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Kumar P.M.,Padmashree Institute of Management and Sciences | Venkataranganna M.V.,Connexios Life science Pvt Ltd | Manjunath K.,Bangalore University | Ashok G.,Radiant Research Services Pvt Ltd.
Chinese Journal of Natural Medicines | Year: 2014

The present study was undertaken to evaluate the influence of the methanolic fruit extract of Momordica cymbalaria (MFMC) on PPARγ (Peroxisome Proliferator Activated Receptor gamma) and GLUT-4 (Glucose transporter-4) with respect to glucose transport. Various concentrations of MFMC ranging from 62.5 to 500 μg·mL-1 were evaluated for glucose uptake activity in vitro using L6 myotubes, rosiglitazone was used as a reference standard. The MFMC showed significant and dose-dependent increase in glucose uptake at the tested concentrations, further, the glucose uptake activity of MFMC (500 μg·mL-1) was comparable with rosigilitazone. Furthermore, MFMC has shown up-regulation of GLUT-4 and PPARγ gene expressions in L6 myotubes. In addition, the MFMC when incubated along with cycloheximide (CHX), which is a protein synthesis inhibitor, has shown complete blockade of glucose uptake. This indicates that new protein synthesis is required for increased GLUT-4 translocation. In conclusion, these findings suggest that MFMC is enhancing the glucose uptake significantly and dose dependently through the enhanced expression of PPARγ and GLUT-4 in vitro. © 2014 China Pharmaceutical University.


PubMed | Padmashree Institute of Management and Sciences, Bangalore University, Connexios Life science Pvt. Ltd. and Radiant Research Services Pvt. Ltd.
Type: Journal Article | Journal: Journal of intercultural ethnopharmacology | Year: 2016

The present study was undertaken to evaluate the effect of methanolic leaf extract of Gymnema sylvestre (MLGS) on glucose transport (GLUT) and insulin resistance in vitro.Peroxisome proliferator-activated receptor-gamma (PPAR-) and GLUT-4 expression were assessed in L6 myotubes for concluding the GLUT activity, and adiponectin and leptin expression was studied in 3T3 L1 murine adipocyte cell line to determine the effect of MLGS (250-750 g/ml) on insulin resistance.The findings of the experiments have demonstrated a significant and dose-dependent increase in glucose uptake in all the tested concentrations of MLGS, further the glucose uptake activity of MLGS (750 g/ml) was at par with rosiglitazone (50 g/ml). Concomitantly, MLGS has shown enhanced GLUT-4 and PPAR- gene expressions in L6 myotubes. Furthermore, cycloheximide (CHX) had completely abolished the glucose uptake activity of MLGS when co-incubated, which further confirmed that glucose uptake activity of MLGS was linked to enhanced expression of GLUT-4 and PPAR-. In addition, in another experimental set, MLGS showed enhanced expression of adiponectin and leptin, thus confirms the ameliorative effect of MLGS on insulin resistance.These findings suggest that MLGS has an enhanced glucose uptake activity in L6 myotubes, and ameliorate the insulin resistance in 3T3 L1 murine adipocyte cell line in vitro.


Baliga M.S.,Father Muller Hospital Road | Joseph N.,Father Muller Hospital Road | Venkataranganna M.V.,Connexios Life science Pvt Ltd | Saxena A.,University of South Carolina | And 2 more authors.
Food and Function | Year: 2012

Inflammatory bowel disease (IBD) comprising of ulcerative colitis (UC) and Crohn's disease (CD) is a major ailment affecting the small and large bowel. In clinics, IBD is treated using 5-amninosalicylates, antibiotics, the steroids and immunomodulators. Unfortunately, the long term usages of these agents are associated with undue side effects and compromise the therapeutic advantage. Accordingly, there is a need for novel agents that are effective, acceptable and non toxic to humans. Preclinical studies in experimental animals have shown that curcumin, an active principle of the Indian spice turmeric (Curcuma longa Linn) is effective in preventing or ameliorating UC and inflammation. Over the last few decades there has been increasing interest in the possible role of curcumin in IBD and several studies with various experimental models of IBD have shown it to be effective in mediating the inhibitory effects by scavenging free radicals, increasing antioxidants, influencing multiple signaling pathways, especially the kinases (MAPK, ERK), inhibiting myeloperoxidase, COX-1, COX-2, LOX, TNF-α, IFN-γ, iNOS; inhibiting the transcription factor NF-κB. Clinical studies have also shown that co-administration of curcumin with conventional drugs was effective, to be well-tolerated and treated as a safe medication for maintaining remission, to prevent relapse and improve clinical activity index. Large randomized controlled clinical investigations are required to fully understand the potential of oral curcumin for treating IBD. This journal is © The Royal Society of Chemistry.


Venkatarangana M.,Connexios Life science Pvt Ltd
Journal of Functional Foods | Year: 2015

Standardization is an essential step in the development of nutraceutical based formulations or products. The objective of the present study was to exemplify screening standardization of the potent antioxidant nutraceuticals (generic), namely curcumin, quercetin, hesperidin, gallic acid, citric acid, L-ascorbic acid, phytic acid and α-tocopherol based on ferric reducing antioxidant power (FRAP) value and also tried to justify the reliability of two different designs of experiments i.e. Plackett-Burman fold-over design and Taguchi L18 in screening related experiments. First screening of antioxidant nutraceutical was performed by Plackett-Burman fold-over design (resolution IV) and the outcome was analysed based on Pareto chart of standardized effect where the quercetin, gallic acid and curcumin have shown p value of <0.05 and the same factors were found to be positive outliner in half normal probability analysis. Further, the results were validated using factorial Taguchi orthogonal array, based on SN ratio (maximum the best response). Both statistical designs have given the same order of potency based on FRAP value as: quercetin > gallic acid > curcumin. Therefore it can be concluded that the statistical design of experiments is reliable in screening related experiments for development of nutraceutical formulations or products. © 2015 Elsevier Ltd.


The present invention relates to certain amide derivatives that have the ability to inhibit 11--hydroxysteroid dehydrogenase type 1 (11-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.


Patent
Connexios Life science Pvt. Ltd. | Date: 2013-06-19

The embodiments disclosed here in relates to use of activators of ADSL for the production of pharmaceutical agents to achieve glycemic control in mammals and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this enzyme.


Gogna N.,Indian Institute of Science | Krishna M.,Connexios Life science Pvt. Ltd. | Oommen A.M.,Connexios Life science Pvt. Ltd. | Dorai K.,Indian Institute of Science
Molecular BioSystems | Year: 2015

It is well known that obesity/high body mass index (BMI) plays a key role in the evolution of insulin resistance and type-2 diabetes mellitus (T2DM). However, the exact mechanism underlying its contribution is still not fully understood. This work focuses on an NMR-based metabolomic investigation of the serum profiles of diabetic, obese South Indian Asian subjects. 1H 1D and 2D NMR experiments were performed to profile the altered metabolic patterns of obese diabetic subjects and multivariate statistical methods were used to identify metabolites that contributed significantly to the differences in the samples of four different subject groups: diabetic and non-diabetic with low and high BMIs. Our analysis revealed that the T2DM-high BMI group has higher concentrations of saturated fatty acids, certain amino acids (leucine, isoleucine, lysine, proline, threonine, valine, glutamine, phenylalanine, histidine), lactic acid, 3-hydroxybutyric acid, choline, 3,7-dimethyluric acid, pantothenic acid, myoinositol, sorbitol, glycerol, and glucose, as compared to the non-diabetic-low BMI (control) group. Of these 19 identified significant metabolites, the levels of saturated fatty acids, lactate, valine, isoleucine, and phenylalanine are also higher in obese non-diabetic subjects as compared to control subjects, implying that this set of metabolites could be identified as potential biomarkers for the onset of diabetes in subjects with a high BMI. Our work validates the utility of NMR-based metabolomics in conjunction with multivariate statistical analysis to provide insights into the underlying metabolic pathways that are perturbed in diabetic subjects with a high BMI. © The Royal Society of Chemistry 2015.


Patent
Connexios Life science Pvt. Ltd. | Date: 2013-12-05

The present invention relates to use of inhibitors of TAK-1 for the production of pharmaceutical agents to achieve glycemic control in mammals and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme.


Patent
CONNEXIOS LIFE science PVT. LTD. | Date: 2012-12-21

The present invention relates to certain amide derivatives that have the ability to inhibit 11--hydroxysteroid dehydrogenase type 1 (11-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.


Patent
CONNEXIOS LIFE science PVT. LTD. | Date: 2015-01-09

The present invention relates to certain substituted bicyclic compounds that are agonists of RXR and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders.

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