• 한국식품영양학회지
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• 제23권4호
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• pp.562-569
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• 2010

This study was conducted to investigate the hypocholesterolemic effects of porphyran and insoluble dietary fiber isolated from laver in rats fed high fat diet containing 1% cholesterol, 0.25% sodium cholate and 12% lard. Rats were fed, ad libitum, diets containing 5% diet fiber as cellulose(normal control or high fat control), porphyran or insoluble dietary fiber for 4 weeks. Among the groups fed high fat diet, liver weight was significantly lower in high fat porphyran group than high fat control. Plasma GOT, GPT, total cholesterol, cholesteryl ester, LDL-cholesterol and liver total cholesterol concentration were significantly lower in high fat porphyran group than high fat control. The feeding of porphyran significantly increased fecal cholesterol and bile acid excretion. The feeding of insoluble dietary fiber had no significant effect on either plasma or liver cholesterol levels, although fecal cholesterol level in the insoluble dietary fiber group was significantly higher than that in the high fat control. The results indicate that porphyran isolated from the laver may exert their hypocholesterolemic effect by increasing excretion of fecal bile acid and cholesterol.

• Nutritional Sciences
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• 제4권1호
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• pp.26-33
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• 2001

Animal and clinical studies as well as epidemiological data have provided convincing evidence that n-3 polyunsaturated fatty acids can protect against atherosclerosis. However, the effects of the fatty acids on atherogenesis are contradictory. This discrepancy could derive from great susceptibility of the fatty acids to oxidation. We investigated the effect of eicosapentaenoic aced(EPA) on cellular atherogenesis via the scavenger receptor of THP-1 derived macrophages. THP-1 cells were fully differentiated into macrophages by incubating with phorbol 12-myristate 13-acetate for seven days. Atherogenic features of EPA were compared by subsitituting for linoleic acid (LA). Macrophages were also incubated without treatment of the fatty acids as controls. EPA (5-50 nmol/mL) was not cytotoxic and did not measurably induce cellular oxidation compared to bovine serum albumin (BSA) vehicle or identical doses of LA. EPA increased macrophage uptake and degradation of acetylated LDL(AcLDL) up to 14% and 88%, respectively. EPA increased markedly total cellular sterol synthesis and heparin-releasable lipoprotein lipase activity of macrophages, indicating that EPA may enhance accumulation of cellular cholesteryl ester and possibly facilitate formation of foam cells. These results demonstrate that EPA promotes the modified LDL-triggered atherosclerotic process by the modulation of the scavenger receptor and the activation of LPL in macrophages.

• 한국약용작물학회지
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• 제16권5호
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• pp.341-348
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• 2008

Cholesterol acyltransferase (ACAT) catalyzes the acylation of cholesterol to cholesteryl ester with long chain fatty acids and ACAT inhibition is a useful strategy for treating hypercholesterolemia or atherosclerosis. Inhibitory effects on ACAT of the MeOH extracts prepared from 163 edible plants were evaluated. 15 species out of 163 species exhibited higher than 50% of inhibition on the hACAT-1 and 9 species exhibited higher than 50% of inhibition on the hACAT-2 activity at their concentration of $100\;{\mu}g/mL$.

• 한국환경과학회지
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• 제20권8호
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• pp.1031-1039
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• 2011

This study was conducted to examine the influences of chitosan, sericin and collagen extract complexes (1:1:1, w/w/w, CSC-F-005) in blood glucose and lipid concentrations in the sera of streptozotocin (STZ, 55 mg/kg BW, IP injection)-induced diabetic rats (SD strain) fed on experimental diets for 5 weeks. The concentrations of blood glucose, total cholesterol, HDL-cholesterol, ratio of HDL-cholesterol concentration to total cholesterol, atherosclerotic index, LDL-cholesterol, free cholesterol, cholesteryl ester, triglyceride (TG) and phospholipid (PL) in serum were effective on the metabolic regulation in diabetic rats. The activities of alkaline phosphatase (ALP) and aminotransferase (AST, ALT) in serum were lower in the extract complexes (CSC-F-005) than in the diabetic rats. The results shown above suggested that CSC-F-005 extract complexes supplementation effectively improvement of blood glucose and lipid components in the serum of STZ-induced diabetic rats.

• 한국환경과학회지
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• 제20권8호
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• pp.1021-1030
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• 2011

The objective of this study was to assess improvements caused by chitosan, sericin and collagen peptide extract complexes (1:1:1, w/w/w, CSC-F-005) in lipid concentrations in the sera of dyslipidemic rats (SD strain) fed on experimental diets for 5 weeks. Serum concentrations of total cholesterol, HDL-cholesterol, ratio of HDL-cholesterol concentration to total cholesterol, atherosclerotic index, LDL-cholesterol, free cholesterol, cholesteryl ester, triglyceride, phospholipid and blood glucose were effective on the metabolic regulation of dyslipidemic rats. The activities of alkaline phosphatase, aspartate aminotransferase and alanine aminotransferase in serum were remarkably lower in the extract complexes (CSC-F-005) than in the dyslipidemic model. From the above results shows that CSC-F-005 extract complexes were effective on the improvement of the lipid metabolism in sera of dyslipidemic rats.

• Bulletin of the Korean Chemical Society
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• 제30권6호
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• pp.1297-1304
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• 2009

A novel series of imidazo[1,2-$\alpha$]pyridines was designed, synthesized, and tested for their ability to inhibit acyl- CoA:cholesterol acyltransferase. Preliminary lead optimization efforts resulted in the identification of ACAT inhibitors represented by analogues 5b, 5c, 6a, 6c, 7b, and 7c. The ACAT inhibitory activity of these compounds was further established by potent inhibition of cholesteryl ester formation in HepG2 cells by a representative analogue 7b.

• 동아시아식생활학회지
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• 제8권1호
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• pp.1-8
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• 1998

This study was designed to investigate the optimum recommendation level on Gatrodia rhizoma and the effects on the improvement of the lipids in the dietary hypercholesterterolemic rats. Experimental diets mixed with 5% Dioscorea batatas(Group 2), 10% Dioscorea batatas(Group 3), 15% Dioscorea batatas (Group 4) 5% Gastrodia rhizoma (Group 5), 10% Gastrodia rhizoma (Group 6), and 15% Gastrodia rhizoma (Group 7), were administered to the male rats of the Sprague Dawley for 3 weeks. Concentration of total cholesterol in serum was lower in the Gastrodia rhizoma groups than in the other groups, especially total cholesterol concentration of 10% Gastrodia rhizoma(Group 6) was the lowest in the Gastrodia rhizoma groups. Concentration of HDL-cholesterol in serum was higher in the 10% Gastrodia rhizoma and 15% Gastrodia rhizoma than in the other groups. Concentrations of cholesteryl ester, LDL, LDL-cholesterol in serum were the lowest in the 10% Gastrodia rhizoma. Concentration of glucose and activity of GPT in serum were the lowest in the 10% Gastrodia rhizoma group. The activity of GOT in serum was lower in the 10% Gastrodia rhizoma group and 15% Gastrodia rhizoma group than in the other groups. Therefore, we consider that there are effects on the improvement of the lipids in the Gastrodia rhizoma and the optimum recommendation quantity of Gastrodia rhizoma is 10% to quantity of food composition.

• 대한화장품학회지
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• 제21권1호
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• pp.38-52
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• 1995

Liposome은 의약과 화장품 분야에서 많은 발전을 하였다. 본 연구에서는 세포 간지질의 주요 성분인 cholesterol, palmitic acid, cholesterol ester와 lecithin을 사용하여 swelling반응에 의해 MLV liposome을 제조 하였다. 지질베이스와 마이크로플루다이저를 사용하여 MLV liposome 형성에 대한 특성들을 연구 하였다. MLV liposome은 multilamellar vesicle로서 형성되었다. MLV liposome의 gelation효과는 고온(90$\pm$5도씨)에서 polyol과 water phase에 지질을 혼합한 것에 스웰링 반응을 하였다. MLV liposome에 alpha hydroxy acid 성분들을 투입 제조하였다. MLV liposome의 최적 조건은 마이크로플루다이저에 3회 통과하였으며 vesicle의 입자크기는 150-350nm범위이고 이것을 freeze-fracture electron microscopy로 확인 하였다.

• Archives of Pharmacal Research
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• 제27권7호
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• pp.797-805
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• 2004

LPD vectors are non-viral vehicles for gene delivery comprised of polycation-condensed plasmid DNA and liposomes. Here, we described a novel anionic LPD formulation containing protamine-DNA complexes and pH sensitive liposomes composed of DOPE and cholesteryl hemisuccinate (Chems). Central composite design (CCD) was employed to optimize stable LPD formulation with small particle size. A three factor, five-level CCD design was used for the optimization procedure, with the weight ratio of protamine/DNA ($X_1$), the weight ratio of Chems/DNA ($X_2$) and the molar ratio of Chems/DOPE in the anionic liposomes ($X_3$) as the independent variables. LPD size ($Y_1$) and LPD protection efficiency against nuclease ($Y_2$) were response variables. Zeta potential determination was utilized to define the experimental design region. Based on experimental design, responses for the 15 formulations were obtained. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The mathematical model predicted optimized $X_1-X_3$ levels that achieve the desired particle size and the protection efficiency against nuclease. According to these levels, an optimized LPD formulation was prepared, resulting in a particle size of 185.3 nm and protection efficiency of 80.22％.

• Biomolecules & Therapeutics
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• 제29권1호
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• pp.22-30
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• 2021

Till the 21st century, fatty acids were considered as merely building blocks for triglycerides, phospholipids, or cholesteryl esters. However, the discovery of G protein-coupled receptors (GPCRs) for free fatty acids at the beginning of the 21st century challenged that idea and paved way for a new field of research, merged into the field of receptor pharmacology for intercellular lipid mediators. Among the GPCRs for free fatty acids, free fatty acid receptor 4 (FFA4, also known as GPR120) recognizes long-chain polyunsaturated fatty acids such as DHA and EPA. It is significant in drug discovery because it regulates obesity-induced metaflammation and GLP-1 secretion. Our study reviews information on newly developed FFA4 agonists and their application in pathophysiologic studies and drug discovery. It also offers a potency comparison of the FFA4 agonists in an AP-TGF-α shedding assay.