1-1-diphenyl-2-picrylhydrazyl and Diabetes-Mellitus

Oxidative stress is one of the significant precursors of various metabolic diseases such as diabetes, Parkinson's disease, cardiovascular diseases, cancer, etc. Various scientific reports have indicated that secondary plant metabolites play an important role in preventing oxidative stress and its harmful effects. In this respect, this study was planned to investigate the phenolic profile and antioxidant and antidiabetic potentials of the aqueous extracts from Turkish

Topics: alpha-Amylases; alpha-Glucosidases; Antioxidants; Biphenyl Compounds; Cistus; Diabetes Mellitus; Dose-Response Relationship, Drug; Glycation End Products, Advanced; Humans; Hypoglycemic Agents; Molecular Structure; Oxidative Stress; Phenols; Picrates; Plant Extracts; Structure-Activity Relationship; Turkey; Water

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

Plane tree (Platanus orientalis L.) leaves have been employed for centuries in various countries due to their pharmacological value. Therefore, determination of the biological activity of the leaves is of interest. The aim of the study was to evaluate the inhibitory effects against Alzheimer's disease-related enzymes Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE), diabetes mellitus related enzymes α-glucosidase and α-amylase. The antioxidant, anticancer, and antimicrobial activities of the leaves were also studied. According to the results, both water and methanol extracts of P. orientalis demonstrated more α-glucosidase and α-amylase inhibition activity than the antidiabetic drug-acarbose at the same concentration level. In addition, extracts showed good inhibition activity against AChE and BuChE. Significant results were obtained regarding antioxidant, anticancer, and antimicrobial activities. These results are very promising especially for the improvement of pharmaceutical formulations to treat various diseases such as age-related diseases, cancer, diabetes etc. and it is necessary to conduct further experiments.

Topics: Alzheimer Disease; Anti-Infective Agents; Antioxidants; Biphenyl Compounds; Cell Line, Tumor; Cell Proliferation; Diabetes Mellitus; Fluorescence Recovery After Photobleaching; Glycoside Hydrolase Inhibitors; Humans; Hypoglycemic Agents; Picrates; Plant Extracts; Plant Leaves

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

The steady increase of diabetes is becoming a major burden on health care systems. As diabetic complications arise from oxidative stress, an antioxidant therapy along with anti-diabetic drugs is recommended. Myrmecodia or ant plant is highly valued as a traditional medicine in West Papua. It is used as an alternative treatment for diabetes, as the substances produced by ants can reduce blood sugar levels. The aim of this study was to develop and establish high-performance thin-layer chromatographic (HPTLC)-bioautographic methods to measure the antioxidant and hypoglycemic effects in different extracts from Myrmecodia platytyrea and to compare them with sterol content. Antioxidant activity in methanol, ethanol, dichloromethane (DCM) and ethyl acetate (EA) extracts were measured with a direct HPTLC-2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) assay, while hypoglycemic effects were assessed using a newly developed α-amylase inhibitory activity assay. Stigmasterol is observed, after derivatization with anisaldehyde, as purple colored zones under visible light at hRF values of 0.66. The highest antioxidant activity was observed in the ethanol extract which is rich in polyphenols and flavonoids, while the DCM extract did not show antioxidant activity, but had significant α-amylase inhibitory activity. The highest α-amylase inhibitory activity was observed in the EA and DCM extracts and was related to their stigmasterol content.

Topics: alpha-Amylases; Antioxidants; Biphenyl Compounds; Chromatography, Thin Layer; Diabetes Mellitus; Flavonoids; Hypoglycemic Agents; Magnoliopsida; Oxidation-Reduction; Oxidative Stress; Picrates; Plant Extracts; Polyphenols; Sterols

Diabetes mellitus is normally characterized by chronic hyperglycemia associated with disturbances in the fat, carbohydrate, and protein metabolism. There is an increasing trend of using natural products instead of synthetic agents as alternative therapy for disorders due to their fewer side effects. In this study, antidiabetic and antioxidant activities of different Melicope lunu-ankenda (ML) ethanolic extracts were evaluated using inhibition of α-glucosidase and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radicals scavenging activity, respectively; whereas, proton nuclear magnetic resonance ((1) H NMR) and ultra-high performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) techniques were used for metabolite profiling of ML leaf extracts at different concentrations of ethanol and water. Sixty percent of ethanolic ML extract showed highest inhibitory effect against α-glucosidase enzyme (IC50 of 37 μg/mL) and DPPH scavenging activity (IC50 of 48 μg/mL). Antidiabetic effect of ML extracts was also evaluated in vivo and it was found that the high doses (400 mg/Kg BW) of ML extract exhibited high suppression in fasting blood glucose level by 62.75%. The metabolites responsible for variation among ML samples with variable ethanolic levels have been evaluated successfully using (1) H-NMR-based metabolomics. The principal component analysis (PCA) and partial least squares(PLS) analysis scores depicted clear and distinct separations into 4 clusters representing the 4 ethanolic concentrations by PC1 and PC2, with an eigenvalue of 69.9%. Various (1) H-NMR chemical shifts related to the metabolites responsible for sample difference were also ascribed. The main bioactive compounds identified attributing toward the separation included: isorhamnetin, skimmianine, scopoletin, and melicarpinone. Hence, ML may be used as promising medicinal plant for the development of new functional foods, new generation antidiabetic drugs, as a single entity phytomedicine or in combinational therapy.

Topics: alpha-Glucosidases; Animals; Antioxidants; Biphenyl Compounds; Diabetes Mellitus; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Male; Picrates; Plant Extracts; Plant Leaves; Rats, Sprague-Dawley; Rutaceae; Tandem Mass Spectrometry

The objective of the current study was to verify antidiabetic effects of different types of mushrooms as folk medicines in treating diabetes. The antidiabetic effects were evaluated by in vitro α-glycosidase and aldose reductase (AR) inhibitory assays and antioxidant activity assay. Ganoderma lucidum extract exhibited the best dose-dependent inhibitory activity against α-glycosidase with IC50 at 4.88 mg/mL, and also exhibited aldose reductase inhibitory potential with IC50 value of 9.87 mg/mL. Tremella fuciformis demonstrated the highest AR inhibitory activity (IC50=8.39 mg/mL). Antioxidant activities of selected mushrooms were evaluated based on the total phenolic content (TPC), total flavonoids content (TFC), and DPPH free radical scavenging activity. The result showed that G. lucidum contained the highest TPC (39.3 mg GAE/g sample extract), TFC (15.1 mg CE/g sample extract), and the strongest DPPH free radical scavenging activity (IC50=3.66 mg/mL) among the mushroom samples.

Topics: Agaricales; Aldehyde Reductase; alpha-Glucosidases; Animals; Antioxidants; Biological Products; Biphenyl Compounds; China; Diabetes Mellitus; Enzyme Inhibitors; Flavonoids; Fungi; Ganoderma; Grifola; Hypoglycemic Agents; Phenols; Phytotherapy; Picrates; Swine

Cirsium japonicum var. australe, used as a folk medicine in Taiwan, has been employed traditionally in the treatment of diabetes and inflammatory symptoms. Bioactivity-guided fractionation of its ethanolic extract, utilizing centrifugal partition chromatography monitored by DPPH-TLC analysis, led to the isolation of three new acetylenic phenylacrylic acid esters (1-3) and two new polyacetylenes (4 and 5), together with seven known compounds (6-12). The structures of 1-5 were elucidated by spectroscopic methods including 1D and 2D NMR techniques. The absolute configurations of 4 and 7 were determined utilizing Mosher's method and ECD/CD experiments. The DPPH scavenging activity of the constituents isolated from the C. japonicum var. australe ethanolic extract was evaluated. The potential antidiabetic activity of some of the isolates was evaluated using in vitro cellular glucose uptake and oil red staining assays.

Topics: Anti-Inflammatory Agents; Azo Compounds; Biphenyl Compounds; Cirsium; Diabetes Mellitus; Glucose; Medicine, Traditional; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Picrates; Polyynes; Taiwan

One of the therapeutic approaches in treating diabetes is to reduce postprandial hyperglycemia by inhibiting major carbohydrate hydrolyzing enzymes. In the present study, crude extracts of marine seaweed, Turbinaria ornata, were tested for their antidiabetic potential using enzyme inhibitory assays (α-amylase, α-glucosidase, and dipeptidyl peptidase-IV). Among the tested extracts, methanol and acetone extracts showed significant inhibitory effects on α-amylase (IC50 250.9 μg/mL), α-glucosidase (535.6 μg/mL), and dipeptidyl peptidase-4 (55.2 μg/mL), respectively. Free radical scavenging activity of these extracts was analyzed using DPPH assay (65%). Extracts were tested for in vitro toxicity using DNA fragmentation assay, haemolytic assay, and MTT assay. None of the extracts showed toxicity in tested models. Furthermore, GC-MS analysis of lead extracts showed the presence of major compounds, hentriacontane, z, z-6, 28-heptatriactontadien-2-one, 8-heptadecene, and 1-heptacosanol. Our findings suggest that Turbinaria ornata can be used as a potential source for further in vivo studies in controlling hyperglycemia.

Topics: alpha-Amylases; alpha-Glucosidases; Animals; Biphenyl Compounds; Cell Death; Cell Line; Cell Survival; Diabetes Mellitus; Dipeptidyl Peptidase 4; DNA Fragmentation; Enzyme Inhibitors; Free Radical Scavengers; Gas Chromatography-Mass Spectrometry; Hemolysis; Humans; Metabolic Networks and Pathways; Mice; Oligopeptides; Phytotherapy; Picrates; Plant Extracts; Seaweed

Ginger, the rhizome of Zingiber officinale Roscoe (Zingiberaceae), a perennial herbaceous plant is native to Southern Asia. Study was aimed to evaluate antioxidant and antidiabetic potential of ginger extract and its characterization. Possible mode of action to elicit antidiabetic activity was also evaluated.. Ethyl acetate extract of ginger (EAG) was evaluated for its antioxidant activity in terms of DPPH radical scavenging potential with an IC₅₀ value of 4.59 µg/ml. Antidiabetic activity of EAG was evaluated by estimating antiglycation potential (IC₅₀ 290.84 µg/ml). HPLC profiling of EAG revealed the presence of phenolic components, gingerol and shoagol as major constituents. After determining sub-toxic concentration of EAG (50 µg/ml), efficacy of extract to enhance glucose uptake in cell lines were checked in L6 mouse myoblast and myotubes. EAG was effective at 5 µg/ml concentration in both cases. Antibody based studies in treated cells revealed the effect of EAG in expressing Glut 4 in cell surface membrane compared to control.. The antidiabetic effect of ginger was experimentally proved in the study and has concluded that the activity is initiated by antioxidant, antiglycation and potential to express or transport Glut4 receptors from internal vesicles.

Topics: Adipocytes; Adipogenesis; Animals; Antioxidants; Biological Transport; Biphenyl Compounds; Catechols; Cell Membrane; Diabetes Mellitus; Fatty Alcohols; Glucose; Glucose Transporter Type 4; Glycation End Products, Advanced; Hypoglycemic Agents; Mice; Muscle Fibers, Skeletal; Myoblasts; Phytotherapy; Picrates; Plant Extracts; Proteins; Rhizome; Zingiber officinale

The matured fruits of Diospyros peregrina possess significant antidiabetic activity. The present investigation was undertaken to evaluate the target of action of the hydroalcoholic extract of D. peregrina fruit in diabetic pathophysiology. The extract was tested in vitro for inhibition of glucose absorption by α-amylase inhibition assay, glucose uptake study by isolated rat hemidiaphragm method and free radical scavenging activity by DPPH method. The extract exhibited significant α-amylase inhibition (IC₅₀ 136.5 µg mL⁻¹), peripheral glucose utilisation and radical scavenging (IC₅₀ 167.5 µg mL⁻¹) activity. From the results, it may be concluded that the hydroalcoholic extract of D. peregrina fruit can counteract diabetes by multiple mechanisms, namely inhibition of carbohydrate absorption, improving peripheral glucose utilisation and antioxidant defence.

Topics: alpha-Amylases; Animals; Biphenyl Compounds; Blood Glucose; Diabetes Mellitus; Diospyros; Free Radical Scavengers; Fruit; Glucose; Hypoglycemic Agents; Picrates; Plant Extracts; Rats

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 intent of this study was to purify and characterize a polysaccharide named LA from the fruiting bodies of the edible mushroom Pleurotus abalones.. The 120-kDa polysaccharide was obtained by extraction with boiling water, ethanol precipitation, ion exchange chromatography on Diethylaminoethyl-cellulose and gel filtration on Sephadex G-200.. The LA was composed of glucose, rhamnose, glucuronic acid, xylose, galactose and arabinose in the molar ratio of 26.3:2.7:1:1.4:1.8:1.2. The FITR and 1H-NMR spectrum of LA disclosed that it was a saccharide with an α-configuration. Its 13C-NMR spectrum revealed that its main chain was [→6)-α-D-Gly(1→]n. The LA exhibited antioxidant activities, especially in scavenging 1,1- diphenyl-2-picryl-hydrazyl radicals and hydroxyl radicals. It manifested antiproliferative activity towards breast cancer MCF7 cells with an IC50 of 3.7 µm, and also exerted some antiproliferative activity against HepG2 cells. It manifested a hypoglycemic action on diabetic mice. It inhibited HIV-1 reverse transcriptase with an IC50 of 8.7 × 10(-2) µm.. The polysaccharide from the abalone mushroom.

Topics: Antineoplastic Agents; Antioxidants; Biological Products; Biphenyl Compounds; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Diabetes Mellitus; Female; Fruiting Bodies, Fungal; Hep G2 Cells; HIV Reverse Transcriptase; Humans; Hydroxyl Radical; Hyperglycemia; Hypoglycemic Agents; Inhibitory Concentration 50; Liver Neoplasms; Phytotherapy; Picrates; Pleurotus; Polysaccharides; Reverse Transcriptase Inhibitors

The antioxidant properties of diabenol and gliclazide with reference to mexidol have been studied in vitro on several model systems, including chemiluminescence (CL) of lipids, CL with generation of reactive oxygen species (ROS), CL dependent on luminol oxidation by peroxy radicals, and the Glavind DPPH free-radical method. Diabenol exhibited the properties of a scavenger of superoxide anions and hydroxy and peroxy radicals in model CL systems with ROS generation. The activity of diabenol in inactivating ROS was about 8 times higher compared to mexidol. However, the antioxidant activity of diabenol in CL with peroxy radical generation was 3 times lower compared to mexidol. Gliclazide demonstrated dose-dependent antioxidant activity only on the model with stable DPPH radicals, where its inhibitory effect was 15 times greater than that of the reference drug.

Topics: Benzimidazoles; Biphenyl Compounds; Diabetes Mellitus; Free Radical Scavengers; Free Radicals; Gliclazide; Humans; Hypoglycemic Agents; Lipid Peroxidation; Luminescence; Luminol; Oxidation-Reduction; Peroxides; Picolines; Picrates; Solutions; Superoxides

Eleven antidiabetic traditional Chinese medicine (TCM) extracts rich in saponins were examined for their antioxidant and antiglycation activities. The antioxidant activities of these extracts were evaluated by studying the inhibition of lipid peroxidation in rat liver microsomes induced by ascorbate/Fe2+, cumine hydroperoxide (CHP) or CCl4/reduced form of nicotinamide-adenine dinucleotide phosphate (NADPH). The antioxidant capacities were also evaluated by studying the scavenging of 2,2'-diphenyl-1-picrylhydrazyl (DPPH) free radical. The antiglycation activities of these extracts were evaluated by hemoglobin-delta-gluconolactone (delta-Glu) assay, bovine serum albumin (BSA)-glucose assay and N-acetyl-glycyl-lysine methyl ester (GK peptide)-ribose assay. Aralia taibaiensis outperformed other extracts in most of the assays except inhibition of early glycation products formation, where Acanthopanax senticosus showed higher activity. Aralia taibaiensis was particularly potent in inhibiting the late glycation and formation of advanced glycation end products (AGEs) on proteins. The antioxidant and antiglycation activities of most extracts were correlated with the saponin content. The results demonstrate that the antidiabetic activities of most extracts could be explained, at least in part, by their combined antioxidant and antiglycation properties.

Topics: Animals; Antioxidants; Ascorbic Acid; Biphenyl Compounds; Diabetes Mellitus; Drugs, Chinese Herbal; Free Radical Scavengers; Hydrazines; Lipid Peroxidation; Microsomes, Liver; Nitrosamines; Oxidation-Reduction; Picrates; Rats; Rats, Sprague-Dawley; Saponins

Selection, collection and preparation of 35 plant species used by traditional healers in the boreal regions of Canada for treatment of the symptoms of diabetes were supported empirically by antioxidant activity of the plants. Because antioxidants fluctuate with growth parameters and environmental factors, these remedies were evaluated in relation to the affect of plant part, life form and growing condition on the level of activity. The parts used here more frequently as medicines were roots and bark. Activity (IC(50)) of the bark extracts used medicinally averaged to 21.38+/-3.84 ppm while root extracts used medicinally had an IC(50) of 185.11+/-32.18 ppm in a free radical DPPH assay. In contrast the analysis of extracts of overall parts (medicinal or not) in these species found leaves and bark to have the least activity (112.22+/-30.63 ppm and 123.02+/-21.13 ppm, respectively). The highest activity was found in tree extracts (24.88+/-3.32 ppm) as compared to herbs and shrubs, and increased activity was found in plant extracts from growing conditions of decreased water/fertility. The antioxidant activity of these traditional plant remedies have the potential to be partially deduced through environment signals interpreted by the traditional herbalist.

Topics: Antioxidants; Biphenyl Compounds; Canada; Diabetes Mellitus; Ecosystem; Flowers; Free Radical Scavengers; Fruit; Humans; Hypoglycemic Agents; Picrates; Plant Bark; Plant Extracts; Plant Leaves; Plant Roots; Plants, Medicinal

Hydnocarpus wightiana is advocated in traditional Indian medicine to possess strong antidiabetic activity. In the course of identifying bioactive fractions from Indian medicinal plants we observed that acetone extract of the seed hulls of H. wightiana possess strong free radicals (DPPH and ABTS) scavenging, alpha-glucosidase and moderate N-acetyl-beta-D-glucosaminidase inhibitory activities. Further fractionation of the extract led to the isolation of hydnocarpin, luteolin and isohydnocarpin in substantial yields. All the compounds showed strong ABTS scavenging property. However, only luteolin could display strong DPPH scavenging activity. Furthermore, all the three compounds also showed varying degrees of alpha-glucosidase and N-acetyl-beta-D-glucosaminidase inhibitory activity, luteolin being the superior. The kinetics of alpha-glucosidase inhibition by these compounds showed that acetone extract inhibits the enzyme in competitive manner however, luteolin and isohydnocarpin showed mixed-type inhibition. This is the first report assigning hydnocarpin and isohydnocarpin free radical scavenging, alpha-glucosidase and N-acetyl-beta-D-glucosaminidase inhibitory properties and luteolin as N-acetyl-beta-D-glucosaminidase inhibitor. This study suggests that presence of amphiphilic antioxidant molecules along with enzyme inhibitory activities in the acetone extract of H. wightiana seed hulls may be responsible for the antidiabetic properties as advocated in traditional medicine.

Topics: Biphenyl Compounds; Diabetes Mellitus; Enzyme Inhibitors; Free Radical Scavengers; Glycoside Hydrolase Inhibitors; Humans; Hypoglycemic Agents; Malpighiaceae; Medicine, Ayurvedic; Phytotherapy; Picrates; Plant Extracts; Seeds; Sulfonic Acids