• YAKHAK HOEJI
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• v.37 no.1
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• pp.100-106
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• 1993

Designed system, in which the $\beta$-hydroxy-$\delta$-lactone moiety is connected to benzimdazole ring by ethylene bridge, was propared from 2-sustd. benzimidazole as a potential HMG-CoA reductase inhibitor.

• Microbiology and Biotechnology Letters
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• v.34 no.1
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• pp.52-57
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• 2006

For the purpose of production of a novel antihyperlipemial HMG-CoA reductase inhibitor from bacteria, a bacterium which showed the highest HMG-CoA reductase inhibitory activity was isolated from traditional Doenjang. This strain was identified as Bacillus cereus (D-3) based on its microbiological characteristics and 165 rRNA sequence analysis. The maximal HMG-CoA reductase inhibitor production from Bacillus cereus D-3 was obtained by cultivation in a Glucose-CSL broth containing 2% glucose, 0.6% corn steep liquor, $0.04%\;K_{2}HPO_4$ and $0.05%\;KH_{2}PO_4$ at $30^{\circ}C$ for 36 h. The final HMG-CoA reductase inhibitory activity under the above conditions was 39.4%.

• Archives of Pharmacal Research
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• v.18 no.3
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• pp.206-212
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• 1995

New hypolipaemic agents, in which substituted indazole nucleus is connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to show significant inhibitory activity against microsomal HMG-CoA reductase in rat liver.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.158-170
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• 1997

New HMG-CoA reductase inhibitors, in which 3-substituted 4, 5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor $(11cc, IC_{50}=0.01{\mu}M)$ is 4-fold more potent than lovastatin.

• Journal of the Korean Society of Food Science and Nutrition
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• v.45 no.2
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• pp.293-297
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• 2016

Hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase) is the rate-limiting enzyme in biosynthesis of cholesterol in animals. In this study, inhibitory effects of isoflavone glycosides on HMG-CoA reductase were investigated. At sample concentration of $100{\mu}M$, genistein-7-O-triglucoside (G2-genistin) inhibited HMG-CoA reductase activity by approximately 18%, whereas daidzein-7-O-triglucoside had no inhibitory effect. In the kinetic experiments with Syrian hamster HMG-CoA reductase, G2-genistin showed inhibitory efficacy with an invariable $V_{max}$ value, suggesting that G2-genistin works as a competitive inhibitor of HMG-CoA reductase and has potential for hypocholesterolemic action through direct regulation of HMG-CoA reductase.

• Preventive Nutrition and Food Science
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• v.5 no.4
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• pp.184-188
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• 2000

HMG-CoA reductase is th rate-limiting enzyme of cholesterol biosynthesis. As intracellular levels of cholesterol should be regulated elaborately in response to external stimuli an internal needs, the expression of the HMG-CoA reductase gene is regulated intricately at several different levels from transcription to post-translational modification. In this study, we investigated the regulatory mechanism of HMG-CoA reductase gene expression at the post-transcriptional/pre-translational levels in a baby hamster kidney cell line, C100. when 25-hydroxycholesterol was added to cells cultured in medium containing 5% delipidized fetal bovine serum and 25$\mu$M lovastatin, the levels of HMG-CoA reductase mRNA decreased rapidly, which seemed to be due to the increased degradation of reductase mRNA. These suppressive effects of 25-hydroxycholesterol on MG-CoA reductase mRNA levels were blocked by a translation inhibitor, cycloheximide. Similarly, actinomycin D and 5,6-dichloro-1-$\beta$-D-ribofuranosylbenzimidazole, transcription inhibitors, blocked the 25-hydroxycholesterol-mediated degradation of HMG-CoA reductase mRNA. These results indicate that new protein/RNA synthesis is required for the degradation of HMG-CoA reductase mRNA. In addition, data from the transfection experiments shows that cis-acting determinants, regulating the stability of reductase mRNA, were scattered in the sequence corresponding to 1766-4313 based on the sequence of Syrian hamster HMG-CoA reductase cDNA. Our data suggests that sterol-mediated destabilization of reductase mRNA might be one of the important regulatory mechanism of HMG-CoA reductase gene expression.

• Korean Journal of Food Science and Technology
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• v.30 no.1
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• pp.224-229
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• 1998

A study was conducted to screen the inhibitory activity of 3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase, which is known to be rate-limiting enzyme in cholesterol bosynthesis, from the extracts of 80% methanol and 70% ethanol of cereals and regumes. The strongest inhibitory activity was shown in the ethanol extract of sorghum among the ethanol extracts. The inhibitory activity of HMG-CoA reductase of prosomillilet methanol extract was 73%, and highest among the methanol extracts. The inhibitory activity of 44.7% was observed in sorghum methanol extract. The methanol extracts of prosomillet and sorghum were further fractionated with hexane, chloroform, ethylacetate, butanol and water. HMG-CoA reductase inhibitory activity was shown in all fractions of prosomillet and sorghum methanol extracts. Hexan fraction of both prosomillet and sorghum had the strongest inhibitory activity among five fractions, and the inhibitory activity was increased compared to each crude extracts.

• Food Engineering Progress
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• v.13 no.4
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• pp.243-250
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• 2009

Pravastatin sodium, competitive inhibitors of HMG-CoA(3-hydroxy-3-methylglutaryl coenzyme A) reductase, is produced from the culture broth of Streptomyces carbophilus KCCM 10370, The production of Pravastatin sodium was increased about 45 fold compared to wild type by UV mutation. Production of Pravastatin was also improved by continuous feeding of Compactin sodium to 24% and bioconversion ratio was also increased to 4.3% by intermittent addition. In main culture, concentration of Compactin sodium was kept less than 0.1%(w/v) under continuous feeding of Compactin sodium then product was 0.49% and bioconversion was 70%. After finishing the fermentation, Pravastatin was purified by various chromatographies such as Diaion HP20 resin column, Partition, and ODS(Octa-Decylsilyl Silicagel) resin column with a final yield of 70~72% and over 99.7% purity. The IR, UV, and NMR study of the purified Pravastatin sodium showed the same pattern as that of EP(European Pharmacopoeia).

• KSBB Journal
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• v.6 no.1
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• pp.55-61
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• 1991

The objective of this in vitro study is to screen a possible inhibitor, originated from some chinese herb medicines, of 3-hydroxy-3-methylglutaryl Coenzyme A (HMG-CoA) reductase that is the major regulatory enzyme of hepatic cholesterol biosynthesis. Fourteen kinds of herbal plant were extracted with water and evaporated for prescreening. The methanol extracts of the effective 3 kinds (9 species) were fractionated with chloroform, ethylacetate, butanol and water, and vacuum evaporated. The degree of inhibition of the extracts to HMG-CoA reductase activity was calculated by the spectrophotometric method using microsomal protein of Saccharomyces cerevisiae ATCC 42949 as an enzyme source. Among these samples, marked inhibitory effects were observed in the extracts of ethylacetate and chloroform fractions of the Rosa rugosa roots, and those of butanol, ehtylacetate and water fractions of pine leaves. Also, the inhibitory effects of the extracts obtained from buckwheat shell and the roots of Rosaceae were found.

• Archives of Pharmacal Research
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• v.17 no.3
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• pp.161-165
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• 1994

New hypolipaemic agents, in which benzotriazole moiety is connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to show sinificant cholesterol-lowering effect comparable to mevinolin.