Compactin?a review

Chakravarti, Ritu; Sahai, Vaibhav

doi:10.1007/s00253-003-1553-7

Cited by 56 publications

(41 citation statements)

References 62 publications

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“…The structural similarity and high affinity of the acid form of statin for HMGCoA-R result in specific and effective inhibition of this enzyme. 23 Atorvastatin has rapid oral absorption with an Figure 6. Effects of inflammation on 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCoA-R) expression in the liver and aorta of mice.…”

Section: Discussionmentioning

confidence: 99%

Inflammatory Stress Induces Statin Resistance by Disrupting 3-Hydroxy-3-Methylglutaryl-CoA Reductase Feedback Regulation

Chen

Zhao

et al. 2014

ATVB

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Objective-The risk of cardiovascular disease is increased by up to 33 to 50× in chronic inflammatory states and convention doses of statins may not provide the same cardiovascular protection as in noninflamed patients. This study investigated whether the increase in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCoA-R)-mediated cholesterol synthesis observed under inflammatory stress was resistant to the action of statins and if so, whether this was because of interference with the sterol regulatory element binding protein cleavage-activating protein pathway. Approach and Results-Inflammatory stress was induced by adding cytokines (interleukin-1β, tumor necrosis factor-α, and interleukin-6) and lipopolysaccharides to vascular smooth muscle cells in vitro and by subcutaneous casein injection in apolipoprotein E/scavenger receptors class A/CD36 triple knockout mice in vivo. Inflammatory stress exacerbated cholesterol ester accumulation and was accompanied in vitro and in vivo by increased HMGCoA-R mRNA and protein expression mediated via activation of the sterol regulatory element binding protein cleavageactivating protein/sterol regulatory element binding protein-2 pathway. Atorvastatin reduced HMGCoA-R enzymatic activity and intracellular cholesterol synthesis in vitro. However, inflammatory stress weakened these suppressive effects. Atorvastatin at concentrations of 16 μmol/L inhibited HMGCoA-R activity by 50% in vascular smooth muscle cells, but the same concentration resulted in only 30% of HMGCoA-R activity in vascular smooth muscle cells in the presence of interleukin-1β. Knocking down sterol regulatory element binding protein cleavage-activating protein prevented statin resistance induced by interleukin-1β, and overexpression of sterol regulatory element binding protein cleavage-activating protein induced statin resistance even without inflammatory stress. In vivo, the amount of atorvastatin required to lower serum cholesterol and decrease aortic lipid accumulation rose from 2 to 10 mg/kg per day in the presence of inflammatory stress. Conclusions-Increased

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Section: Discussionmentioning

confidence: 99%

Inflammatory Stress Induces Statin Resistance by Disrupting 3-Hydroxy-3-Methylglutaryl-CoA Reductase Feedback Regulation

Chen

Zhao

et al. 2014

ATVB

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“…Statins are bioactive compounds synthesized by some micro-organisms which are known to inhibit cholesterol biosynthesis by inhibiting the HMGR (HMG CoA Reductase) enzyme [6]. Previous research stated that the discovery of Lactobacillus (lactic acid bacteria) as a statin-producing bacterium was a novelty because previous statin-producing microorganisms are known as fungi such as Aspergillus terreus, Penicillium brevicompactum, Streptomyces roseochromogenus, Streptomyces carbophilus, Streptomyces halstedii, Actinomadura sp., Streptomyces sp., and Bacillus megaterium [7].…”

Section: Results and Discussion Decreasing Total Cholesterol Levels VImentioning

confidence: 99%

Therapy of Lactobacillus casei Shirota strain Fermented Milk to Rats with High-Cholesterol Diet toward Cholesterol Levels and SOD Activity

Rohma

Mahdi

Aulanni’am

2017

J. Pure App. Chem. Res.

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This study aimed to determine the fermented milk of Lactobacillus casei Shirota strain potential on cholesterol levels, SOD activity, LPL enzyme activity, and cardiac histopathology. This study used 25 rats (Rattus novergicus) Wistar strain aged 2-3 months, weighing 150-200 grams. These rats were divided into 5 groups: negative control group, positive control group with high-cholesterol diet for 21 days, and therapy group with 1.0 ; 1.5 ; 2.0 mL/rat/day of fermented milk for 14 days. The analysis methods used in this study are One Way ANOVA and Tukey. The results showed that the fermented milk of Lactobacillus casei Shirota strain had a strong effect on blood cholesterol levels and increasing the SOD activity. This study also showed that the fermented milk of Lactobacillus casei with 2.0 mL/rat/day is the most effective dose to decrease the total cholesterol and increase the SOD activity.Keywords: cholesterol, fermented milk of Lactobacillus casei Shirota strain, total cholesterol, SOD INTRODUCTIONCholesterol is a steroid alcohol on the class of lipids (fats) which play a part as a source of calories. In addition, cholesterol is a component of fat found in the blood of animals and humans that produced by the liver and used as an energy producer. It is also the wallforming cells in the body and as a basic ingredient of the steroid hormones formation in the body. Cholesterol is the precursor of all steroids, such as corticosteroids, sex hormones, bile acids, and vitamin D.Consuming lots of high-cholesterol diet can lead to the increasing of cholesterol levels. It causes hypercholesterolemia, atherosclerosis in the arteries, and blood vessels constriction in the heart, brain, kidneys, and eyes when it reaches beyond the normal limits. Hypercholesterolemia is a condition when the blood cholesterol level exceeds the normal value of 200 mg/dL. In the body, cholesterol found in lipoproteins, such as chylomicrons, which contains triglycerides, VLDL (very low density lipoprotein) to transport triglycerides. The triglycerides formed by the heart, LDL (low density lipoprotein) or beta-lipoprotein consisting of 25% protein and 40% cholesterol and HDL (high density lipoprotein) or alpha lipoprotein contain 50% protein and 20% cholesterol [1].

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“…There exists another class of synthetic statins (e.g. rosuvastatin, atorvastatin, pitavastatin, and cerivastatin) which are prepared by a series of chemical reactions and have low inhibition constant (K i ) values than the statins derived by the fermentation route [15,45,46,65].…”

Section: Origin and Routes Of Synthesis Of Hypo-cholesterolemic Compomentioning

confidence: 99%

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

Seenivasan¹,

Panda

Théodore³

2011

TOEIJ

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Studies on the various cholesterol-lowering agents is one of the important areas in clinical research. Identification and characterization of potential molecules from various sources have been carried out in the past and their relationship with the enzymes which are involved in the cholesterol cascade is gaining interest. In this review, we have highlighted 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 characterization 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.

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Compactin?a review

Cited by 56 publications

References 62 publications

Inflammatory Stress Induces Statin Resistance by Disrupting 3-Hydroxy-3-Methylglutaryl-CoA Reductase Feedback Regulation

Inflammatory Stress Induces Statin Resistance by Disrupting 3-Hydroxy-3-Methylglutaryl-CoA Reductase Feedback Regulation

Therapy of Lactobacillus casei Shirota strain Fermented Milk to Rats with High-Cholesterol Diet toward Cholesterol Levels and SOD Activity

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

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