Characterization, Modes of Synthesis, and Pleiotropic Effects of Hypocholesterolemic Compounds – A Review

  title={Characterization, Modes of Synthesis, and Pleiotropic Effects of Hypocholesterolemic Compounds – A Review},
  author={A. Seenivasan and T. Panda and T. Th{\'e}odore},
  journal={The Open Enzyme Inhibition Journal},
Studies on the various cholesterol-lowering agents is one of the important areas in clinical research. Identifica- tion and characterization of potential molecules from various sources have been carried out in the past and their relation- ship with the enzymes which are involved in the cholesterol cascade is gaining interest. In this review, we have high- lighted various inhibitors involved in the cholesterol cascade as well as cholesterol-lowering agents, viz., tocotrienol, flavonoids… Expand

Tables from this paper

Phenolics from grapefruit peels inhibit HMG-CoA reductase and angiotensin-I converting enzyme and show antioxidative properties in endothelial EA.Hy 926 cells
Abstract This study sought to investigate the possible mechanisms for the use of phenolic extracts from grapefruit peels in the management/prevention of cardiovascular complications. The effects ofExpand
From folk medicine to functional food: a review on the bioactive components and pharmacological properties of citrus peels
The phenolic compounds and volatile compounds which have been linked with the biological activities of the peels have been characterized and the bioactive compounds of citrus peels and the mechanisms for the biological Activities are looked at. Expand
Cellular Localization and Production of Lovastatin from Monascus purpureus
Lovastatin is the first FDA-approved antihypercholesterolemic drug for the treatment of cardiovascular diseases with pleiotropic clinical applications. Monascus purpureus is one of the safest moldsExpand
Modulation of HMG-CoA reductase and glutathione-linked enzymes and protection against pro-oxidant induced oxidative damage in colon (Caco-2) cells and rat colon homogenates by phenolic extracts from Shaddock (Citrus maxima) peels
This study sought to characterize the soluble free and bound phenolic compounds from shaddock (Citrus maxima) peels and investigate their effect on 3-hydroxy-methyl-3-glutaryl coenzyme A reductaseExpand
Hypolipidemic Activity of Solvents Extracts of Khaya senegalensis Stem Bark in Diet Induced Hyperlipidemic Rats
Introduction: Hyperlipidemia is a modifiable risk factor of an important killer disease “cardiovascular diseases”, which account for as much mortality as infectious disease, nutritional deficiencyExpand
Quantification of Lovastatin Produced by Monascus purpureus
Development of a novel method for the quantification of lovastatin is an interesting problem in the analytical field. In the literature, many reports use spectrophotometric method for theExpand
Comparison of the elution characteristics of individual forms of lovastatin in both isocratic and gradient modes and HPLC-PDA method development for pure and fermentation-derived lovastatin
The fermentation broth (pH not adjusted) extracted with ethyl acetate at a ratio of 1:1 (v/v) at 60°C for 30 min was the optimal extraction condition for lovastatin. Expand
Metabolic pathway analysis and dynamic macroscopic model development for lovastatin production by Monascus purpureus using metabolic footprinting concept
Abstract Understanding and modeling of the metabolic pathway of a cell by probing the fraction of extracellular metabolites is gaining much interest in biological reactions. This communication dealsExpand


Biosynthesis and biotechnological production of statins by filamentous fungi and application of these cholesterol-lowering drugs
The use of statins can lead to a reduction in coronary events related to hypercholesterolemia, but the relationship between benefit and risk, and any possible interaction with other drugs, must be taken into account. Expand
Statins: mechanism of action and effects
  • C. Stancu, A. Sima
  • Biology, Medicine
  • Journal of cellular and molecular medicine
  • 2001
Being the most efficient hypolipidemic compounds that have reduced the rate of mortality in coronary patients, statins reduce significantly the incidence of coronary events, both in primary and secondary prevention. Expand
Tocotrienol: a review of its therapeutic potential.
The physiological activities of tocotrienol suggest it to be superior than alpha-tocopherol in many situations, indicating that tocotrianol may serve as an effective agent in the prevention and/or treatment of cardiovascular disease and cancer. Expand
Inhibitory effect of novel diallyldisulfide analogs on HMG-CoA reductase expression in hypercholesterolemic rats: CREB as a potential upstream target.
The results show that DADS analogs are effective in reducing the total lipid levels which could be correlated with a significant decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity, and their unique anti-inflammatory effect and hypolipidemic action may be beneficial in preventing the vascular complications that are induced by hyperlipidemia. Expand
Inhibition of cholesterol biosynthesis by Delta22-unsaturated phytosterols via competitive inhibition of sterol Delta24-reductase in mammalian cells.
In conclusion, inhibition of sterol (24)-reductase was achieved at physiologically relevant concentrations, and may represent an additional mechanism for the cholesterol-lowering action of phytosterols, and opens up the possibility of using certain (22)-unsaturated sterols as effective hypocholesterolaemic agents. Expand
Flavonoid antioxidants: chemistry, metabolism and structure-activity relationships.
The diversity and multiple mechanisms of flavonoid action, together with the numerous methods of initiation, detection and measurement of oxidative processes in vitro and in vivo offer plausible explanations for existing discrepancies in structure-activity relationships. Expand
Regulation and degradation of HMGCo-A reductase
  • T. Panda, V. Devi
  • Biology, Medicine
  • Applied Microbiology and Biotechnology
  • 2004
This review presents the importance of regulation and degradation of the HMGR enzyme in different systems to gain possible insight into alternative schemes for regulating this enzyme and, if these exist, the feasibility of extending them same to studies in mammalian systems. Expand
Structural mechanism for statin inhibition of 3-hydroxy-3-methylglutaryl coenzyme A reductase.
  • E. Istvan
  • Medicine, Chemistry
  • American heart journal
  • 2002
3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase catalyzes the committed step in cholesterol biosynthesis, which is the target of compounds that are very effective in lowering serum cholesterol levels. Expand
Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin.
Findings clearly differentiate the OSC inhibitor Ro 48-8.071 from simvastatin, and support the view that OSC is a distinct key component in the regulation of the cholesterol synthesis pathway. Expand
Microbial Production and Biomedical Applications of Lovastatin
The structure, biosynthesis, various modes of fermentation and applications of lovastatin, a potent hypercholesterolemic drug used for lowering blood cholesterol, are reviewed. Expand