• Bulletin of the Korean Chemical Society
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• v.30 no.6
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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.

• The Korean Journal of Food And Nutrition
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• v.36 no.4
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• pp.296-308
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• 2023

This study investigated the anti-obesity effects of Coriandrum sativum L. ethanol extracts in a high fat diet-induced obesity model (DIO). We confirmed the anti-obesity effects by analysing the expression of the related proteins, weight gain, dietary intake, dietary efficiency, blood biochemistry, histological analysis and western blot analysis. After oral administration of Coriandrum sativumL. ethanol extracts at concentrations of 250 and 500 mg/kg, a significant improvement in dietary efficiency, reduction in weight gain, triglycerides, total cholesterol and LDL-cholesterol in blood lipid was observed for 8 weeks. In addition, improvement in blood glucose and metabolism confirmed through glucose tolerance test was observed. Further, the concentration of alanine transaminase (ALT) in blood was significantly decreased, which improved the fatty liver caused by high-fat diet intake as confirmed by liver tissue analysis. This phenomenon was confirmed to decrease the expression of fat accumulation-related PPARγ and FAS protein in the liver tissue. Especially, it is believed that FAS, a liposynthetic enzyme, has a stronger inhibitory effect than PPARγ. Therefore, Coriandrum sativum L. ethanol extract is thought to improve obesity by reducing blood lipids levels, improving glucose metabolism and inhibiting synthesis of the fat that accumulates in the liver in high-fat diet-induced obesity animal models.

• Journal of Korean Medicine Rehabilitation
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• v.27 no.2
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• pp.1-8
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• 2017

Objectives Ethanol is a potent inhibitor of muscle protein synthesis. Muscle mass is regulated by the balance between rates of protein synthesis and protein breakdown. Both acute and chronic alcohol consumption inhibits synthesis to a greater extent than degradation. Protein synthesis is more intensely decreased in type II fibers than in type I fibers. Apoptosis has been shown to occur frequently in a variety of tissues in response to chronic alcohol feeding. Increased muscle fiber apoptosis has been shown in alcoholics with myopathy. Pueraria radix has been used for many disorders such as fevers, gastrointestinal disorders, muscle aches, allergies, respiratory problems, skin problems, high blood pressure, migraine headaches, lowering cholesterol and treating chronic alcoholism. We therefore tested the hypothesis that oral treatment with Pueraria radix could reduce the ethanol-induced muscle atrophy. Methods Young male Sprague-Dawley rats were orally given 25% ethanol (5 ml/kg, body weight) daily with Ethanol for 4 weeks. Normal group was similarly administrated with saline. The Rats of Pueraria radix treated group (EtOH+PR) were orally administrated Pueraria radix water extract, and rats of EtOH group were given with the vehicle only. After 4 week, the morphology of gastrocnemius and plantaris muscles were assessed by hematoxylin and eosin staining. The immunoreactivities of pre-apoptotic BAX and anti-apoptotic Bcl-2 proteins were also measured. Results The muscles from rats of EtOH group represented a significant reduction in average cross section area compared to Normal group. EtOH+PR group had increased fiber compared to the EtOH group. Moreover, to investigate the ethanol-induced muscular apoptosis, the immunohistochemical analysis of Bax and Bcl-2 was carried out. The treatment with Pueraria radix (EtOH+PR) significantly decreased BAX expression and increased Bcl-2 expression 4 weeks after ethanol administration when compared with Normal group. Conclusions These results suggest that Pueraria radix water extract has protective effects on chronic alcohol induced myopathy.

• Journal of Animal Science and Technology
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• v.53 no.3
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• pp.237-252
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• 2011

In this study, four different oils containing either CLA, GLA, GLA+Carnitine or corn oil (control) were supplemented to finishing pigs (average 70.8 kg initial BW) diet for 28 d of feeding period. To evaluate the values of the dietary fatty acids, especially in view of sensory and nutritional characteristics of pork; pig performances, carcass characteristics, serum cholesterol, neutrophil phagocytosis, TBARS, electronic nose flavor and fatty acids profile of pork were measured. There were no differences in daily gain and nutrients digestion among treatments, but daily feed intake of CLA enriched diet was lower (P<0.05) than that of other diets. There were no differences in backfat thickness, dressing percentage and carcass grade among pigs fed diets supplemented with different oils. Serum total cholesterol showed a tendency to be lowered in pigs fed GLA enriched diet. TBARS values during storage of pork were higher in belly from pigs fed control diet whereas the values of belly from pigs fed GLA+Carnitine diet were lower than others. However, difference in TBARS was not remarkable in adipose tissue and 4 weeks extended storage regardless of pork parts. Proportion of saturated fatty acids such as C16:0 and C18:0 were higher (P<0.05) in pork loin and thin skirt from pigs fed CLA enriched diet compared to those from other diets. There were no differences in fatty acids profiles of belly and adipose tissue. CLA accumulation in pork was increased by the dietary CLA supplementation and this could be also confirmed by a slight de novo synthesis of CLA in pork from pigs fed CLA free diets. GLA was selectively accumulated to pork adipose tissue and loin from pigs fed GLA enriched diets. There was no accumulation of GLA when GLA was not supplemented, indicating no de novo synthesis of GLA. Phagocytic activity was the highest (p<0.05) in neutrophil of pigs fed GLA+Carnitine supplemented diet, then, followed by pigs fed GLA supplemented diet. There was no difference in phagocytosis between control and CLA treatment although the phagocytosis was numerically lowest in pig fed CLA enriched diet. There were distinct differences in electronic nose flavor pattern among treatments regardless of the parts. This study showed that dietary supplementation of functional fatty acids like CLA or GLA was able to result in characteristic differences in feed intake, TBARS, fatty acids profile and flavor of pork, serum cholesterol regulation and neutrophil phagocytosis.

• Journal of Life Science
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• v.33 no.12
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• pp.967-977
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• 2023

Rubus crataegifolius (RC) is a traditional Asian medicinal plant belonging to the Rosaceae family. The fruits of RC are known to prevent adult diseases through antioxidants. In this study, the effects of RC extract (RCex) on obesity and nonalcoholic fatty liver disease (NAFLD) were evaluated in animal models. Twenty-eight male C57BL/6J mice were induced to become obese for 8 weeks and then the extract was orally administered for 8 weeks. RCex reduced body weight, adipose tissue, liver weight. RCex improved biochemical biomarkers including lipid metabolism (alanine aminotransferase (ALT), aspartate aminotransferase (AST), plasma triglyceride (TG), total cholesterol (TC), high-density lipoprotein (HDL) cholesterol and low-density lipoprotein (LDL) cholesterol). The activation of AMP-activated protein kinase (AMPK) reduced the expression of adipogenesis genes (liver × receptor (LXR), sterol regulatory element-binding protein-1c (SREBP-1c), fatty acid synthesis (FAS), acetyl-CoA carboxylase 1 (ACC1) and the effect of enhancing carnitine palmitoyltransferase (CPT) activity by RCex was verified. RCex also influence on plasma production of hormones (adiponectin & leptin) related on energy expenditure and metabolism. In addition, we confirmed that RCex improved glucose intolerance in HFD-induced obese rats. RCex was first demonstrated to have anti-obesity as well as anti-NAFLD effects by regulating fatty acid oxidation and fatty acid synthesis by phosphorylation of AMPK. This suggests that RCex could be a good supplement for the prevention of obesity and related NAFLD.

• Asian-Australasian Journal of Animal Sciences
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• v.25 no.9
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• pp.1229-1236
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• 2012

Our previous studies showed that kisspeptin-10 (Kp-10) injected in vivo can markedly increase lipid anabolism in liver of quails. In order to investigate the direct effect of Kp-10 on lipid metabolism of hepatocytes in birds, cells were separated from embryos livers and cultured in vitro with 0, 100 and 1,000 nM Kp-10, respectively. The results showed that after 24 h treatment, cells viability was not affected by 100 nM Kp-10, but showed a mild decrease with 1,000 nM Kp-10 compared to the control cells. Based on the results of the cell viability, 100 nM dosage of Kp-10 was selected for the further study and analysis. Compared with control cells, total cholesterol (Tch) contents in 100 nM treated cells were increased by 51.23%, but did not reach statistical significance, while the level of triglyceride (TG), high density of lipoprotein-cholesterol (HDL-C) and low density of lipoprotein-cholesterol (LDL-C) were significantly increased. Real-time PCR results showed that ApoVLDL-II mRNA expression had a tendency to increase, genes including sterol regulatory element-binding protein-1 (SREBP-1), acetyl coenzyme A carboxylase ${\alpha}$ ($ACC{\alpha}$), carnitine palmitoyltransferase 1 (CPT1), 3-hydroxyl-3-methylglutaryl-coenzyme A reductases (HMGCR) and stearyl coenzyme A dehydrogenase-1 (SCD1) mRNA in hepatocytes were significantly down-regulated by 100 nM Kp-10. However, contrary to its gene expression, SREBP-1 protein expression was significantly up-regulated by 100 nM Kp-10. Some of the significant correlations in mRNA expression were found between genes encoding hepatic factors or enzymes involved in lipid metabolism in liver of birds. These results indicate that Kp-10 stimulates lipid synthesis directly in primary cultured hepatocytes of chickens.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.2
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• pp.358-369
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• 1997

Hypercholesterolemia is a main risk factor to develop cardiovascular disease, a major cause of death in Korea currently. Dietary factors which shows hypocholesterolemic effect have been reported, which includes plant proteins, unsaturated fatty acids, milk, calcium, flavonoids. Numerous animal and human studies confirmed the pronounced hypocholesterolemic effects of soluble dietary fiber, such as psyllium husk, pectin, sodium alginate, guar gum. Several hypotheses have been proposed to explain the hypocholesterolemic effect of dietary fiber, including binding of bile acids by fiber, interference of lipid absorption and reduced hepatic cholesterol synthesis by propionate, a product of soluble dietary fiber fermentation. Several other hypotheses have been proposed, and these hypotheses are not mutually exclusive.

• Journal of Physiology & Pathology in Korean Medicine
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• v.31 no.6
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• pp.348-355
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• 2017

Aster yomena (AY) have been used as a traditional medicine to treat cough, bronchial asthma, and insect bites in Korea. In this study, we evaluated the inhibition of adipogenesis in 3T3-L1 cells and in high-fat diet (HFD)-induced obese mice by AY ethanol extract. Lipid accumulation measurement indicates that AY markedly inhibited adipogenesis in a dose-dependent manner. qRT-PCR results demonstrated that the mRNA expression of adipogenic transcription factors such as peroxisome proliferator-activated receptor-${\gamma}$ ($PPAR-{\gamma}$) in 3T3-L1 cells were significantly down-regulated by AY treatment. And inhibited the expression of FAS, a protein responsible for lipid synthesis, transport and storage. Oral administration of AY (100, 250, and 500 mg/kg, P.O/daily for 4 weeks) was conducted in high-fat diet induced obese mice and C57BL/6 mice. AY was orally administered for 4 weeks to extract liver and epididymal fat, and hematoxylin and eosin staining(H&E staining) was observed. Observation showed that the fat concentration of liver tissue tended to decrease dose-dependently and decreased significantly at 500 mg/kg concentration. The AY-administered group of HFD-induced mice had a lower body weight gain, along with decreased triglycerides and total cholesterol compared with the control mice, however, the HDL-cholesterol/total cholesterol ratio was increased. These results indicate that AY exhibits anti-obesity effects in obese mice by decreasing in serum lipid levels and lipogenesis related gene.

• Biomolecules & Therapeutics
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• v.25 no.2
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• pp.140-148
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• 2017

Hyperlipidemia, which is closely associated with a fatty diet and aging, is commonly observed in the western and aged society. Therefore, a novel therapeutic approach for this disease is critical, and an immunological view has been suggested as a novel strategy, because hyperlipidemia is closely associated with inflammation and immune dysfunction. In this study, the effects of an aqueous extract of Rubus occidentalis (RO) in obese mice were investigated using immunological indexes. The mice were fed a high-fat diet (HFD) to induce hyperlipidemia, which was confirmed by biochemical analysis and examination of the mouse physiology. Two different doses of RO and rosuvastatin, a cholesterol synthesis inhibitor used as a control, were orally administered. Disturbances in immune cellularity as well as lymphocyte proliferation and cytokine production were significantly normalized by oral administration of RO, which also decreased the elevated serum tumor necrosis factor $(TNF)-{\alpha}$ level and total cholesterol. The specific immune-related actions of RO comprised considerable improvement in cytotoxic T cell killing functions and regulation of antibody production to within the normal range. The immunological evidence confirms the significant cholesterol-lowering effect of RO, suggesting its potential as a novel therapeutic agent for hyperlipidemia and associated immune decline.

• YAKHAK HOEJI
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• v.44 no.5
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• pp.391-398
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• 2000

Leptin, the product of the ob gene, is a small peptide molecule synthesized by white adipocytes with an important role in the regulation of body fat and food intake. Based on the evidence that synthesis of leptin is regulated by female sex hormone, estrogen, this present study was investigated whether sex hormone precursor DHEA, can regulate obese gene expression in lean and genetically obese (ob/ob) mice. Antiobesity activity of DHEA was evaluated by determining body weight, food consumption, epididymal fat weight and serum levels of cholesterol and triglyceride in ICR, C57BL/6J, and ob/ob mice. The treatment of C57BL/6J lean and obese mice with a diet containing 0.3% and 0.6% DHEA resulted in lowered rates of weight gain in comparison to non-treated mice, although much greater response was found in the obese mice. All other concentrations of DHEA (0.015%, 0.06%, 0.15%, 0.3%) except the highest one(0.6%) showed no significant effects on weight gain in ICR mice. Food consumption was significantly decreased in all mice treated with 0.6% DHEA, whereas it was not decreased in ICR mice at lower concentrations than 0.6% DHEA. DHEA decreased significantly epididymal adipose tissue weight and serum triglyceride levels dose dependently in lean and obese mice. However serum cholesterol levels were decreased at lower concentrations than 0.15% DHEA and increased at concentrations of 0.3% and 0.6% DHEA in lean and obese mice. These increases in serum cholestrol levels at high concentrations of DHEA might result from the fact that DHEA has a cholesterol moiety thereby interfered the assay system. As an approach to elucidate the mechanism for antiobesity activity of DHEA, we examined mRNA levels of obese gene in the adipocyte and obese gene product (leptin) in the serum. The results showed that DHEA did not affect obese gene expression in ICR and C57BL/6J mice. Therefore, we concluded that antiobesity activity of DHEA was not modulated by obese gene expression.