Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking

Bharti, Sudhanshu Kumar; Krishnan, Supriya; Kumar, Amit; Rajak, Kaushal Kishor; Murari, Krishna; Bharti, Binod Kumar; Gupta, Ashok

doi:10.1016/j.phymed.2012.09.009

Cited by 62 publications

(39 citation statements)

References 46 publications

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“…However, DPP-IV inhibitors have been discovered in foods, herbal preparations, natural sources, and traditional Chinese medicines, including phenolic compounds from blueberry–blackberry wine blends [24], alkaloids from seed extract of Castanospermum australe [25], and procyanidins from grape seed [26], all of which have shown good DPP-IV inhibitory activity. Various foods, including milk, fish, wheat gluten, beans, egg, and bivalve mollusks, are natural protein sources; after enzymatic hydrolysis, microbial fermentation, decoction, or some other physical and/or chemical processing, their proteins may be degraded and release various DPP-IV inhibitory peptides [27,28,29,30,31,32].…”

Section: Introductionmentioning

confidence: 99%

Discovery of Food-Derived Dipeptidyl Peptidase IV Inhibitory Peptides: A Review

Liu

Cheng

2019

IJMS

119

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Diabetes is a chronic metabolic disorder which leads to high blood sugar levels over a prolonged period. Type 2 diabetes mellitus (T2DM) is the most common form of diabetes and results from the body’s ineffective use of insulin. Over ten dipeptidyl peptidase IV (DPP-IV) inhibitory drugs have been developed and marketed around the world in the past decade. However, owing to the reported adverse effects of the synthetic DPP-IV inhibitors, attempts have been made to find DPP-IV inhibitors from natural sources. Food-derived components, such as protein hydrolysates (peptides), have been suggested as potential DPP-IV inhibitors which can help manage blood glucose levels. This review focuses on the methods of discovery of food-derived DPP-IV inhibitory peptides, including fractionation and purification approaches, in silico analysis methods, in vivo studies, and the bioavailability of these food-derived peptides. Moreover, food-derived DPP-IV inhibitory peptides discovered during this decade are listed and distributed in a 3D scatter plot graph based on their IC50, molecular weight, and grand average of hydropathicity values, which can help us to understand the relationship between the features of the peptides and their activities.

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Section: Introductionmentioning

confidence: 99%

Discovery of Food-Derived Dipeptidyl Peptidase IV Inhibitory Peptides: A Review

Liu

Cheng

2019

IJMS

119

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“…Therefore, inhibiting DPP-IV can prevent the rapid degradation of incretin hormones which, in turn, increases the levels of biologically active incretins (GLP-1 and GIP), which reduce glucose production by inhibiting glucagon from the α-cells of the pancreas and increasing insulin production (Havale & Pal 2009). Commercially available antidiabetic drugs such as sitagliptin and saxagliptin are used for DPP-IV inhibition (Bharti et al 2012). Although powerful synthetic α-amylase, α-glucosidase and DPP-IV inhibitors including acarbose, voglibose, sitagliptin and saxagliptin are available, they are known to cause hepatic disorders and other gastrointestinal symptoms (Murai et al 2002).…”

Section: Introductionmentioning

confidence: 99%

Antidiabetic potential of marine algae by inhibiting key metabolic enzymes

Unnikrishnan

Suthindhiran

Jayasri

2015

Frontiers in Life Science

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Two edible seaweeds, Sargassum polycystum and Sargassum wightii, were investigated for their antidiabetic potential using in vitro enzyme inhibitory assays. Among the various extracts, petroleum ether and ethyl acetate extracts of S. wightii showed significant inhibitory effects against α-amylase (IC 50 378.3 μg/ml) and α-glucosidase (IC 50 314.8 μg/ml). Methanol extract of S. wightii showed the highest inhibition against dipeptidyl peptidase-IV (DPP-IV) (IC 50 38.27 μg/ml) and moderate antioxidant activity was observed in acetone extract of S. wightii (44%). Similarly, ethyl acetate extract of S. polycystum showed the highest inhibition against α-amylase (IC 50 438.5 μg/ml) and methanol extract of S. polycystum showed maximum inhibition against α-glucosidase (IC 50 289.7 μg/ml) and DPP-IV (36.94 μg/ml). The antioxidant activity was poor (22%). The extracts were investigated for in vitro cytotoxicity, DNA fragmentation in macrophages and haemolytic activity against erythrocytes, but no notable toxicity was observed with any of the tested extracts. Gas chromatography-mass spectrometry revealed the presence of the antidiabetic compound fucosterol and other major bioactive compounds, giving an insight into the antidiabetic and antioxidant properties of these algae. This study reveals the possible mechanisms of antidiabetic action in vitro, and these two seaweeds may also have an antidiabetic action in vivo.

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“…Numerous research has been carried out world wide on molecular targets towards the development of newer antidiabetic agents like nuclear receptor PPAR-γ (peroxisome proliferator-activated receptor gamma) [4,5], human incretin-degrading enzyme DPP-IV (dipeptidyl peptidase IV) [5], protein-tyrosine phosphatase 1B (PTP1B) [6], etc. These therapeutic targets may improve the efficacy-to-safety ratio, resulting in durable maintenance of glycaemic control in the majority of people with diabetes.…”

Section: Introductionmentioning

confidence: 99%

Essential Oil of Cymbopogon Citratus Against Diabetes: Validation by In vivo Experiments and Computational Studies

Bharti¹

2013

J Bioanal Biomed

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This study evaluates the antidiabetic activities of essential oil obtained by steam distillation of the leaf sheath of Cymbopogon citratus (CCEO) in poloxamer-407 induced type 2 diabetic (T2D) Wistar rats. The sample was then analyzed by gas chromatography-mass spectroscopy (GCMS) identifying 23 compounds representing 96.9% of the oil. The major compounds of essential oil were geranial (42.4%), neral (29.8%), myrcene (8.9%) and geraniol (8.5%). When compared to diabetic control rats, the CCEO treated diabetic rats presented significant amelioration of glycaemia, insulinamia and lipid dysmetabolism, accompanied by increased GLP-1 content in cecum and remarkable reduction of oxidative markers. Histopatholgical analysis of pancreas showed increase in β-cell mass, islet number and quality of insulitis. HYBRID and FRED docking were performed for 48 documented CCEO phytoconstituents for putative action mechanism concerning three proteins namely PTP-1B, PPAR-γ and DPP-IV having diabetic therapeutic properties. Phytoconstituents like myrcenol, linalool, α-elemol and β-Eudesmol showed significant interaction with PPAR-γ and DPP-IV while only pimelyl dihydrazide showed interaction with PTP-1B. The results provided a pharmacological evidence of CCEO as antidiabetic mediated by interaction of various phytoconstituents with multiple targets operating in diabetes mellitus.

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Antihyperglycemic activity with DPP-IV inhibition of alkaloids from seed extract of Castanospermum australe: Investigation by experimental validation and molecular docking

Cited by 62 publications

References 46 publications

Discovery of Food-Derived Dipeptidyl Peptidase IV Inhibitory Peptides: A Review

Discovery of Food-Derived Dipeptidyl Peptidase IV Inhibitory Peptides: A Review

Antidiabetic potential of marine algae by inhibiting key metabolic enzymes

Essential Oil of Cymbopogon Citratus Against Diabetes: Validation by In vivo Experiments and Computational Studies

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