Anti-α-glucosidase and Anti-dipeptidyl Peptidase-IV Activities of Extracts and Purified Compounds from <i>Vitis thunbergii</i> var. <i>taiwaniana</i>

Lin, Yin Shiou; Chen, Chiy Rong; Wu, Wei Hau; Wen, Chi Luan; Chang, Chi I.; Hou, Wen Chi

doi:10.1021/acs.jafc.5b02069

Cited by 49 publications

(51 citation statements)

References 31 publications

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“…In the present study, the protein hydrolysate of raw, boiled and backed of seven edible insects have significant α-glucosidase inhibitory activity. This study was correlated with a previous investigation, which was determined by the α-glucosidase inhibitory activity of protein hydrolysates from B. mori proteins 37,[57][58][59][60] .…”

Section: Discussionsupporting

confidence: 77%

Untitled

2020

IJPSR

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The bioactive peptides derived from food have increased consideration for their function in averting numerous chronic diseases, comprising, diabetes and obesity. Edible insects are the feasible composition of bioactive peptides owing to their high protein content and viable production. The present study was aimed to evaluate the antidiabetic and anti-obesity effects of seven edible insects' protein hydrolysates after simulated gastrointestinal enzymatic digestion. Antidiabetic and anti-obesity efficiency was determined by the inhibition of digestive enzymes viz., dipeptidyl peptidase-IV, α-glucosidase, and α-lipase activity. Three active protein hydrolysate extracts (1.25, 2.5, and 5mg/dl) were selected and analyzed in terms of their IC 50 values, and all tested extracts inhibited those enzyme activities in a dose-dependent manner. Based on the present study, we conclude the seven edible insects' hydrolysate have potential enzyme inhibitory activities and thereby proved as an antidiabetic and anti-obesity activity. INTRODUCTION: Diabetes Mellitus is wellknown metabolic syndromes measured by high blood glucose and failings of insulin synthesis or insulin action, or both, which may cause serious complications, including retinopathy, nephropathy, neuropathy, obesity, and cardiovascular diseases 1-3. Diabetes and its hitches have established significant attention due to augmented health menaces, and its treatment costs 4, 5. The number of individuals suffering from diabetes and obesity has been tripled since 1990 and becomes the main challenge for our society globally 6, 7. Diabetes with overweight and obesity are the foremost risk factors for numerous chronic diseases, including cardiovascular diseases and various cancers 8-10 .

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Section: Discussionsupporting

confidence: 77%

Untitled

2020

IJPSR

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“…The straight lines were joined at a single point in the second quadrant suggesting a mixed noncompetitive type of inhibition ( Figure 3A). A similar mode of inhibition was proposed earlier for the porcine kidney DPP-IV-(−)-vitisin B complex [50]. This type of inhibition indicates that phenolics can bind to the enzyme irrespective of whether the enzyme is previously bound to the substrate or not.…”

Section: Kinetics Of Enzyme Inhibitionsupporting

confidence: 82%

Fenugreek (Trigonellafoenum-Graecum L) Seed Phytochemicals Protect DNA from Free Radical Induced Oxidative Damage and Inhibit Dipeptidyl Peptidase-IV an Enzyme Associated with Hyperglycemia

Sreerama

2019

JNB

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Fenugreek (Trigonellafoenum-graecum L.; methi) seeds and leaves are used in Asia, Africa, and Mediterranean countries for their nutritional and therapeutic value. It is an ingredient in many traditional Unani and Ayurvedic medicinal systems in India and proven to be very effective in managing blood glucose homeostasis. However, there is a dearth of information on the biochemical rationale for its use in the management of diabetes. In this study, protective effects of fenugreek seed phytochemicals on oxidative stress and inhibition of dipeptidyl peptidase-IV (DPP-IV), a key enzyme associated with diabetes were evaluated. Compositional analysis of phenolics by HPLC revealed that gallic and ferulic acids were the major phenolic acids, and myricetin and rutin were predominant flavonoids in phenolic extracts of fenugreek seeds. Trigonelline content in alkaloid extract was quantitatively determined by reverse phase HPLC and found to be 8.6 mg/g. Alkaloid extract showed superior radical scavenging and metal chelating activities. Besides, these phytochemical extracts also prevented OH• radical-induced DNA damage. Michaelis-Menton and Line weaver-Burk derivations were applied to establish modes of inhibition of DPP-IV activity. Phenolic and alkaloid extracts inhibited DPP-IV activity by mixed non-competitive and non-competitive inhibition mechanisms, respectively. Inhibitory constants of enzyme inhibitor complexes indicate strong affinity of phenolic (Ki, 34.93 ± 0.14 μg) and alkaloid extracts (Ki, 32.3 ± 4.8 μg) for DPP-IV. These results suggest that isolated phytochemicals have the potential as lead compounds for the development of DPP-IV inhibitors to control hyperglycemia and manage diabetes.

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“…(-)-Hopeaphenol, vatalbinoside A, vaticanol B, and related stilbenoids and their stereoisomers have been isolated from a variety of plant sources including Hopea, Vitis, Shorea, Anisoptera, and Vatica species, among others (29)(30)(31)(32)(33)(34)(35)(36)(37). These compounds have been reported to exhibit several in vitro properties including antiproliferative (32)(33)(37)(38), antibacterial (through inhibition of the type III secretion system of Gram-negative bacteria) (30,39), antifungal (40), anti-influenza and herpes simplex virus (41)(42), and anti-inflammatory (34,43) activities, among others.…”

Section: Discussionmentioning

confidence: 99%

The natural stilbenoid (–)-hopeaphenol inhibits cellular entry of SARS-CoV-2 USA-WA1/2020, B.1.1.7 and B.1.351 variants

Tietjen¹,

Cassel²,

et al. 2021

Preprint

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Antivirals are urgently needed to combat the global SARS-CoV-2/COVID-19 pandemic, supplement existing vaccine efforts, and target emerging SARS-CoV-2 variants of concern. Small molecules that interfere with binding of the viral spike receptor binding domain (RBD) to the host ACE2 receptor may be effective inhibitors of SARS-CoV-2 cell entry. Here we screened 512 pure compounds derived from natural products using a high-throughput RBD/ACE2 binding assay and identified (-)-hopeaphenol, a resveratrol tetramer, in addition to vatalbinoside A and vaticanol B, as potent and selective inhibitors of RBD/ACE2 binding and viral entry. For example, (-)-hopeaphenol disrupted RBD/ACE2 binding with a 50% inhibitory concentration (IC50) of 0.11 uM in contrast to an IC50 of 28.3 uM against the unrelated host ligand/receptor binding pair PD-1/PD-L1 (selectivity index = 257.3). When assessed against the USA-WA1/2020 variant, (-)-hopeaphenol also inhibited entry of a VSVdeltaG-GFP reporter pseudovirus expressing SARS-CoV-2 spike into ACE2-expressing Vero-E6 cells and in vitro replication of infectious virus in cytopathic effect assays (IC50 = 10.2 uM) without cytotoxicity. Notably, (-)-hopeaphenol also inhibited two emerging variants of concern originating from the United Kingdom (B.1.1.7) and South Africa (B.1.351) in both cytopathic effect and spike-containing pseudovirus assays with similar (B.1.1.7) or improved (B.1.351) efficacies over the USA-WA1/2020 variant. These results identify (-)-hopeaphenol and related stilbenoid analogues as potent and selective inhibitors of viral entry across multiple SARS-CoV-2 variants including those with increased infectivity and/or reduced susceptibility to existing vaccines.

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Anti-α-glucosidase and Anti-dipeptidyl Peptidase-IV Activities of Extracts and Purified Compounds from Vitis thunbergii var. taiwaniana

Cited by 49 publications

References 31 publications

Untitled

Untitled

Fenugreek (Trigonellafoenum-Graecum L) Seed Phytochemicals Protect DNA from Free Radical Induced Oxidative Damage and Inhibit Dipeptidyl Peptidase-IV an Enzyme Associated with Hyperglycemia

The natural stilbenoid (–)-hopeaphenol inhibits cellular entry of SARS-CoV-2 USA-WA1/2020, B.1.1.7 and B.1.351 variants

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