Phenolic bioactives from developmental stages of highbush blueberry (Vaccinium corymbosum) for hyperglycemia management using in vitro models

2015 ◽  
Vol 95 (4) ◽  
pp. 653-662 ◽  
Author(s):  
Susan Cheplick ◽  
Dipayan Sarkar ◽  
Prasanta Bhowmik ◽  
Kalidas Shetty
Keyword(s):  
Type 2 Diabetes ◽  
Antioxidant Activity ◽  
Inhibitory Activity ◽  
Developmental Stages ◽  
Vaccinium Corymbosum ◽  
In Vitro Models ◽  
In Vitro Assays ◽  
Highbush Blueberry

Cheplick, S., Sarkar, D., Bhowmik, P. and Shetty, K. 2015. Phenolic bioactives from developmental stages of highbush blueberry (Vaccinium corymbosum) for hyperglycemia management using in vitro models. Can. J. Plant Sci. 95: 653–662. Blueberry is a rich source of soluble phenolics as well as human health relevant antioxidants. Phenolic-linked bioactive functionality of blueberry for type 2 diabetes management was screened during fruit maturation, especially from green to ripening stages using in vitro assays. Green fruit showed the highest total soluble phenolic content, whereas all three developmental stages of blueberry fruit exhibited high total antioxidant activity. Overall, ripe fruit had higher α-amylase and α-glucosidase inhibitory activity than green or green/pink fruit, and showed significant potential to improve glucose metabolism through in vitro assays. High phenolic-linked antioxidant activity along with moderate to high α-amylase and α-glucosidase inhibitory activity in ripe blueberry indicated its potential relevance as part of diet-based prevention and management of early stages of hyperglycemia associated with development of type 2 diabetes. This in vitro screening study provides a biochemical rationale and dietary strategy to develop the right blueberry cultivar and stage of fruit development for further validation in animal and clinical studies.

Evaluation of Rubus grandifolius L. (wild blackberries) activities targeting management of type-2 diabetes and obesity using in vitro models

2019 ◽  
Vol 123 ◽  
pp. 443-452 ◽  
Author(s):  
Vítor Spínola ◽  
Joana Pinto ◽  
Eulogio J. Llorent-Martínez ◽  
Helena Tomás ◽  
Paula C. Castilho
Keyword(s):  
Type 2 Diabetes ◽  
In Vitro Models ◽  
Diabetes And Obesity

Pyrano[3,2-c]quinoline Derivatives as New Class of α-glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in vitro Biological Evaluation and Kinetic Study

2019 ◽  
Vol 15 (1) ◽  
pp. 8-16 ◽  
Author(s):  
Zahra Heydari ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Somaye Imanparast ◽  
Mohammad A. Faramarzi ◽  
Mohammad Mahdavi ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Kinetic Study ◽  
Inhibitory Activity ◽  
Cycloaddition Reaction ◽  
Competitive Inhibitor ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Standard Drug

Background: Pyrano[3,2-c]quinoline derivatives 6a–n were synthesized via simple two-step reactions and evaluated for their in vitro α-glucosidase inhibitory activity. </P><P> Methods: Pyrano[3,2-c]quinoline derivatives 6a–n derivatives were prepared from a two-step reaction: cycloaddition reaction between 1-naphthyl amine 1 and malonic acid 2 to obtain benzo[h]quinoline-2(1H)-one 3 and reaction of 3 with aryl aldehydes 4 and Meldrum’s acid 5. The anti- α-glucosidase activity and kinetic study of the synthesized compounds were evaluated using α-glucosidase from Saccharomyces cerevisiae and p-nitrophenyl-a-D-glucopyranoside as substrate. The α-glucosidase inhibitory activity of acarbose was evaluated as positive control. Results: All of the synthesized compounds, except compounds 6i and 6n, showed more inhibitory activity than the standard drug acarbose and were also found to be non-cytotoxic. Among the synthesized compounds, 1-(2-bromophenyl)-1H-benzo[h]pyrano[3,2-c]quinoline-3,12(2H,11H)-dione 6e displayed the highest α-glucosidase inhibitory activity (IC50 = 63.7 ± 0.5 µM). Kinetic study of enzyme inhibition indicated that the most potent compound, 6e, is a non-competitive inhibitor of α-glucosidase with a Ki value of 72 µM. Additionally, based on the Lipinski rule of 5, the synthesized compounds were found to be potential orally active drugs. Conclusion: Our results suggest that the synthesized compounds are promising candidates for treating type 2 diabetes.

scholarly journals A Novel Dipeptidyl Peptidase IV Inhibitory Tea Peptide Improves Pancreatic β-Cell Function and Reduces α-Cell Proliferation in Streptozotocin-Induced Diabetic Mice

2019 ◽  
Vol 20 (2) ◽  
pp. 322 ◽  
Author(s):  
Yating Lu ◽  
Peng Lu ◽  
Yu Wang ◽  
Xiaodong Fang ◽  
Jianming Wu ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Type 2 Diabetes ◽  
Inhibitory Activity ◽  
Black Tea ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Inhibitory Peptides ◽  
Dpp Iv

Dipeptidyl peptidase IV (DPP-IV) inhibitors occupy a growing place in the drugs used for the management of type 2 diabetes. Recently, food components, including food-derived bioactive peptides, have been suggested as sources of DPP-IV inhibitors without side effects. Chinese black tea is a traditional health beverage, and it was used for finding DPP-IV inhibitory peptides in this study. The ultra-filtrated fractions isolated from the aqueous extracts of black tea revealed DPP-IV inhibitory activity in vitro. Four peptides under 1 kDa were identified by SDS-PAGE and LC-MS/MS (Liquid Chromatography-Mass Spectrometry-Mass Spectrometry) from the ultra-filtrate. The peptide II (sequence: AGFAGDDAPR), with a molecular mass of 976 Da, showed the greatest DPP-IV inhibitory activity (in vitro) among the four peptides. After administration of peptide II (400 mg/day) for 57 days to streptozotocin (STZ)-induced hyperglycemic mice, the concentration of glucagon-like peptide-1 (GLP-1) in the blood increased from 9.85 ± 1.96 pmol/L to 19.22 ± 6.79 pmol/L, and the insulin level was increased 4.3-fold compared to that in STZ control mice. Immunohistochemistry revealed the improved function of pancreatic beta-cells and suppressed proliferation of pancreatic alpha-cells. This study provides new insight into the use of black tea as a potential resource of food-derived DPP-IV inhibitory peptides for the management of type 2 diabetes.

INHIBITORY POTENCY OF WITHANIA SOMNIFERA EXTRACTS AGAINST DPP-4: AN IN VITRO EVALUATION

2017 ◽  
Vol 15 (1) ◽  
pp. 11
Author(s):  
Praveen Kumar Kempegowda ◽  
Farhan Zameer ◽  
Chethan Kumar Narasimashetty ◽  
Shiva Prasad Kollur ◽  
Satish Kumar Murari
Keyword(s):  
Type 2 Diabetes ◽  
13C Nmr ◽  
Inhibitory Activity ◽  
Withania Somnifera ◽  
Methanol Extract ◽  
Nmr Studies ◽  
1H And 13C Nmr ◽  
Rp Hplc

Background: Pharmacologic treatments for type 2 diabetes are based upon increasing insulin availability and improving sensitivity to insulin. Nowadays, glucagon like peptide-1 (GLP-1) based therapies aims at glucose control through DPP-4 inhibitors. DPP-4 is a transmembrane glycoprotein belongs to prolyl oligopeptidase family, with the specificity of removing X-Pro or X-Ala dipeptides from the N-terminus of polypeptides. GLP-1 effect by stimulating glucose-dependent insulin release from the pancreatic islets, inhibit inappropriate post-meal glucagon release and slow gastric emptying promoting leaky gut. The current study investigated DPP-4 inhibitory activity of catechin, isolated from Withania somnifera (WS), for ethnopharmacological treatment of type 2 diabetes and aimed to increase availability of GLP-1and sensitivity to insulin. Materials and Methods: Young and matured fresh roots, leaves, and fruits of WS plant extract were considered and were systematically evaluated for DPP-4 inhibitory activity using in vitro method, enzyme kinetics, phytochemical analysis, RP-HPLC, LCMS and 1H and 13C NMR method and structure-activity relationship (SAR) studies. Results: In this study, methanol (100% and 80%) extracts of WS matured root exhibited maximum DPP-4 inhibitory activity when compared to other extracts. The maximum DPP-4 inhibitory activity was found in 100% methanol extract of matured root. Phytobioactive was purified by RP-HPLC. The compound purified was found to be flavonoid and was characterized (LCMS, 1H and 13C NMR studies), identified as catechin. Auxiliary, molecular docking was performed using Ligand Fit method using PatchDock package. The study revealed the binding affinity of catechin with DPP-4 to be -6.601 kcal/mol with 13 hydrogen interactions with the receptor and was very similar to the standard potent blockers withaferin A and others (cuscohygrine, scopoletin, sitoindoside IV, tropine), further confirming its hyperglycemic potency. Conclusion: The study reveals that, 100% methanol extract of WS matured roots contains the compound- catechin, which exhibits DPP-4 inhibitory activity resulting in increased level of bioactive GLP-1 and GIP. In this background, we concluded that the WS will be a better source for further development as new antidiabetic drugs.

scholarly journals Anti-diabetic potential of crude extracts of medicinal plants used as substitutes for Swertia chirayita using in vitro assays

1970 ◽  
Vol 7 ◽  
pp. 48-55 ◽  
Author(s):  
Susanna Phoboo ◽  
Prasanta C Bhowmik ◽  
Pramod Kumar Jha ◽  
Kalidas Shetty
Keyword(s):  
Type 2 Diabetes ◽  
Antioxidant Activity ◽  
Early Stage ◽  
Andrographis Paniculata ◽  
Total Phenolic ◽  
Swertia Chirayita ◽  
Inhibitory Potential ◽  
Swertia Species

Swertia chirayita is a highly traded medicinal plant of Nepal widely used for its anti-diabetic potential. In this study, two herbs (Swertia nervosa and Andrographis paniculata) often used as adulterants and substitutes of Swertia chirayita were analyzed for their antioxidant activity, α-glucosidase inhibitory potential and total phenolic content and compared with that of Swertia chirayita. Aqueous and 12% ethanolic extracts of the three herbs showed moderate to high antioxidant activity and moderate α-glucosidase inhibitory potential. HPLC/ DAD revealed the presence of swertiamarin and mangiferin in all the Swertia species, while Andrographis paniculata contained cinnamates such as cinnamic acid, p-coumaric acid and chlorogenic acid. The antioxidant activity and α-glucosidase inhibitory potential was evident in the two herbs indicating their relevance as substitutes for Swertia chirayita for potential early stage management of type-2 diabetes and related complications. Key-words: Andrographis paniculata; antioxidant activity; cinnamates; mangiferin; Swertia nervosa; swertiamarin; α-glucosidase; type-2 diabetes. DOI: 10.3126/botor.v7i0.4373Botanica Orientalis – Journal of Plant Science (2010) 7: 48-55

Evaluation of phenolic bioactive-linked functionality of blackberry cultivars targeting dietary management of early stages type-2 diabetes using in vitro models

2016 ◽  
Vol 212 ◽  
pp. 193-202 ◽  
Author(s):  
Dipayan Sarkar ◽  
Jordan Orwat ◽  
Tim Hurburt ◽  
Floyd Woods ◽  
James A. Pitts ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
In Vitro Models ◽  
Dietary Management ◽  
Early Stages
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