• Korean Journal of Poultry Science
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• v.23 no.3
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• pp.129-134
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• 1996

his study was conducted to determine the effect of dietary garlic supplementation on the growing performance and activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase in broiler chicks from 3 to 5 wk post hatching. Fifty chicks were divided into 5 groups with 10 replicates per treatment and placed in a wire battery cage. Five levels of dietary garlic(0, 0.1, 0.3, 0.6 and 1.0%) were provided in an one way analysis. Feed and water were given ad libitum. Feed intake, weight gain and feed conversion rate(FCR) were not affected by the garlic supplementations. The HMG-CoA reductase activity decreased significantly(P<0.05) with the supplementation of garlic powder, compared to the garlic free group. As the dietary garlic level was increased, chicks showed decreased lipid contents in liver and blood serum. The results of this study indicate that blood cholesterol of chicks fed garlic supplemented diet might be reduced by inhibition of RMG-CoA reductase activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.4
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• pp.958-962
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• 1999

Hydroxy methylglutaryl CoA(HMG CoA) reductase and acyl CoA:cholesterol acyltransferase(ACAT) are two important enzymes that are associated with regulation of cholesterol metabolism. The inhibitors of HMG CoA reductase and ACAT are very effective in lowering serum cholesterol in most animal species. In present study, various plant extracts with hot water were used to examine the inhibitory activities against HMG CoA reductase and ACAT that are involved in cholesterol biosynthesis and cholesterol esterification in tissues, respectively. The extracts of Fagophyrum rotundatum, Rosa multiflora, Rosa rugosa and Alisma orientalis exhibited significant inhibitory activities against the ACAT, 29%, 24%, 19%, and 18%, respectively. However the extracts of Typha augustifolia, Polygonum cuspidatum, Crataegus pinnatifida, Polygonum multiflorum inhibited the HMG CoA reductase activity by 53%, 42%, 37%, and 33% respectively. Results suggest that these plant extracts might play important roles in the regulation of the cholesterol metabolism in vivo.

• Proceedings of the Korean Society of Food Hygiene and Safety Conference
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• 2003.11a
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• pp.46-46
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• 2003

Hypocholesterolemic peptide isolated from glycimin (11S protein) hydrolyzate by trypsin was purified and identified as LPYP and IAVPGEVA. To investigate the effects of phyiscal properties of side chains of the hypocholesterolemic activity, some of mutant peptides were designed and synthesized chemically. The structure related structures of each peptide were simulated and constructed and their conformations were observed by using spectropolarimeter. The hypocholesterolemic activities were monitored by assaying the inhibition of 3-hydroxy-3-methylglutaryl CoA reductase (HMG-CoA reductase) in vitro and by the determination of cholesterol content in mice serum. For LPYP derivatives, Hypocholesterolemic activity was lost when hydrophobic leucine residue at N-terminus was not so critical for maintaining hypocholesterolemic activity. For idealogical design of hypocholesterolemic peptides, the structure of HMG-CoA reductase are shown and inhibition mechanism of some peptides or inhibitors will be presented. For IAVPGEVA derivative inhibition of HMG-CoA reductase has been studied. For detail study of hypocholesterolemic activity, kinetic study of inhibition of peptides on HMG-CoA reductase and structural view of ligand binding should be investigated.

• Journal of the Korean Society of Food Science and Nutrition
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• v.21 no.5
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• pp.496-501
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• 1992

The present work tested the inhibitory effects of bile acids on the cholesterol biosynthesis and the activity of HMG-CoA reductase in cultured rat hepatocytes. The uptake of bile acids in hepatocytes were increased in according to the different bile acid concentrations and culture times. The rate of cholesterol synthesis in cells were inversely decreased to the bile acid concentrations and culture times. As expected, insulin injection (4 units/100g body weight) showed an enhancing effect of the cholesterol synthesis and the HMG-CoA reductase activity. The addition of bile acids in medium of insulin-treated hepatocytes also showed the suppressing effect. This effect was directly confirmed in isolated hepatic icrosomes by the test of HMG-CoA reductase activity. In the test of $Na^+$,$K^+$-ATPase activity in the isolated hepatocyte membrane, only the cholic acid did not stimulate the enzyme system. The reason of such difference is not obvious, but this result indicates that the cholic acid could be absorbed by simple diffusion.

• Journal of Life Science
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• v.27 no.3
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• pp.325-333
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• 2017

High level of plasma cholesterol is strongly associated with the development of atherosclerosis and coronary heart disease. Clinical trials designed to reduce plasma cholesterol level by diet or pharmacological intervention have resulted in marked reduction of disease incidence. The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which reduces cholesterol biosynthesis in the liver is the key enzyme of the mevalonate pathway that produces cholesterol. In this study, 71 naturally occurring phenolic compounds were tested for inhibitory activities against HMG-CoA reductase. Eleven compounds out of 71 showed inhibitory activities: three hydrolyzable tannin (geraniin, acetonyl geraniin and pentagalloyl ${\beta}-D-glucose$), four benzoic acid derivatives (benzoic acid, trans-cinnamic acid, 2,4-dihydroxybenzoic acid and 2,5-dihydroxybenzoic acid), and four naphthoquinone derivatives (1,2-naphthoquinone, 1,4-naphthoquinone, plumbagin and shikonin). At the concentration of $10{\mu}g/ml$, 1,4-naphthoquinone inhibited HMG-CoA reductase by 99.4%, and then plumbagin 91.4%, pentagalloyl ${\beta}-D-glucose$ 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonyl geraniin 30.2%, benzoic acid 28.5%, geraniin 28.3% and 2,5-dihydroxybenzoic acid 22.3%, respectively. $IC_{50}$ values of 1,4-naphthoquinone and plumbagin was $2.1{\mu}g/ml$ and $5.8{\mu}g/ml$, respectively.

• 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 Life Science
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• v.18 no.4
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• pp.427-434
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• 2008

Osteonecrosis of the femoral head (ONFH) is a multifactorial disease and certain individuals are more at risk or may be predisposed to it. An altered lipid metabolism is one of the major risk factors for osteonecrosis, especially corticosteroid therapy and alcoholism. 3-hydroxy-3-methylglutaryl coenzyme A. (HMG-CoA) reductase inhibitors, stalin used as lipid-clearing agent, have been known to decrease the risk of osteonecrosis in patients receiving steroids and affect coagulation and fibrinolysis. Therefore we evaluated the association of HMG-CoA reductase gene polymorphisms and haplotypes between osteonecrosis patients and normal controls. We directly sequenced the HMG-CoA reductase gene in 24 Korean individuals, and identified five sequence variants. Four SNPs (-6933C>T, -6045T>G, +12673G>A, and +18128C>T) were selected and genotyped in 349 male ONFH patients and 300 male control subjects. The genotypes, allele frequencies, and haplotypes of the polymorphisms in the total patients as well as in the subgroup by etiology were not significantly different from those in the control group. In addition, no significant differences between each genotype of the polymorphisms and plasma lipid level could be found in the control group. These results suggest that the polymorphisms and haplotypes of HMG-CoA reductase gene are unlikely to be associated with a susceptibility to ONFH.

• Journal of the Korean Society of Food Culture
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• v.4 no.2
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• pp.185-189
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• 1989

Effect of perilla oil on the fatty acid composition, ACAT and HMG-CoA reductase in the liver microsomes, or cholesterol and protein in serum of rabbit were examined. 1. The content of total protein in serum was almost same amount of both groups, but ${\alpha_1}-globulin$ and r-globuline were incresed or ${\beta}-globulin$ was decresed compared with control. 2. The content of high density lipoprotein incresed, and the content of low density lipoprotein decresed in lipoprotein. 3. Total cholesterol and triglyceride were decresed, and the content of phospholipid was incresed. 4. Perilla oil did not effect for changing blood glucose and $Na^+,\;K^+$ electrolytes. 5. Perilla oil did not effect for changing serum GOT and GPT in rabbit. 6. The activity of ACAT decresed and the activity of HMG-CoA reductase incresed. The activity of ACAT and HMG-CoA reductase in liver microsomes were reciprocal. 7. There were arachidonic acid 20:4, eicosapentaenoic acid 20:5, and docosahexaenoic acid 22:6 in the liver microsomes of rabbits. These highly polyunsaturated fatty acids were convented from linolenic acid 18:3 n-3.

• Journal of Nutrition and Health
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• v.35 no.10
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• pp.1015-1022
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• 2002

This study was conducted to examine the effects of dietary xylooligosaccharides on hepatic HMG-CoA reductase activity and morphological exchange of liver in rats fed high fat diet. Sprague-Dawley male rats weighing 100 $\pm$ 10 g were randomly divided into four groups, two normal diets and two high fat diets containing 1% cholesterol and 10% lard. Two normal diets were classified into a basal diet (normal group) and 10% xylooligosaccharide diet (NX group). The high fat diet groups were classified into a HF group without xylooligosaccharides diet and HFX group supplemented 10% xylooligosacchride diet. Experimental diets were fed ad libidum to the rats for 4 weeks and then they were sacrificed. The body weight of high fat diet (HF group) was increased more than that of normal group, but it was significantly decreased by xylooligosacchrides supplementation. The food intake was not significantly different among the all groups. The weight of liver, small intestine and cecum of all xylooligosaccharide supplemented groups were significantly heavier than those of normal and HF groups. The activity of hepatic HMG-CoA reductase, a rate limiting enzyme of cholesterol biosynthesis, in xylooligosaccharide supplemented groups was higher than that of HF group. Light micrographs revealed that the structures of hepatocytes in xylooligosaccharide supplemented groups were preserved well, compared to HF group. The xylooligosaccharide supplementation exerted a lipid-lowering action by decreasing cholesterol and triglycerides contents in hepatic tissue. In conclusion, the activity of hepatic HMG-CoA reductase and damage of liver in rats fed high fat diets were improved by dietary xylooligosaccharides.

• Journal of the Korean Wood Science and Technology
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• v.32 no.1
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• pp.17-27
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• 2004

Cholesterol inhibitory activity was investigated to develop the functional food from edible forest resources such as Allium victorialis var. platyphyllum and other 12 species. Among tested samples by enzyme-linked immunosorbant assay (ELISA), leaf extracts of A. victorialis var. platyphyllum inhibited 73.9% of the activities of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) which is the highly regulated and major rate-limiting of the cholesterol biosynthesis pathway. Moreover, those extracts inhibited 76.7% of squalene synthase which catalyzes the head-to-head condensation of two farnesyl pyrophosphate molecules to form squalene in the biosynthesis of cholesterol. In order to find out the compounds which would play a key role in inhibitory activity of cholesterol, kaempferol and quercetin were isolated from the dichloromethane soluble fraction of extracts of A. victorialis var. platyphyllum. Kampferol, quercetin and each soluble fraction was also subjected to the test of the mRNA expression of HMG-CoA reductase and squalene synthase by reverse transcriptase-polymerase chain reaction (RT-PCR) assay, respectively. By treating both enzymes with 10 ㎍/㎖ of kaempferol and quercetin for 24 hours, respectively, the mRNA expression was not observed, suggesting that both compounds inhibited the biosynthesis of cholesterol at mRNA level. In this regard, it could be inferred that cholesterol inhibitory activity of A. victorialis var. platyphyllum was derived from kaempferol and quercetin. Both compounds have already been found in many plant extracts including hardwood and softwood, but it might be first known that they have cholesterol inhibitory activity.