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Specialty: Drugs & Pharmacology
Condition: Diabetes

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Total 224 results found since Jan 2013.

Diacylglycerol Signaling Pathway in Pancreatic β-Cells: An Essential Role of Diacylglycerol Kinase in the Regulation of Insulin Secretion.
Abstract Diacylglycerol (DAG) is a lipid signal messenger and plays a physiological role in β-cells. Since defective glucose homeostasis increases de novo DAG synthesis, DAG may also contribute to β-cell dysfunction in type 2 diabetes. Although the primary function of DAG is to activate protein kinase C (PKC), the role of PKC in insulin secretion is controversial: PKC has been reported to act as both a positive and negative regulator of insulin secretion. In addition to the PKC pathway, DAG has also been shown to mediate other pathways such as the Munc-13-dependent pathway in β-cells. The intracellular levels o...
Source: Biological and Pharmaceutical Bulletin - May 9, 2015 Category: Drugs & Pharmacology Authors: Kaneko YK, Ishikawa T Tags: Biol Pharm Bull Source Type: research

Myricetin inhibits advanced glycation end product (AGE)-induced migration of retinal pericytes through phosphorylation of ERK1/2, FAK-1, and paxillin in vitro and in vivo.
In this study, we investigated the pathological mechanisms of AGE on the migration of retinal pericytes and confirmed the inhibitory effect of myricetin on migration in vitro and in vivo. Migration assays of bovine retinal pericytes (BRP) were induced using AGE-BSA and phosphorylation of Src, ERK1/2, focal adhesion kinase (FAK-1) and paxillin were determined using immunoblot analysis. Sprague-Dawley rats (6 weeks old) were injected intravitreally with AGE-BSA and morphological and immunohistochemical analysis of p-FAK-1 and p-paxillin were performed in the rat retina. Immunoblot analysis and siRNA transfection were used to...
Source: Biochemical Pharmacology - October 22, 2014 Category: Drugs & Pharmacology Authors: Kim YS, Kim J, Kim KM, Jung DH, Choi S, Kim CS, Kim JS Tags: Biochem Pharmacol Source Type: research

PPARβ activation restores the high glucose‐induced impairment of insulin signalling in endothelial cells
Conclusion and ImplicationsPPARβ activation in vitro and in vivo restores the endothelial function, preserving the insulin‐Akt‐eNOS pathway impaired by high glucose, at least in part, through PDK4 activation.
Source: British Journal of Pharmacology - May 27, 2014 Category: Drugs & Pharmacology Authors: A M Quintela, R Jiménez, L Piqueras, M Gómez‐Guzmán, J Haro, M J Zarzuelo, A Cogolludo, M J Sanz, M Toral, M Romero, F Pérez‐Vizcaíno, J Duarte Tags: RESEARCH PAPER Source Type: research

Peroxisome proliferator‐activated receptor‐β activation restores the high glucose‐induced impairment of insulin signaling in endothelial cells
Conclusions And ImplicationsPPAR‐β activation in vitro and in vivo restores the endothelial function, preserving the insulin‐Akt‐eNOS pathway impaired by high glucose, at least in part, through PDK4 activation.
Source: British Journal of Pharmacology - February 16, 2014 Category: Drugs & Pharmacology Authors: A M Quintela, R Jiménez, L Piqueras, M Gómez‐Guzmán, J Haro, M J Zarzuelo, A Cogolludo, M J Sanz, M Toral, M Romero, F Pérez‐Vizcaíno, J Duarte Tags: Research Paper Source Type: research

Marine natural product des-O-methyllasiodiplodin effectively lowers the blood glucose level in db/db mice via ameliorating inflammation.
Conclusion:DML effectively lowers the blood glucose level in db/db mice possibly via ameliorating the expression of obesity-related pro-inflammatory cytokines, highlighting the potential of the marine natural product as a drug lead for the treatment of metabolic disorders. PMID: 23852084 [PubMed - as supplied by publisher]
Source: Acta Pharmacologica Sinica - July 15, 2013 Category: Drugs & Pharmacology Authors: Zhou R, Lin ZH, Jiang CS, Gong JX, Chen LL, Guo YW, Shen X Tags: Acta Pharmacol Sin Source Type: research

Glycolaldehyde induces cytotoxicity and increases glutathione and multidrug-resistance-associated protein levels in schwann cells.
Abstract Schwann cell injury is observed in diabetic neuropathy. It is speculated that glycolaldehyde (GA), a precursor of advanced glycation end products (AGEs), contributes to the pathogenesis and development of diabetic neuropathy. Here, we demonstrated for the first time that GA at near-physiological concentration decreased the viability of rat Schwann cells. In contrast, methylglyoxal, glyoxal, and 3-deoxyglucosone, all of which are AGE precursors, had no effects on cell viability. It is well known that methylglyoxal causes oxidative damage. In the present study, however, GA failed to induce reactive oxygen s...
Source: Biological and Pharmaceutical Bulletin - July 6, 2013 Category: Drugs & Pharmacology Authors: Sato K, Tatsunami R, Yama K, Tampo Y Tags: Biol Pharm Bull Source Type: research

Quercetin and allopurinol reduce liver thioredoxin‐interacting protein to alleviate inflammation and lipid accumulation in diabetic rats
Conclusions and ImplicationsInhibition of hepatic TXNIP by quercetin and allopurinol contributes to the reduction in liver inflammation and lipid accumulation under hyperglycaemic conditions. The targeting of hepatic TXNIP by quercetin and allopurinol may have therapeutic implications for prevention of type 1 diabetes‐associated NAFLD.
Source: British Journal of Pharmacology - June 21, 2013 Category: Drugs & Pharmacology Authors: Wei Wang, Chuang Wang, Xiao‐Qin Ding, Ying Pan, Ting‐Ting Gu, Ming‐Xing Wang, Yang‐Liu Liu, Fu‐Meng Wang, Shui‐Juan Wang, Ling‐Dong Kong Tags: Research Paper Source Type: research

Quercetin and Allopurinol Reduce Liver Thioredoxin‐Interacting Protein to Improve Inflammation and Lipid Accumulation in Diabetic Rats
Conclusions and ImplicationsThese results demonstrate that hepatic TXNIP inhibition by quercetin and allopurinol contributes to the improvement of liver inflammation and lipid accumulation under hyperglycemia condition. Therefore, quercetin and allopurinol targeting hepatic TXNIP may have therapeutic application to prevent type 1 diabetes‐associated NAFLD.
Source: British Journal of Pharmacology - May 3, 2013 Category: Drugs & Pharmacology Authors: Wei Wang, Chuang Wang, Xiao‐Qin Ding, Ying Pan, Ting‐Ting Gu, Ming‐Xing Wang, Yang‐Liu Liu, Fu‐Meng Wang, Shui‐Juan Wang, Ling‐Dong Kong Tags: Research Paper Source Type: research

Inhibitory Cross‐talk between the AMPK and ERK pathways mediates endoplasmic reticulum stress‐induced insulin resistance in skeletal muscle
Conclusions And ImplicationsInhibition of ERK signaling pathways by a chemical inhibitor and knockdown of ERK improved AMPK and Akt signalings and reversed ER stress‐induced insulin resistance in L6 myotubes. These findings suggest that ERK signaling plays an important role in the regulation of insulin signals in muscle cells under ER stress.
Source: British Journal of Pharmacology - February 4, 2013 Category: Drugs & Pharmacology Authors: Seung‐Lark Hwang, Yong‐Tae Jeong, Xian Li, Yong Deuk Kim, Lu Yue, Young‐Chae Chang, In‐Kyu Lee, Hyeun Wook Chang Tags: Research Paper Source Type: research

Metformin Induces Cytotoxicity by Down‐Regulating Thymidine Phosphorylase and ERCC1 Expression in Non‐Small Cell Lung Cancer Cells
In conclusion, metformin induces cytotoxicity by down‐regulating TP and ERCC1 expression in NSCLC cells.
Source: Basic and Clinical Pharmacology and Toxicology - January 31, 2013 Category: Drugs & Pharmacology Authors: Jen‐Chung Ko, Yu‐Ching Huang, Huang‐Jen Chen, Sheng‐Chieh Tseng, Hsien‐Chun Chiu, Ting‐Yu Wo, Yi‐Jhen Huang, Shao‐Hsing Weng, Robin Y.Y. Chiou, Yun‐Wei Lin Tags: Original Article Source Type: research

Elevated transcriptional co-activator p102 mediates angiotensin II type 1 receptor up-regulation and extracellular matrix overproduction in the high glucose-treated rat glomerular mesangial cells and isolated glomeruli.
Abstract P102 is a multifunctional transcriptional co-activator. This experiment is designed to investigate the role of p102 in the activation of renin-angiotensin system (RAS) and sequentially extracellular matrix (ECM) over synthesis in diabetic nephropathy. Rat glomerular mesangial cells (MCs) or isolated glomeruli were cultured in normal glucose (NG, 5.5mM) or high glucose (HG, 25mM) DMEM. The generation of reactive oxygen species was measured by 2',7'-Dichlorodihydrofluorescein diacetate (DCFH-DA) fluorescent probe assay. The protein levels were analyzed by Western blot and the mRNA levels were evaluated by r...
Source: European Journal of Pharmacology - January 30, 2013 Category: Drugs & Pharmacology Authors: Wang Z, Ni J, Shao D, Liu J, Shen Y, Zhou L, Huang Y, Yu C, Wang J, Xue H, Lu L Tags: Eur J Pharmacol Source Type: research

Ginkgo biloba Extract Reduces High-Glucose-Induced Endothelial Reactive Oxygen Species Generation and Cell Adhesion Molecule Expression by Enhancing HO-1 Expression via Akt/eNOS and P38 MAP Kinase Pathways.
CONCLUSION: GBE could reduce high glucose-induced endothelial adhesion via enhancing HO-1 expression through the Akt/eNOS and P38/MAPK pathways. Our findings suggest a potential strategy targeting on HO-1 induction by GBE for endothelial protection in the presence of high glucose such as that in diabetes mellitus. PMID: 23357604 [PubMed - as supplied by publisher]
Source: European Journal of Pharmaceutical Sciences - January 25, 2013 Category: Drugs & Pharmacology Authors: Tsai HY, Huang PH, Lin FY, Chen JS, Lin SJ, Chen JW Tags: Eur J Pharm Sci Source Type: research

AMP-Activated Protein Kinase as Regulator of P2Y6 Receptor-Induced Insulin Secretion in Mouse Pancreatic β-Cells.
Abstract 5'-AMP-activated protein kinase (AMPK) and its pharmacological modulators have been targeted for treating type 2 diabetes. Extracellular uridine 5'-diphosphate (UDP) activates P2Y(6) receptors (P2Y(6)Rs) in pancreatic β-cells to release insulin and reduce apoptosis, which would benefit diabetes. Here, we studied the role of P2Y(6)R in activation of AMPK in MIN6 mouse pancreatic β-cells and insulin secretion. Treatment with a potent P2Y(6)R dinucleotide agonist MRS2957 (500nM) activated AMPK, which was blocked by P2Y(6)R-selective antagonist MRS2578. Also, MRS2957 induced phosphorylation of acetyl-coenzy...
Source: Biochemical Pharmacology - January 17, 2013 Category: Drugs & Pharmacology Authors: Balasubramanian R, Maruoka H, Jayasekara MP, Gao ZG, Jacobson KA Tags: Biochem Pharmacol Source Type: research

Metformin-mediated downregulation of p38 mitogen-activated protein kinase-dependent excision repair cross-complementing 1 decreases DNA repair capacity and sensitizes human lung cancer cells to paclitaxel.
Abstract Metformin, an extensively used and well-tolerated drug for treating individuals with type 2 diabetes, has recently gained significant attention as an anticancer drug. On the other hand, paclitaxel (Taxol) is a new antineoplastic drug that has shown promise in the treatment of non-small cell lung cancer (NSCLC). High expression levels of excision repair cross-complementary 1 (ERCC1) in cancers have been positively associated with the DNA repair capacity and a poor prognosis in NSCLC patients treated with platinum-containing chemotherapy. In this current study, paclitaxel was found to increase phosphorylati...
Source: Biochemical Pharmacology - December 7, 2012 Category: Drugs & Pharmacology Authors: Tseng SC, Huang YC, Chen HJ, Chiu HC, Huang YJ, Wo TY, Weng SH, Lin YW Tags: Biochem Pharmacol Source Type: research