scholarly journals In Vivo and In Vitro Antidiabetic Activity of Terminalia paniculata Bark: An Evaluation of Possible Phytoconstituents and Mechanisms for Blood Glucose Control in Diabetes

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Subramaniam Ramachandran ◽  
Aiyalu Rajasekaran ◽  
Natarajan Adhirajan

The present study was aimed to investigate in vivo, in vitro antidiabetic activity of aqueous extract of Terminalia paniculata bark (AETPB) and characterize its possible phytoconstituents responsible for the actions. Type 2 diabetes was induced in rats by streptozotocin-nicotinamide (65 mg/kg–110 mg/kg; i.p.) administration. Oral treatment of AETPB using rat oral needle at 100 and 200 mg/kg doses significantly () decreased blood glucose and glycosylated haemoglobin levels in diabetic rats than diabetic control rats. AETPB-treated diabetic rats body weight, total protein, insulin, and haemoglobin levels were increased significantly () than diabetic control rats. A significant () reduction of total cholesterol and triglycerides and increase in high-density lipoprotein levels were observed in type 2 diabetic rats after AETPB administration. Presence of biomarkers gallic acid, ellagic acid, catechin, and epicatechin in AETPB was confirmed in HPLC analysis. AETPB and gallic acid showed significant () enhancement of glucose uptake action in presence of insulin in muscle cells than vehicle control. Also AETPB inhibited pancreatic α-amylase and α-glucosidase enzymes. In conclusion, the above actions might be responsible for the antidiabetic activity of AETPB due to presence of gallic acid and other biomarkers.

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Mohamed Akram Melakhessou ◽  
Salah Eddine Marref ◽  
Naima Benkiki ◽  
Cherine Marref ◽  
Imene Becheker ◽  
...  

Abstract Background Diabetes mellitus is a serious complex multifactorial disorder that imposes huge health and economic burden on societies. Because the currently available medications have many drawbacks, it's important to look for alternative therapies. Medicinal plants utilized in folk medicine are ideal candidates. Therefore, this work assessed the antidiabetic action of n-butanol extract from the whole plant Atractylis flava Desf (BEAF). These ethnomedicinal properties of BEAF were scientifically validated using in vitro and in vivo assays. In vitro antidiabetic effect of the BEAF was conducted using α-Glucosidase and α-Amylase assays. While the antihyperglycemic activity was assessed using two rat models: Alloxan-induced diabetic rats and oral glucose challenged rats. Experimental diabetes was induced by a single intraperitoneal injection of alloxan at a dose of 150 mg/kg and animals with fasting blood glucose levels (BGL) > 200 mg/dL were considered diabetic. Glibenclamide (5 mg/kg) was used as a typical drug. Results The BEAF at all tested dose levels (100, 250, and 500 mg/kg) showed a significant decrease in blood glucose level in all the two animal models. Besides, the plant extract exhibited a potent inhibitory effect on α-Amylase and α-Glucosidase activity at a concentration of 1000 µg/mL with 76.17% and 89.37%, respectively. Conclusion BEAF exerts in vitro and in vivo antidiabetic effects, these results suggest that the plant extract can be a therapeutic resource in the treatment of diabetes and hyperlipidemia.


Author(s):  
Supriya Agnihotri ◽  
Gurvirender Singh ◽  
Santosh Kumar Verma

Looking at the increasing prevalence and inadequate treatments for diabetes mellitus, this study was carried to trace out hypoglycemic potentials of Typha elephantina leaves using in vitro and in vivo studies. α -amylase and α-glucosidase in vitro enzyme inhibition assay were incorporated to determine percent inhibition of Typha elephantina extracts. Typha elephantina methanol extract (TEME) at 125µg/ml in both α-amylase and α-glucosidase exhibited 57.48±1.42 and 53.64±0.92 percent inhibition in contrast to 66.7±0.94 and 70.31±1.25 of standard Acarbose, respectively. However, results obtained in Typha elephantina petroleum ether and chloroform extracts were insignificant. Further TEME antidiabetic properties were investigated by in vivo study, using Streptozotocin induced diabetic rats. Selected 250mg/kg and 500mg/kg doses of TEME were administered orally, which significantly (𝑃 < 0.001) reduces blood glucose of treated animals in contrast to diabetic control. 500mg/kg dose of TEME reduces blood glucose more efficiently. A significant linear rise of body weight and HDL were observed, while there was also remarkable reduction in cholesterol, TG, LDL, VLDL. Reduction in Liver function SGOT, SGPT along with creatinine and urea levels were observed in contrast to diabetic control group. In addition, antioxidant study of Typha elephantina extracts reflected significant results in comparison to that of ascorbic acid in DPPH and H2O2 assay. The whole study signified that Typha elephantina has hypoglycemic potentials.


2014 ◽  
Vol 92 (5) ◽  
pp. 405-417 ◽  
Author(s):  
Xian-Wei Li ◽  
Yan Liu ◽  
Wei Hao ◽  
Jie-Ren Yang

Sequoyitol decreases blood glucose, improves glucose intolerance, and enhances insulin signaling in ob/ob mice. The aim of this study was to investigate the effects of sequoyitol on diabetic nephropathy in rats with type 2 diabetes mellitus and the mechanism of action. Diabetic rats, induced with a high-fat diet and a low dose of streptozotocin, and were administered sequoyitol (12.5, 25.0, and 50.0 mg·(kg body mass)−1·d−1) for 6 weeks. The levels of fasting blood glucose (FBG), serum insulin, blood urea nitrogen (BUN), and serum creatinine (SCr) were measured. The expression levels of p22phox, p47phox, NF-κB, and TGF-β1 were measured using immunohistochemisty, real-time PCR, and (or) Western blot. The total antioxidative capacity (T-AOC), as well as the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) were also determined. The results showed that sequoyitol significantly decreased FBG, BUN, and SCr levels, and increased the insulin levels in diabetic rats. The level of T-AOC was significantly increased, while ROS and MDA levels and the expression of p22phox, p47phox, NF-κB, and TGF-β1 were decreased with sequoyitol treatment both in vivo and in vitro. These results suggested that sequoyitol ameliorates the progression of diabetic nephropathy in rats, as induced by a high-fat diet and a low dose of streptozotocin, through its glucose-lowering effects, antioxidant activity, and regulation of TGF-β1 expression.


2021 ◽  
Author(s):  
Heera Ram ◽  
Pramod Kumar ◽  
Ashok Purohit ◽  
Priya Kashyap ◽  
Suresh Kumar ◽  
...  

Abstract Context: Withania coagulans (Stocks) Dunal fruits are used in the therapeutics of several ailments due to possessing of potent phytoconstituents which is also used traditionally for curing the diabetes. Objective: The present study was assessing the amelioration potential of the phytochemicals of an ethanol fruit extract of Withania coagulans (Stocks) Dunal in the HOMA (Homeostatic model assessment) indices and pancreatic endocrinal tissues by inhibition of DPP-4 and antioxidants activities.Material and methods: The identification of phytoconstituents of the test extract was performed by LCMS. Further, assessments of in-vitro, in-vivo and in-silico were achieved by following standard methods. In-vivo studies were conducted on type-2 diabetic ratsResults: The chosen extract inhibited DPP-4 activity by 63.2% in an in vitro assay as well as significantly inhibit serum DPP-4 levels. Accordingly, the administration of the ethanol fruit extract resulted in a significant (𝑃≤ 0.001) alterations in the lipid profile, antioxidant levels, and HOMA indices. Moreover, pancreatic endocrinal tissues (islet of Langerhans) appeared to have the restoration of normal histoarchitecture as evidenced by increased cellular mass. Molecular docking (Protein - ligands) of identified phytoconstituents with DPP-4 (target enzyme) shown incredibly low binding energy (Kcal/mol) as required for ideal interactions. ADMET analysis of the pharmacokinetics of the identified phytoconstituents indicated an ideal profile as per Lipinski laws. Conclusion: It can be concluded that the phytoconstituents of an ethanol fruit extract of Withania coagulans have the potential to inhibit DPP-4 which result in improved glucose homeostasis and restoration of pancreatic endocrinal tissues in type-2 diabetic rats.


Author(s):  
KAMNI RAJPUT ◽  
RAMESH CHANDRA DUBEY

Objective: In vitro antioxidant activity, in vivo antidiabetic property and intestinal attachment by two potential probiotic bacterial strains, namely, Enterococcus faecium and Enterococcus hirae were studied using albino rats. Methods: Antioxidant the activity was assessed using 2,2-Diphenyl-1-picrylhydrazyl radicals scavenging assay. Alloxan was administered intraperitoneally to induce diabetic conditions in experimental rats. Animals were treated with oral administration of Enterococcus spp., such as E. faecium, and E. hirae isolated from goat and sheep milk. The control animal group received normal saline for the same days. Glibenclamide drug was used as a positive control against probiotic bacterial cells. Results: However, administration of probiotic bacterial strains E. faecium and E. hirae, in albino rats significantly (p<0.05) at varying doses lowered blood glucose levels in diabetic rats as compared to the diabetic control group. Both the species of Enterococcus increased the bodyweight of experimental rats. However, E. faecium was the best antidiabetic strain having the antioxidant activities also in comparison to E. hirae. The attachment of probiotic bacterial cells E. faecium on the rat’s intestine wall against pathogens was examined. Furthermore, E. faecium showed its aggregation with pathogens by attachment of the intestines of albino rats. This showed that both the bacterial strains exhibited in vivo antidiabetic effect. Conclusion: The results of this study showed that probiotic bacteria possess antioxidant, antidiabetic activities, and attachment of intestine.


2020 ◽  
Author(s):  
Heera Ram ◽  
Pramod Kumar ◽  
Ashok Purohit ◽  
Priya Kashyap ◽  
Suresh Kumar ◽  
...  

Abstract Context: Withania coagulans (Stocks) Dunal fruits are used in the therapeutics of several ailments due to possessing of potent phytoconstituents which is also used traditionally for curing the diabetes. Objective: The present study was assessing the amelioration potential of the phytochemicals of an ethanol fruit extract of Withania coagulans (Stocks) Dunal in the HOMA (Homeostatic model assessment) indices and pancreatic endocrinal tissues by inhibition of DPP-4 and antioxidants activities.Material and methods: The identification of phytoconstituents of phytochemicals of the test extract was performed by LCMS. Further, assessments of in-vitro, in-vivo and in-silico were achieved by following standard methods. In-vivo studies were conducted on type-2 diabetic ratsResults: The chosen extract inhibited DPP-4 activity by 63.2% in an in vitro assay. Accordingly, the administration of the ethanol fruit extract resulted in a significant (𝑃≤ 0.001) alterations in the lipid profile, antioxidant levels, and HOMA indices. Moreover, pancreatic endocrinal tissues (islet of Langerhans) appeared to have the restoration of normal histoarchitecture as evidenced by increased cellular mass. Molecular docking (Protein - ligands) of identified phytoconstituents with DPP-4 (target enzyme) shown incredibly low binding energy (Kcal/mol) as required for ideal interactions. ADMET analysis of the pharmacokinetics of the identified phytoconstituents indicated an ideal profile as per Lipinski laws. Conclusion: It can be concluded that the phytoconstituents of an ethanol fruit extract of Withania coagulans have the potential to inhibit DPP-4 which result in improved glucose homeostasis and restoration of pancreatic endocrinal tissues in type-2 diabetic rats.


2019 ◽  
Vol 20 (6) ◽  
pp. 1517 ◽  
Author(s):  
Kai Wang ◽  
Yu Su ◽  
Yuting Liang ◽  
Yanhui Song ◽  
Liping Wang

Type 2 diabetes mellitus (T2DM) is associated with pancreatic β-cell dysfunction which can be induced by oxidative stress. Deuterohemin-βAla-His-Thr-Val-Glu-Lys (DhHP-6) is a microperoxidase mimetic that can scavenge reactive oxygen species (ROS) in vivo. In our previous studies, we demonstrated an increased stability of linear peptides upon their covalent attachment to porphyrins. In this study, we assessed the utility of DhHP-6 as an oral anti-diabetic drug in vitro and in vivo. DhHP-6 showed high resistance to proteolytic degradation in vitro and in vivo. The degraded DhHP-6 product in gastrointestinal (GI) fluid retained the enzymatic activity of DhHP-6, but displayed a higher permeability coefficient. DhHP-6 protected against the cell damage induced by H2O2 and promoted insulin secretion in INS-1 cells. In the T2DM model, DhHP-6 reduced blood glucose levels and facilitated the recovery of blood lipid disorders. DhHP-6 also mitigated both insulin resistance and glucose tolerance. Most importantly, DhHP-6 promoted the recovery of damaged pancreas islets. These findings suggest that DhHP-6 in physiological environments has high stability against enzymatic degradation and maintains enzymatic activity. As DhHP-6 lowered the fasting blood glucose levels of T2DM mice, it thus represents a promising candidate for oral administration and clinical therapy.


2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Xiaofei Huang ◽  
Pan Weng ◽  
Huixin Zhang ◽  
Yingli Lu

Objective. As a complicated symbiotic system, intestinal flora is reported closely related to the development of type 2 diabetes recently. Sleeve gastrectomy is one of the approaches of bariatric surgery and could improve blood glucose control in type 2 diabetes patients. This study was to explore the relationship between remodeled intestinal flora and glucose metabolism in diabetic rats.Methods. 20 male diabetic rats were operated; 10 of them underwent sleeve gastrectomy, and 10 of them underwent sham operation. Meanwhile 10 male normal rats underwent sleeve gastrectomy as control. The animals’ weight and FBG had been measured. The composition changes of intestinal flora were detected by 16S rDNA sequence analysis.Results. In diabetic rats, weight and fasting blood glucose decreased significantly after sleeve gastrectomy. However, there was no significant change for weight and blood glucose in normal rats after operation. The intestinal flora of diabetic rats reduced in the proportion of Firmicutes and increased in the proportion of Bacteroidetes after sleeve gastrectomy.Conclusion. The change of dominant microorganisms in intestinal flora might play an important role in the glucose metabolism.


2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Rathinavelusamy Paramaguru ◽  
Papiya Mitra Mazumder ◽  
Dinakar Sasmal ◽  
Venkatesan Jayaprakash

The present study was designed to estimate the detailed antidiabetic activity ofPterospermum acerifolium(L.) Willd flowers.In vitroalpha amylase inhibition study was carried out on 50% ethanol extract of flowers (PAFEE) and its various fractions. The active ethyl acetate fraction (PAFEF) was subfractionated into three subfractions (PAFE1, PAFE2, and PAFE3) and subjected to acute toxicity studies followed by antidiabetic screeningin vivoby streptozotocin-nicotinamide induced type II diabetes. Diabetic animals treated with PAFE2 (30 mg/kg) reduced the levels of fasting blood glucose, significantly (P<0.001) compared to that of diabetic control animals. Histological studies on drug treated groups did not show remarkable positive changes inβ-cells. PAFE2 showed32.6±1.93% glucose uptake over control and, in the presence of PI3K inhibitor wortmannin, declined to13.7±2.51%. HPLC analysis of PAFE2 reveals the presence of quercetin and apigenin as major constituents and both are inhibiting the glycogen phosphorylase enzyme in molecular modelling studies. The study evidenced strongly that the probable glucose lowering mechanism of action of active subfraction PAFE2 is by increasing the glucose uptake in peripheral tissues and by inhibition of gluconeogenesis.


2020 ◽  
Vol 16 (1) ◽  
pp. 13-23
Author(s):  
Nazmina Vhora ◽  
Ujjal Naskar ◽  
Aishwarya Hiray ◽  
Abhijeet S. Kate ◽  
Alok Jain

BACKGROUND: A higher rate of attenuation of molecules in drug discovery has enabled pharmaceutical companies to enhance the efficiency of their hit identification and lead optimization. Selection and development of appropriate in-vitro and in-vivo strategies may improve this process as primary and secondary screening utilize both strategies. In-vivo approaches are too relentless and expensive for assessing hits. Therefore, it has become indispensable to develop and implement suitable in-vitro screening methods to execute the required activities and meet the respective targets. However, the selection of an appropriate in-vitro assay for specific evaluation of cellular activity is no trivial task. It requires thorough investigation of the various parameters involved. AIM: In this review, we aim to discuss in-vitro assays for type 2 diabetes (T2D), which have been utilized extensively by researchers over the last five years, including target-based, non-target based, low-throughput, and high-throughput screening assays. METHODS: The literature search was conducted using databases including Scifinder, PubMed, ScienceDirect, and Google Scholar to find the significant published articles. DISCUSSION and CONCLUSION: The accuracy and relevance of in-vitro assays have a significant impact on the drug discovery process for T2D, especially in assessing the antidiabetic activity of compounds and identifying the site of effect in high-throughput screening. The report reviews the advantages, limitations, quality parameters, and applications of the probed invitro assays, and compares them with one another to enable the selection of the optimal method for any purpose. The information on these assays will accelerate numerous procedures in the drug development process with consistent quality and accuracy.


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