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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

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

Berberine induces GLP-1 secretion through activation of bitter taste receptor pathways.
This study was designed to ascertain whether berberine-induced secretion of GLP-1 was related with activation of bitter taste receptors expressed in gastrointestinal tract. Western blotting results showed that TAS2R38, a subtype of bitter taste receptor, was expressed on human enteroendocrine NCI-H716 cells. GLP-1 secretion induced by berberine from NCI-H716 cells was inhibited by incubation with anti-TAS2R38 antibody. We further performed gene silencing using siRNA to knockdown TAS2R38 from NCI-H716 cells, which showed that siRNA knockdown of the TAS2R38 reduced berberine-mediated GLP-1 secretion. We adopted inhibitors of...
Source: Biochemical Pharmacology - July 20, 2015 Category: Drugs & Pharmacology Authors: Yu Y, Hao G, Zhang Q, Hua W, Wang M, Zhou W, Zong S, Huang M, Wen X Tags: Biochem Pharmacol Source Type: research

Wnt/ β-catenin signaling plays an essential role in α7 nicotinic receptor-mediated neuroprotection of dopaminergic neurons in a mouse Parkinson's disease model.
The objective of the present study was to explore the potential functions of α7-nAChRs in PD pathology, and to determine whether these effects are exerted via Wnt/β-catenin signaling in a mouse PD model. In the in vivo study, α7-nAChR knockout (α7-KO) reversed the beneficial effects of nicotine on motor deficits, dopaminergic neuron loss, astrocyte and microglia activation, and reduced striatal dopamine release induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. Injury to SH-SY5Y cells by 1-methyl-4-phenylpyridinium treatment was also ameliorated by nicotine, and this effect was abolished by methyllycaconitine (ML...
Source: Biochemical Pharmacology - May 24, 2017 Category: Drugs & Pharmacology Authors: Liu Y, Hao S, Yang B, Fan Y, Qin X, Chen Y, Hu J Tags: Biochem Pharmacol Source Type: research

The Neurotoxicant PCB-95 By Increasing the Neuronal Transcriptional Repressor REST Down-Regulates Caspase-8 and Increases Ripk1, Ripk3 and Mlkl Expression Determining Necroptotic Neuronal Death.
Abstract Our previous study showed that the environmental neurotoxicant non-dioxin-like polychlorinated biphenyl (PCB)-95 increases RE1-Silencing Transcription Factor (REST) expression, which is related to necrosis, but not apoptosis, of neurons. Meanwhile, necroptosis is a type of a programmed necrosis that is positively regulated by receptor interacting protein kinase 1 (RIPK1), RIPK3 and mixed lineage kinase domain-like (MLKL) and negatively regulated by caspase-8. Here we evaluated whether necroptosis contributes to PCB-95-induced neuronal death through REST up-regulation. Our results demonstrated that in cort...
Source: Biochemical Pharmacology - July 1, 2017 Category: Drugs & Pharmacology Authors: Guida N, Laudati G, Serani A, Mascolo L, Molinaro P, Montuori P, Di Renzo G, Mt Canzoniero L, Formisano L Tags: Biochem Pharmacol Source Type: research

Heme oxygenase-1 induction by rosiglitazone via PKC α/AMPKα/p38 MAPKα/SIRT1/PPARγ pathway suppresses lipopolysaccharide-mediated pulmonary inflammation.
In this study, we found that upregulation of HO-1 in vitro or in vivo by rosiglitazone attenuated VCAM-1 gene expression and monocyte adhesion to HPAEpiCs challenged with lipopolysaccharide (LPS). The inhibitory effects of rosiglitazone on LPS-mediated responses were reversed by transfection with HO-1 siRNA. LPS-induced VCAM-1 expression was mediated through NF-κB activation which was attenuated by rosiglitazone via suppressing p65 activation and translocation into the nucleus. Moreover, pretreatment with the inhibitor of PKCs (H7), PKCα (Gö6976), AMPKα (Compound C), p38 MAPKα (p38i VIII), SIRT1 (Sirtinol), or PPARγ ...
Source: Biochemical Pharmacology - January 5, 2018 Category: Drugs & Pharmacology Authors: Cho RL, Lin WN, Wang CY, Yang CC, Hsiao LD, Lin CC, Yang CM Tags: Biochem Pharmacol Source Type: research

FCPR03, a novel phosphodiesterase 4 inhibitor, alleviates cerebral ischemia/reperfusion injury through activation of the AKT/GSK3 β/ β-catenin signaling pathway.
This study aimed to investigate the effects of FCPR03 on neuronal injury after cerebral ischemia/reperfusion and the underlying signaling pathway. The effects of FCPR03 on cellular apoptosis, intracellular accumulation of reactive oxygen species (ROS), and mitochondrial membrane potential (MMP) were evaluated in HT-22 neuronal cells and cortical neurons exposed to oxygen-glucose deprivation (OGD). The impact of FCPR03 on brain injury, neurological scores and behavioral performance was investigated in rats subjected to middle cerebral artery occlusion (MCAO). The protein kinase B (AKT) inhibitor MK-2206 and β-catenin siRNA...
Source: Biochemical Pharmacology - February 21, 2019 Category: Drugs & Pharmacology Authors: Xu B, Wang T, Xiao J, Dong W, Wen HZ, Wang X, Qin Y, Cai N, Zhou Z, Xu J, Wang H Tags: Biochem Pharmacol Source Type: research

Systemic delivery of Eg5 shRNA-expressing plasmids using PEGylated DC-Chol/DOPE cationic liposome: long-term silencing and anticancer effects in vivo.
Abstract Duration of gene silencing due to the short-term silencing effects induced by exogenous siRNA have limited the therapeutic applications of RNAi and the development of RNAi-based therapeutics. We here generated Eg5 shRNA-expressing plasmids using the inverted terminal repeats (ITRs) sequences to produce Eg5 hairpin RNA under the control of U6 promoter. Using PEGylated DC-Chol/DOPE cationic liposomes, we demonstrated that a single systemic administration of Eg5 shRNA-expressing plasmid/liposome lipoplexes induced the long-term Eg5 silencing in the tumor sites of tumor-bearing mice, and ultimately lead to mo...
Source: Biochemical Pharmacology - May 22, 2019 Category: Drugs & Pharmacology Authors: Seraj S, Lee J, Ahn HJ Tags: Biochem Pharmacol Source Type: research

α-Linolenic acid inhibits the migration of human triple-negative breast cancer cells by attenuating twist1 expression and suppressing twist1-mediated epithelial-mesenchymal transition.
Abstract α-Linolenic acid (ALA), an essential fatty acid, has anticancer activity in breast cancer, but the mechanism of its effects in triple-negative breast cancer (TNBC) remains unclear. We investigated the effect of ALA on Twist1, which is required to initiate epithelial-mesenchymal transition (EMT) and promotes tumor metastasis, and Twist1-mediated migration in MDA-MB231, MDA-MB468 and Hs578T cells. Twist1 protein was constitutively expressed in these TNBC cells, particularly MDA-MB-231 cells. Treatment with 100 uM ALA and Twist1 siRNA markedly decreased the Twist1 protein level and cell migration. Moreover,...
Source: Biochemical Pharmacology - July 13, 2020 Category: Drugs & Pharmacology Authors: Wang SC, Sun HL, Hsu YH, Liu SH, Lii CK, Tsai CH, Liu KL, Huang CS, Li CC Tags: Biochem Pharmacol Source Type: research

Antisense Drug Discovery and Development Technology Considered in a Pharmacological Context.
Abstract When coined, the term "antisense" included oligonucleotides of any structure, with any chemical modification and designed to work through any post-RNA hybridization mechanism. However, in practice the term "antisense" has been used to describe single stranded oligonucleotides (ss ASOs) designed to hybridize to RNAswhile the term "siRNA" has come to mean double stranded oligonucleotides designed to activate Ago2. However, the two approaches share many common features. The medicinal chemistry developed for ASOs greatly facilitated the development of siRNA technology and remains the chemical basis for both a...
Source: Biochemical Pharmacology - August 11, 2020 Category: Drugs & Pharmacology Authors: Crooke ST, Liang XH, Crooke RM, Baker BF, Geary RS Tags: Biochem Pharmacol Source Type: research

AMPK upregulates KCa2.3 channels and ameliorates endothelial dysfunction in diet-induced obese mice.
Abstract The opening of endothelial small-conductance calcium-activated potassium channels (KCa2.3) is essential for endothelium-dependent hyperpolarization (EDH), which predominantly occurs in small resistance arteries. Adenosine monophosphate-activated protein kinase (AMPK), an important metabolic regulator, has been implicated in regulating endothelial nitric oxide synthase activity. However, it was unclear whether AMPK regulated endothelial KCa2.3-mediated EDH-type vasodilation. Using bioinformatics analysis and myograph system, we investigated the regulation by AMPK of KCa2.3 in human umbilical vein endotheli...
Source: Biochemical Pharmacology - November 10, 2020 Category: Drugs & Pharmacology Authors: Pang ZD, Wang Y, Song Z, She G, Ma XZ, Sun X, Wu W, Lai BC, Zhang J, Zhang Y, Du XJ, Shyy JYJ, Deng XL Tags: Biochem Pharmacol Source Type: research

Metformin-conjugated micellar system with intratumoral pH responsive de-shielding for co-delivery of doxorubicin and nucleic acid.
Abstract A novel PMet-P(cdmPEG2K) polymeric micellar carrier was developed for tumor-targeted co-delivery of DOX and nucleic acids (NA), based on polymetformin and a structure designed to lose the PEG shell in response to the acidic extracellular tumor environment. NA/DOX co-loaded micelleplexes exhibited enhanced inhibition of cell proliferation compared to DOX-loaded micelles, and displayed a higher level of cytotoxicity at an acidic pH (6.8) which mimicks the tumor microenvironment. The PMet-P(cdmPEG2K) micelles achieved significantly improved transfection with either a reporter plasmid or Cy3-siRNA, and enhanc...
Source: Biochemical Pharmacology - February 2, 2021 Category: Drugs & Pharmacology Authors: Liu Y, Sun J, Huang Y, Chen Y, Li J, Liang L, Xu J, Wan Z, Zhang B, Li Z, Li S Tags: Biochem Pharmacol Source Type: research

Valdecoxib attenuates lipid-induced hepatic steatosis through autophagy-mediated suppression of endoplasmic reticulum stress
This study investigated the effects of VAL on lipid accumulation and lipogenesis in human primary hepatocytes. Treatment with VAL suppressed lipid accumulation and expressions of lipogenic genes, such as processed sterol regulatory element binding proteins (SREBP1) and stearoyl-CoA desaturase-1 (SCD1) in palmitate-treated hepatocytes. Furthermore, VAL ameliorated dose-dependently palmitate-induced ER stress markers. Treatment of hepatocytes with VAL increased AMPK phosphorylation and SIRT6 expression. siRNA-mediated suppression of AMPK or SIRT6 abolished the effects of VAL on lipid accumulation, lipogenesis, and endoplasmi...
Source: Biochemical Pharmacology - March 31, 2022 Category: Drugs & Pharmacology Authors: Seung Yeon Park Wonjun Cho A M Abd El-Aty Ahmet Hacimuftuoglu Ji Hoon Jeong Tae Woo Jung Source Type: research

Inhibition of T-type calcium channels disrupts Akt signaling and promotes apoptosis in glioblastoma cells.
In this study, we found that inhibition of T-type Ca(2+) channels in GBM cells significantly reduced their survival and resistance to therapy. Moreover, either T-type selective antagonists, such as mibefradil, or siRNA-mediated knockdown of the T-type channel alpha subunits not only reduced cell viability and clonogenic potential, but also induced apoptosis. In response to channel blockade or ablation, we observed reduced phosphorylation of Akt and Rictor, suggesting inhibition of the mTORC2/Akt pathway. This was followed by reduction in phosphorylation of anti-apoptotic Bad and caspases activation. The apoptotic response ...
Source: Biochemical Pharmacology - December 31, 2012 Category: Drugs & Pharmacology Authors: Valerie NC, Dziegielewska B, Hosing AS, Augustin E, Gray LS, Brautigan DL, Larner JM, Dziegielewski J Tags: Biochem Pharmacol Source Type: research