• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.3
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• pp.371-379
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• 1994

The effect of milk in low and high cholesterol diets were investigated on serum cholesterol esterification. Weanling male Sprague-Dawley rats were divided into low(0.01% w/w) and high (1.01% w/w) cholesterol-diets groups. Bothlow and high cholesterol groups were consisted of three groups : control , LM(low heat milk), and HM (high heat milk) groups. After feeding these experimental diets for six weeks, serum cholesterol (free cholesterol and cholestryl ester) concentration and activity of lecithin.: cholesterol acyltransferase (LCAT) were measured, and serum lipoprotein profile was examined using gel column chromatography. According to the result, activity of LCAT was elevated independently by intakes of high cholesterol and milk , which resulted in the increase of daily turnover of serum cholesteryl ester. However, the turnover of HDL-cholesteryl ester increased only by milk. LCAT activity was moderately correlated with levels of total-and HDL-free choelsterol. It is concluded from the present study that milk had the cholesterol-lowering effect which partly appears to be mediated through facilitated reverse cholesterol transport.

• Journal of Nutrition and Health
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• v.26 no.7
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• pp.819-828
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• 1993

The reaction of lecithin cholesterol acyltransferase(LCAT) and cholesteryl ester transfer protein (CETP) are important in cholesterol esterification and transfer for the reverse cholesterol transport(RCT) system. The purpose of this study were to assess the effects of fatty acid unsaturation on RCT system. After 12 female human subjects consumed a prescribed high saturated fat diet prior to the period, two groups of six subjects were provided with a high PUFA(corn oil) or a high SFA(butter) as major fats in a 40 en % fat diet. Butter feeding increased plasma total-(34%), esterified-(96%), HDL_3$-(23%), LDL-(20%), and VLDL plus LDL(35%) cholesterol while corn oil feeding decreased esterified-(25%), LDL(15%) cholesterol and TG(27%). There were significant differences of fats on total-(p=0.0001), esterified-(p=0.0001), total HDL-(p=0.005), $HDL_2$-(p=0.01)and LDL-(p=0.0001) cholesterol. LCAT activity did not change during the period but highly correlated to apo A-I in HDL which was increased in the corn oil group. The 2.5 fold increased CETP activity in the butter group during the period might be related to changes in plasma VLDL plus LDL cholesterol level which were increased in the butter group.

• Proceedings of the Korean Nutrition Society Conference
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• 1995.05c
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• pp.32-32
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• 1995

• 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.

• Natural Product Sciences
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• v.15 no.2
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• pp.110-113
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• 2009

Acyl-coenzyme A: cholesterol acyltransferase (ACAT) catalyzes cholesterol esterification and plays important roles in intestinal absorption of cholesterol, hepatic production of lipoproteins and accumulation of cholesteryl ester within macrophages and smooth muscle cells. In our study, eight polyacetylenes (1 - 8), were isolated from the roots of Gymnaster koraiensis, and their chemical structures were identified on the basis of spectroscopic analysis and mass. Compound 2 with the (10S)-15,16-epoxy group in skeleton strongly inhibited ACAT enzyme with $IC_{50}$ value of 35.8 ${\mu}g$/mL, meanwhile the other compounds displayed significant inhibition of ACAT enzyme with the $IC_{50}$ values from 45.5 to 55.1 ${\mu}g$/mL.

• Applied Chemistry for Engineering
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• v.17 no.4
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• pp.375-380
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• 2006

In the paper, lipophilic derivatives of $\beta$-sitosterol, which are known to have a potential to reduce blood cholesterol level, were synthesized by the esterification of $\beta$-sitosterol and fatty acids. When the esterification reactions using stearic acid, oleic acid or linoleic acid as fatty acids were carried out in the presence of an acidic catalyst, the reaction for unsaturated fatty acids such as oleic acid and linoleic acid afforded a significant amount of side products which may be produced by oxidation of unsaturated groups. On the other hand, esterification reactions in the presence of dehydrating agents and a basic catalyst gave pure products regardless of the nature of fatty acids. The solubilities of lipophilic derivatives of $\beta$-sitostero to organic solvents and edible oil were observed to increase as the degree of unsaturation of fatty acids increases.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.3
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• pp.625-631
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• 1999

A study was carried out to investigate the effects of safflower seed powder on the improvement of lipid metabolism in high fat and high cholesterol fed rats. Male Sprague Dawley rats of 10 weeks old, weighing 325$\pm$5g, were divided into two groups; the control group(C group, high fat(10% lard) and high cholesterol(1% cholesterol)) and safflower seed group(S group, 10% safflower seed powder), they were fed experimental diets for 6 weeks. Food intake, body weight gains and organ weight had little differences between the groups. Concentration of lipoprotein in serum was remarkably lower in S group than in C group. Serum cholesterol levels were significantly lower in S group(72.94$\pm$4.08 mg/dl) than in C group(89.41$\pm$4.19mg/dl). The level of serum HDL cholesterol was higher in S group than in C group. The level of serum LDL C was significantly lower in S group than in C group. The ratio of HDL cholesterol to total cholesterol were higher in the S group than in the C group, too. The value of atherogenic index(AI) was determined to be low in S group. The content of liver triglyceride and cholesterol in the S group was lower than that of C group. ACAT activities which involves in cholesterol esterification in liver, was not significantly different between two groups.

• Nutrition Research and Practice
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• v.15 no.4
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• pp.431-443
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• 2021

BACKGROUND/OBJECTIVES: Nobiletin (NOB), a citrus flavonoid, is reported to have beneficial effects on cardiovascular and metabolic health. However, there is limited research investigating the effect of long-term supplementation with low-dose NOB on high-cholesterol diet (HCD)-induced hypercholesterolemia and non-obese nonalcoholic fatty liver disease (NAFLD). Therefore, we investigated the influence of NOB on hypercholesterolemia and NAFLD in HCD-fed mice. SUBJECTS/METHODS: C57BL/6J mice were fed a normal diet (ND) or HCD (35 kcal% fat, 1.25% cholesterol, 0.5% cholic acid) with or without NOB (0.02%) for 20 weeks. RESULTS: HCD feeding markedly reduced the final body weight compared to ND feeding, with no apparent energy intake differences. NOB supplementation suppressed HCD-induced weight loss without altering energy intake. Moreover, NOB significantly decreased the total cholesterol (TC) levels and the low-density lipoprotein (LDL)/very-LDL-cholesterol to TC ratio, and increased the high-density lipoprotein-cholesterol/TC ratio in plasma, compared to those for HCD feeding alone. The plasma levels of inflammatory and atherosclerosis markers (C-reactive protein, oxidized LDL, interleukin [IL]-1β, IL-6, and plasminogen activator inhibitor-1) were significantly lower, whereas those of anti-atherogenic adiponectin and paraoxonase were higher in the NOB-supplemented group than in the HCD control group. Furthermore, NOB significantly decreased liver weight, hepatic cholesterol and triglyceride contents, and lipid droplet accumulation by inhibiting messenger RNA expression of hepatic genes and activity levels of cholesterol synthesis-, esterification-, and fatty acid synthesis-associated enzymes, concomitantly enhancing fatty acid oxidation-related gene expression and enzyme activities. Dietary NOB supplementation may protect against hypercholesterolemia and NAFLD via regulation of hepatic lipid metabolism in HCD-fed mice; these effects are associated with the amelioration of inflammation and reductions in the levels of atherosclerosis-associated cardiovascular markers. CONCLUSIONS: The present study suggests that NOB may serve as a potential therapeutic agent for the treatment of HCD-induced hypercholesterolemia and NAFLD.

• Journal of Microbiology and Biotechnology
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• v.18 no.10
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• pp.1663-1665
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• 2008

Acyl-coenzyme A: cholesterol acyltransferase (ACAT) catalyzes cholesterol esterification and plays an important role in the intestinal absorption of cholesterol, hepatic production of lipoproteins, and accumulation of cholesteryl ester within cells. During the course of screening to find ACAT inhibitors from microbial sources, the present authors isolated pyripyropene A from Penicillium griseofulvum F1959. Pyripyropene A, an ACAT2-specific inhibitor, has already been produced from Aspergillus fumigatus. Yet, Aspergillus fumigatus is a pathogen and only produces a limited amount of pyripyropene A, making the isolation of pyripyropene A troublesome. In contrast, Penicillium griseofulvum F1959 was found to produce approximately 28 times more pyripyropene A than Aspergillus fumigatus, plus this report also describes the ideal conditions for the production of pyripyropene A by Penicillium griseofulvum F1959 and its subsequent purification.

• Archives of Pharmacal Research
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• v.6 no.2
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• pp.115-121
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• 1983

Cholesteryl p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioaccetate (2) was synthesized : an intermediate, p-[3(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid (1) is a congener of an antitumor chlorambucil which both the -CH$_{2}$CH$_{2}$-linkage and -N(CH$_{2}$CH$_{2}$Cl)$_{2}$ group of chlorambucil molecule is doubly modified into the respective -S-linkage and -NH-CO-NNO-CH$_{2}$CH$_{2}$CL group. The attackment of cholesterol moiety as a carrier group to p-[3-(2-chloroethyl-3nitrosoureido] phenylthioacetic acid was accomplished through the esterification of cholesterol with p-[3-(2-chloroethyl-3-nitrosoureido] phenylthioacetyl chloride which was obtained from the treatment of p-[3-(2-chloroethyl)-3-nitrosourei-do] phenylthioaceticacid with SOCL$_{2}$, p-[3-(2-chloroethyl)ureido]]-phenythioacetic acid was nitrosated with NaNO$_{2}$ IN 98-100% HCOOH to give exclusively p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid. Antitumor evaluation of compounds, 1 and 2 on L 1210 leukemia did show significant activity (ED$_{40}$ : 1.14.mu./ml and 8.4.mu.g/ml, repectively). Further studies were subjected..