scholarly journals Bornyl Derivatives of p-(Benzyloxy)Phenylpropionic Acid: In Vivo Evaluation of Antidiabetic Activity

2020 ◽  
Vol 13 (11) ◽  
pp. 404
Author(s):  
Sergey Kuranov ◽  
Olga Luzina ◽  
Mikhail Khvostov ◽  
Dmitriy Baev ◽  
Darya Kuznetsova ◽  
...  
Keyword(s):  
Computational Prediction ◽  
Tolerance Test ◽  
Antidiabetic Activity ◽  
Oral Glucose ◽  
In Vivo Evaluation ◽  
Phenylpropionic Acid ◽  
Biological Targets ◽  
Lipid Metabolism Disorders ◽  
Derivatives Of

A series of bornyl derivatives of p-(benzyloxy)phenylpropionic acid were prepared, and their hypoglycemic activities were examined by an oral glucose tolerance test in mice. The results of this test revealed two compounds, 1 and 3, that can reduce the blood level of glucose similarly to reference compound vildagliptin. Both compounds were tested in an experiment on mice with metabolic disorders: the C57BL/6Ay strain. Along with hypoglycemic properties, the two compounds showed different abilities to correct lipid metabolism disorders. In silico prediction revealed that the studied substances are most likely bifunctional multitarget hypoglycemic compounds whose mechanism of action is based on a pronounced reduction in insulin resistance and a strong incretin-mimetic effect. The difference in the size of effects of these compounds on biochemical parameters of blood in the experiment on C57BL/6Ay mice was in good agreement with the computational prediction of the priority ranking of biological targets for these compounds. These results indicate that bornyl derivatives of p-(benzyloxy)phenylpropionic acid have a good potential as new agents for diabetes mellitus treatment due to their hypoglycemic and lipid-normalizing properties.

scholarly journals Evaluation of Aqueous Extract of Alphonsea sclerocarpa for in vivo and in vitro Antidiabetic Potentials in Wistar Rats

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Ravi Shankar N ◽  
Ram Kishore ◽  
Puranik SB
Keyword(s):  
Blood Glucose ◽  
Glucose Uptake ◽  
Aqueous Extract ◽  
Insulin Level ◽  
Antidiabetic Activity ◽  
Albino Rats ◽  
Oral Glucose ◽  
In Vivo Evaluation

The purpose of current investigation was to investigate in vivo and in vitro anti-diabetic potentials of aqueous extract of Alphonsea sclerocarpa leaves against alloxan induced diabetes in albino rats. Two in vivo and one in vitro methods were performed for the evaluation of aqueous extract for antidiabetic activity. For in-vivo evaluation, diabetes was induced in albino rats by administering a single dose of alloxan. The study was designed to test the acute effect of aqueous extract of Alphonsea sclerocarpa (AEAS) to reduce blood glucose in OGTT. The chronic study of 21 days was performed against diabetic rats and blood glucose was determined at 1st , 7 th, 14th and 21st day. In chronic in vivo study, serum parameters insulin, urea, creatinine, total cholesterol, triglycerides, ALT and AST were also estimated at 21st day to determine the effects of aqueous and aqueous extracts on complications of diabetes mellitus. Glucose uptake by hemidiaphragm assay was performed to test the ability of extract to utilize glucose. In Oral Glucose Tolerance Test, standard glibenclamide and aqueous extract (200mg/kg and 400mg/kg) treated animals have shown significant reduction in blood glucose at 90 mins but at 120 mins. In chronic model the aqueous extract effectively reduced blood glucose levels (P<0.001) at 14th and 21st day of study in therapeutic groups and effect was comparable to that of standard. The extract could also significantly (P<0.001) reduce concentrations of SGOT, triglycerides, cholesterol and urea in serum and significantly (P<0.001) increased the insulin level in blood which proves beneficial effects of the extract in diabetes. The change in concentrations of SGPT and urea were less significant (P>0.01). The presence of extract in glucose uptake assay could significantly increase utilization of the glucose by rat hemidiaphragm. The aqueous extract of Alphonsea sclerocarpa possess significant antidiabetic properties against alloxan induced diabetic animals.

scholarly journals Antidiabetic Potential of Selected Medicinal Plants: A Literature Review

2021 ◽  
pp. 1-11
Author(s):  
Abdulrahman Altalhi ◽  
Mashhour Alsufyani ◽  
Khalid Alqurashi ◽  
Hussain Alshalwi ◽  
Abdullah Althobaiti ◽  
...  
Keyword(s):  
Plant Species ◽  
Scientific Evidence ◽  
Tolerance Test ◽  
Protein Glycation ◽  
Antidiabetic Activity ◽  
In Vivo Evaluation ◽  
Traditional Use ◽  
Alpha Glucosidase

Aims: To investigated for any scientific evidence indicating traditional use of different plant species in the management of diabetes. Study Design: Review Article. Place and Duration of Study: Conducted in Saudi Arabia from December 2020 to August 2021. Methodology: The literature was thoroughly investigated for any scientific evidence indicating traditional use of different plant species in the management of diabetes. The search was done in databases of Google Scholar, Saudi Digital Library and PubMed. Accordingly, the used plant species are classified into six groups. These are: Plants with antidiabetic activity, Plants with hypoglycemic activity, plants with alpha-glucosidase activity, Plants with alpha-amylase activity, Plants with glucose tolerance test, Plants with hypolipemic, anti-cholesterol, LDL and HDL activity. Conclusion: We have done in vitro and in vivo evaluation of M. arvensis L. for antidiabetic activity.  The leaves extracts of M. arvensis L. showed significant antioxidant potential and significantly inhibited protein glycation, which correlated well with its phenolics along with other phytoconstituents. the methanolic extract of M. arvensis L.

Antidiabetic Effects of Ethanolic Extract of Ficus glomerata (L.) Roots

2020 ◽  
Vol 16 (1) ◽  
pp. 33-41
Author(s):  
Mohini C. Upadhye ◽  
Uday Deokate ◽  
Rohini Pujari ◽  
Vishnu Thakare
Keyword(s):  
Body Weight ◽  
Glucose Tolerance ◽  
Density Lipoprotein ◽  
Ethanolic Extract ◽  
Tolerance Test ◽  
Diabetic Rats ◽  
Antidiabetic Activity ◽  
Control Group ◽  
Oral Glucose ◽  
Ficus Glomerata

Background: Ficus glomerata (F. glomerata) Linn. Family Moraceace is a large tree found all over India including outer Himalayan ranges, Punjab, Chota Nagpur, Bihar, Orissa, West Bengal, Rajasthan, Deccan and also as a common plant in South India. It is planted around the home and temples. It is cultivated throughout the year, distributed in evergreen forests and moist localities. Objective: The Ethanolic Extract of roots of F. Glomerata (EEFG) belonging to the family Moraceace, was investigated for its antidiabetic activity using alloxan induced diabetic rats. Methods: Thirty rats were divided into 5 groups having 6 rats in each group. The alloxan was administered to the rats of all groups except normal control group through intraperitoneal route at a concentration of 140mg/kg body weight. A dose of 100mg/kg and 200 mg/kg body weight of EEFG was administered to alloxan induced diabetic rats. The administration of the extract was lasted for 11 days. Effectiveness of the extract on glucose, cholesterol, triglycerides, and high density lipoprotein and protein concentrations was analyzed. Results: Significant (p<0.05) reduction in the levels of glucose, cholesterol, triglyceride of the diabetic rats was observed after treatment with ethanolic extract. After subjecting to oral glucose tolerance test EEFG also showed significant improvement in glucose tolerance. Conclusion: F. glomerata root ethanolic extract showed that it possesses antidiabetic effect and can be found useful for the management of diabetes mellitus.

scholarly journals Studies of insulin resistance in patients with clinical and subclinical hypothyroidism

2009 ◽  
Vol 160 (5) ◽  
pp. 785-790 ◽  
Author(s):  
Eirini Maratou ◽  
Dimitrios J Hadjidakis ◽  
Anastasios Kollias ◽  
Katerina Tsegka ◽  
Melpomeni Peppa ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Plasma Membrane ◽  
Glucose Transport ◽  
Subclinical Hypothyroidism ◽  
Tolerance Test ◽  
Oral Glucose ◽  
Model Assessment ◽  
Increased Risk

ObjectiveAlthough clinical hypothyroidism (HO) is associated with insulin resistance, there is no information on insulin action in subclinical hypothyroidism (SHO).Design and methodsTo investigate this, we assessed the sensitivity of glucose metabolism to insulin both in vivo (by an oral glucose tolerance test) and in vitro (by measuring insulin-stimulated rates of glucose transport in isolated monocytes with flow cytometry) in 21 euthyroid subjects (EU), 12 patients with HO, and 13 patients with SHO.ResultsAll three groups had comparable plasma glucose levels, with the HO and SHO having higher plasma insulin than the EU (P<0.05). Homeostasis model assessment index was increased in HO (1.97±0.22) and SHO (1.99±0.13) versus EU (1.27±0.16, P<0.05), while Matsuda index was decreased in HO (3.89±0.36) and SHO (4.26±0.48) versus EU (7.76±0.87, P<0.001), suggesting insulin resistance in both fasting and post-glucose state. At 100 μU/ml insulin: i) GLUT4 levels on the monocyte plasma membrane were decreased in both HO (215±19 mean fluorescence intensity, MFI) and SHO (218±24 MFI) versus EU (270±25 MFI, P=0.03 and 0.04 respectively), and ii) glucose transport rates in monocytes from HO (481±30 MFI) and SHO (462±19 MFI) were decreased versus EU (571±15 MFI, P=0.04 and 0.004 respectively).ConclusionsIn patients with HO and SHO: i) insulin resistance was comparable; ii) insulin-stimulated rates of glucose transport in isolated monocytes were decreased due to impaired translocation of GLUT4 glucose transporters on the plasma membrane; iii) these findings could justify the increased risk for insulin resistance-associated disorders, such as cardiovascular disease, observed in patients with HO or SHO.

scholarly journals Chronic peptide-based GIP receptor inhibition exhibits modest glucose metabolic changes in mice when administered either alone or combined with GLP-1 agonism

PLoS ONE ◽  
2021 ◽  
Vol 16 (3) ◽  
pp. e0249239
Author(s):  
Jason A. West ◽  
Anastasia Tsakmaki ◽  
Soumitra S. Ghosh ◽  
David G. Parkes ◽  
Rikke V. Grønlund ◽  
...  
Keyword(s):  
Glucose Tolerance ◽  
Fasting Blood Glucose ◽  
Chronic Administration ◽  
Dual Therapy ◽  
Tolerance Test ◽  
Oral Glucose ◽  
Beneficial Effects ◽  
Gut Hormone ◽  
Gip Receptor

Combinatorial gut hormone therapy is one of the more promising strategies for identifying improved treatments for metabolic disease. Many approaches combine the established benefits of glucagon-like peptide-1 (GLP-1) agonism with one or more additional molecules with the aim of improving metabolic outcomes. Recent attention has been drawn to the glucose-dependent insulinotropic polypeptide (GIP) system due to compelling pre-clinical evidence describing the metabolic benefits of antagonising the GIP receptor (GIPR). We rationalised that benefit might be accrued from combining GIPR antagonism with GLP-1 agonism. Two GIPR peptide antagonists, GIPA-1 (mouse GIP(3–30)NH2) and GIPA-2 (NαAc-K10[γEγE-C16]-Arg18-hGIP(5–42)), were pharmacologically characterised and both exhibited potent antagonist properties. Acute in vivo administration of GIPA-1 during an oral glucose tolerance test (OGTT) had negligible effects on glucose tolerance and insulin in lean mice. In contrast, GIPA-2 impaired glucose tolerance and attenuated circulating insulin levels. A mouse model of diet-induced obesity (DIO) was used to investigate the potential metabolic benefits of chronic dosing of each antagonist, alone or in combination with liraglutide. Chronic administration studies showed expected effects of liraglutide, lowering food intake, body weight, fasting blood glucose and plasma insulin concentrations while improving glucose sensitivity, whereas delivery of either GIPR antagonist alone had negligible effects on these parameters. Interestingly, chronic dual therapy augmented insulin sensitizing effects and lowered plasma triglycerides and free-fatty acids, with more notable effects observed with GIPA-1 compared to GIPA-2. Thus, the co-administration of both a GIPR antagonist with a GLP1 agonist uncovers interesting beneficial effects on measures of insulin sensitivity, circulating lipids and certain adipose stores that seem influenced by the degree or nature of GIP receptor antagonism.

The effect of melatonin on incretin hormones – results from experimental and randomized clinical studies

2021 ◽  
Author(s):  
Esben Stistrup Lauritzen ◽  
Julie Støy ◽  
Cecilie Bæch-Laursen ◽  
Niels Grarup ◽  
Niels Jessen ◽  
...  
Keyword(s):  
Insulin Secretion ◽  
Glucose Homeostasis ◽  
Tolerance Test ◽  
University Hospital ◽  
Oral Glucose ◽  
Incretin Hormones ◽  
Intravenous Glucose ◽  
In Situ Study

Abstract Context Glucose homeostasis is under circadian control through both endocrine and intracellular mechanisms with several lines of evidence suggesting that melatonin affects glucose homeostasis. Objective To evaluate the acute in-vivo and in-situ effects of melatonin on secretion of the incretin hormones, GLP-1 and GIP, and their impact on β-cell insulin secretion. Design A human randomized, double-blinded, placebo-controlled crossover study combined with a confirmatory in-situ study of perfused rat intestines. Setting Aarhus University Hospital. Methods: Fifteen healthy male participants were examined 2 x 2 times: An oral glucose tolerance test (OGTT) was performed on day one and an isoglycemic intravenous glucose infusion replicating the blood glucose profile of the OGTT day was performed on day two. These pairs of study days were repeated on treatment with melatonin and placebo, respectively. For the in-situ study, six rat intestines and four rat pancreases were perfused arterially with perfusion buffer ± melatonin. The intestines were concomitantly perfused with glucose through the luminal compartment. Results In humans, melatonin treatment resulted in reduced GIP secretion compared with placebo (ANOVA p=0.003), an effect also observed in the perfused rat intestines (ANOVA p=0.003) in which GLP-1 secretion also was impaired by arterial melatonin infusion (ANOVA p&lt;0.001). Despite a decrease in GIP levels, the in-vivo glucose-stimulated insulin secretion was unaffected by melatonin (p=0.78). Conclusion Melatonin reduced GIP secretion during an oral glucose challenge in healthy young men but did not affect insulin secretion. Reduced GIP secretion was confirmed in an in-situ model of the rat intestine.

scholarly journals Inhibition of α-Glucosidase, Intestinal Glucose Absorption, and Antidiabetic Properties by Caralluma europaea

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Hayat Ouassou ◽  
Touda Zahidi ◽  
Saliha Bouknana ◽  
Mohamed Bouhrim ◽  
Hassane Mekhfi ◽  
...  
Keyword(s):  
Ethyl Acetate Fraction ◽  
Inhibitory Effect ◽  
Tolerance Test ◽  
Glucose Absorption ◽  
Significant Inhibition ◽  
Oral Glucose ◽  
Glucosidase Activity ◽  
Intestinal Glucose Absorption

Many medicinal plants around the world are used for therapeutic purposes against several diseases, including diabetes mellitus. Due to their composition of natural substances that are effective and do not represent side effects for users, unlike synthetic drugs, in this study, we investigated the inhibitory effect of Caralluma europaea (CE) on α-glucosidase activity in vitro; then the kinetics of the enzyme were studied with increasing concentrations of sucrose in order to determine the inhibition type of the enzyme. In addition, this effect of Caralluma europaea (CE) was confirmed in vivo using rats as an experimental animal model. Among the five fractions of CE, only the ethyl acetate fraction of C. europaea (EACe) induced a significant inhibition of α-glucosidase and its inhibition mode was competitive. The in vivo studies were conducted on mice and rats using glucose and sucrose as a substrate, respectively, to determine the oral glucose tolerance test (OGTT). The results obtained showed that the EACe and the aqueous extract of C. europaea (AECe) have significantly reduced the postprandial hyperglycemia after sucrose and glucose loading in normal and diabetic rats. AECe, also, significantly decreased intestinal glucose absorption, in situ. The results obtained showed that Caralluma europaea has a significant antihyperglycemic activity, which could be due to the inhibition of α-glucosidase activity and enteric absorption of glucose.

Highly water-soluble derivatives of the anesthetic agent propofol: in vitro and in vivo evaluation of cyclic amino acid esters

2003 ◽  
Vol 20 (1) ◽  
pp. 17-26 ◽  
Author(s):  
Cosimo Altomare ◽  
Giuseppe Trapani ◽  
Andrea Latrofa ◽  
Mariangela Serra ◽  
Enrico Sanna ◽  
...  
Keyword(s):  
Amino Acid ◽  
Water Soluble ◽  
Anesthetic Agent ◽  
Amino Acid Esters ◽  
In Vivo Evaluation ◽  
Derivatives Of ◽  
Acid Esters
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