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lipids lowering drugs

Damilola D Adingupu, Suvi E Heinonen, Anne-Christine Andréasson, Mikael Brusberg, Andrea Ahnmark, Margareta Behrendt, Brendan Leighton, Ann-Cathrine Jönsson-Rylander
Aim. Models combining diabetes and atherosclerosis are important in evaluating the cardiovascular (CV) effects and safety of antidiabetes drugs in the development of treatments targeting CV complications. Our aim was to evaluate if crossing the heterozygous glucokinase knockout mouse (GK(+/-)) and hyperlipidemic mouse deficient in apolipoprotein E (ApoE(-/-)) will generate a disease model exhibiting a diabetic and macrovascular phenotype. Methods. The effects of defective glucokinase on the glucose metabolism and on the progression and regression of atherosclerosis on high-fat diets were studied in both genders of GK(+/-)ApoE(-/-) and ApoE(-/-) mice...
2016: Journal of Diabetes Research
Sayantan Nath, Sankar Kumar Ghosh, Yashmin Choudhury
INTRODUCTION: A murine model of type 2 diabetes mellitus was used to compare the antidiabetic effects of the dipeptidyl peptidase-4 (DPP4) inhibitor vildagliptin and biguanide, metformin. METHODS: Swiss albino mice (n=20 males; n=25 females) were given high fat diet (HFD) ad libitum for 3weeks followed by low dose (40mgkg(-1) body weight, bw daily) of streptozotocin (STZ) intraperitoneally five times from the 22nd day of treatment onwards, with HFD continued up to 26th day...
October 20, 2016: Journal of Pharmacological and Toxicological Methods
Lin-Hu Ye, Ling-Ti Kong, Ming-Zhu Yan, Fang-Rui Cao, Li-Sha Wang, Yong-Hong Liao, Rui-Le Pan, Qi Chang
ETHNOPHARMACOLOGICAL RELEVANCE: The Chinese herbal medicine He-Ye, the leaves of the lotus (Nelumbo nucifera) plant, is traditionally used in China for the treatment of sunstroke, thirst, diarrhea, and fever. Currently, the leaf is used not only as an herbal tea to reduce lipid level and control body weight, but also as a major ingredient in some lipid-lowering Chinese patented medicines. Our previous study demonstrated that the alkaloid fraction (AF) of the herb has a strong inhibitory effect on CYP2D6 isoenzyme activity in vitro...
October 19, 2016: Journal of Ethnopharmacology
Werner J Geldenhuys, Li Lin, Altaf S Darvesh, Prabodh Sadana
Although statins and other pharmacological approaches have improved the management of lipid abnormalities, there exists a need for newer treatment modalities especially for the management of hypertriglyceridemia. Lipoprotein lipase (LPL), by promoting hydrolytic cleavage of the triglyceride core of lipoproteins, is a crucial node in the management of plasma lipid levels. Although LPL expression and activity modulation is observed as a pleiotropic action of some the commonly used lipid lowering drugs, the deliberate development of drugs targeting LPL has not occurred yet...
October 19, 2016: Drug Discovery Today
Hui Yao, Guangchun He, Shichao Yan, Chao Chen, Liujiang Song, Thomas J Rosol, Xiyun Deng
Triple-negative breast cancer (TNBC), which accounts for 15-20% of all breast cancers, does not express estrogen receptor (ER) or progesterone receptor (PR) and lacks human epidermal growth factor receptor 2 (HER2) overexpression or amplification. These tumors have a more aggressive phenotype and a poorer prognosis due to the high propensity for metastatic progression and absence of specific targeted treatments. Patients with TNBC do not benefit from hormonal or trastuzumab-based targeted therapies because of the loss of target receptors...
September 27, 2016: Oncotarget
Michael B Boffa
PURPOSE OF REVIEW: Elevated plasma concentrations of lipoprotein(a) (Lp(a)) are an independent and causal risk factor for cardiovascular diseases including coronary artery disease, ischemic stroke, and calcific aortic valve stenosis. This review summarizes the rationale for Lp(a) lowering and surveys relevant clinical trial data using a variety of agents capable of lowering Lp(a). RECENT FINDINGS: Contemporary guidelines and recommendations outline populations of patients who should be screened for elevated Lp(a) and who might benefit from Lp(a) lowering...
December 2016: Current Atherosclerosis Reports
Connie M Rhee, Csaba P Kovesdy, Kamyar Kalantar-Zadeh
Like other biguanide agents, metformin is an anti-hyperglycemic agent with lower tendency towards hypoglycemia compared to other anti-diabetic drugs. Given its favorable effects on serum lipids, obese body habitus, cardiovascular disease, and mortality, metformin is recommended as the first-line pharmacologic agent for type 2 diabetes in the absence of contraindications. However, as metformin accumulation may lead to type B non-hypoxemic lactic acidosis, especially in the setting of kidney injury, chronic kidney disease, and overdose, regulatory agencies such as the United States Food and Drug Administration (FDA) have maintained certain restrictions regarding its use in kidney dysfunction...
October 20, 2016: Nephron
Rajkumar Bharatia, Manoj Chitale, Ganesh Narain Saxena, Raman Ganesh Kumar, Chikkalingaiah, Abhijit Trailokya, Kalpesh Dalvi, Suhas Talele
INTRODUCTION: Hypertension (HTN), being a major risk factor for cardiovascular diseases (CVDs), is an important issue of medical and public health. High blood pressure (BP) is ranked as the third most important risk factor for attributable burden of disease in south Asia (2010). Hypertension (HTN) exerts a substantial public health burden on cardiovascular health status and healthcare systems in India. Uncontrolled hypertension among adults with hypertension is associated with increased mortality...
July 2016: Journal of the Association of Physicians of India
Jie-Eun Lee, Se Hee Min, Dong-Hwa Lee, Tae Jung Oh, Kyoung Min Kim, Jae Hoon Moon, Sung Hee Choi, Kyong Soo Park, Hak Chul Jang, Soo Lim
BACKGROUND: Early detection of atherogenic dyslipidemia is crucial. We investigated lipoprotein subfraction parameters according to glucose metabolism status. METHODS: We recruited 1255 lipid-lowering drug-naïve subjects with normal fasting glucose (NFG; n=200, 15.9%), impaired fasting glucose (IFG; n=443, 35.3%), or type 2 diabetes (T2D; n=612, 48.8%). Lipoprotein subfractions (1-7) were determined by polyacrylamide gel electrophoresis, separating low-density lipoprotein (LDL) into large buoyant LDL (lbLDL, LDL1-2) and small dense LDL (sdLDL, LDL3-7)...
October 6, 2016: International Journal of Cardiology
(no author information available yet)
No abstract text is available yet for this article.
October 24, 2016: Medical Letter on Drugs and Therapeutics
V V Muthusamy
Cardiovascular disease burden is increasing all over the world. The diagnosis of hypertension is considered when a person has persistently elevated BP (Systolic BP more than 140 mmHg and/or Diastolic BP more than 90 mmHg). Dyslipidemia denotes abnormal levels of lipids in the blood (Total Cholesterol >200 mg%, Low density lipoprotein (LDL) >100 mg%, Triglycerides (TGL) >150 mg% and High density lipoprotein (HDL) <40 mg in men and < 50 mg in women. Hypertension and Dyslipidemia constitute the important components of metabolic syndrome as per the definition of NCEP Guidelines-Adult Treatment Panel III (ATP III)...
September 2016: Journal of Hypertension
Wen Wang, Liyuan Ma, Hui Sui, Lisheng Liu
OBJECTIVE: Chinese Hypertension Intervention Efficacy Study (CHIEF) is a multi-center randomized controlled clinical trial. The objective is to evaluate the collective effects of antihypertensive therapy, lipid lowering treatment and lifestyle modification in patients with hypertension. This paper merely present blood pressure lowering effect of intensive lifestyle intervention compared with standard lifestyle intervention. CLINICAL TRIAL REGISTRATION: Clinical Trials...
September 2016: Journal of Hypertension
Zachary R Noel, Craig J Beavers
Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) inhibitors serve as a valuable addition to the armamentarium of lipid lowering agents and have promising potential. By inhibiting the PCSK9 enzyme, this novel molecule leads to increase low density lipoprotiein (LDL) receptor density and decreased circulation of LDL. The fact the agent is a monoclonal antibody has led to limited drug interactions and minimized adverse drug events. It is critical for all providers to have a basic understanding of these novel therapies with their introduction and use for treatment...
October 14, 2016: American Journal of Medicine
Kamal Awad, Peter Penson, Maciej Banach
Reduction of elevated cholesterol levels, particularly low-density lipoprotein cholesterol (LDL-C), is essential in primary and secondary prevention of cardiovascular disease (CVD). Therefore there is still a large need for new effective drugs, which would be able to essentially reduce LDL-C and in the consequence CV residual risk. D-003 is a mixture of high aliphatic primary acids purified from sugarcane (Saccharum officinarum) wax. It showed promising hypocholesterolemic effects in both animal and human studies; it significantly lowers both serum total cholesterol (TC) and LDL-C, and increases high-density lipoprotein cholesterol (HDL-C)...
October 14, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Adele Bahar, Zahra Kashi, Ezzatossadat Daneshpour, Ozra Akha, Shahram Ala
BACKGROUND: Cabergoline is a long-acting agonist of dopamine, which has a high affinity to dopamine receptors (type 2). Treatment using a dopaminergic agonist reduces hypothalamic stimulation that increases during liver gluconeogenesis, lipids synthesis, and insulin resistance. Our aim was to evaluate the effects of cabergoline on blood glucose levels in patients with type 2 diabetes mellitus (DM). METHODS: This study was a double-blind, controlled clinical trial in patients with type 2 DM...
October 2016: Medicine (Baltimore)
Dick C Chan, P Hugh R Barrett, Gerald F Watts
PURPOSE OF REVIEW: Dysregulated lipoprotein metabolism leads to increased plasma concentrations of atherogenic lipoproteins. We highlight the findings from recent studies of the effect of lipid-regulating therapies on apolipoprotein metabolism in humans employing endogenous labelling with stable isotopically labelled isotopomers. RECENT FINDINGS: Fish oil supplementation and niacin treatment both reduce fasting and postprandial triglyceride levels by decreasing the hepatic secretion of VLDL-apoB-100 (apoB) and apoB-48-containing chylomicron particles in obese and/or type 2 diabetes...
October 5, 2016: Current Opinion in Lipidology
Anton Chechushkov, Natalia Zaitseva, Elena Vorontsova, Petr Kozhin, Elena Menshchikova, Vyacheslav Shkurupiy
AIMS: Linear dextrans are often proposed as drug delivery systems with milder adverse effects and lower effective drug concentrations. Linear dextrans are polysaccharides that can potentially be used to load macrophages with drugs to transport them to a site of inflammation. Recently, it was reported that dextrans may exert a protective effect vis-à-vis drug cytotoxicity and during wound healing. The aim of the current work was to evaluate molecular mechanisms of action of dextrans that may be relevant to the cytoprotective effects...
October 13, 2016: Life Sciences
David Martí, Edurne López, Salvador Álvarez, Jorge Palazuelos, Ignacio Rada, Fernando Alfonso
The unique physical properties of optical coherence tomography (OCT) make it a useful technique in the study of restenosis mechanisms. In fact, OCT is able to differentiate between neointimal proliferation and neoatherosclerosis within the stent. We report a rare case of occlusive neoatherosclerosis presenting beyond one year after a successful drug-eluting stent implantation. The impact of OCT findings in the clinical decision making process is emphasized.
September 30, 2016: Cardiovascular Revascularization Medicine: Including Molecular Interventions
Matthew Kochem, Paul A S Breslin
T1R2-T1R3 is a heteromeric receptor that binds sugars, high potency sweeteners, and sweet taste blockers. In rodents, T1R2-T1R3 is largely responsible for transducing sweet taste perception. T1R2-T1R3 is also expressed in non-taste tissues, and a growing body of evidence suggests that it helps regulate glucose and lipid metabolism. It was previously shown that clofibric acid, a blood lipid-lowering drug, binds T1R2-T1R3 and inhibits its activity in vitro The purpose of this study was to determine whether clofibric acid inhibits sweetness perception in humans and is, therefore, a T1R2-T1R3 antagonist in vivo Fourteen participants rated the sweetness intensity of 4 sweeteners (sucrose, sucralose, Na cyclamate, acesulfame K) across a broad range of concentrations...
October 14, 2016: Chemical Senses
Shweta Sharma, Ashwni Kumar Verma, Jyotsana Singh, B Venkatesh Teja, Naresh Mittapelly, Gitu Pandey, Sandeep Urandur, Ravi Shukla, Rituraj Konwar, Prabhat Ranjan Mishra
This study reports the development of Vitamin B6 (VitB6) modified pH sensitive charge reversal nanoparticles for efficient intracellular delivery of Doxorubicin (DOX). Herein, VitB6 was conjugated to stearic acid and the nanoparticles of the lipid were formulated by solvent injection method (DOX-B6-SA-NP). Due to the pKa (5.6) of VitB6, DOX-B6-SA-NP showed positive charge and enhanced release of DOX at pH 5. Confocal microscopy illustrated that DOX-B6-SA-NP treatment keep higher DOX accumulation inside the cells that conventional pH insensitive lipid nanoparticles (DOX-SA-NP)...
October 14, 2016: ACS Applied Materials & Interfaces
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