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Chemistry Matrices of Biotransformation
Published in Shrikaant Kulkarni, Neha Kanwar Rawat, A. K. Haghi, Green Chemistry and Green Engineering, 2020
Atorvastatin is an intermediate and an active ingredient of the cholesterol-reducing drug, Lipitor. As many as three-enzyme processes have been designed as a part of green-by-design, for the synthesis of a key intermediate in the manufacture of atorvastatin, the active ingredient of the cholesterol-lowering drug Lipitor [59, 60]. The process has been commercialized by Codexis. The first step involves the biocatalytic reduction of ethyl-4-chloroacetoacetate, using a ketoreductase (KRED) in presence of glucose and an NADP-dependent glucose dehydrogenase (GDH). The product, ethyl-4-chloro-3-hydroxybutyrate is obtainable with a 96% yield in isolation and >99.5% Enantiomeric excess (ee). It is followed by the application of halohydrin dehalogenase (HHDH) to catalyze a nucleophilic substitution of chloride with cyanide, using HCN under pH = 7 and room temperature (RT) conditions. Table 4.3 shows the directed evolution of KRED & GDH Biocatalyst.
Atorvastatin ameliorated PM2.5-induced atherosclerosis in rats
Published in Archives of Environmental & Occupational Health, 2023
Hongmei Yao, Xingxing Zhao, Lili Wang, Yi Ren
In the present study, atorvastatin (ATO), one of the most widely-used statins, was employed to investigate if amelioration of PM2.5-induced atherosclerosis development could be achieved. Statins, the inhibition of 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, can effectively decrease the LDL level and meanwhile increase the HDL level.18–20 It is common sense that statins have a lipid-lowering effect. Recently, statins were found to have anti-atherogenic effects, because the lipid-lowering effect of statins could slow the formation of atherosclerotic plaque, suppress smooth muscle cell proliferation and aggregation, reduce the size of atherosclerotic plaques, and prevent from further development of atherosclerotic plaque.21–23 As previously reported, atorvastatin inhibited HMG-CoA reductase and blocked the reaction of HMG-CoA to methylpentanoic acid, which significantly reduces cholesterol synthesis and neutralizes cholesterol concentrations in plasma and tissues.24 Because of the decrease of cholesterol level in the liver, the inhibition of LDL receptor genes was lifted, and thus LDL receptor density in the liver increased, which resulted in high concentrations of LDL molecules in the plasma being taken up and cleared by the liver. As represented in Table 1, in our PM2.5 - atorvastatin treated model, TC, TG, and LDL levels decreased significantly, demonstrating that atorvastatin presented an obvious lipid-lowing effect. Increasing LDL levels could provoke the formation of atherosclerosis by vasoconstriction, inflammation, proliferation of smooth muscle cells, and degradation of collagen fibers.16
Development and in vitro appraisal of Soluplus® and/or Carbopol® 971 buccoadhesive patches releasing atorvastatin
Published in The Journal of Adhesion, 2022
Aseel Abu-Rumman, Rana Abu-Huwaij, Rania Hamed
Atorvastatin (ATR) is an HMG-CoA reductase inhibitor that is used to lower cholesterol. Nonetheless, its high protein binding capacity (>95%), low oral bioavailability of 12–14% in humans owing to first-pass metabolism, and marginal solubility in phosphate buffer (pH 7.4) and distilled water, contradict its oral use .[3] It is categorized as class II according to the Biopharmaceutics Classification System of low solubility and high permeability .[4] Thus, it is an ideal candidate for improving bioavailability by merely boosting its solubility.
Pomegranate juice supports therapeutic –treatment of atorvastatin against maternal hypercholesterolemia induced retinopathy of rat offspring
Published in Egyptian Journal of Basic and Applied Sciences, 2021
Hassan IH EL-Sayyad, Hebattallah A Abd El-Gallil, Heba A El-Ghawet
Atorvastatin is used to reduce the biosynthesis of cholesterol by inhibiting the precursor enzyme 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. The applied dose of 0.5 g atorvastatin calcium trihydrate (Sigma – Aldrich, company) was dissolved in 1 mL 70% ethyl alcohol and diluted with 50 mL saline solution. Applied dose of 1 mL3 containing 10 mg/kg body weight was administered by sterile stomach tube on alternating days from the 6th day of conception, during gestation and lactation period up to 21 days post-partum [29].