scholarly journals Potent Natural Inhibitors of Alpha-Glucosidase and Alpha-Amylase against Hyperglycemia in Vitro and in Vivo

2017 ◽  
Author(s):  
Jirawat Riyaphan ◽  
Chien-Hung Jhong ◽  
May-Jwan Tsai ◽  
Der-Nan Lee ◽  
Max K. Leong ◽  
...  
Keyword(s):  
Type Ii Diabetes ◽  
Herbal Medicines ◽  
Alpha Amylase ◽  
Type Ii ◽  
Reference Drug ◽  
Significant Difference ◽  
Natural Inhibitors ◽  
Alpha Glucosidase

The inhibition of alpha-glucosidase and alpha-amylase is one of clinic strategies for remedy the type II diabetes. Herbal medicines are reported to alleviate hyperglycemia. However, the constituents from those sources whether are targeted to the alpha-glucosidase and alpha-amylase still unexplored. This study attempted to select the compounds for efficacy of hypoglycemia via cellular and mouse levels. The results illustrated that the cytotoxicity in all tested compounds at various concentrations except the concentration of 16-hydroxy-cleroda-3,13-dine-16,15-olide (HCD) at 30 µM were not significant difference (p > 0.05) when compared with the untreated control. Acarbose (reference drug), Antroquinonol, Catechin, Quercetin, Actinodaphnine, Curcumin, HCD, Docosanol, Tetracosanol, Berberine, and Rutin could effectively inhibit the alpha-glucosidase activity of Caco-2 cells when compared with the control (maltose). The compounds (Curcumin, HCD, Tetracosanol, Antroquinonol, Berberine, Catechin, Actinodaphnine, and Rutin) could reduce blood sugar level at 30 min in tested mice. The effects of tested compounds on area under curve (AUC) were significant (p < 0.05) among Acarbose, Tetracosanol, Antroquinonol, Catechin, Actinodaphnine, and Rutin along with Berberine and Quercetin. In in vitro (alpha-glucosidase) with in vivo (alpha-amylase) experiments suggest that bioactive compounds can be a potential inhibitor candidate of alpha-glucosidase and alpha-amylase for the alleviation of type II diabetes.

In vitro and in vivo sustained release of exenatide from vesicular phospholipid gels for type II diabetes

2015 ◽  
Vol 42 (7) ◽  
pp. 1042-1049 ◽  
Author(s):  
Yu Zhang ◽  
Ying Zhong ◽  
Mei Hu ◽  
Nanxi Xiang ◽  
Yao Fu ◽  
...  
Keyword(s):  
Sustained Release ◽  
Type Ii Diabetes ◽  
Type Ii

Type II pneumocyte hypertrophy without activation of surfactant biosynthesis after partial pneumonectomy

1993 ◽  
Vol 264 (2) ◽  
pp. L153-L159 ◽  
Author(s):  
B. D. Uhal ◽  
M. D. Etter
Keyword(s):  
Cell Cycle ◽  
Cell Cycle Progression ◽  
Tritiated Thymidine ◽  
Cell Cycle Distribution ◽  
Type Ii ◽  
Adult Rats ◽  
Type Ii Pneumocyte ◽  
Significant Difference

Hypertrophic and normotrophic type II pneumocytes were isolated from pneumonectomized adult rats by unit gravity (1 g) sedimentation or by fluorescence-activated cell sorting (FACS). In vivo or in vitro, hypertrophic cells incorporated significantly more 5-bromo-2'-deoxyuridine or tritiated thymidine into acid-insoluble material than did normotrophic cells. By FACS analysis of cell subpopulations isolated by 1 g, > 97% of normotrophic cells had G0-phase DNA content. In contrast, the cell cycle distribution of hypertrophic cells was 75% G1, 5% S, and 20% G2/M phases. Rates of incorporation of tritiated choline into total cellular phosphatidylcholine (PC) were identical in type II cells isolated from normal or pneumonectomized rats. The intracellular contents of disaturated phosphatidylcholine (DSPC) and total PC, as well as the ratio of these two lipids, were the same in hypertrophic and normotrophic cells from pneumonectomized rats and in cells isolated from normal rats. No significant difference was observed in the rate at which hypertrophic or normotrophic cells incorporated choline into DSPC. These results demonstrate that type II pneumocyte hypertrophy after pneumonectomy reflects balanced cell growth secondary to cell cycle progression in vivo. The data also indicate that epithelial cell hypertrophy after pneumonectomy, in contrast to that which develops after more acute lung injury, occurs without activation of surfactant biosynthesis or storage.

Insulin resistance in obesity, type II diabetes and stress

1983 ◽  
Vol 104 (4_Suppl) ◽  
pp. S67-S69
Author(s):  
Ulf Smith
Keyword(s):  
Insulin Resistance ◽  
Glucose Tolerance ◽  
Key Words ◽  
Glucose Transport ◽  
Type Ii Diabetes ◽  
Insulin Receptors ◽  
In Vitro Studies ◽  
Type Ii

ABSTRACT. Insulin resistance plays a major role for the reduced glucose tolerance in obesity, type II diabetes and stress. Both in vivo and in vitro studies strongly support the major importance of post-receptor perturbations as the cause of the insulin resistance in these conditions. One likely level for the post-receptor alterations is the reported reduction in glucose transport. Key words: Insulin resistance, diabetes, obesity, insulin receptors, glucose transport.

Paraoxonase-1 (PON-1) genotype and activity and in vivo oxidized plasma low-density lipoprotein in Type II diabetes

2005 ◽  
Vol 109 (2) ◽  
pp. 189-197 ◽  
Author(s):  
Mike J. Sampson ◽  
Simon Braschi ◽  
Gavin Willis ◽  
Sian B. Astley
Keyword(s):  
Type Ii Diabetes ◽  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Paraoxonase 1 ◽  
Ldl Oxidation ◽  
Phenyl Acetate ◽  
Low Density ◽  
Type Ii

The HDL (high-density lipoprotein)-associated enzyme PON (paraoxonase)-1 protects LDL (low-density lipoprotein) from oxidative modification in vitro, although it is unknown if this anti-atherogenic action occurs in vivo. In a cross-sectional study of 58 Type II diabetic subjects and 50 controls, we examined the fasting plasma LDL basal conjugated diene concentration [a direct measurement of circulating oxLDL (oxidatively modified LDL)], lipoprotein particle size by NMR spectroscopy, PON-1 polymorphisms (coding region polymorphisms Q192R and L55M, and gene promoter polymorphisms −108C/T and −162G/A), PON activity (with paraoxon or phenyl acetate as the substrates) and dietary antioxidant intake. Plasma oxLDL concentrations were higher in Type II diabetic patients (males, P=0.048; females, P=0.009) and unrelated to NMR lipoprotein size, PON-1 polymorphisms or PON activity (with paraoxon as the substrate) in any group. In men with Type II diabetes, however, there was a direct relationship between oxLDL concentrations and PON activity (with phenyl acetate as the substrate; r=0.611, P=0.0001) and an atherogenic NMR lipid profile in those who were PON-1 55LL homozygotes. Circulating oxLDL concentrations in vivo were unrelated to PON-1 genotypes or activity, except in male Type II diabetics where there was a direct association between PON activity (with phenyl acetate as the substrate) and oxLDL levels. These in vivo data contrast with in vitro data, and may be due to confounding by dietary fat intake. Male Type II diabetic subjects with PON-1 55LL homozygosity have an atherogenic NMR lipid profile independent of LDL oxidation. These data do not support an in vivo action of PON on LDL oxidation.

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

2020 ◽  
Vol 10 (3) ◽  
pp. 31-35
Author(s):  
R ARATHY ◽  
K MURUGAN ◽  
KV DINESH BABU ◽  
GS MANOJ
Keyword(s):  
International Diabetes Federation ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Herbal Remedies ◽  
Antidiabetic Activity ◽  
Public Health Issue ◽  
Impatiens Balsamina ◽  
Alpha Glucosidase

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 corollary 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: Alpha amylase, alpha glucosidase, diabetes, herbal remedies, Impatiens balsamina L.

Trastuzumab versus MYL-1401O (a proposed trastuzumab biosimilar) in a phase I bioequivalence study: In vivo and in vitro immunomodulation.

2017 ◽  
Vol 35 (7_suppl) ◽  
pp. 10-10
Author(s):  
Régine Audran ◽  
Haithem Chtioui ◽  
Anne-Christine Thierry ◽  
Carole Mayor ◽  
Laure Vallotton ◽  
...  
Keyword(s):  
Phase I ◽  
Mononuclear Cell ◽  
Ex Vivo ◽  
Reference Drug ◽  
Gm Csf ◽  
Significant Difference ◽  
Ifn Γ ◽  
The Impact

10 Background: Trastuzumab is a humanized monoclonal antibody targeting breast cancer cells overexpressing the HER2-oncoprotein. During a Phase-I single centre, single dose, randomized, double-blind, cross-over study assessing the bioequivalence of a proposed trastuzumab biosimilar (MYL-1401O) versus the initially marketed drug (Herceptin), we investigated in addition a large panel of pharmacodynamics parameters comparing the immunomodulatory activity of both drugs. Methods: 22 healthy males were included, 19 subjects receiving randomly a single intravenous infusion of MYL-1401O and 22 of Herceptin, separated by 16 to 22 week wash-out. Blood samples drawn pre- and post- infusion were assessed for in vivo serum cytokines induction (IL-1β, IL-2, IL-6, IL-10, IL-12, TNF-α, GM-CSF and IFN-γ) whereas the impact of treatment on mononuclear cell subsets and their level of activation was tested ex vivo. Volunteers’ PBMC (peripheral blood monocnuclear cells) were stimulated in vitro with recall antigens and mitogen for cytokine production. At baseline, we performed in addition a cytokine release assay on PBMC upon stimulation with trastuzumab as a preclinical safety test. Results: Trastuzumab infusion induced a transient and weak peak of serum IL-6 at 6h, and a modulation of mononuclear cell subset profile and level of activation. Notably CD16+ cells frequency decreased at 3h and peaked at 48h. Except for CD8+ T cells, there were no significant differences between Herceptin and its proposed biosimilar ex vivo. PBMC stimulated in vitro with trastuzumab secreted IL-6, TNF-a, IL-1β, GM-CSF, IFN-γ, and IL-10, but no IL-2. There was no significant difference between the two mAbs. Conclusions: Based on these in vivo, ex vivo and in vitro experiments, there is a strong assumption that MYL-1401O is biosimilar to the reference drug Herceptin for its immunomodulation properties as already proven for its bioequivalence. Clinical trial information: 2011-001406-94.

scholarly journals In-vitro anti-diabetic activity and in-silico studies of binding energies of palmatine with alpha-amylase, alpha-glucosidase and DPP-IV enzymes

Pharmacia ◽  
2020 ◽  
Vol 67 (4) ◽  
pp. 363-371
Author(s):  
Patrick Okechukwu ◽  
Mridula Sharma ◽  
Wen Hui Tan ◽  
Hor Kuan Chan ◽  
Kavita Chirara ◽  
...  
Keyword(s):  
In Silico ◽  
Binding Energies ◽  
Alpha Amylase ◽  
Binding Interactions ◽  
Inhibiting Effect ◽  
Dpp Iv ◽  
In Silico Studies ◽  
Significant Difference ◽  
Alpha Glucosidase

Palmatine a protoberberine alkaloid has been previously reported to possess in vivo antidiabetic and antioxidant property. The aim of the experiment is to evaluate the in vitro antidiabetic activity and in-silico studies of the binding energies of Palmatine, acarbose, and Sitagliptin with the three enzymes of alpha-amylase, alpha-glucosidase, and dipeptidyl peptidase-IV (DPP-IV). The in vitro antidiabetic study was done by evaluating the inhibitory effect of palmatine on the activities of alpha-amylase, alpha-glucosidase, and DPP-IV. Acarbose, and sitagliptin was used as standard drug. The molecular docking study was performed to study the binding interactions of palmatine with alpha-glucosidase, a-amylase, and DPP-IV. The binding interactions were compared with the standard compounds Sitagliptin and acarbose. Palmatine with IC50 (1.31 ± 0.27 µM) showed significant difference of (< 0.0001) higher inhibiting effect on alpha-amylase and weak inhibiting effect on alpha-glucosidase enzyme with IC50 (9.39 ± 0.27 µM) and DPP-IV with IC50 (8.7 ± 1.82 µM). Palmatine possess inhibition effect on the three enzymes.

scholarly journals A SYNERGISTIC INSULINOTROPIC EFFECT OF GREEN TEA EXTRACT AND POMEGRANATE EXTRACT WITH ROSIGLITAZONE: BOTH IN VIVO AND IN VITRO EXPERIMENT

2020 ◽  
pp. 96-99
Author(s):  
REKHA S ◽  
CHANDRASHEKHARA S
Keyword(s):  
Green Tea ◽  
Type Ii Diabetes ◽  
Body Weight Gain ◽  
Serum Insulin ◽  
In Vivo Studies ◽  
Albino Rats ◽  
Type Ii ◽  
Insulinotropic Effect

Objective: Scientists have growing interest in traditional medicinal plants as they contain active ingredients for the treatment of various diseases. Tea is one of the most popular beverages worldwide. The variety of tea and tea extracts in the market has different polyphenol profiles, which are the bioactive chemical entities. We performed a direct comparison between Thea sinensis, green tea extracts (GTEs), and Punica granatum peel powder (PGPP), which have been chemically well characterized in a type II diabetic mouse model. Methods: We conducted both in vivo and in vitro experiments in the present paper. In vivo studies were carried out on male Swiss albino rats having type II diabetes, induced by single intravenous injection of streptozotocin (0.7 mg/Kg i.m.) and IDDM rats received either PGPP (200 mg/kg) or GTE (100 mg/kg) as a single oral dose. After the above result, the extracts were further subjected to know the effect of insulin secretion by RIN-5F cells providing confirmation of insulinotropic effect. Results: The results revealed that both PGPP and GTE substantially lowered blood glucose levels and ameliorated glucose intolerance, both were effective in antihyperglycemic activity and in lowering body weight gain. Serum insulin levels significantly increased in GTE group as well as in PGPP group, suggesting that they were exerting hypoglycemic effects through different pathways. Conclusion: Synergistic action of PGPP and GTE is an effective alternative for the treatment of type II diabetes through the regeneration of β cells of pancreas.

scholarly journals In vitro (anti-alpha-glucosidase) activity and in vivo anti-diabetic activity of Androsace foliosa (common rock jasmine) in alloxan-induced diabetic BALB/c mice

2019 ◽  
Vol 17 ◽  
pp. 205873921985742
Author(s):  
Jawad Zaheer ◽  
Qazi Najam-Us-Saqib ◽  
Misba Qamar ◽  
Muhammad Akram
Keyword(s):  
Body Weight ◽  
Inhibitory Concentration ◽  
Methanolic Extract ◽  
Type Ii ◽  
Standard Drug ◽  
Diabetes Mellitus Type Ii ◽  
Reduce Body Weight ◽  
Alpha Glucosidase

Androsace foliosa syn. Androsace sarmentosa (botanical name of common rock jasmine) ( Primulaceae) is used in the treatment various disorders. The aim of this study is to evaluate in vitro anti-diabetic activity of crude methanolic extract of leaves and roots of A. foliosa by anti -alpha-glucosidase (α-Glc) and in vivo anti-diabetic activity of n-hexane fraction on alloxan-induced diabetic mice. Results of in vitro anti-diabetic (α-Glc) activity showed that n-hexane leaves fraction was most potent among all the fractions and showed IC50 (half maximal inhibitory concentration) value of 64.91 ± 0.16 µg and % inhibition of 89.35 ± 0.45, comparable to that of standard acarbose. In vivo n-hexane leaves fraction decreases blood glucose level and reduces body weight similar to that of standard drug glibenclamide. Based on the conclusion of both in vitro and in vivo activities, it can be accomplished that the plant A. foliosa acquires noteworthy anti-diabetic action and can be used to treat diabetes mellitus type II and to reduce body weight.

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