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Disturbing the programmed cell death.
Walter M van den Bergh
Critical care medicine, 41(9), 2250-2251 (2013-08-28)
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Arie Markel
The Israel Medical Association journal : IMAJ, 13(6), 368-374 (2011-08-04)
Hypercholesterolemia is one of the main factors in the development of atherosclerotic cardiovascular disease. The advent of statins led to huge progress in the treatment of hypercholesterolemia, yet the proportion of patients with prohibitive lipid values and the high incidence
P Douglas Boatman et al.
Bioorganic & medicinal chemistry letters, 20(9), 2797-2800 (2010-04-07)
Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.
M Verdú et al.
Journal of animal science, 93(6), 3018-3033 (2015-06-27)
A total of 240 Holstein bulls (121 ± 2.0 kg initial BW; 99 ± 1.0 d of age), from 2 consecutive fattening cycles, were randomly allocated in 1 of 6 pens and assigned to 1 of the 3 treatments consisting
D K Dastur et al.
The British journal of nutrition, 36(2), 143-159 (1976-09-01)
1. The B-vitamin status of fifty-nine patients, mainly from the lower socio-economic classes in Bombay, with a history of chronic malnutrition, and of alcoholism of 1-5-20 years' duration, was studied before and during treatment, and in relation to their clinical
Niacin for reduction of cardiovascular risk.
Miao Hu et al.
The New England journal of medicine, 371(20), 1941-1942 (2014-11-13)
R Preston Mason et al.
Biochimica et biophysica acta, 1848(2), 502-509 (2014-12-03)
Lipid oxidation leads to endothelial dysfunction, inflammation, and foam cell formation during atherogenesis. Glucose also contributes to lipid oxidation and promotes pathologic changes in membrane structural organization, including the development of cholesterol crystalline domains. In this study, we tested the
Hong C Shen et al.
Bioorganic & medicinal chemistry letters, 18(18), 4948-4951 (2008-08-30)
Pyrazolopyrimidines were discovered as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of
Erin M Kropp et al.
Stem cells translational medicine, 4(5), 483-493 (2015-04-03)
The tumorigenic potential of human pluripotent stem cells (hPSCs) is a major limitation to the widespread use of hPSC derivatives in the clinic. Here, we demonstrate that the small molecule STF-31 is effective at eliminating undifferentiated hPSCs across a broad
Antonio F Santidrian et al.
The Journal of clinical investigation, 123(3), 1068-1081 (2013-02-22)
Despite advances in clinical therapy, metastasis remains the leading cause of death in breast cancer patients. Mutations in mitochondrial DNA, including those affecting complex I and oxidative phosphorylation, are found in breast tumors and could facilitate metastasis. This study identifies
Malte Lohölter et al.
Archives of animal nutrition, 67(3), 202-218 (2013-06-08)
The objective of this study was to investigate the effects of niacin and dietary concentrate proportion on body temperature, ruminal pH and milk production of dairy cows. In a 2 × 2 factorial design, 20 primiparous Holstein cows (179 ±
W H Sutherland et al.
Atherosclerosis, 25(1), 45-53 (1976-10-01)
In epididymal adipose tissue from rats, human serum antagonizes inhibition of basal lipolysis by nicotinic acid in vitro. Under similar conditions caffeine-stimulated lipolysis was unaffected by the presence of human serum. Very low density (VLDL), low density (LDL) and high
James M McKenney
Postgraduate medicine, 124(1), 7-20 (2012-02-09)
Patients with dyslipidemia receive a cardiovascular benefit from lowering low-density lipoprotein cholesterol (LDL-C). Atorvastatin is currently one of the most effective approved medications for lowering LDL-C, and has been shown to significantly reduce cardiovascular risk in many patient groups. However
M Kobayashi et al.
Nihon rinsho. Japanese journal of clinical medicine, 57(10), 2211-2217 (1999-12-14)
Nicotinic acid and nicotinamide are called niacin. They are the antipellagra vitamin essential to many animals for growth and health. In human being, niacin is believed necessary together with other vitamins for the prevention and cure of pellagra. Niacin is
Beth A Connolly et al.
Metabolism: clinical and experimental, 62(12), 1840-1849 (2013-09-17)
Niacin has been used for more than 50 years to treat dyslipidemia, yet the mechanisms underlying its lipid-modifying effects remain unknown, a situation stemming at least in part from a lack of validated animal models. The objective of this study
Karine Meisser Redeuil et al.
Journal of chromatography. A, 1422, 89-98 (2015-11-03)
This manuscript reports a validated analytical approach for the quantification of 21 water soluble vitamins and their main circulating forms in human plasma. Isotope dilution-based sample preparation consisted of protein precipitation using acidic methanol enriched with stable isotope labelled internal
Kaihua Zhang et al.
Nature, 509(7498), 115-118 (2014-03-29)
P2Y receptors (P2YRs), a family of purinergic G-protein-coupled receptors (GPCRs), are activated by extracellular nucleotides. There are a total of eight distinct functional P2YRs expressed in human, which are subdivided into P2Y1-like receptors and P2Y12-like receptors. Their ligands are generally
Heng Li et al.
Bioprocess and biosystems engineering, 38(1), 189-197 (2014-07-18)
Comparative studies of immobilized and free cells of Gibberella intermedia CA3-1 in bioconversion of 3-cyanopyridine to nicotinic acid were performed. Entrapping method was chosen based on the advantages in enzymatic activity recovery, mechanical strength and preparation procedure. Four entrapment matrices
Tonglei Wu et al.
FEMS microbiology letters, 362(12), fnv078-fnv078 (2015-05-10)
Copper is a potent antimicrobial agent. Multiple mechanisms of copper tolerance are utilized by some pathogenic bacteria. BMEII0580, which is significantly similar to the multicopper oxidase from Escherichia coli, was predicted to be the probable blue copper protein YacK precursor
N Hengen et al.
Clinical chemistry, 24(10), 1740-1743 (1978-10-01)
We report a liquid-chromatographic procedure for determining free nicotinic acid and a metabolite, nicotinuric acid, in plasma and urine. Five-tenths milliliter of urine or deproteinized plasma is evaporated and the residue analyzed isocratically by reversed-phase ion-pair chromatography, with measurement of
Henry N Ginsberg et al.
Current opinion in lipidology, 24(6), 475-479 (2013-11-05)
To provide an update on recent mechanistic and clinical trial data related to the actions and efficacy of niacin. Recent mechanistic studies have provided novel insights regarding the mechanism of action of niacin. Studies of the purported niacin receptor, GPR109A
John R Guyton et al.
Journal of the American College of Cardiology, 62(17), 1580-1584 (2013-08-07)
This study sought to examine the relationship between niacin treatment, lipoproteins, and cardiovascular (CV) outcomes in this secondary analysis of the AIM-HIGH (Atherothrombosis Intervention in Metabolic Syndrome With Low HDL/High Triglycerides and Impact on Global Health Outcomes) trial. During a
Insug Kang et al.
The Journal of clinical endocrinology and metabolism, 96(10), 3048-3055 (2011-08-06)
Nicotinic acid (NA), or niacin, lowers circulating levels of lipids, including triglycerides, very low-density lipoprotein-cholesterol, and low-density lipoprotein-cholesterol. The lipid-lowering effects have been attributed to its effect to inhibit lipolysis in adipocytes and thus lower plasma free fatty acid (FFA)
Huan Gui et al.
CNS neuroscience & therapeutics, 19(3), 178-182 (2013-02-28)
To examine the effects of combination with levamlodipine and bisoprolol on stroke in rats. For acute study, Systolic blood pressure (SBP) and heart period (HP) were monitored in conscious stroke prone-spontaneously hypertensive rats (SHR-SP) and sinoaortic denervation (SAD) rats before
Elisa Brasili et al.
The Journal of nutrition, 143(10), 1549-1557 (2013-08-16)
Age-related dysbioses of intestinal microbiota and decline in the overall metabolic homeostasis are frequently found in the elderly. Probiotic supplementation may represent a way to prevent or reduce the senescence-associated metabolic disorders. The present study evaluated the metabolic impact of
Fabrizio Montecucco et al.
Expert review of cardiovascular therapy, 8(10), 1457-1467 (2010-10-13)
Nicotinic acid (at a daily dose of grams) has been shown to induce potent anti-atherosclerotic effects in human and animal models. Evidence from clinical studies performed in the 1950s has shown that nicotinic acid treatment remarkably improves the plasma lipid
H Hertle et al.
Arzneimittel-Forschung, 29(1), 114-116 (1979-01-01)
Bound nicotinic acid in feces after oral administration of phosphatidyl inositol pentanicotinate (PIN) was determined by chromatographical isolation from acid hydrolysate and UV absorbance of the eluted nicotinic acid. With all species tested, the absorption of nicotinic acid after administration
Douglas MacKay et al.
Nutrition reviews, 70(6), 357-366 (2012-06-01)
Elevated low-density lipoprotein cholesterol (LDL-C) has been the main target of lipid-altering therapy to reduce cardiovascular risk associated with dyslipidemia. Residual cardiovascular risk remains, however, after achievement of goal LDL-C levels and is associated in part with other risk markers
Julien Hanson et al.
Pharmacology & therapeutics, 136(1), 1-7 (2012-06-30)
Nicotinic acid (NA) and fumaric acid esters (FAE) such as monomethyl fumarate or dimethyl fumarate are drugs that elicit a cutaneous reaction called flushing as a side effect. NA is used to reduce progression of atherosclerosis through its anti-dyslipidemic activity
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