• 한국생물공학회:학술대회논문집
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• 2002.04a
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• pp.184-187
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• 2002

Lovastatin is a cholesterol-lowering agent, which plays a role of an inhibitor of 3-hydroxy-3- methylglutaryl coenzyme A reductase (HMG-CoA). When thiamine was supplemented in 3L batch fermentation, the production of lovastatin was improved. At the same time, the levels of pyruvic acid and NAD(P)H were estimated in the course of the fermentation of A. terreus. For the high level production of lovastatin, semi fed-batch fermentation was performed. And the thiamine level was maintained to a concentration of 20 mg/L and glucose was supplied. The final dry cell weight was lowered by 30 % and final lovastatin concentration was increased by 33 %. Final lovastatin concentration of 3.3 g/L was achieved in 8 days.

• Food Science and Biotechnology
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• v.15 no.4
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• pp.647-649
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• 2006

Mevinolin, a fungal metabolite, is a potent inhibitor of 3-hydroxy-methyl-3-glutaryl-coenzyme A (HMG-CoA) reductase, the rate-controlling enzyme in cholesterol biosynthesis. In this investigation, the optimum factors for mevinolin production by Monascus pilosus IFO 480 in soymeal fermentation were studied. The highest yield of mevinolin, 2.82 mg mevinolin per g dry weight, without citrinin (a toxic fungal secondary metabolite) was obtained after 21 days of fermentation at $30^{\circ}C$ at 65% moisture content, particle size 0.6-0.9 mm, and initial substrate pH of 6.0. Mevinolin was present in the fermentation substrate predominantly in the hydroxycarboxylate form (open lactone, 92.1-97.3%), which is currently being used as a hypocholesterolemic agent.

• Biomedical Science Letters
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• v.26 no.2
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• pp.101-108
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• 2020

There has been a lot of interest in medicinal effects for hyperlipidemia from the natural product since the therapy of atherosclerosis has emerged as social concern. Rats were acclimated to the feeding environment for one week and induced to obesity with high fat diet during 4 weeks until their body weight were more than 30% of normal range. To evaluate the effect of hyperlipidemia of mulberry leaf of Morus alba and yacon tuber of Smallanthus sonchifolia extracts (MLYT), 1%, 3%, 5% of MLYT were treated to Sprague-Dawley rats. Aspartate transaminase (AST) was significantly increased 26.2% in high fat diet group (G2) compared to normal diet group (G1) (P<0.05). But AST were significantly decreased in high fat diet with 0.5% hydroxycitric acid diet group (G3) and all the MLYT treated groups compared to G2. Total cholesterol, low-density lipoprotein (LDL), triglycerides and phospholipids were observed significant improvements in the MLYT-treated groups (P<0.05). These improvements in liver and feces were further supported by the lipid content. MLYT remarkably suppressed the level of lipid peroxidation caused by high-fat diet in rats. The level of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase activity. As a result, the proper combination of mulberry leaves and yacon tuber extract will have a synergistic effect on hyperlipidemia. These results indicate that MLYT could be a candidate for the improvement of hyperlipidemia.

• Journal of Pharmaceutical Investigation
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• v.41 no.4
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• pp.239-247
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• 2011

Simvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in the biosynthesis of cholesterol. Simvastatin has good permeability, but it also has low solubility (BCS class II), which reduces its bioavailability. To overcome this problem, a solid dispersion is formed using a spray-dryer with polymeric material carrier to potentially enhance the dissolution rate and extend drug absorption. As carriers for solid dispersion, Gelucire$^{(R)}$44/14 and Gelucire$^{(R)}$ 50/13 are semisolid excipients that greatly improve the bioavailability of poorly-soluble drugs. To avoid any toxic effects of an organic solvent, we used aqueous medium to melt Tween$^{(R)}$ 80 and distilled water. The structural behaviors of the raw materials and the solid dispersion were analyzed by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The DSC and PXRD data indicated that the crystalline structure of simvastatin was transformed to an amorphous structure through solid dispersion. Then, solid dispersion-based tablets containing 20 mg simvastatin were prepared with excipients. Dissolution tests were performed in distilled water and artificial intestinal fluid using the USP paddle II method. Compared with that of the commercial tablet (Zocor$^{(R)}$ 20 mg), the release of simvastatin from solid dispersion based-tablet was more efficient. Although the stability study is not complete, this solid dispersion system is expected to deliver poorly water-soluble drugs with enhanced bioavailability and less toxicity.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.237-237
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• 2002

Creatine phosphokinase (CPK) was a marker in diagnosis of rhabdomyolysis. The CPK abnormality could be induced by intake of HMG CoA reductase inhibitors (statins). The objective of this study was to estimate the incidence rate of CPK abnormality by each statin. (omitted)

• Biomolecules & Therapeutics
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• v.16 no.1
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• pp.28-33
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• 2008

Atorvastatin calcium salt (1) was obtained through the preparation of lactone compound (8) from 2-((4R,6R)-6-(2-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-ethyl)-2-phenyl-1,3,2-dioxaborinan-4-yl)acetic acid tert-butyl ester (9) by hydrolysis in basic condition. Efficient hydrolysis of boronate compound 9 aimed at the viable synthesis for commercial production and purification of Atorvastatin calcium is reported. Detail studies of evaluation procedure are also reported.

• Korean Journal of Acupuncture
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• v.27 no.2
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• pp.121-140
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• 2010

Objectives & Methods : The purpose of this study is to observe the effects of Bupleuri Radix Herbal-acupuncture at GB34(Yangneungcheon) of hyperlipidemic rats. The author performed several items to analyze body-weight of the rats, weight of its liver, serum as well as urine changes in each group. Results : 1. Bupleuri Radix herbal-acupuncture(BR-HA) infused solution (MCR-HAS) increased both DPPH radical scavenging activity and HMG-CoA reductase inhibition rate in rat liver cells. 2. BR-HA at GB34 significantly decreased the level of serum total cholesterol and atherogenic index(AI), while significantly increased the ratios of high-density lipoprotein (HDL)/total cholesterol and phospholipid/total cholesterol in hyperlipidemic rats. 3. BR-HA at GB34 significantly decreased urine glucose in hyperlipidemic rats. Conclusions : From the results above, it is suggested that Bupleuri Radix herbal -acupuncture at GB34 has a therapeutic effect on hyperlipidemia.

• The Journal of Internal Korean Medicine
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• v.30 no.2
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• pp.338-354
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• 2009

Objective : Gamijihwang-tang(GJT) has been used as a therapeutic agent for hyperlipidemia in oriental medicine for several years. This study was performed to investigate the effects of GJT on hyperlipidemia in rats using diverse biological methods. Method : Hyperlipidemia was induced by a hyper-lipidemic diet fed for 4 weeks. Total cholesterol, LDL-cholesterol, HDL-cholesterol, triglyceride, and glucose were measured in the serum after an oral administration of GJT. Lipid peroxidase, SOD, catalase, ACAT, and HMG-CoA were measured in liver after oral administration of GJT. Result: 1. GJT showed safety against cytotoxicity and toxicity in liver. 2. GJT significantly decreased rat's body and liver weight. 3. GJT significantly decreased serum total cholesterol and LDL-cholesterol, but increased serum HDL-cholesterol. 4. GJT significantly decreased serum triglyceride and glucose. 5. GJT significantly decreased lipid peroxidation and increased SOD and catalase in liver. 6. GJT significantly decreased ACAT and HMG-CoA reductase of cholesterol manifestation in liver. Conclusions : These results suggest that GJT might be effective in treatment and prevention of hyperlipidemia.

• Proceedings of the Korea Society of Poultry Science Conference
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• 2006.11a
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• pp.64-65
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• 2006

The effects of garlic extracts, lactic acid bacteria, copper and selenium as cholesterol lowering material on productivity and content of egg cholesterol in layer were investigated. The layers were divided into seven treatment groups and fed commercial diet or experimental diets containing probiotics, garlic powder, selenium and copper for 6 weeks. There was no significant difference in egg production between groups. The content of egg yolk cholesterol by combination feeding of probiotics, garlic powder, selenium and copper were significantly reduced by 13.5-29.8% as compared to that of control. The levels of mRNA expression of HMG-CoA reductase were significantly decreased by dietary treatments.

• Journal of Nutrition and Health
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• v.31 no.2
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• pp.135-142
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• 1998

This study was undertaken to determine whether dehulled defatted flour has an effect on postprandial plasma lipoprotein composition, hepatic lipid composition, enzyme and hormone levels in rats. Control(casein) and experimental (dehulled defatted soy flour)diets were fed to rats for 7 weeks. all animals (S. D. rats, male) were sacrificed 2 hrs after the feeding of 5g of each diet. Defatted soy flour feeding significantly lowered postprandial plasma total cholesterol, chylomicron/VLDL-cholesterol, hepatic cholesterol and triglyceride(TG) as compared with casein feeding, whereas no significant effect on plasma TG was observed. Intestinal kipase activity was elevated , whereas trypsin activity was suppressed in the dehulled defatted soy flour group. Plasma glucagon, thyroid hormone and hepatic HMG-coA reductase levels were not affected by diet treatment. These results hypothesize that dehulled defatted soy flour affects cholesterol digestion and absorption in guts, thus delaying the appearance of chylomicron cholesterol in plasma or affecting the disappearance of chylomicron remnant to high-density-lipoprotein(HDL).