Characterization, Modes of Synthesis, and Pleiotropic Effects of Hypocholesterolemic Compounds – A Review
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TLDR
Major natural sources as well as synthetic and biological routes of synthesis of these compounds are reviewed in a concise manner and various HMG-CoA analogues including statins have been reviewed specifically.Abstract:
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, phytosterols, phytostanols, statins, DADS, and synthetic compounds. The mechanism of action and characteri- zation of these hypocholesterolemic compounds are discussed in this communication. Major natural sources as well as synthetic and biological routes of synthesis of these compounds are reviewed in a concise manner. Especially, various HMG-CoA analogues including statins have been reviewed specifically. In this respect, researchers have identified 2,3- oxidosqualene cyclase-lanosterol synthase (lanosterol syn- thase, oxidosqualene-lanosterol cyclase, lanosterol synthase, 2,3-oxidosqualene-lanosterol cyclase, human lanosterol syn- thase (EC 5.4.99.7)) having a molecular weight of 83 kDa, catalyzing the highly selective cyclization reaction from the substrate 2,3-oxidosqualene (squalene 2,3-epoxide, squalene 2,3-oxide, (S)-squalene-2,3-epoxide, 2,3-epoxisqualene, oxidosqualene) into lanosterol, as an appropriate step for the inhibition of cholesterol biosynthesis (3). Oxidosqualene cyclase inhibitors (OSCI) arrest the downstream of 2,3- oxidosqualene which helps to stimulate epoxysterols toread more
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Cellular Localization and Production of Lovastatin from Monascus purpureus
TL;DR: Lovastatin is the first FDA-approved antihypercholesterolemic drug for the treatment of cardiovascular diseases with pleiotropic clinical applications and Monascus purpureus is one of the safest molds for the production of lovastatin.
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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.
TL;DR: 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.
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Hypolipidemic Activity of Solvents Extracts of Khaya senegalensis Stem Bark in Diet Induced Hyperlipidemic Rats
A. J. Alhassan,I. U. Muhammad,M. A. Dangambo,A. Idi,A.M. Gadanya,Arifullah Mohammed,S.M. Adamu +6 more
TL;DR: The research found that aqueous methanol extract of Khaya senegalensis possess hypolipidemic ability with the ethyl acetate extract showing the highest potency with a significant (p<0.01) decrease in serum total cholesterol, triglyceride and LDL-cholesterol level when compared to hyperlipidemic control.
References
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TL;DR: 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.
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Eva S. Istvan,Johann Deisenhofer +1 more
TL;DR: The structures of the catalytic portion of human HMGR complexed with six different statins are determined, which show several catalytically relevant residues are disordered in the enzyme-statin complexes.
Journal ArticleDOI
Chemical, pharmacokinetic and pharmacodynamic properties of statins: an update
TL;DR: Clinical studies have demonstrated rosuvastatin to be the most effective for reducing low‐density lipoprotein cholesterol, followed by atorvastsatin, simvastasin and pravastatin, and the bioavailability of the statins differs greatly, from 5% for lovastatin and simvASTatin to 60% or greater for cerivastatinand pitavastatin.
Journal ArticleDOI
Cholesteryl Ester Transfer Protein: A Novel Target for Raising HDL and Inhibiting Atherosclerosis
Philip J. Barter,H. Bryan Brewer,M. John Chapman,Charles H. Hennekens,Daniel J. Rader,Alan R. Tall +5 more
TL;DR: Small-molecule inhibitors of CETP have now been tested in human subjects and shown to increase the concentration of HDL cholesterol while decreasing that of LDL cholesterol and apoB, and test the hypothesis in randomized trials of humans that pharmacological inhibition of CETp retards the development of atherosclerosis.
Journal ArticleDOI
Statins: mechanism of action and effects
Camelia S. Stancu,Anca Sima +1 more
TL;DR: 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.