Pharmacological profile of a new antilipolytic agent: 5-methyl-pyrazine-2-carboxylic acid 4-oxide (acipimox) II — Antilipolytic and blood lipid lowering activity

1981 ◽  
Vol 13 (2) ◽  
pp. 163-174 ◽  
Author(s):  
P.P. Lovisolo ◽  
G. Briatico-Vangosa ◽  
G. Orsini ◽  
R. Ronchi ◽  
R. Angelucci
Keyword(s):  
Carboxylic Acid ◽  
Blood Lipid ◽  
Lipid Lowering ◽  
Pharmacological Profile ◽  
Lowering Activity

Synthesis, Characterization and In vitro Evaluation of N-Substituted- Sulfomoyl-Phenyl-Amino Carboxylic Acid Derivatives as Squalene Synthase Inhibitors

2019 ◽  
Vol 15 (4) ◽  
pp. 415-426
Author(s):  
Avani B. Chokshi ◽  
Mahesh T. Chhabria ◽  
Pritesh R. Desai
Keyword(s):  
Carboxylic Acid ◽  
Cell Line ◽  
Hepatic Cell ◽  
Squalene Synthase ◽  
Lipid Lowering ◽  
Assay Method ◽  
Aromatic Substituent ◽  
Hepatic Cell Line ◽  
Amino Carboxylic Acid

Background:Squalene Synthase is one of the cholesterol biosynthetic pathway enzymes, inhibition of which produces potent lipid lowering action. A variety of chemical classes have been evaluated for its inhibition to provide alternate antihyperlipidemic agents to statins.Methods:A series of N-substituted-sulfomoyl-phenyl-amino carboxylic acid derivatives were designed through pharmacophore modelling as Squalene Synthase inhibitors. We report here the synthesis, characterization and in vitro pharmacological screening of the designed molecules as Squalene synthase inhibitors. The target molecules were synthesized by a simple procedure and each molecule was characterized by IR, Mass, 1HNMR and 13CNMR spectroscopic techniques. As a primary site of action for cholesterol biosynthesis is liver, each of the molecules were first screened for in vitro cytotoxicity over human hepatic cell line (HepG2) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. The enzyme inhibition assay was performed on cell lysates prepared from HepG2 cells by Human Squalene Synthase ELISA kit, where test compounds were added in the nontoxic concentrations only.Results:Compound 5f was found to be most potent with the IC50 value of 11.91 µM. The CTC50 value for 5f on human hepatic cell line was > 1000 µM so it was considered that the compound was relatively safe and might be free of hepatotoxicity.Conclusion:From the results of our studies, it was observed that compounds with poly nuclear aromatic or hetero aromatic substituent on a side chain were more potent enzyme inhibitors and a distance of 4-5 atoms is optimum between amide nitrogen and hydroxyl group of carboxylic acid.

Evaluation of Glucose and Lipid Lowering Activity of Arganimide A in Normal and Streptozotocin-Induced Diabetic Rats

2019 ◽  
Vol 19 (4) ◽  
pp. 503-510 ◽  
Author(s):  
Mohamed Eddouks ◽  
Farid Khallouki ◽  
Robert W. Owen ◽  
Morad Hebi ◽  
Remy Burcelin
Keyword(s):  
Body Weight ◽  
Blood Glucose ◽  
Oral Administration ◽  
Lipid Profile ◽  
Plasma Cholesterol ◽  
Diabetic Rats ◽  
Lipid Lowering ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
Lowering Activity

Aims: Arganimide A (4,4-dihydroxy-3,3-imino-di-benzoic acid) is a compound belonging to a family of aminophenolics found in fruit of Argania spinosa. The purpose of this study was to investigate the glucose and lipid lowering activity of Arganimide A (ARG A). Methods: The effect of a single dose and daily oral administration of Arganimide A (ARG A) on blood glucose levels and plasma lipid profile was tested in normal and streptozotocin (STZ) diabetic rats at a dose of 2 mg/kg body weight. Results: Single oral administration of ARG A reduced blood glucose levels from 26.50±0.61 mmol/L to 14.27±0.73 mmol/L (p<0.0001) six hours after administration in STZ diabetic rats. Furthermore, blood glucose levels were decreased from 5.35±0.30 mmol/L to 3.57±0.17 mmol/L (p<0.0001) and from 26.50±0.61 mmol/L to 3.67±0.29 mmol/L (p<0.0001) in normal and STZ diabetic rats, respectively, after seven days of treatment. Moreover, no significant changes in body weight in normal and STZ rats were shown. According to the lipid profile, the plasma triglycerides levels were decreased significantly in diabetic rats after seven days of ARG treatment (p<0.05). Moreover, seven days of ARG A treatment decreased significantly the plasma cholesterol concentrations (p<0.001). Conclusion: ARG A possesses glucose and lipid-lowering activity in diabetic rats and this natural compound may be beneficial in the treatment of diabetes.

Lipid lowering activity of Eclipta prostrata in experimental hyperlipidemia

2006 ◽  
Vol 105 (3) ◽  
pp. 332-335 ◽  
Author(s):  
C. Santhosh Kumari ◽  
S. Govindasamy ◽  
E. Sukumar
Keyword(s):  
Lipid Lowering ◽  
Eclipta Prostrata ◽  
Experimental Hyperlipidemia ◽  
Lowering Activity

Pharmacological profile of a new anti-lipolytic agent: 5-methyl-pyrazine-2-carboxylic acid 4-oxide (acipimox) I — Mechanism of action

1981 ◽  
Vol 13 (2) ◽  
pp. 151-161 ◽  
Author(s):  
P.P. Lovisolo ◽  
G. Briatico-Vangosa ◽  
G. Orsini ◽  
R. Ronchi ◽  
R. Angelucci ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Mechanism Of Action ◽  
Pharmacological Profile

Design of a pharmaceutical composition with a low-dose statin and a high lipid-lowering activity

2021 ◽  
Vol 70 (1) ◽  
pp. 52-56
Author(s):  
Natalia Dmitrievna Bunyatyan ◽  
Anastasia Evgen'evna Kozlova ◽  
Vladimir Pavlovich Balashov ◽  
Alexey Vladimirovich Balashov ◽  
Ruslan Evgenievich Kazakov ◽  
...  
Keyword(s):  
Low Dose ◽  
Lipid Lowering ◽  
High Lipid ◽  
Pharmaceutical Composition ◽  
Lowering Activity

scholarly journals The Impact of Changes in Population LDL-C Levels on LDL-C Control in Patients After PCI in China: A Retrospective Cohort Study

2020 ◽  
Author(s):  
Huan Liu ◽  
Zhipeng Zhou ◽  
Yanqing Wu ◽  
Jingsong Xu
Keyword(s):  
Low Density Lipoprotein ◽  
Density Lipoprotein ◽  
Blood Lipid ◽  
Coronary Intervention ◽  
Lifestyle Changes ◽  
Treatment Goal ◽  
Lipid Lowering ◽  
Lipid Control ◽  
The Impact

Abstract BANKGROUND: Mortality from coronary artery disease continues to rise, and secondary prevention and treatment are particularly important. OBJECTIVE: The objective of this study is to evaluate low-density lipoprotein cholesterol (LDL-C) levels in patients after percutaneous coronary intervention (PCI), to describe how treatment outcomes for individual patients changed over time and to examine the potential impact of lipid control rates through population LDL-C levels changes.METHODS: This retrospective study was conducted in patients who underwent PCI between July 2017 and June 2019. The main results included LDL-C levels after PCI. To assess the outcome of prevention, three separate measures of LDL-C were considered: baseline, first follow-up, and final follow-up, and LDL-C control rates were analyzed according to different guidelines. we examine the impact of 0.1mmol/l decreases or increases in population LDL-C levels on LDL-C control.RESULTS: Data were analyzed for 423 patients (mean age, 62 ±10 years), and the baseline LDL-C level was 3.11 ± 0.99 mmol/l. 51.5% of the patients achieved the Chinese Lipids Guidelines treatment goal, 22% and 11.6% of the patients achieved the 2016 ESC Lipids Guidelines and 2019 ESC Lipids Guidelines treatment goal at the final follow-up period respectively. LDL-C levels fluctuated during the follow-up period, and the long-term maintenance results could not be guaranteed after PCI. Population LDL-C levels changes in lifestyle could have a very large impact on LDL-C control in China.CONCLUSION: LDL-C control with statins is not ideal in patients after PCI, which is far from the requirements of the latest guidelines. Although clinicians understand the lipid-lowering effect of statins, they should not give up active lifestyle changes, and should strengthen the comprehensive management of blood lipid control.

scholarly journals Lipid Lowering Activity and Free Radical Scavenging Effect of Cinnamomum tamala (Fam: Lauraceae)

1970 ◽  
Vol 1 (4) ◽  
pp. 93-96
Author(s):  
R Al-Mamun ◽  
A Hamid ◽  
MK Islam ◽  
JA Chowdhury ◽  
ATM Zafrul Azam
Keyword(s):  
Free Radical ◽  
Lipid Profile ◽  
Total Cholesterol ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antioxidant Property ◽  
Free Radical Scavenging ◽  
Lipid Lowering ◽  
Increased Risk ◽  
Lowering Activity

Lipid profile is a blood test that measures the amount of lipids, or fats, in your blood. The lipids measured are usually total cholesterol, HDL-C, LDL-C and triglycerides. When levels of these lipids are abnormal, there is an increased risk of heart attack and stroke. In our study, we use methanol crude extract for lipid lowering activity on rabbit and found that lipid profile was reduced by 14.0, 1.0, 4.0 and 15.0 mg/dl for total cholesterol, HDL-C, LDL-C and triglyceride respectively after using the plant extract (dose 500mg/rabbit for 10 days); where atorvastatin (0.005mg/rabbit) was used as standard lipid lowering agent. We also focused on the antioxidant property of crude methanol extract. Here we also carried out free radical-scavenging activity study and found the IC50 value for C. tamala is 6.00 μg/ml where the standard antioxidant (ascorbic acid) gave the value of 3.21μg/ml. DOI: http://dx.doi.org/10.3329/ijns.v1i4.9735 IJNS 2011 1(4): 93-96

The role of apolipoprotein E polymorphism in improving dyslipidemia in obese adolescents following physical exercise and National Cholesterol Education Program Step II intervention

2015 ◽  
Vol 28 (5-6) ◽  
Author(s):  
Lanny C. Gultom ◽  
Damayanti R. Sjarif ◽  
Herawati A. Sudoyo ◽  
Muchtaruddin Mansyur ◽  
Sri Rezeki S. Hadinegoro ◽  
...  
Keyword(s):  
Physical Exercise ◽  
Apolipoprotein E ◽  
Blood Lipid ◽  
Lifestyle Changes ◽  
Lipid Lowering ◽  
Exercise Interventions ◽  
Obese Adolescents ◽  
Lipid Lowering Drugs ◽  
Apo E ◽  
Before And After

AbstractLifestyle changes are important factors for managing dyslipidemia before considering blood lipid-lowering drugs. However, genetic factors can influence the response outcome.We aimed to determine a dyslipidemia management strategy in obese adolescents.: A total of 60 dyslipidemic obese adolescents received physical exercise and the NCEP step II diet for 28 days. Apolipoprotein E (apo E) genotypes and blood lipid levels were compared before and after interventions.The apoApo E alleles might influence improvement in lipid profiles after diet and exercise interventions. These results could inform personalized dyslipidemia management in obese adolescents, to determine which subjects would benefit from blood lipid-lowering drugs.

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