scholarly journals Inhibition of intestinal .ALPHA.-glucosidase and postprandial hyperglycemia by N-substituted moranoline derivatives.

1988 ◽  
Vol 11 (5) ◽  
pp. 356-362 ◽  
Author(s):  
Yoshiaki YOSHIKUNI ◽  
Yohji EZURE ◽  
Yoshiaki AOYAGI ◽  
Hiroshi ENOMOTO
Keyword(s):  
Postprandial Hyperglycemia ◽  
Alpha Glucosidase

Recent Developments in Alpha-Glucosidase Inhibitors for Management of Type-2 Diabetes: An Update

2019 ◽  
Vol 25 (23) ◽  
pp. 2510-2525 ◽  
Author(s):  
Bashir Usman ◽  
Neha Sharma ◽  
Saurabh Satija ◽  
Meenu Mehta ◽  
Manish Vyas ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Patient Compliance ◽  
Postprandial Hyperglycemia ◽  
Diabetic Patients ◽  
Poor Patient ◽  
Glucosidase Inhibitors ◽  
Poor Patient Compliance ◽  
Recent Developments ◽  
Alpha Glucosidase

The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes of drugs are available for the management of type 2 diabetes but were having certain limitations of their safety. Alphaglucosidase is a family of enzyme originated from the pancreas which plays a role in the anabolism of 80-90% of carbohydrate consumed into glucose. This glucose is absorbed into the blood and results in frank postprandial hyperglycemia and worsens the conditions of diabetic patients which precipitate complications. Inhibition of these enzymes helps to prevent postprandial hyperglycemia and the formation of glycated end products. Alphaglucosidase inhibitors are reported to be more important in adequate control of type 2, but marketed drugs have various side effects, such as poor patient compliance and also expensive. This proves the needs for other class of drugs with better efficacy, safety, patient compliance and economic. In this review, we have emphasized the recent advances in the field of new alpha-glucosidase inhibitors with improved safety and pharmacological profile.

Inhibitory Effects of Hyssop (Hyssopus officinalis) Extracts on Intestinal .ALPHA.-Glucosidase Activity and Postprandial Hyperglycemia

2003 ◽  
Vol 49 (5) ◽  
pp. 346-349 ◽  
Author(s):  
Hiroyuki MIYAZAKI ◽  
Hideyuki MATSUURA ◽  
Chikako YANAGIYA ◽  
Junya MIZUTANI ◽  
Masayoshi TSUJI ◽  
...  
Keyword(s):  
Postprandial Hyperglycemia ◽  
Inhibitory Effects ◽  
Glucosidase Activity ◽  
Alpha Glucosidase ◽  
Hyssopus Officinalis

scholarly journals Antioxidant rich grape pomace extract suppresses postprandial hyperglycemia in diabetic mice by specifically inhibiting alpha-glucosidase

2010 ◽  
Vol 7 (1) ◽  
pp. 71 ◽  
Author(s):  
Shelly Hogan ◽  
Lei Zhang ◽  
Jianrong Li ◽  
Shi Sun ◽  
Corene Canning ◽  
...  
Keyword(s):  
Postprandial Hyperglycemia ◽  
Grape Pomace ◽  
Diabetic Mice ◽  
Alpha Glucosidase

scholarly journals Multimodal α-Glucosidase and α-Amylase Inhibition and Antioxidant Effect of the Aqueous and Methanol Extracts from the Trunk Bark of Ceiba pentandra

2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Telesphore Benoit Nguelefack ◽  
Christian Kuete Fofie ◽  
Elvine Pami Nguelefack-Mbuyo ◽  
Adeline Kaptue Wuyt
Keyword(s):  
Protein Oxidation ◽  
Postprandial Hyperglycemia ◽  
Alpha Amylase ◽  
Total Phenolic ◽  
Noncompetitive Inhibition ◽  
Ceiba Pentandra ◽  
Flavonoid Compounds ◽  
Alpha Glucosidase ◽  
Phenolic And Flavonoid ◽  
Phenolic And Flavonoid Compounds

Postprandial hyperglycemia and oxidative stress are important factors that worsen the health condition of patients with type 2 diabetes. We recently showed that extracts from Ceiba pentandra mitigate hyperglycemia in dexamethasone- and high diet/streptozotocin-induced diabetes. Herein, we evaluated the postprandial regulatory properties and the antioxidant effects of the aqueous (AE) and methanol (ME) extracts from the stem bark of Ceiba pentandra. The phytochemical analysis of AE and ME was performed using the LC-MS technique and the total phenolic and flavonoid assays. Both extracts were tested for their ability to inhibit superoxide anion (O2•ـ), hydrogen peroxide (H2O2), protein oxidation, alpha-amylase, and alpha-glucosidase activities. The mode of enzyme inhibition was also determined in a kinetic study. AE and ME were both rich in phenolic and flavonoid compounds. ME was 2.13 and 1.91 times more concentrated than AE in phenolic and flavonoid compounds, respectively. LC-MS allowed the identification of 5 compounds in both extracts. ME and AE inhibited O2•ـ with IC50 of 51.81 and 34.26 μg/ml, respectively. On H2O2, they exhibited IC50 of 44.84 and 1.78 μg/ml, respectively. Finally, they exhibited IC50 of 120.60 and 140.40 μg/ml, respectively, in the inhibition of protein oxidation induced by H2O2, while showing IC50 of 39.26 and 97.95 μg/ml on the protein oxidation induced by AAPH. ME and AE inhibited alpha-amylase with IC50 of 6.15 and 54.52 μg/ml, respectively. These extracts also inhibited alpha-glucosidase, demonstrating IC50 of 76.61 and 86.49 μg/ml. AE exhibited a mixed noncompetitive inhibition on both enzymes, whereas ME exhibited a competitive inhibition on α-amylase and a pure noncompetitive inhibition on α-glucosidase. These results demonstrate that ME and AE scavenge reactive oxygen species and prevent their effects on biomolecules. Besides, ME and AE inhibit carbohydrate digestive enzymes. These properties may contribute to reduce postprandial hyperglycemia and regulate glycemia in diabetic patients.

scholarly journals Inhibitory Properties of Aqueous Ethanol Extracts of Propolis on Alpha-Glucosidase

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Hongcheng Zhang ◽  
Guangxin Wang ◽  
Trust Beta ◽  
Jie Dong
Keyword(s):  
Aqueous Ethanol ◽  
Competitive Inhibition ◽  
Inhibitory Effect ◽  
Postprandial Hyperglycemia ◽  
Baker’S Yeast ◽  
Baker's Yeast ◽  
Ethanol Extracts ◽  
Alpha Glucosidase ◽  
Mammalian Intestine ◽  
Intestinal Sucrase

The objective of the present study was to evaluate the inhibitory properties of various extracts of propolis on alpha-glucosidase from baker’s yeast and mammalian intestine. Inhibitory activities of aqueous ethanol extracts of propolis were determined by using 4-nitrophenyl-D-glucopyranoside, sucrose and maltose as substrates, and acarbose as a positive reference. All extracts were significantly effective in inhibitingα-glucosidase from baker’s yeast and rat intestinal sucrase in comparison with acarbose (P<0.05). The 75% ethanol extracts of propolis (75% EEP) showed the highest inhibitory effect onα-glucosidase and sucrase and were a noncompetitive inhibition mode. 50% EEP, 95%, EEP and 100% EEP exhibited a mixed inhibition mode, while water extracts of propolis (WEP) and 25% EEP demonstrated a competitive inhibition mode. Furthermore, WEP presented the highest inhibitory activity against maltase. These results suggest that aqueous ethanol extracts of propolis may be used as nutraceuticals for the regulation of postprandial hyperglycemia.

Efficacy and cardiovascular safety of Alpha glucosidase inhibitors .

2020 ◽  
Vol 15 ◽  
Author(s):  
Nizam Ud Din Khwaja ◽  
Ganesan Arunagirinathan
Keyword(s):  
Far East ◽  
Asian Population ◽  
Glycated Haemoglobin ◽  
Postprandial Hyperglycemia ◽  
Systemic Absorption ◽  
Mortality And Morbidity ◽  
Local Site ◽  
Glucosidase Inhibitors ◽  
Alpha Glucosidase ◽  
Cardiovascular Benefit

: Alpha Glucosidase Inhibitors (AGIs) are a group of drugs which acts on the gastrointestinal tract and helps in reducing fasting and postprandial hyperglycemia by reducing the absorption of carbohydrates. This group comprises of Acarbose, Miglitol and Voglibose. They are available in the market for almost three decades now. When used as monotherapy Glycated Haemoglobin (HBA1c) reduction can be as high as 0.77% which is predominantly noted in Eastern Asian population and those on high carbohydrate diet. There is more pronounced reduction in HbA1c in those who present with higher baseline values. Despite not showing a significant cardiovascular benefit with regards to mortality and morbidity, they have proven to be a safe class of drugs which can be used in patients not tolerating various other antidiabetic agents due to their local site of action and poor systemic absorption. Though they are available worldwide AGIs are used more often in the Far East and South Asia. They have shown benefits in reducing the development of diabetes when used in those with impaired glucose tolerance or pre-diabetes. They have shown to improve postprandial hyperglycemia, which in itself is an independent risk factor for cardiovascular morbidity. These have proven their safety from both cardiovascular and non-cardiovascular perspectives and can be combined with any class of anti diabetic agents. They are not favoured in most of the current Western Guidelines due to their modest HbA1c reduction, neutrality with cardiovascular benefit as well as their significant gastrointestinal side effect profile.

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