensation reaction of 5-amino-1H-pyrazoles 1a, b with 2-(arylidene)malononitriles and 3-(dimethylamino)-1-aryl-prop-2-en-1-ones, respectively. The structures of the new pyrazolo[1,5-a]pyrimidine compounds were confirmed via spectroscopic techniques. The in vitro biological activities of all pyrazolo[1,5-a]pyrimidines 3a-l and 5a-f were evaluated by assaying total antioxidant capacity, iron-reducing power, the scavenging activity against 1-diphenyl-2-picryl-hydrazyl (DPPH) and 2, 2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals, anti-diabetic, anti-Alzheimer, and anti-arthritic biological activities. All compounds displayed good to potent bioactivity, and three compounds 3g, 3h, and 3l displayed the most active derivatives. Among these derivatives, compound 3l exhibited the highest antioxidant (total antioxidant capacity [TAC] = 83.09 mg gallic acid/g; iron-reducing power [IRP] = 47.93 µg/ml) and free radicals scavenging activities with (DPPH = 18.77 µg/ml; ABTS = 40.44%) compared with ascorbic acid (DPPH = 4.28 µg/ml; ABTS = 38.84%). Furthermore, compound 3l demonstrated the strongest inhibition of α-amylase with a percent inhibition of 72.91 ± 0.14 compared to acarbose = 67.92 ± 0.09%. Similarly, it displayed acetylcholinesterase inhibition of 62.80 ± 0.06%. However, compound 3i showed a significantly higher inhibition percentage for protein denaturation and proteinase at 20.66 ± 0.00 and 26.42 ± 0.06%, respectively. Additionally, some in silico ADMET properties were predicted and studied. Finally, molecular docking simulation was performed inside the active site of α-amylase and acetylcholinesterase to study their interactions.

Topics: Acetylcholinesterase; Antioxidants; Diabetes Mellitus; Humans; Iron; Molecular Docking Simulation; Molecular Structure; Pyrimidines; Structure-Activity Relationship

In situ visualization for the diagnosis of diabetic syndrome and visual monitoring the response to drug treatment is a challenge. Herein, we designed and prepared an autocatalytically-activatable hydrogen peroxide photoacoustic (PA) sensor. We first prepared the FeMoO

Topics: Biosensing Techniques; Diabetes Mellitus; Humans; Hydrogen Peroxide; Photoacoustic Techniques; Sulfonic Acids

Topics: alpha-Amylases; Benzofurans; Chalcones; Diabetes Mellitus; Humans

Topics: Animals; Antioxidants; Asteraceae; Citrus; Diabetes Mellitus; Glucosidases; Hypoglycemic Agents; Plant Extracts; Rats; Rats, Wistar

Natural product studies explore potential and interesting new compounds to discover innovative drugs.

Topics: Antioxidants; Benzothiazoles; Biphenyl Compounds; Chromatography, High Pressure Liquid; Diabetes Mellitus; Flavonoids; Glycoside Hydrolase Inhibitors; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Mass Spectrometry; Molecular Structure; Nigella sativa; Oleanolic Acid; Picrates; Plant Components, Aerial; Plant Extracts; Protein Tyrosine Phosphatases; Saponins; Sulfonic Acids; Triterpenes

Diabetes mellitus is one of the most common endocrinal disorders and medicinal plants continue to play an important role in the management of this disease. In this study,. Methanolic extract of

Topics: Amylases; Antioxidants; Benzothiazoles; Biphenyl Compounds; Diabetes Mellitus; Flavonoids; Hypoglycemic Agents; Phenols; Picrates; Plant Extracts; Rosa; Sulfonic Acids

To elevate the Cyclo-His-Pro (CHP) content in yeast, the yeast hydrolysate that was obtained from enzymatic hydrolysis was subjected to various treatments. Flavourzyme-treated hydrolysate showed the highest CHP content (674.0 μg/g) among the various proteases treatments. Ultrafiltration was selected as the best method for concentrating CHP in yeast hydrolysate, based on the yields and CHP contents. In addition, we evaluated the radical scavenge and glucose tolerance of yeast hydrolysate with a high content of CHP. Yeast hydrolysate showed intense scavenging abilities of both 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radicals. The IC(50) values of yeast hydrolysate on DPPH and ABTS radicals were 1.9 and 0.9 mg/mL, respectively. There were significant differences in glucose level between the diabetes-control and yeast hydrolysate group at 30, 60, 90, and 120 min after injection in a type 1 diabetes model (P < 0.01). Also, there were significant differences in blood glucose levels between the 2 groups at 30, 60, and 100 min after injection in the type 2 diabetes group (P < 0.05). Therefore, it is possible to use the yeast hydrolysate with high levels of CHP as an antioxidative and/or antidiabetic material for the preparation of functional foods.. This study tried to develop a material containing a high content of CHP using yeast for possible applications of this cyclic dipeptide in the therapy of metabolic disorders. The yeast hydrolysate prepared with Flavourzyme showed a high level of CHP. The hydrolysate with a high content of CHP showed high levels of radical scavenging activities and oral glucose tolerance activity. Therefore, it is possible to use the yeast hydrolysate with high levels of CHP as an antioxidative and/or antidiabetic material for the preparation of functional foods.

Topics: Animals; Antioxidants; Benzothiazoles; Biphenyl Compounds; Blood Glucose; Chemical Phenomena; Diabetes Mellitus; Dipeptides; Endopeptidases; Free Radical Scavengers; Glucose Tolerance Test; Hydrolysis; Hypoglycemic Agents; Insulin Resistance; Male; Mice; Mice, Inbred ICR; Peptides, Cyclic; Picrates; Protein Hydrolysates; Saccharomyces cerevisiae; Sulfonic Acids

The aim of the study was to analyse the relation between total antioxidant capacity and immunosuppressive therapies, renal function and hematocrit in kidney transplant patients. The study included 46 adult patients during the maintenance period (>1 year) following renal transplantation, treated with different combinations of immunosuppressive agents--most commonly with cyclosporine (n = 23) or tacrolimus (n = 15). The total antioxidant capacity (TAOC) of plasma was measured using Trolox-equivalent antioxidant capacity (TEAC) assay. Patients treated with cyclosporine had significantly greater TAOC compared with those treated with tacrolimus (1.16 +/- 0.46 mmol/L vs. 0.80 +/- 0.37 mmol/L, p = 0.018, respectively). There was a significantly negative correlation between TAOC and plasma creatinine (rs = -0.551, p = 0.033) and a positive correlation between TAOC and creatinine clearance or hematocrit in patients treated with tacrolimus but not with cyclosporine (r = 0.525, p = 0.045 or rs = 0.629, p = 0.012, respectively). Immunosuppressive therapy with cyclosporine was associated with higher TAOC. Anemia can be an independent risk factor for an increase of oxidative stress. Although subject numbers werelimited, TAOC was positively associated with renal function in patients treated with tacrolimus.

Topics: Adult; Aged; Antioxidants; Benzothiazoles; Calibration; Chromans; Creatinine; Cyclosporine; Diabetes Mellitus; Female; Hematocrit; Humans; Immunosuppressive Agents; Indicators and Reagents; Kidney Function Tests; Kidney Transplantation; Male; Middle Aged; Sulfonic Acids; Young Adult

We have developed a simple method for determination of 1,5-anhydro-D-glucitol in plasma, based on use of pyranose oxidase (EC 1.1.3.10), an enzyme with specificity toward pyranoid compounds such as 1,5-anhydro-D-glucitol and glucose. Plasma samples deproteinized with trichloroacetic acid are passed through a two-layer mini-column packed with strongly basic anion (OH- form, the upper layer) and strongly acidic cation (H+ form, the lower layer) exchange resins. 1,5-Anhydro-D-glucitol is efficiently recovered in the flow-through fraction, which is almost devoid of other sugars that are sensitive to pyranose oxidase. The hydrogen peroxide formed in the enzymatic oxidation of 1,5-anhydro-D-glucitol is detected by a standard method utilizing an enzymatic color-developing system. The overall assay system is highly specific for 1,5-anhydro-D-glucitol. The correlation between results obtained in the present method (x) and in the gas-liquid chromatographic (GLC) method (y) was: y = 1.062x-0.293 mg/L (r = 0.997, n = 49, Sxy = 10.78 mg/L). Compared with GLC, our method is simpler in the sample treatment step and quicker in the measuring step. The precisions of the two methods are comparable.

Topics: Benzothiazoles; Carbohydrate Dehydrogenases; Chromatography, Gas; Deoxy Sugars; Deoxyglucose; Diabetes Mellitus; Humans; Spectrophotometry; Sulfonic Acids