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Specialty: Drugs & Pharmacology
Condition: Cholesterol

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Total 94 results found since Jan 2013.

HNF-4 α regulated miR-122 contributes to development of gluconeogenesis and lipid metabolism disorders in Type 2 diabetic mice and in palmitate-treated HepG2 cells.
We examined how HNF-4α regulated gluconeogenesis and lipid metabolism through miR-122 in vivo and in vitro. Expression of miR-122, HNF-4α, phosphoenolpyruvate carboxykinase (PEPCK), glucose-6-phosphatase (G6Pase), sterol response elementary binding protein-1 (SREBP-1), fatty acid synthase-1 (FAS-1), carnitine palmitoyltransferase-1 (CPT-1) and acetyl Coenzyme A carboxylase alpha (ACCα) were determined in livers of Type 2 diabetic mice and in insulin resistant palmitate-treated HepG2 cells. CPT-1 and phosphorylated ACCα expression were significantly decreased in livers of Type 2 diabetic mice and in palmitated-treated H...
Source: European Journal of Pharmacology - August 30, 2016 Category: Drugs & Pharmacology Authors: Wei S, Zhang M, Yu Y, Xue H, Lan X, Liu S, Hatch G, Chen L Tags: Eur J Pharmacol Source Type: research

Modulated cellular delivery of anti-VEGF siRNA (bevasiranib) by incorporating supramolecular assemblies of hydrophobically modified polyamidoamine dendrimer in stealth liposomes
Publication date: 20 August 2016 Source:International Journal of Pharmaceutics, Volume 510, Issue 1 Author(s): Nasim Golkar, Soliman Mohammadi Samani, Ali Mohammad Tamaddon A novel lipopolymer based system was designed and characterized for cellular delivery of anti-VEGF siRNA in SKBR-3 breast tumor cell line. Polyamidoamine (PAMAM) dendrimers of low generations (G1, G2 and G3) were incorporated into polyethylene glycol (PEG)-stabilized liposomes by following the consecutive steps: (a) synthesis of the cholesterol conjugates (40% molar ratio of cholesterol to primary amines of PAMAM), (b) incorporation of the conjugat...
Source: International Journal of Pharmaceutics - June 17, 2016 Category: Drugs & Pharmacology Source Type: research

Involvement of Pregnane X Receptor in the Impaired Glucose Utilization Induced by Atorvastatin in Hepatocytes.
In conclusion, atorvastatin impaired glucose utilization in hepatocytes via repressing GLUT2 and GCK expressions, which may be partly due to PXR activation. PMID: 26616219 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - November 23, 2015 Category: Drugs & Pharmacology Authors: Ling Z, Shu N, Xu P, Wang F, Zhong Z, Sun B, Li F, Zhang M, Zhao K, Tang X, Wang Z, Zhu L, Liu L, Liu X Tags: Biochem Pharmacol Source Type: research

AMP-activated protein kinase attenuates oxLDL uptake in macrophages through PP2A/NF-κB/LOX-1 pathway.
Abstract The differentiation of macrophages into lipid-laden foam cells is a hallmark in early-stage atherosclerosis. The developmental role of adenosine monophosphate-activated protein kinase (AMPK) in a transformation of foam cells, especially in macrophage cholesterol uptake that remains undetermined. Here we demonstrate that AMPK activation in response to IMM-H007 or AICAR resulted in a decrease in macrophage cholesterol uptake and thus inhibited foam cell formation in macrophages mediated by oxidized low-density lipoprotein (oxLDL). This functional change was caused by a downregulation of mRNA and protein exp...
Source: Vascular Pharmacology - August 19, 2015 Category: Drugs & Pharmacology Authors: Chen B, Li J, Zhu H Tags: Vascul Pharmacol Source Type: research

One-step scalable preparation method for non-cationic liposomes with high siRNA content
Publication date: 25 July 2015 Source:International Journal of Pharmaceutics, Volume 490, Issues 1–2 Author(s): Masaharu Somiya , Kotomi Yamaguchi , Qiushi Liu , Tomoaki Niimi , Andrés Daniel Maturana , Masumi Iijima , Nobuo Yoshimoto , Shun’ichi Kuroda Cationic liposomes (LPs) have been utilized for short interfering RNA (siRNA) delivery in vitro and in vivo owing to their high affinity for siRNA via electrostatic binding. However, both cytotoxicity and non-specific adsorption of cationic LPs in the body have prevented clinical siRNA applications. These situations have led to siRNA encapsulation in non-cationic LPs...
Source: International Journal of Pharmaceutics - June 8, 2015 Category: Drugs & Pharmacology Source Type: research

Atorvastatin attenuates homocysteine-induced migration of smooth muscle cells through mevalonate pathway involving reactive oxygen species and p38 MAPK.
This article is protected by copyright. All rights reserved. PMID: 26041506 [PubMed - as supplied by publisher]
Source: Clinical and Experimental Pharmacology and Physiology - June 4, 2015 Category: Drugs & Pharmacology Authors: Bao XM, Zheng H Tags: Clin Exp Pharmacol Physiol Source Type: research

Atorvastatin reduces long pentraxin 3 expression in vascular cells by inhibiting protein geranylgeranylation.
CONCLUSIONS: Results suggest that statins may interfere with PTX3 expression in vascular cells via inhibition of protein geranylgeranylation. Since PTX3 is increasingly regarded as an important mediator of the inflammatory response underlying atherosclerosis and its complications, these results highlight the need for further studies of the role of PTX3 and its potential pharmacological modulation in cardiovascular disease. PMID: 25849951 [PubMed - as supplied by publisher]
Source: Vascular Pharmacology - April 4, 2015 Category: Drugs & Pharmacology Authors: Baetta R, Lento S, Ghilardi S, Barbati E, Corsini A, Tremoli E, Banfi C Tags: Vascul Pharmacol Source Type: research

siRNA Delivery into Tumor Cells by Cationic Cholesterol Derivative-Based Nanoparticles and Liposomes.
In this study, we synthesized new diamine-type cationic cholesteryl carbamate (OH-C-Chol, cholesteryl (2-((2-hydroxyethyl)amino)ethyl)carbamate) and triamine-type carbamate (OH-NC-Chol, cholesteryl (2-((2-((2-hydroxyethyl)amino)ethyl)amino)ethyl)carbamate), and prepared cationic nanoparticles composed of OH-C-Chol or OH-NC-Chol with Tween 80 (NP-C and NP-NC, respectively), as well as cationic liposomes composed of OH-C-Chol or OH-NC-Chol with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (LP-C and LP-NC, respectively) for evaluation of their possible use as siRNA delivery vectors. LP-C and LP-NC/siRNA complexes (lip...
Source: Biological and Pharmaceutical Bulletin - March 8, 2015 Category: Drugs & Pharmacology Authors: Hattori Y, Hara E, Shingu Y, Minamiguchi D, Nakamura A, Arai S, Ohno H, Kawano K, Fujii N, Yonemochi E Tags: Biol Pharm Bull Source Type: research

Development of anti-E6 pegylated lipoplexes for mucosal application in the context of cervical preneoplastic lesions
In conclusion, pegylated anti-E6 lipoplexes have demonstrated their efficiency to cross the cellular membrane and to release siRNA into the cytoplasm confirmed by final p53 protein production. Graphical abstract
Source: International Journal of Pharmaceutics - February 27, 2015 Category: Drugs & Pharmacology Source Type: research

Aspirin may influence cellular energy status.
Abstract In our previous findings, we have demonstrated that aspirin/acetyl salicylic acid (ASA) might induce sirtuins via aryl hydrocarbon receptor (Ah receptor). Induction effects included an increase in cellular paraoxonase 1 (PON1) activity and apolipoprotein A1 (ApoA1) gene expression. As predicted, ASA and salicylic acid (SA) treatment resulted in generation of H2O2, which is known to be an inducer of mitochondrial gene Sirt4 and other downstream target genes of Sirt1. Our current mass spectroscopic studies further confirm the metabolism of the drugs ASA and SA. Our studies show that HepG2 cells readily conv...
Source: European Journal of Pharmacology - December 31, 2014 Category: Drugs & Pharmacology Authors: Kamble P, Litvinov D, Aluganti Narasimhulu C, Jiang X, Parthasarathy S Tags: Eur J Pharmacol Source Type: research

Autocrine secretion of 15d‐PGJ2 mediates simvastatin‐induced apoptotic burst in human metastatic melanoma cells
Conclusions and ImplicationsWe characterized simvastatin‐induced activation of the 15d‐PGJ2/FABP5 signalling cascades, which triggered an apoptotic burst in melanoma cells but did not affect primary human melanocytes. These data support the rationale for the pharmacological targeting of 15d‐PGJ2 in metastatic melanoma.
Source: British Journal of Pharmacology - December 1, 2014 Category: Drugs & Pharmacology Authors: Christine Wasinger, Martin Künzl, Christoph Minichsdorfer, Christoph Höller, Maria Zellner, Martin Hohenegger Tags: RESEARCH PAPER Source Type: research

Statins upregulate cystathionine γ-lyase transcription and H2S generation via activating Akt signaling in macrophage
In this study, we examined the effects of three different statins (fluvastatin, atorvastatin and pravastatin) on H2S formation in raw264.7 macrophages. There was a remarkable rise in H2S level in fluvastatin- and atorvastatin-stimulated macrophages, while pravastatin failed to show any significant effect on it. Moreover, fluvastatin and atorvastatin enhanced the mRNA and protein expression of cystathionine γ-lyase (CSE) in dose- and time-dependent manners. Fluvastatin also markedly enhanced the CSE activity. However, fluvastatin did not alter the mRNA or protein expression of another H2S-producing enzyme 3-mercaptopyruvat...
Source: Pharmacological Research - November 6, 2014 Category: Drugs & Pharmacology Source Type: research

In vivo siRNA delivery system for targeting to the liver by poly-l-glutamic acid-coated lipoplex
In this study, we developed anionic polymer-coated liposome/siRNA complexes (lipoplexes) with chondroitin sulfate C (CS), poly-l-glutamic acid (PGA) and poly-aspartic acid (PAA) for siRNA delivery by intravenous injection, and evaluated the biodistribution and gene silencing effect in mice. The sizes of CS-, PGA- and PAA-coated lipoplexes were about 200 nm and their ζ-potentials were negative. CS-, PGA- and PAA-coated lipoplexes did not induce agglutination after mixing with erythrocytes. In terms of biodistribution, siRNAs after intravenous administration of cationic lipoplexes were largely observed in the lungs, but t...
Source: Results in Pharma Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research

Development and Characterization of siRNA Lipoplexes: Effect of Different Lipids, In Vitro Evaluation in Cancerous Cell Lines and In Vivo Toxicity Study.
Abstract Cationic liposomes have long been used as non-viral vectors for small interfering RNA (siRNA) delivery but are associated with high toxicity, less transfection efficiency, and in vivo instability. In this investigation, we have developed siRNA targeted to RRM1 that is responsible for development of resistance to gemcitabine in cancer cells. Effect of different lipid compositions has been evaluated on formation of stable and less toxic lipoplexes. Optimized cationic lipoplex (D2CH) system was comprised of dioleoyl-trimethylammoniumpropane (DOTAP), dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), hydrogena...
Source: AAPS PharmSciTech - August 22, 2014 Category: Drugs & Pharmacology Authors: Khatri N, Baradia D, Vhora I, Rathi M, Misra A Tags: AAPS PharmSciTech Source Type: research

Autocrine secretion of 15d‐PGJ2 mediates simvastatin induced apoptotic burst in human metastatic melanoma cells
ConclusionWe here delineate simvastatin induced activation of the 15d‐PGJ2/FABP5 signalling cascades, which trigger an apoptotic burst in melanoma cells, while primary human melanocytes were unaffected. These data support new rational ground for pharmacological targeting of 15d‐PGJ2 in metastatic melanoma.
Source: British Journal of Pharmacology - August 4, 2014 Category: Drugs & Pharmacology Authors: Christine Wasinger, Martin Künzl, Christoph Minichsdorfer, Christoph Höller, Maria Zellner, Martin Hohenegger Tags: Research Paper Source Type: research