Kinetics of inhibitory effect of ethyl acetate leaf fraction of Lecaniodiscus cupanoides on enzymes linked to carbohydrate metabolism: An in vitro assessment

Background and aims: This study investigates the kinetics of inhibitory activities of ethyl acetate leaf fraction of Lecanodiscus cupanoides o

Therapeutic potentials of black tea medicaments

Tea; a product of Camellia Sinensis plant is the most broadly used beverage in the world. Tea phytochemicals have been studied for the prevention of various chronic diseases, such as cancer, obesity, diabetes, jaundice, hypertension and inflammation related disorders. Whereas many studies have revealed the potential efficiency of tea for the prevention of these physiological disorders, the underlying mechanisms remain unclear. In this work, we evaluated the evidence and discussed the significance of proposed mechanisms for the prevention of the diseases such as Alzheimer’s, obesity, diabetes mellitus type II, hypertension and asthma by tea. Molecular docking method was used to explore the ability of tea phytochemicals to inhibit the key enzymes. The three dimensional structure of target enzymes were either retrieved from protein data bank or modelled using swiss model. Autodock4.2 software was used for molecular docking that applies Lamarckian Genetic Algorithm. The ligand structures were retrieved from PubChem and KNApSAcK-3D database. PreADMET web server was used for Toxicity and ADME predictions. Based on this analysis, it has been found that theaflavin, rutin and 8-c-ascorbyl epigallocatechin could be the potential lead molecules as they act as inhibitor for most of the target enzymes and has a good drug score and also qualifies the toxicity and ADME test. Further the tea extract is loaded in liposomal drug delivery system and pectin-HEMA hydrogel system to analyse their drug delivery potential and it was found that liposomal system is best suitable for delivery to brain and hydrogel system better serve as colon specific delivery system. We concluded that these phytochemicals or their derivatives can be used for further in-vitro and in-vivo studies to produce valuable lead drug candidates

Traditional Medicinal Herbs and Food Plants Have the Potential to Inhibit Key Carbohydrate Hydrolyzing Enzymes In Vitro and Reduce Postprandial Blood Glucose Peaks In Vivo

We hypothesized that some medicinal herbs and food plants commonly used in the management of diabetes can reduce glucose peaks by inhibiting key carbohydrate hydrolyzing enzymes. To this effect, extracts of Antidesma madagascariense (AM), Erythroxylum macrocarpum (EM), Pittosporum senacia (PS), and Faujasiopsis flexuosa (FF), Momordica charantia (MC), and Ocimum tenuiflorum (OT) were evaluated for α-amylase and α-glucosidase inhibitory effects based on starch-iodine colour changes and PNP-G as substrate, respectively. Only FF and AM extracts/fractions were found to inhibit α-amylase activity significantly (P < 0.05) and coparable to the drug acarbose. Amylase bioassay on isolated mouse plasma confirmed the inhibitory potential of AM and FF extracts with the ethyl acetate fraction of FF being more potent (P < 0.05) than acarbose. Extracts/fractions of AM and MC were found to inhibit significantly (P < 0.05) α-glucosidase activity, with IC50 comparable to the drug 1-deoxynojirimycin. In vivo studies on glycogen-loaded mice showed significant (P < 0.05) depressive effect on elevation of postprandial blood glucose following ingestion of AM and MC extracts. Our findings tend to provide a possible explanation for the hypoglycemic action of MC fruits and AM leaf extracts as alternative nutritional therapy in the management of diabetes

The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents

Obesity is a global epidemic associated with significant morbidity and mortality in adults and ill health in children. A proven successful approach in weight management has been the disruption of nutrient digestion, with orlistat having been used to treat obesity for the last 10 years. Although orlistat-induced weight loss remains modest, it produces meaningful reductions in risk factors for obesity-related conditions such as diabetes and cardiovascular disease. Moreover, this lipase inhibitor is free of the serious side effects that have dogged appetite-suppressing drugs. This success had driven investigation into new generation nutraceuticals, supplements and pharmaceutical agents that inhibit the breakdown of complex carbohydrates and fats within the gut. This review focuses on agents purported to inhibit intestinal enzymes responsible for macronutrient digestion. Except for some synthetic products, the majority of agents reviewed are either botanical extracts or bacterial products. Currently, carbohydrate digestion inhibitors are under development to improve glycemic control and these may also induce some weight loss. However, colonic fermentation induced side effects, such as excess gas production, remain an issue for these compounds. The α-glucosidase inhibitor acarbose, and the α-amylase inhibitor phaseolamine, have been used in humans with some promising results relating to weight loss. Nonetheless, few of these agents have made it into clinical studies and without any clinical proof of concept or proven efficacy it is unlikely any will enter the market soon

The effect of commercial starch blockers on starch hydrolysis in vitro

This study investigated the effects of a commercial starch blocker product, a legume a-amylase inhibitor, on amylase activity utilizing starch solutions of amylose, amylopectin, potato, corn, waxy corn, and wheat. The starch blockers were assayed for their inhibitory properties using the 3,5-dinitrosalicylic (DNS) acid reducing method and the iodine-starch test. Both of these protocols utilize colorimetric absorbance principles to indicate the a-amylase activity in vitro. The DNS method measured the amount of reducing ends generated as a result of amylase activity whereas the iodine-starch test measured the amount of starch present in the solution. The data were analyzed using a two-way analysis of variance. From these data, no significant difference (p&gt;0.05) was found in amylase activity using various starches in the presence or absence of the starch blocker products. There was also no significant difference (p&gt;0.05) between the different starch blockers in their ability to inhibit a-amylase activity. From these results, it can be concluded that the tested commercial starch blocker formulations did not inhibit the activity of α-amylase in vitro.Includes bibliographical references (pages 30-32)California State University, Northridge. Department of Home Economics

Assessment of In Vitro Antidiabetic Potential of Purified Anthocyanin Extract from Floral Petals of Wild Balsam Species

Diabetes is a notorious and growing clinical and public health issue. The International Diabetes Federation assumes that 592 million had diabetes by 2035 and that by 2040 the number will increase to 642 million. Cardiovascular&nbsp;corollary&nbsp;accounts for four million deaths annually attributable to diabetes. Evidence reveals that certain glucose-lowering phytochemicals can improve vascular outcomes with type 2 diabetes, which, together with better understanding of using multiple therapies concurrently, offers opportunities for beneficial personalization of medication regimens. Anthocyanins are coloured pigments and are natural antioxidants. Keeping this in focus, this study was undertaken to evaluate the in vitro antidiabetic activity in the petals of wild Impatiens balsamina L. The anthocyanin was extracted from floral petals of wild balsam species and purified to homogeneity using chromatographic techniques. Evaluation of in vitro antidiabetic properties of anthocyanin extract revealed a dose-dependent increase in the inhibitory effect on the alpha-glucosidase (200 μg/ml) and alpha-amylase enzymes (500 μg/ml) and was comparable with the standard acarbose drug (189 μg/ml and 50 μg/ml). These results indicated that anthocyanin could be used as a source of functional food and nutraceuticals. This information from wild species will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Future studies are planned to substantiate the antidiabetic power of anthocyanin using in vivo animal models. Keywords:&nbsp;Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L

BIOLOGICAL ACTIVITIES OF NOVEL IN VITRO RAISED STEVIA PLANT

  Objective: This communication explores a lead fraction from methanolic extract of novel Stevia species raised under in vitro conditions for its various biological activities.Methods: The dried Stevia leaves were crushed in methanol to get the polar extract. This methanol extract was tested for pancreatic lipase and alpha-amylase inhibitory activity using quantitative plate assays. Antibacterial property of the extract was also evaluated against Staphylococcus epidermidis, Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. Further, the antioxidant potential was evaluated using 1,1-diphenyl-2-picrylhydrazyl.Results: The methanolic extract inhibited pancreatic lipase with IC50 of 5.74 μg/ml in a similar manner to a well-known anti-obesity drug in the market orlistat. The methanolic extract also showed a better pancreatic α-amylase inhibitory activity (IC50=88 μg/ml) than acarbose. Further, the lead fraction exhibited 88.48% antioxidant activity. It also exhibited broad spectrum antimicrobial activity against the spectrum of Gram-positive and Gram-negative bacteria tested under laboratory conditions with a minimal inhibitory concentration ranging from 1.95 to 31.25 μg/ml.Conclusion: Thus, this study signifies the vast potential of the lead fraction from a novel Stevia species for further development into a herbal formulation for prevention of various infectious and non-infectious diseases

GC-MS analysis and In-vitro anti-diabetic activity of ethanolic extract of theAtrocarpus Heterophylus (Unriped Jack Fruit)

Objective: In the present study the ethanolic extracts of Atrocarpus Heterophylus (ETAH) were studied for Aldose reductase, alpha (α)- amylase and alpha (α)-glucosidase inhibition using an in-vitro anti diabetic and evaluate the GC-MS analysis of active compounds of ETAH. Methods: The serial extraction was carried out with a series of solvents: Petroleum ether, ethyl acetate and ethanol with increasing polarity using Soxhlet apparatus. The concentrated and dried extracts were subjected to the antidiabetic activity was assessed by employing standard in-vitro techniques. Results and discussion: The result showed ethanolic extract exhibited significant aldose reductase, α-amylase and α-glucosidase inhibitory activities with an all plant extracts respectively and well compared with standard acarbose drug.&nbsp; GC-MS analysis results revealed that ETAH contain the compounds are Cyclohexanol and Nonadecene. This knowledge will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics. Conclusion: The investigation confirms that ethanolic extract exhibited highest antidiabetic activity among all extracts, Additional studies on needed for purification, characterization and structural elucidation of bioactive compounds from ethanolic extrac