The enzyme 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase is crucial to insect development and reproduction, as revealed by the sterilising properties of some specific inhibitors of it. In the present paper, we study the sterilising effects of a number of HMG-CoA reductase inhibitors on the German cockroach, Blattella germanica (L). The inhibitors tested were naringenin, lovastatin, mevasta...

Members of the statin family of 3-hydroxy-3-methylglutaryl CoA reductase inhibitors are being investigated for the therapy and prevention of cancers because of their growth-inhibitory effects on epithelial cells. Some epidemiologic studies show that patients taking statins show a lower incidence of cancer compared with those taking other cholesterol-lowering medication. In contrast, other studi...

The objective of the present study was to determine the efflux transporters responsible for acid and lactone statin drug efflux using transporter knockdown Caco-2 cells. The bidirectional transport was determined in Caco-2 cell monolayers in which the expression of P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), or multidrug resistance associated protein 2 (MRP2) was knocked dow...

Hypercholesterolaemia plays a crucial role in the development of atherosclerotic diseases in general and coronary heart disease in particular. The risk of progression of the atherosclerotic process to coronary heart disease increases progressively with increasing levels of total serum cholesterol or low density lipoprotein (LDL) cholesterol at both the individual and the population level. The s...

To the Editor: In his editorial,1 Furberg cites CURVES2 as demonstrating that atorvastatin “unfavorably influences” HDL cholesterol (HDL-C) concentrations. In fact, atorvastatin 10 to 40 mg/d increased HDL-C 4.8% to 5.5%, typical for a statin. In a much smaller group, atorvastatin 80 mg/d did not affect HDL-C levels.2 The sample size (10 patients) raises questions, because HDL-C response with s...

OBJECTIVE To evaluate the comparative efficacy and safety of the 4 currently available hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors, fluvastatin, lovastatin, pravastatin, and simvastatin, in the treatment of primary hypercholesterolemia. DATA SOURCES English-language clinical studies, abstracts, and review articles identified from MEDLINE searches and bibliographies of iden...

Interactions between UCN-01 and HMG-CoA reductase inhibitors (ie, statins) have been examined in human leukemia and myeloma cells. Exposure of U937 and U266 cells to minimally toxic concentrations of UCN-01 and various statins (eg, lovastatin, simvastatin, or fluvastatin) dramatically increased mitochondrial dysfunction, caspase activation, and apoptosis. Comparable effects were observed in oth...

Pilot-scale libraries of eight-membered medium ring lactams (MRLs) and related tricyclic compounds (either seven-membered lactams, thiolactams or amines) were screened for their ability to inhibit the catalytic activity of human recombinant 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase in vitro. A dozen of the synthetic compounds mimic the inhibition of purified HMG-CoA reductase ac...