• Biomolecules & Therapeutics
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• 제16권1호
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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.

• Journal of Animal Science and Technology
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• 제51권4호
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• pp.307-314
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• 2009

육계사료 내 마늘분말의 첨가급여가 육계의 성장성적과 간 HMG-CoA reductase의 발현에 미치는 영향을 규명하기 위해 본 연구를 수행하였다. 1일령의 육계 Ross 수평아리에게 마늘분말을 0%(항생제 첨가 또는 항생제 무첨가), 1%, 3% 및 5%의 수준으로 첨가한 실험사료를 각각 6주간 급여하였다. 증체량은 항생제 무첨가 대조구에 비하여 마늘분말 3% 및 5%를 첨가한 처리구에서 유의하게 증가하였으며(P<0.05), 사료섭취량은 처리구간 차이가 없었다. 육계 사료 내 5%까지의 마늘분말의 첨가급여는 증체량과 사료섭취량에 부정적인 영향을 주지 않았다. 간, 비장, 맹장 및 가슴 근육에 대한 상대적 중량은 처리가 유의한 차이가 관찰되지 않았다. 근육 내 콜레스레롤 함량은 항생제 첨가 대조구에 비해 감소하였으나 통계적인 유의차는 나타나지 않았다. IB 항체 생성량은 항생제 무첨가 대조구에 비하여 유의적으로 증가하였다(P<0.05). 간의 HMGCoA reductase mRNA의 발현은 대조구에 비해 마늘분말을 첨가한 모든 처리구에서 저하된 것으로 관찰되었다. 본 연구에서 사료 내 마늘의 첨가급여는 육계의 성장촉진 효과를 나타내었으며, 콜레스테롤 대사에 영향을 미칠 수 있음이 시사되었다.

• Applied Biological Chemistry
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• 제47권3호
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• pp.366-369
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• 2004

Myristica fragrans Houtt were extracted in 80% aq. MeOH and solvent fractionated sing $CHCl_3$, EtOAc, n-BuOH and water, successively. The n-BuOH fraction gave three phenylpropanoids through application of silica gel column chromatographies. The chemical structures of the phenylpropanoids were determined by the interpretation of several spectral data, including NMR and MS as meso-dihydroguaiaretic acid (1), nectandrin B (2) and syringin methyl ether (3). Compound 1, which was first isolated from this plant by authors, showed inhibitory activities with $60.0{\pm}2.1%\;(100\;{\mu}g/ml),\;42.6{\pm}0.9%\;(140\;{\mu}g/ml)\;and\;12.2{\pm}0.2%\;(200\;{\mu}g/ml)$ on ACAT(acyl-CoA:Cholesterol Acyltransferase), chitin synthase III and HMG-CoA reductase (3-hydroxy-3-methylglutaryl coenzyme A reductase), respectively. Compound 3 showed inhibitory activities with $27.2{\pm}0.9%\;(100\;{\mu}g/ml),\;45.5{\pm}0.8%\;(200\;{\mu}g/ml)$ on ACAT and chitin synthase III.

• 한국식품영양과학회지
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• 제42권1호
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• pp.1-7
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• 2013

본 연구에서는 3T3-L1 전지방세포를 이용하여 발효 삼정환의 지방 분화 억제 효과를 확인하고자 하였다. 삼정환을 5가지 주요 유산균으로 각각 발효시킨 후, Oil Red O 염색법으로 지방세포 분화 억제 여부를 알아보고, 이의 기전을 알기 위해서 지방생성에 핵심적인 역할을 하는 transcription factor 및 지질 조절 효소의 유전자 발현량을 비교하여 보았다. Oil Red O 염색 분석에서는 Lactobacillus plantarum, Enterococcus faecium으로 발효한 삼정환에서 지방구 수의 감소를 확인할 수 있었다. 또한 transcription factor로 $C/EPB{\alpha}$, $PPAR{\gamma}$, UCP-2 및 콜레스테롤 조절과 관련된 효소인 HMG-CoA reductase의 4가지 유전자 발현 정도를 분석하였는데, 발효시키지 않은 삼정환의 경우 농도가 $100{\mu}L/mL$ 이상일 때 네 가지 항목에서 억제 효과를 나타냈으며, 발효시켰을 때는 유산균의 종류에 따라 효과 억제효과가 있었는데, Lactobacillus plantarum으로 발효한 삼정환이 효과가 가장 좋은 것으로 나타났다. Lactobacillus plantarum으로 발효한 삼정환은 동일 농도의 발효하지 않은 삼정환과 비교했을 때, Oil Red O 실험에서 염색된 지방구 수가 더욱 감소하였으며, $PPAR{\gamma}$, UCP-2, HMG-CoA reductase의 경우 농도가 $200{\mu}L/mL$일 때 각각 35%, 57%, 54%로 5가지 발효 삼정환 중 가장 높은 억제율을 나타내었다. 이에 지방분화 억제 효과를 가진 삼정환을 발효시키면 그 효과가 더욱 증가하는 것으로 나타났는데, 특히 Lactobacillus plantarum으로 발효한 삼정환은 $PPAR{\gamma}$, UCP-2, HMG-CoA reductase의 유전자 발현조절을 통해 지방 분화를 억제시키는 것으로 밝혀져 발효 삼정환은 항비만 혹은 항고지혈증 약물로 개발 가능성이 있는 것으로 사료된다.

• Journal of Applied Biological Chemistry
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• 제42권2호
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• pp.92-96
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• 1999

To study the regulatory mechanism of isoprenoid (carotenoid) biosynthesis, we have compared the expression patterns of nine isoprenoid biosynthetic genes in Korean red pepper (Capsicum. annuum cv. NocKaung). The expression of geranylgeranyl pyrophosphate synthase gene was initially induced at early ripening stage (I1) and was rather slightly decreased during pepper fruit ripening. The ex-pression of phytoene synthase gene was strongly induced at semi-ripening stage (I2) and the phytoene desaturase transcript was maximally induced at the fully ripened stage (R). Our results suggest that genes encoding two 3-hydroxy-3-methylglutaryl-CoA reductase isozymes (HMGR1 and HMGR2) and farnesyl pyrophosphate synthase might be not so critical in pepper carotenoid biosynthesis but three genes encoding geranylgeranyl pyrophosphate synthase, phytoene synthase and phytoene desaturase were induced in a sequential manner and coordinately regulated during the ripening of pepper fruit.

• 한국식품영양과학회지
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• 제26권2호
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• pp.236-241
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• 1997

일부 식용식물 추출물의 HMG-CoA reductase 저해 활성을 탐색한 결과 파, 마늘, 호박의 물 추출물에서 $10{\sim}14%$의 저해활성이 관찰되었고 그외 부추, 생강 등의 물 추출물도 약간의 저해활성을 보였다. Methanol 추출물의 경우는 참취, 마늘, 생강, 미나리, 신선초 등에서 $51{\sim}29%$의 강한 저해활성이 관찰되었고, 그 외 느타리, 호박, 양송이, 고추, 토란줄기, 부추, 당근 등에서도 $12{\sim}3%$의 저해활성이 나타났다. 저해활성이 비교적 높은 신선초의 methanol 추출물을 극성의 차이에 따라 chloroform, ethyl acetate, n-butanol, 물층의 순서로 분획하여 각 분획별로 HMG-CoA reductase 저해활성을 측정한 결과 ethyl acetate 분획에서 가장 높은 저해 활성이 관찰되었으며 n-butanol, chloroform, 물층에서도 비교적 높은 저해 활성이 보였다. 신선초의 methanol 추출물 분획 중 HMG-CoA reductase 저해 활성이 가장 높게 나타난 ethyl acetate 분획을 silica gel column chromatography를 이용하여 hyperoside와 luteolin $7-O-{\beta}-D-glucoside$를 순수 분리하여 HMG-CoA reductase 저해활성을 측정한 결과 luteolin-7-O-glucoside는 $30{\mu}M$ 농도에서 65.5%의 강한 저해활성을 보였고 hyperoside는 14.8%의 비교적 약한 저해활성을 나타내었다.

• 생약학회지
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• 제30권4호
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• pp.368-376
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• 1999

Twenty-four Oriental herbal medicines including Platycodi Radix and Scutellariae Radix, etc., which have been used for the cure of hyperlipidemia, coronary heart, disease were evaluated for the 3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase inhibition and antioxidant effect on a free radical, 1,1-diphenyl-2-picrylhydrazyl(DPPH) in vitro, and antihyperlipidemic effect on hyperlipidemic rats induced by Triton WR-1339 in vivo. 80% MeOH extract of eight herbs including Scutellariae Radix, Coptidis Rhizoma, Paeoniae Radix Rubra, Moutan Cortex Radicis, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam, Cinnamomi Ramulus and Crataegi Fructus inhibited the HMG-CoA reductase activities and exhibited a radical-trapping action on a stable free radical, DPPH. On Triton WR-1339-induced hyperlipidemic rats, four herbs including Scutellariae Radix, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam and Cinnamomi Ramulus showed respectively the significant suppression of serum total cholesterol, triglyceride, phospholipid and LDL-cholesterol levels and serum transaminase(ALT and AST) activities. From these results, it is suggested that each 80% MeOH extract of Scutellariae Radix, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam and Cinnamomi Ramulus have effective antihyperlipidemic action against hyperlipidemia.

• 한국축산식품학회지
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• 제38권2호
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• pp.350-361
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• 2018

Hypercholesterolemia is one of the primary risk factors for cardiovascular diseases. The use of lactobacilli probiotics to reduce blood cholesterol levels have been extensively reported. However, more information is needed to evaluate the possible mechanisms involved and to identify possible targets for further therapeutic development. In this study, strains of lactobacilli were screened based on the ability to assimilate cholesterol, and prevention of cholesterol accumulation in hepatic (HepG2) and intestinal (HT-29) cells. Cell free supernatant (CFS) from Lactobacillus plantarum DR7 showed a higher ability to assimilate cholesterol, reduction in cholesterol accumulation in both HepG2 and HT-29 cells, accompanied by reduced mRNA expression of HMG-CoA reductase (HMGCR) in HepG2 (p<0.05), compared to other lactobacilli. The reduction of HMGCR expression was also diminished in the presence of an AMPK inhibitor (Compound C), suggesting that L. plantarum DR7 exerted its effect via the AMPK pathway, typically via the phosphorylation of AMPK instead of the AMPK mRNA expression in HepG2 (p<0.05). Altogether, our present study illustrated that lactobacilli could exert cholesterol lowering properties along the AMPK pathway, specifically via phosphorylation of AMPK that led to reduced expression of HMGCR.

• Preventive Nutrition and Food Science
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• 제4권3호
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• pp.188-192
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• 1999

To study effects of methanol extract of prosomillet on lopid metabolism , five groups of male Sprang-Dawley rats weighing 116$\pm$9 g were fed test diets for four weeks. The five diets consisted of one low fat(5% w/w) diet containing starch as carbohydrate source(normal) and four high fat diets(15% w/w) containing 40.5%(w/w)sucrose(control) and additional 80% nethanol extractof prosomillet at the levels of 0.3% and 1%(w/w) or prosomillet powder at the level of 20%(w/w). Serum level of total cholesterol was a little higher but that of triglyceride was 41% lower in 20% (w/w) prosomillet powder group than in the control group. The cholesterol levels of two Liver cholesterol levels were lower and phospolipid levels higher in all three prosomillet powder group . Fecal excretionof bile acid was most increased in the prosomillet powder group among all five test groups. Acitivity of liver microsomal 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase was significantly lower in 0.3% methanol extract fed group than the control and also appeared to be reduced in 1% extract fed one, wherease those of 20 cholesterol 7$\alpha$-hydroxylase were not different among the five groups. Activities of liver cytosilic glucose-6-phosphate dehydrogenase(G6PDH) and malic enzyme were decreased in 0.3% prosomillet methanol extract and 20% powder groups. The results indicate that in addition to fiber, certain active components in prosomillet have potential to exert hypolipidemic effects via regulating hepatic cholesterogenesis and lipogenesis.

• 한국식품영양학회지
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• 제26권3호
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• pp.526-534
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• 2013

This study was conducted to examine the effects of Opuntia ficus-indica complex (OF) on the lipid metabolism, bile acid in feces, alanine aminotransferase (ALT) activity, aspatate aminotransferase (AST) activity, composition of urine and expression of cholesterol related mRNA in streptozotocin (STZ)-induced diabetic rats. Thirty two male Sprague-Dawley rats were randomly divided into non-diabetic control (NC), diabetic control (DC), diabetic OF of 2% (OF-2) and diabetic OF of 5% (OF-5), then each group was fed for 3 weeks. Plasma total cholesterol, non-esterified fatty acids (NEFA), total cholesterol, low density lipoprotein (LDL), very low density lipoprotein (VLDL) were decreased significantly (p<0.05) in OF-5 group compared to DC, but high density lipoprotein (HDL) was not changed. AST and ALT were also reduced and bile acid excretion was improved. Composition of urine in OF-5 was almost same in NC. The expression of cholesterol $7{\alpha}$-hydroxylase (CYP7A1), 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA-R), Low density lipoprotein receptor (LDL-R) mRNA indicated that feeding OF have the effects of cholesterol decreation in plasma by synthesis of bile acid from cholesterol. These results provide experimental evidence about improved lipid metabolism of the OF feeding in the STZ-induced diabetic rats.