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

Some foods and drinks contain special ingredients, causing impressive effects on human health. The aim of the current study was to assess the health effects of apple vinegar in patients with diabetes and dyslipidemia.. Seventy participants with type 2 diabetes and hyperlipidemia were randomly assigned into an intervention and control group in order to assess the effect of 20 ml apple vinegar per day using an 8-week parallel study. Fasting blood sugar (FBS), homeostasis model assessment for insulin resistance (HOMA-IR), homeostasis model assessment for b-cell function (HOMA-B), quantitative insulin sensitivity checks index (QUICKI), insulin, malondialdehyde (MDA), 2,20-Diphenyl-1- picrylhydrazyl (DPPH), homocysteine, systolic blood pressure (SBP), and diastolic blood pressure (DBP) were measured at the beginning and end of the study.. The intervention with apple vinegar could significantly improve FBS (mean change: -10.16 ± 19.48 mg/dl, p = 0.006) and DPPH (mean change: 16.58 ± 11.56, p < 0.001) within intervention group and in comparison with control group (p < 0.001). Additionally, the significant increase of MDA in control group (p < 0.05) caused a considerable difference between two groups. Glycemic indices containing insulin, HOMA-IR, HOMA-B, and QUICKI decrease significantly in both groups (p < 0.05). No considerable effect was observed on blood pressure and homocysteine in intervention group as well as control group.. This trial provided some evidences that apple vinegar consumption may cause beneficial effects on glycemic indices and oxidative stress in individuals with diabetes and dyslipidemia. This randomized clinical trial was registered in the Iranian Registry of Clinical Trials (https://www.irct.ir/) as 2013070710826N5.

Topics: Acetic Acid; Adult; Biphenyl Compounds; Blood Glucose; Blood Pressure; Diabetes Mellitus, Type 2; Dyslipidemias; Female; Glycemic Index; Homeostasis; Homocysteine; Humans; Insulin; Insulin Resistance; Iran; Male; Malondialdehyde; Malus; Middle Aged; Oxidative Stress; Picrates

Type 2 Diabetes mellitus is a chronic disease considered one of the most severe global health emergencies. Chlorogenic acid (1) has been shown to delay intestinal glucose absorption by inhibiting the activity of α-glucosidase (α-Glu) and α-amylase (α-Amy). In the present work, eleven chlorogenic acid amides have been synthesized and evaluated for their antioxidant properties (as DPPH and ORAC) and inhibition activity towards the two enzymes and, with the aim to obtain dual-action antidiabetic agents. The two most promising hypoglycemic compounds, bearing a tertiary amine function on an alkyl chain (8) and a benzothiazole scaffold (11), showed IC

Topics: Acarbose; alpha-Amylases; alpha-Glucosidases; Amides; Animals; Antioxidants; Biphenyl Compounds; Chlorogenic Acid; Diabetes Mellitus, Type 2; Dose-Response Relationship, Drug; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Molecular Docking Simulation; Molecular Structure; Pancreas; Picrates; Saccharomyces cerevisiae; Structure-Activity Relationship; Swine

Dysregulation of glucose homeostasis followed by chronic hyperglycemia is a hallmark of diabetes mellitus (DM), a disease spreading as a worldwide pandemic for which there is no satisfactory dietary treatment or cure. The development of glucose-controlling drugs that can prevent complications of DM, such as hyperglycemia and oxidative stress, which contribute to the impairment of the key physiological processes in the body, is of grave importance. In pursuit of this goal, this study screened 41 plant extracts for their antidiabetic and antioxidant activities by employing assays to test for α-amylase inhibition and free radical scavenging activity (FRSA) and by measuring glucose uptake in L6-GLUT4myc cells. While extracts of Rhus coriaria, Punica granatum, Olea europaea, Pelargonium spp., Stevia rebaudiana, and Petroselinum crispum demonstrated significant α-amylase inhibition, the extracts of Rhus coriaria and Pelargonium spp. also demonstrated increased FRSA, and the extract of Rhus coriaria stimulated glucose uptake. These natural extracts, which are believed to have fewer side effects because they are prepared from edible plants, interfere with the process in the small intestine that breaks down dietary carbohydrates into monosaccharide and disaccharide derivatives, and thereby suppress increases in diet-induced blood glucose; hence, they may have clinical value for type 2 diabetes management. The Pelargonium spp. and Rhus coriaria extracts demonstrated the highest antidiabetic and antioxidant activities. Both plants may offer valuable medical benefits, especially because they can be taken as dietary supplements by patients with diabetes and can serve as sources of new, natural-based antidiabetic drug candidates. The enhancement of cellular glucose uptake stimulated by Rhus coriaria extract could lead to the development of clinical applications that regulate blood glucose levels from within the circulatory system. Isolating bioactive substances from these plant extracts and testing them in diabetic mice will significantly advance the development of natural drugs that have both antidiabetic and free radical-scavenging properties, likely with lesser side effects.

Topics: alpha-Amylases; Animals; Antioxidants; Biphenyl Compounds; Cell Survival; Cells, Cultured; Diabetes Mellitus, Experimental; Diabetes Mellitus, Type 2; Drug Evaluation, Preclinical; Enzyme Inhibitors; Humans; Hypoglycemic Agents; Mice; Pelargonium; Picrates; Plant Extracts; Rhus

We report here a new class of compounds, quinoline derivatives, as potential inhibitors of in vitro bovine serum albumin-methylglyoxal glycation. Among compounds 1-19, compound 14 was found to be the most active analog with IC₅₀ of 282.98 ± 8.4 µM. Compounds 12 (IC₅₀ = 661.78 ± 8.7 µM) and 15 (IC₅₀ = 629.43 ± 7.85 7 µM) were also identified as modest inhibitors, in comparison to the standard inhibitor, rutin (IC₅₀ = 294.50 ± 1.5 µM). When evaluated for antioxidant activity through in vitro DPPH radical scavenging assay, compounds 3 (IC₅₀ = 2.19 ± 0.27 µM), 6 (IC₅₀ = 7.35 ± 2.27 µM), 11 (IC₅₀ = 8.96 ± 0.56 µM), and 12 (IC₅₀ = 10.11 ± 2.03 µM), and 15 (IC₅₀ = 7.01 ± 3.87 µM) were found to be more active than the standard i.e. gallic acid (IC₅₀ = 23.34 ± 0.43 µM). These compounds were also evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line). All compounds were found to be non-toxic in cellular model. This study identifies quinoline derivatives as a new class of inhibitors of protein glycation in vitro, along with antioxidant and non-toxic nature. These properties make them interesting leads for further studies as potential anti-diabetic agents.

Topics: Animals; Antioxidants; Biphenyl Compounds; Cattle; Diabetes Mellitus, Type 2; Glycation End Products, Advanced; Glycosylation; Guanidines; Hypoglycemic Agents; Mice; NIH 3T3 Cells; Picrates; Pyruvaldehyde; Quinolines; Reactive Oxygen Species; Rutin; Schiff Bases; Serum Albumin, Bovine; Structure-Activity Relationship

Recent studies have shown that vegetables consumption could lower the risk of diabetes mellitus. Therefore, this study sought to investigate the inhibitory effect of Struchium sparganophora (Ewuro Odo) leaf on key enzyme linked to type-2 diabetes (α-amylase and α-glucosidase) as well as assessing the effect of blanching (a commonly practiced food processing technique) of this leafy vegetable on these key enzymes. Fresh leaves of Struchium sparganophora were blanched in hot water for 10 minutes, and the 70% ethanolic extracts of the fresh and blanched vegetables were prepared and used for subsequent analysis. The antioxidant properties and interaction of the extracts on α - amylase and α - glucosidase activities was determined in vitro. The result revealed that Struchium sparganophora leaf scavenged DPPH free radical and also inhibited α -amylase and α - glucosidase activities in a dose dependent manner (0.05 -0.2 mg/ml). However, blanching of this leafy vegetables caused a significant (P<0.05) increase in the antioxidant properties as typified by the DPPH radical scavenging ability and reducing property but decrease their ability to inhibit α - amylase and α - glucosidase activities. This antioxidant properties and enzyme inhibition could be part of the mechanism by which green leafy vegetables exert their anti-diabetic properties. However, blanching of the vegetable could reduce their ability to inhibit both α - amylase and α - glucosidase activity, but enhance their antioxidant properties in vitro.

Topics: alpha-Amylases; alpha-Glucosidases; Antioxidants; Asteraceae; Biphenyl Compounds; Cooking; Diabetes Mellitus, Type 2; Dose-Response Relationship, Drug; Enzyme Inhibitors; Hypoglycemic Agents; Picrates; Plant Leaves

Seven different wild legume seeds (Acacia leucophloea, Bauhinia variegata, Canavalia gladiata, Entada scandens, Mucuna pruriens, Sesbania bispinosa and Tamarindus indica) from various parts of India were analyzed for total free phenolics, l-Dopa (l-3,4 dihydroxyphenylalanine), phytic acid and their antioxidant capacity (ferric-reducing antioxidant power [FRAP] and 2,2-diphenyl-1-picrylhydrazyl [DPPH] assay) and type II diabetes-related enzyme inhibition activitiy (α-amylase). S. bispinosa had the highest content in both total free phenolics and l-Dopa, and relatively low phytic acid when compared with other seeds. Phytic acid content, being highest in E. scandens, M. pruriens and T. indica, was highly predictive for FRAP (r = 0.47, p < 0.05) and DPPH (r = 0.66, p < 0.001) assays. The phenolic extract from T. indica and l-Dopa extract from E. scandens showed significantly higher FRAP values among others. All seed extracts demonstrated a remarkable reducing power (7-145 mM FeSO4 per mg extract), DPPH radical scavenging activity (16-95%) and α-amylase enzyme inhibition activity (28-40%).

Topics: alpha-Amylases; Antioxidants; Biphenyl Compounds; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Fabaceae; India; Levodopa; Phenols; Phytic Acid; Phytotherapy; Picrates; Seeds

Traditional Indian and Australian medicinal plant extracts were investigated to determine their therapeutic potential to inhibit key enzymes in carbohydrate metabolism, which has relevance to the management of hyperglycemia and type 2 diabetes. The antioxidant activities were also assessed.. The evaluation of enzyme inhibitory activity of seven Australian aboriginal medicinal plants and five Indian Ayurvedic plants was carried out against α-amylase and α-glucosidase. Antioxidant activity was determined by measuring (i) the scavenging effect of plant extracts against 2, 2-diphenyl-1-picryl hydrazyl (DPPH) and 2, 2'-azinobis-3-ethylbenzothiazoline-6-sulfonate (ABTS) and (ii) ferric reducing power. Total phenolic and total flavonoid contents were also determined.. Of the twelve plant extracts evaluated, the highest inhibitory activity against both α-amylase and α-glucosidase enzymes was exerted by Santalum spicatum and Pterocarpus marsupium with IC50 values of 5.43 μg/ml and 0.9 μg/ml, respectively, and 5.16 μg/ml and 1.06 μg/ml, respectively. However, the extracts of Acacia ligulata (IC50 = 1.01 μg/ml), Beyeria leshnaultii (0.39 μg/ml), Mucuna pruriens (0.8 μg/ml) and Boerhaavia diffusa (1.72 μg/ml) exhibited considerable activity against α-glucosidase enzyme only. The free radical scavenging activity was found to be prominent in extracts of Acacia kempeana, Acacia ligulata followed by Euphorbia drummondii against both DPPH and ABTS. The reducing power was more pronounced in Euphorbia drummondii and Pterocarpus marsupium extracts. The phenolic and flavonoid contents ranged from 0.42 to 30.27 μg/mg equivalent of gallic acid and 0.51 to 32.94 μg/mg equivalent of quercetin, respectively, in all plant extracts. Pearson's correlation coefficient between total flavonoids and total phenolics was 0.796.. The results obtained in this study showed that most of the plant extracts have good potential for the management of hyperglycemia, diabetes and the related condition of oxidative stress.

Topics: alpha-Amylases; Antioxidants; Australia; Benzothiazoles; Biphenyl Compounds; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Ferric Compounds; Flavonoids; Glycoside Hydrolase Inhibitors; Hyperglycemia; India; Magnoliopsida; Medicine, Ayurvedic; Oxidative Stress; Phenols; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Sulfonic Acids; Thiazoles

In this study, the total phenolic and flavonoid contents, the 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging ability and the ferric reducing power (FRAP) of Aloe vera were measured to determine the antioxidant activity of this species. The in vivo antidiabetic effects of the plant were also investigated using streptozotocin-induced type 2 diabetic model rats that were divided into five groups based on the treatment received: (1) water (WC); (2) glibenclamide; (3) concentrated gel extract (Gel-C); (4) ethanol (80%) gel extract (Gel-Et); and (5) ethanol (80%) skin extract of Aloe vera (Skin-Et). Skin-Et, which contained the highest level of total phenolics (62.37 ± 1.34 mg(gallic acid)/kg) and flavonoids (20.83 ± 0.77 mg/kg), exhibited the highest scavenging activity (85.01 ± 0.52%) and the greatest reducing power (185.98 ± 0.41 µM), indicating that the skin contained the highest level of antioxidants. The oral consumption of Gel-Et for 4 weeks a caused significant reduction in the fasting serum glucose levels of the rats. The rats in the Gel-C-, Gel-Et- and Skin-Et-treated groups experienced a reduction in their total cholesterol levels by 11%, 17% and 25%, respectively and a reduction in their LDL cholesterol levels by 45%, 3% and 69%, respectively. The in vivo experimental antioxidant parameter MDA is strongly correlated with the in vitro antioxidant parameters of flavonoids and polyphenols, namely the DPPH and FRAP values (r = 0.94, 0.92, 0.93, 0.90), thus confirming the antioxidant potential of the Aloe vera extracts.

Topics: Aloe; Animals; Biphenyl Compounds; Blood Glucose; Cholesterol; Diabetes Mellitus, Experimental; Diabetes Mellitus, Type 2; Erythrocytes; Female; Free Radical Scavengers; Free Radicals; Hypoglycemic Agents; Hypolipidemic Agents; Insulin; Lipoproteins, HDL; Lipoproteins, LDL; Malondialdehyde; Picrates; Plant Extracts; Plant Leaves; Rats; Rats, Long-Evans; Streptozocin; Triglycerides

Type 2 diabetes is a chronic metabolic disease, and the current treatment for type 2 diabetes targets oxidative stress and postprandial hyperglycemia via the inhibition of α-glucosidase and α-amylase, key enzymes linked to type 2 diabetes. In the present study, two varieties of sprouted and non-sprouted Bengal gram (white coated and brown coated) extracts were assayed for total phenolic content, DPPH radical scavenging activity, total antioxidative capability and the inhibition of α-glucosidase and α-amylase activity. Sprouting increased the total phenolic content in both the varieties of Bengal gram and exhibited significant DPPH radical scavenging activity and antioxidant capability compared with that of non-sprouted Bengal gram. Sprouting also increased the inhibitory potential of Bengal gram against α-glucosidase and α-amylase compared with the non-sprouted variety. The overall results suggest that increased antioxidant and inhibitory potential of sprouted Bengal gram against α-glucosidase and α-amylase makes them desirable for dietary management/prevention of diabetes. This finding also provides essential information for the development of sprouted Bengal gram-derived antidiabetic products.

Topics: alpha-Amylases; Antioxidants; Biphenyl Compounds; Cicer; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Germination; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Phenols; Phytotherapy; Picrates; Plant Extracts; Seeds

The present study evaluated the flavonoid content, antioxidant as well as type II diabetes-related enzyme inhibition activities of ethanolic extract of certain raw and traditionally processed indigenous food ingredients including cereals, legumes, oil seeds, tubers, vegetables and leafy vegetables, which are commonly consumed by vulnerable groups in Kenya. The vegetables exhibited higher flavonoid content (50-703 mg/100 g) when compared with the grains (47-343 mg/100 g). The ethanolic extract of presently studied food ingredients revealed 33-93% DPPH radical scavenging capacity, 486-6,389 mmol Fe(II)/g reducing power, 19-43% α-amylase inhibition activity and 14-68% α-glucosidase inhibition activity. Among the different food-stuffs, the drumstick and amaranth leaves exhibited significantly higher flavonoid content with excellent functional properties. Roasting of grains and cooking of vegetables were found to be suitable processing methods in preserving the functional properties. Hence, such viable processing techniques for respective food samples will be considered in the formulation of functional supplementary foods for vulnerable groups in Kenya.

Topics: Antioxidants; Biphenyl Compounds; Child, Preschool; Cooking; Diabetes Mellitus, Type 2; Edible Grain; Ethanol; Female; Flavonoids; Food Analysis; Glycoside Hydrolase Inhibitors; HIV Infections; Humans; Infant; Lactation; Malnutrition; Oxidation-Reduction; Picrates; Plant Oils; Pregnancy; Refugees; Seeds; Vegetables; Vulnerable Populations

Local food diversity and traditional crops are essential for cost-effective management of the global epidemic of type 2 diabetes and associated complications of hypertension. Water and 12% ethanol extracts of native Peruvian fruits such as Lucuma (Pouteria lucuma), Pacae (Inga feuille), Papayita arequipeña (Carica pubescens), Capuli (Prunus capuli), Aguaymanto (Physalis peruviana), and Algarrobo (Prosopis pallida) were evaluated for total phenolics, antioxidant activity based on 2, 2-diphenyl-1-picrylhydrazyl radical scavenging assay, and functionality such as in vitro inhibition of alpha-amylase, alpha-glucosidase, and angiotensin I-converting enzyme (ACE) relevant for potential management of hyperglycemia and hypertension linked to type 2 diabetes. The total phenolic content ranged from 3.2 (Aguaymanto) to 11.4 (Lucuma fruit) mg/g of sample dry weight. A significant positive correlation was found between total phenolic content and antioxidant activity for the ethanolic extracts. No phenolic compound was detected in Lucuma (fruit and powder) and Pacae. Aqueous extracts from Lucuma and Algarrobo had the highest alpha-glucosidase inhibitory activities. Papayita arequipeña and Algarrobo had significant ACE inhibitory activities reflecting antihypertensive potential. These in vitro results point to the excellent potential of Peruvian fruits for food-based strategies for complementing effective antidiabetes and antihypertension solutions based on further animal and clinical studies.

Topics: Angiotensin-Converting Enzyme Inhibitors; Antihypertensive Agents; Antioxidants; Biphenyl Compounds; Diabetes Mellitus, Type 2; Free Radical Scavengers; Fruit; Glycoside Hydrolase Inhibitors; Hypoglycemic Agents; Indicators and Reagents; Magnoliopsida; Medicine, Traditional; Peru; Phenols; Picrates; Plant Extracts; Plants, Medicinal

In the current study, we investigated 2 species of the genus Rhodiola for the inhibition of alpha-amylase,alpha-glucosidase and angiotensin converting enzyme (ACE) inhibitory activity. Water extracts of Rhodiola crenulata had the highest alpha-amylase inhibitory activity (IC50,98.1 microg total phenolic /ml) followed by ethanol extract of R.crenulata (IC50, 120.9 microg total phenolic/ml) and ethanol extract of R.rosea (IC50, 173.4 microg total phenolic /ml). Ethanol R.rosea (IC50, 44.7 microg total phenolic/ml), water extract of R.rosea (IC50, 52.3 microg total phenolic/ml), water extract of R.crenulata (IC50, 60.3 microg total phenolic /ml) and ethanol extract of R.crenulata (IC50, 60.2 microg total phenolic/ml) also showed significant alpha-glucosidase inhibitory activity. The alpha-glucosidase inhibitory activity of the extracts was compared to standard tyrosol, which was significantly detected in the extracts using HPLC. Tyrosol had strong alpha-glucosidase inhibitory activity (IC50, 70.8 microg total phenolic/ml) but did not have any inhibitory effect on the alpha-amylase activity. Results suggested that alpha-glucosidase inhibitory activities of both Rhodiola extracts correlated to the phenolic content, antioxidant activity and phenolic profile of the extracts. The ability of the above Rhodiola extracts to inhibit rabbit lung angiotensin I-converting enzyme (ACE) was investigated. The ethanol extracts of R.rosea had the highest ACE inhibitory activity (38.5 %) followed by water extract of R.rosea (36.2 %) and R.crenulata (15.4 %).

Topics: alpha-Amylases; Angiotensin-Converting Enzyme Inhibitors; Antioxidants; Biphenyl Compounds; Chromatography, High Pressure Liquid; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Ethanol; Glycoside Hydrolase Inhibitors; Hypertension; Phenols; Phenylethyl Alcohol; Picrates; Plant Extracts; Rhodiola; Water

Water soluble cranberry-based phytochemical combinations with oregano, rosemary, and Rhodiola rosea were evaluated for total phenolic content, related antioxidant activity and inhibition of diabetes management-related alpha -glucosidase, pancreatic alpha-amylase inhibition, and hypertension-related ACE-I inhibitory activities. Water extracts of oregano had 114.9 mg/g DW of phenolics which was highest among all the extracts tested, whereas the 75% cranberry with 25% oregano combinations had the highest phenolics (38.9 mg/g DW) among all the combinations tested. The water extracts of oregano had the highest DPPH radical inhibition activity (73.6 %), whereas among combinations the 75% cranberry and 25% oregano had the highest DPPH radical inhibition activity (50.8 %). These results indicated a correlation between total phenolic content and antioxidant activity. The water extracts of pure Rhodiola rosea had the highest alpha -glucosidase inhibition, whereas the 75% cranberry and 25% Rhodiola rosea combination had the highest inhibition among the combinations. In the case of alpha -amylase inhibition the water extracts of Rhodiola rosea had the highest inhibition, whereas the 75% cranberry with 25% Rhodiola rosea combination had the highest inhibition among the combinations. All the water extracts tested indicated that they had anti-ACE-I inhibitory activity. More specifically, among the water extracts 100% cranberry had the highest ACE-I inhibitory activity and among the combination the 75% cranberry with 25% rosemary had the highest ACE-I inhibitory activity. The analysis of alpha -glucosidase,alpha -amylase, and ACE-I inhibitory activities suggested that inhibition depend on the phenolic profile of each unique extract and by bringing together synergistic combinations to cranberry, health beneficial functionality was enhanced. This enhanced functionality in terms of high alpha -glucosidase and alpha -amylase inhibitory activities indicate the potential for diabetes management, and high ACE-I inhibitory activity indicates the potential for hypertension management.

Topics: alpha-Amylases; Angiotensin-Converting Enzyme Inhibitors; Antioxidants; Biphenyl Compounds; Diabetes Mellitus, Type 2; Enzyme Inhibitors; Fruit; Glycoside Hydrolase Inhibitors; Humans; Hypertension; Origanum; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Preparations; Rhodiola; Rosmarinus; Vaccinium macrocarpon; Water