Antony Stalin
Loyola College, Chennai
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Featured researches published by Antony Stalin.
Biochimica et Biophysica Acta | 2013
Gopalsamy Rajiv Gandhi; Antony Stalin; K. Balakrishna; Savarimuthu Ignacimuthu; Michael Gabriel Paulraj; Rajagopal Vishal
BACKGROUND The present study was aimed at isolating an antidiabetic molecule from a herbal source and assessing its mechanism of action. METHODS Embelin, isolated from Embelia ribes Burm. (Myrsinaceae) fruit, was evaluated for its potential to regulate insulin resistance, alter β-cell dysfunction and modulate key markers involved in insulin sensitivity and glucose transport using high-fat diet (HFD) fed-streptozotocin (STZ) (40mg/kg)-induced type 2 diabetic rats. Molecular-dockings were performed to investigate the binding modes of embelin into PPARγ, PI3K, p-Akt and GLUT4 active sites. RESULTS Embelin (50mg/kg b wt.) reduced body weight gain, blood glucose and plasma insulin in treated diabetic rats. It further modulated the altered lipid profiles and antioxidant enzymes with cytoprotective action on β-cell. Embelin significantly increased the PPARγ expression in epididymal adipose tissue compared to diabetic control group; it also inhibited adipogenic activity; it mildly activated PPARγ levels in the liver and skeletal muscle. It also regulated insulin mediated glucose uptake in epididymal adipose tissue through translocation and activation of GLUT4 in PI3K/p-Akt signaling cascade. Embelin bound to PPARγ; it disclosed stable binding affinities to the active sites of PI3K, p-Akt and GLUT4. CONCLUSIONS These findings show that embelin could improve adipose tissue insulin sensitivity without increasing weight gain, enhance glycemic control, protect β-cell from damage and maintain glucose homeostasis in adipose tissue. GENERAL SIGNIFICANCE Embelin can be used in the prevention and treatment of type 2 diabetes mellitus caused due to obesity.
European Journal of Pharmacology | 2014
Gopalsamy Rajiv Gandhi; Gnanasekaran Jothi; Poovathumkal James Antony; K. Balakrishna; Michael Gabriel Paulraj; Savarimuthu Ignacimuthu; Antony Stalin; Naif Abdullah Al-Dhabi
In this study, the therapeutic efficacy of gallic acid from Cyamopsis tetragonoloba (L.) Taub. (Fabaceae) beans was examined against high-fat diet fed-streptozotocin-induced experimental type 2 diabetic rats. Molecular-dockings were done to determine the putative binding modes of gallic acid into the active sites of key insulin-signaling markers. Gallic acid (20 mg/kg) given to high-fat diet fed-streptozotocin-induced rats lowered body weight gain, fasting blood glucose and plasma insulin in diabetic rats. It further restored the alterations of biochemical parameters to near normal levels in diabetic treated rats along with cytoprotective action on pancreatic β-cell. Histology of liver and adipose tissues supported the biochemical findings. Gallic acid significantly enhanced the level of peroxisome proliferator-activated receptor γ (PPARγ) expression in the adipose tissue of treated rat compared to untreated diabetic rat; it also slightly activated PPARγ expressions in the liver and skeletal muscle. Consequently, it improved insulin-dependent glucose transport in adipose tissue through translocation and activation of glucose transporter protein 4 (GLUT4) in phosphatidylinositol 3-kinase (PI3K)/phosphorylated protein kinase B (p-Akt) dependent pathway. Gallic acid docked with PPARγ; it exhibited promising interactions with the GLUT4, glucose transporter protein 1 (GLUT1), PI3K and p-Akt. These findings provided evidence to show that gallic acid could improve adipose tissue insulin sensitivity, modulate adipogenesis, increase adipose glucose uptake and protect β-cells from impairment. Hence it can be used in the management of obesity-associated type 2 diabetes mellitus.
European Journal of Medicinal Chemistry | 2012
Rangachari Balamurugan; Antony Stalin; Savarimuthu Ignacimuthu
γ-sitosterol isolated from Lippia nodiflora was taken as ligand for molecular docking. The molecular targets, glucokinase, Fructose 1, 6- bisphosphatase 1, Human multidrug resistance protein 1 and Cytochromes P450 whose crystallographic structures are available on the PDB database as 1V4S, 2JJK, 3LC4, 2CBZ respectively, were used for the docking analysis using the Autodock tool v 4.2 and ADT v1.5.4 programs. The docking studies of the ligand γ- sitosterol with four different target proteins showed that this is a good molecule which docks well with various targets related to diabetes mellitus. Hence γ-sitosterol can be considered for developing into a potent antidiabetic drug.
Life Sciences | 2016
Antony Stalin; Santiagu Stephen Irudayaraj; Gopalsamy Rajiv Gandhi; K. Balakrishna; Savarimuthu Ignacimuthu; Naif Abdullah Al-Dhabi
AIMS This paper investigates the hypoglycemic activity of two derivatives of embelin (1) viz. 6-bromoembelin (2) and vilangin (3), in high-fat diet - STZ induced diabetic rats. MAIN METHODS The effects of 6-bromoembelin (2) and vilangin (3) on insulin resistance, β-cell dysfunction and glucose transport in high-fat diet (HFD) fed-streptozotocin (STZ) (40mg/kg) induced type 2 diabetic rats were evaluated. The binding modes of 6-bromoembelin (2) and vilangin (3) into PPARγ, PI3K, Akt, and GLUT4 were also studied using Autodock 4.2 and ADT 1.5.6 programs. KEY FINDINGS At the dose of 30mg/kg, the plasma glucose, plasma insulin and body weight were reduced by both embelin derivatives in diabetic rats. Additionally the altered lipid profiles and hexokinase, glucose-6-phosphatase and fructose-1,6-bisphosphatase levels were brought to normal. Compared to diabetic control group, there was a significant increase in the expression of PPARγ in epididymal adipose tissue. Inhibition of adipogenic activity and mild activation of PPARγ levels in the skeletal muscle and liver were observed. In epididymal adipose tissue, the compounds increased the insulin-mediated glucose uptake through the activation and translocation of GLUT4 in PI3K/p-Akt signaling cascade. SIGNIFICANCE The derivatives of embelin such as 6-bromoembelin (2) and vilangin (3) may be useful in the prevention and treatment of obesity-linked type 2 diabetes mellitus.
Biomedicine & Pharmacotherapy | 2017
Poovathumkal James Antony; Gopalsamy Rajiv Gandhi; Antony Stalin; K. Balakrishna; Erenius Toppo; Kuppusamy Sivasankaran; Savarimuthu Ignacimuthu; Naif Abdullah Al-Dhabi
Mimosa pudica Linn. (Mimosaceae) has been traditionally used for the management of type 2 diabetes mellitus (T2DM) in India. The present study evaluates the therapeutic efficacy of myoinositol (25 and 50mg/kg) isolated from M. pudica stem methanol extract in Triton WR-1339 induced hyperlipidemic and high-fat diet (HFD) fed-streptozotocin (STZ)-induced insulin-resistant diabetic rats. Lipid biomarkers, fasting blood glucose (FBG), changes in body weight, food and water intakes, plasma insulin, HOMA-IR, oral glucose tolerance, intraperitoneal insulin tolerance, urea, creatinine, marker enzymes of liver function, β-cell function and the expression levels of insulin receptor-induced signaling molecules were studied. Molecular-docking was also carried out to determine the possible interactions of myoinositol into the active sites of insulin-induced signaling markers. In addition, histology of liver, pancreas, kidney, heart and adipose tissues were also performed. In Triton WR-1339 induced hyperlipidemic rats, myoinositol (25 and 50mg/kg) exhibited significant reductions in total cholesterol: 37.5% and 59.73%, triglycerides: 57.75% and 80.14% and LDL-c: 81.44% and 101.75% respectively. HFD fed-STZ receiving myoinositol (25 and 50mg/kg) showed significant reductions in fasting blood glucose: 55.68% and 56.48%, plasma insulin level: 25.45% and 27.06% when compared with diabetic control. It significantly normalized the hyperglycemia induced biochemical abnormalities in insulin-resistant diabetic rats. Furthermore, it demonstrated cytoprotective effects besides increase in the intensity of positive reaction for insulin in pancreas. Myoinositol enhanced the level of PPARγ expression in the adipose tissue of treated rats when compared with rats that did not receive drug treatment; also, it significantly upregulated GLUT4 and IR signaling molecules. Myoinositol had predicted the interactions within the active sites of PPARγ, GLUT4 and IR. These findings suggested that myoinositol could play an effective role in glucose disposal into adipose tissue by insulin-dependent signaling cascade mechanism; hence it could be used in the treatment of obesity-associated T2DM.
Medicinal Chemistry Research | 2015
Rangachari Balamurugan; Antony Stalin; Adithan Aravinthan; Jong-Hoon Kim
A molecular docking analysis has been carried out to examine the hypolipidemic property of γ-sitosterol against five target proteins [acetoacetyl thiolase (PDB ID: 2 F2S), 3-(HMG-CoA) reductase (1DQ8), HMG-CoA synthase (PDB ID: 2P8U), squalene synthase (PDB ID: 3 V66, Oxido squalene cyclase (PDB ID: 1W6J)] which involved in cholesterol biosynthesis. The crystallographic structures of these target proteins were retrieved from PDB data base, and their active sites were identified by CastP server. The target proteins were subjected to docking analysis using Autodock tool v 4.2 and ADT v 1.5.6 programs. The docking studies showed that γ-sitosterol is a good and significant molecule which docks well with least lowest binding energy and inhibition constant values. Hence, γ-sitosterol can be considered for developing into a potent hypolipidemic agent.Graphical Abstract
Applied Biochemistry and Microbiology | 2015
C. Balachandran; Veeramuthu Duraipandiyan; Naif Abdullah Al-Dhabi; Antony Stalin; K. Balakrishna; Savarimuthu Ignacimuthu; F. Tilton
Anticancer activity of 9,10-anthraquinone isolated from soil-derived (Doddabetta forest, Nilgiris, Tamil Nadu, India) filamentous bacterium Streptomyces sp. isolate ERINLG-26 was tested to explore the molecular mechanisms of action. The culture liquid ethyl acetate extract showed high cytotoxic activity against tested colorectal adenocarcinoma cell line COLO320. The ethyl acetate extract was fractionated by column chromatography over silica gel and preparative HPLC. The isolated compound, 9,10-anthraquinone, showed prominent cytotoxic activity in vitro against colorectal adenocarcinoma cell line COLO320. It showed 79.7% cytotoxicity at concentration of compound 300 μg/mL with IC50 value of 75 μg/mL. Treatment of the COLO320 cancer cells with isolated 9,10-anthraquinone significantly reduced cell proliferation and increased formation of fragmented DNA and apoptotic bodies. The expression of p53 and caspase-3 was up-regulated by 9,10-anthraquinone in colorectal adenocarcinoma cell line COLO320.
Biomedicine & Pharmacotherapy | 2018
Erenius Toppo; S. Sylvester Darvin; S. Esakkimuthu; K. Buvanesvaragurunathan; T.P. Ajeesh Krishna; S. Antony Caesar; Antony Stalin; K. Balakrishna; P. Pandikumar; Savarimuthu Ignacimuthu; N.A. Al-Dhabi
The prevalence of Non Alcoholic Fatty Liver Disease (NAFLD) is increasing globally. Terminalia arjuna W. & Arn. (Combretaceae) is an endemic tree found in India and Sri Lanka and used traditionally for its cardioprotective and hepatoprotective effects. Arjunolic acid (AA) is an oleanane triterpenoid found mainly in the heartwood of T. arjuna. This study was aimed to evaluate the hepatoprotective effect of AA using cellular and rodent models of NAFLD. AA was isolated from the ethyl acetate extract of the heartwood of T. arjuna. The structure of AA was confirmed by physical and spectroscopic data. Steatosis was induced in HepG2 cells using palmitate-oleate mixture and the effects of AA on triglyceride accumulation and lipotoxicity were assessed. In vivo effect of AA on NAFLD was assessed using HFD fed rats. The treatment with AA did not affect the cell viability upto 100 μM and showed GI25 value of 379.9 μM in HepG2 cells. The treatment with AA significantly lowered the ORO concentration by 35.98% and triglyceride accumulation by 66.36% at 50 μM concentration (P < 0.005) compared to the vehicle treated group. The treatment with AA also reduced the leakage of ALT and AST by 61.11 and 48.29% in a significant manner (P < 0.005). The in vivo findings clearly demonstrated that the animals treated with AA at 25 and 50 mg/kg concentrations showed a significant decrease in the levels of transaminases, phosphatase and GGT (P < 0.005). In the liver, the expression of PPARα and FXRα expressions were upregulated, while PPARγ expression was downregulated by the treatment with AA. The liver histology of the animals showed reduction in steatosis and MNC infiltration. These preliminary evidences suggested that AA might be a promising lead to treat NAFLD. Future robust scientific studies on AA will lead to tailoring it for the treatment of NAFLD.
Food and Chemical Toxicology | 2014
Gopalsamy Rajiv Gandhi; Pautu Vanlalhruaia; Antony Stalin; Santiagu Stephen Irudayaraj; Savarimuthu Ignacimuthu; Michael Gabriel Paulraj
Chemico-Biological Interactions | 2016
Santiagu Stephen Irudayaraj; Antony Stalin; Christudas Sunil; Veeramuthu Duraipandiyan; Naif Abdullah Al-Dhabi; Savarimuthu Ignacimuthu