• Title/Summary/Keyword: Lipase inhibitor

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Effect of Nordihydroguaiaretic Acid on the Secretion of Lipoprotein Lipase

  • Kim, Sun-Mee;Park, Tae-Won;Park, Jin-Woo
    • BMB Reports
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    • v.35 no.5
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    • pp.518-523
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    • 2002
  • Nordihydroguaiaretic acid (NDGA), an inhibitor of lipoxygenase, inhibits the secretion of proteins and causes the redistribution of resident Golgi proteins into the endoplasmic reticulum (ER). In this study, the effect of NDGA on lipoprotein lipase (LPL) secretion was investigated in 3T3-L1 adipocytes, and compared with those of brefeldin A (BFA), a well-known fungal metabolite that exhibits similar ER-Golgi redistribution. Both BFA and NDGA blocked secretions of LPL. In the presence of BFA, the active and dimeric LPL was accumulated in adipocytes. After endoglycosidase H (endo H) digestion, the proportion of LPL subunits with partially endo H-sensitive oligosaccharide was significantly increased with BFA. However, in the presence of NDGA, the cellular LPL became inactive, and only the endo H-sensitive fraction of the LPL subunit was observed. An increase of the aggregated forms was observed in the fractions of the sucrose-density gradient ultracentrifugation. These properties of LPL in the NDGA-treated cells were similar to those of LPL that is retained in ER, and the effects of NDGA could not be reversed by BFA. These results indicate that the inhibitory mechanism of NDGA on the LPL secretion is functionally different from the ER-Golgi redistribution that is induced by BFA.

Isolation and Characterization of Methyl Jasmonate -Inducible Genes in Chinese Cabbage

  • Park, Yong-Soon;Cho, Tae-Ju
    • Animal cells and systems
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    • v.7 no.4
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    • pp.337-343
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    • 2003
  • Methyl jasmonate (MeJA) is a signal molecule in the activation of defense responses in plants. In this study, we isolated 15 MeJA-inducible genes by subtractive hybridization. These genes encode two myrosinase-binding proteins, five lipase-like proteins, a polygalacturonase inhibitor, a putative chlorophyll-associated protein, a terpene synthase, a dehydroascorbate reductase, an ascorbate oxidase, a cysteine protease, an O-methyltransferase, and an epithiospecifier protein. Northern analysis showed that most of the Chinese cabbage genes are barely expressed in healthy leaves, but are strongly induced by MeJA treatment. We also examined whether these MeJA-inducible genes were activated by ethethon, BTH, and Pseudomonas syringae pv. tomato (Pst), a nonhost pathogen of Chinese cabbage. The results showed that none of the MeJA-inducible genes was strongly induced by ethephon or by BTH. The genes encoding lipase-like proteins and a myrosinase-binding protein were weakly induced by Pst. Other MeJA-inducible genes were not activated at all by the pathogen.

Pancreatic lipase inhibitory activity of taraxacum officinale in vitro and in vivo

  • Zhang, Jian;Kang, Min-Jung;Kim, Myung-Jin;Kim, Mi-Eun;Song, Ji-Hyun;Lee, Young-Min;Kim, Jung-In
    • Nutrition Research and Practice
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    • v.2 no.4
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    • pp.200-203
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    • 2008
  • Obesity has become a worldwide health problem. Orlistat, an inhibitor of pancreatic lipase, is currently approved as an anti-obesity drug. However, gastrointestinal side effects caused by Orlistat may limit its use. In this study the inhibitory activities of dandelion (Taraxacum officinale) against pancreatic lipase in vitro and in vivo were measured to determine its possible use as a natural anti-obesity agent. The inhibitory activities of the 95% ethanol extract of T. officinale and Orlistat were measured using 4-methylumbelliferyl oleate (4-MU oleate) as a substrate at concentrations of 250, 125, 100, 25, 12.5 and $4\;{\mu}g/ml$. To determine pancreatic lipase inhibitory activity in vivo, mice (n=16) were orally administered with com oil emulsion (5 ml/kg) alone or with the 95% ethanol extract of T. officinale (400 mg/kg) following an overnight fast. Plasma triglyceride levels were measured at 0, 90, 180, and 240 min after treatment and incremental areas under the response curves (AUC) were calculated. The 95% ethanol extract of T. officinale and Orlistat, inhibited, porcine pancreatic lipase activity by 86.3% and 95.7% at a concentration of $250\;{\mu}g/ml$, respectively. T. officinale extract showed dose-dependent inhibition with the $IC_{50}$ of $78.2\;{\mu}g/ml$. A single oral dose of the extract significantly inhibited increases in plasma triglyceride levels at 90 and 180 min and reduced AVC of plasma triglyceride response curve (p<0.05). The results indicate that T. officinale exhibits inhibitory activities against pancreatic lipase in vitro and in vivo. Further studies to elucidate anti-obesity effects of chronic consumption of T. officinale and to identify the active components responsible for inhibitory activity against pancreatic lipase are necessary.

Purification and Characterization of the Inhibitory Principle aganist Pancreatic Cholesterol Esterase from Ephedra herba (마황으로부터 췌장 Cholesterol Esterase 저해물질 분리 및 규명)

  • 김희숙;조은정;류병호;송병권;이태훈;서판길;류성호
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.28 no.4
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    • pp.816-821
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    • 1999
  • Cholesterol esterase(pCEH, pancreas cholesterol ester hydrolase, E.C.3.1.1.13) which is secreted from pancreas has been known as an important lipase for cholesterol uptake. cholesteryl acyl esters from a diet must be hydrolyzed to free cholesterol and fatty acid by cholesterol esterase before the absorption in small intestine. For the development of inhibitory substances from natural source, we screened many extracts of oriental herbs for the inhibition of cholesterol esterase in vitro. The ethanol extract of Ephedra herba showed strong inhibitory activity. Solvent fractionation and silica gel column chromatography with the extract lead to the purification of the inhibitory principle in Ephedra herba. Crystallized inhibitor was identified as ( ) ephedrine by using UV, FT IR, 1H NMR, 13C NMR and GC/Mass. These results suggest that ( ) ephedrine can be used as a potential lead compound for the development of inhibitor for cholesterol uptake by cholesterol esterase inhibition.

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Screening of Medicinal Plants for Development of Functional Food Ingredients with Anti-Obesity (항비만 기능성 식품소재 개발을 위한 생약 추출물의 탐색)

  • Kim, Yeong-Jin;Kim, Bo-Hye;Lee, Sun-Yi;Kim, Min-Soo;Park, Chan-Sun;Rhee, Moon-Soo;Lee, Kang-Hyun;Kim, Dong-Seob
    • Applied Biological Chemistry
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    • v.49 no.3
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    • pp.221-226
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    • 2006
  • In order to search anti-obesity agents, the methanol extracts of 155 herbal medicines were screened using with pancreatic lipase, which is involved in conversion of triglycerol to fatty acid. Among the tested medicinal plants, methanol extracts of Amsonia elliptica, Arecae pericarpium, Biota orientalis, Cinnamomum cassia, Curcuma aromatia, Elsholtzia ciliate, Glycyrrhiza uralensis, Mucunae Caulis, Rhus javanica, and Rubus coreanus showed potent inhibition at final concentration of $200\;{\mu}g/ml$ on pancreatic lipase activity. All of them were extracted into chloroform fraction. The relative inhibitory activities against pancreatic lipase by orlistat, the chloroform fraction of Arecae pericarpium and Cinnamomum cassia were 89, 80 and 80%, respectively. These results demonstrated that the screened medicinal plants could be develop as the effective lipase inhibitors in preventing and ameliorating obesity of human beings.

Changes of chemical composition and enzyme activity of soybean by processing method (대두의 처리방법에 따른 일반성분과 효소활성변화)

  • Kim, Nam-Dae;Choi, Soon-Gon;Joo, Hyun-Kyu
    • Applied Biological Chemistry
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    • v.35 no.4
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    • pp.232-236
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    • 1992
  • In order to manufacture of soy paste, Changes of chemical composition and enzyme activity of soybean by different processing method were investigated. The results are summarized as follows: Changes of chemical compositions were; Raw(A) and soaked(B) soybeans contain about 2% of more crude fat than roasted(C) and steamed(D) soybeans, roasted and steamed soybeans contain $1.16{\sim}1.74%$ of more protein than those of raw and soaked soybeans, and Raw and roasted soybeans contain $0.11{\sim}0.41%$ of more crude fiber than those of soaked and steamed soybeans. ${\alpha}-amylase$, ${\beta}-amylase$, protease, lipase activity of raw and soaked soybeans were $2{\sim}5$ folds higher than those of roasted and steamed soybeans. Trypsin inhibitor activity of raw, soaked, roasted and steamed soybeans was indicated 56.7%, 42.9%, 32.9% and 20.8% in the order, respectively.

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Antihyperlipidemic Effects of Red Ginseng, Crataegii Fructus and Their Main Constituents Ginsenoside Rg3 and Ursolic Acid in Mice

  • Min, Sung-Won;Jung, Sang-Hyun;Cho, Ki-Ho;Kim, Dong-Hyun
    • Biomolecules & Therapeutics
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    • v.16 no.4
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    • pp.364-369
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    • 2008
  • Anti-hyperlipidemic effect of red ginseng (RG; the steamed root of Panax ginseng C.A. Meyer) and Crataegii fructus (CF, the fruit of Crataegus pinnatifida BGE), which are used frequently in China and Korea as herbal medicines to treat arteriosclerosis, were investigated. Treatments of RG and CF significantly reduced blood triglyceride (TG) and total cholesterol (TC) levels in Triton WR-1339-induced hyperlipidemic mice and serum TG levels in corn oil-induced hypertriglyceridemic mice. Ginsenoside Rg3 and ursolic acid, the main constituents of RG and CF, respectively, also reduced TG and TC levels in hyperlipidemic mice. RG and CF significantly lowered the high blood TG and TC levels and body and epididymal mass weights induced by long-term feeding of a high-fat diet and increased the high-fat diet-induced decrease in blood HDL cholesterol levels. RG and Rg3 reduced the blood TC levels more than CF and ursolic acid. However, blood TG level were reduced by CF and ursolic acid more than RG and Rg3. RG, CF, and their constituents also inhibited pancreatic lipase and HMG-CoA reductase activities. The most potent inhibitor was Rg3. These findings suggest that RG and CF may be suitable for the therapies of hypercholesterolemia and triglyceridemia, respectively.

Triglyceride-Rich Lipoproteins and Novel Targets for Anti-atherosclerotic Therapy

  • Reiner, Zeljko
    • Korean Circulation Journal
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    • v.48 no.12
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    • pp.1097-1119
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    • 2018
  • Although elevated serum low-density lipoprotein-cholesterol (LDL-C) is without any doubts accepted as an important risk factor for cardiovascular disease (CVD), the role of elevated triglycerides (TGs)-rich lipoproteins as an independent risk factor has until recently been quite controversial. Recent data strongly suggest that elevated TG-rich lipoproteins are an independent risk factor for CVD and that therapeutic targeting of them could possibly provide further benefit in reducing CVD morbidity, events and mortality, apart from LDL-C lowering. Today elevated TGs are treated with lifestyle interventions, and with fibrates which could be combined with omega-3 fatty acids. There are also some new drugs. Volanesorsen, is an antisense oligonucleotid that inhibits the production of the Apo C-III which is crucial in regulating TGs metabolism because it inhibits lipoprotein lipase (LPL) and hepatic lipase activity but also hepatic uptake of TGs-rich particles. Evinacumab is a monoclonal antibody against angiopoietin-like protein 3 (ANGPTL3) and it seems that it can substantially lower elevated TGs levels because ANGPTL3 also regulates TGs metabolism. Pemafibrate is a selective peroxisome proliferator-activated receptor alpha modulator which also decreases TGs, and improves other lipid parameters. It seems that it also has some other possible antiatherogenic effects. Alipogene tiparvovec is a nonreplicating adeno-associated viral vector that delivers copies of the LPL gene to muscle tissue which accelerates the clearance of TG-rich lipoproteins thus decreasing extremely high TGs levels. Pradigastat is a novel diacylglycerol acyltransferase 1 inhibitor which substantially reduces extremely high TGs levels and appears to be promising in treatment of the rare familial chylomicronemia syndrome.

Effects of Heat, pH, and Gamma Irradiation Treatments on Lipase Inhibitory Activity of Sargassum thunbergii Ethanol Extract (지충이(Sargassum thunbergii) 에탄올 추출물의 Lipase 저해활성에 미치는 열, pH 및 감마선 조사의 영향)

  • Kim, Dong-Hyun;Kim, Koth-Bong-Woo-Ri;Kim, Min-Ji;SunWoo, Chan;Jung, Seul-A;Kim, Hyun-Jee;Jeong, Da-Hyun;Kim, Tae-Wan;Cho, Young-Je;Ahn, Dong-Hyun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.4
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    • pp.566-570
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    • 2012
  • Inhibitory activity of $Sargassum$ $thunbergii$ (ST) against porcine pancreatic lipase was assessed after heat treatment, pH changes, and gamma irradiation. This analysis revealed that the ST ethanol extract exhibited high lipase inhibitory activity (37.37%) at 5 mg/mL. The ST ethanol extract was treated with heat at $60^{\circ}C$ for 10, 30, and 60 min; 80 and $100^{\circ}C$ for 10 and 20 min; and $121^{\circ}C$ for 15 min, pH (2, 4, 6, 8 and 10) and ${\gamma}$-irradiation (3, 7 and 20 kGy). The lipase inhibitory activity of the ST ethanol extract increased in all heat treatments, especially at $121^{\circ}C$ for 15 min (51.55%) compared with the control. With regard to pH stability, the ST ethanol extract showed no significant changes at pH 4~8, but somewhat decreased inhibitory activity was revealed at pH 2 (26.25%) and 10 (29.93%). On the other hand, the ST ethanol extract was not affected by ${\gamma}$-irradiation treatment conditions used in this study. These results suggest that ST has a potential role as a functional food agent.

Nutritional Evaluation of Naturally Fermented Soybean and the Enzymatic Activity Changes during the Preparation (자연발효(自然醱酵) 대두식품(大豆食品)의 영양적(營養的) 가치(價値)와 그의 제조(製造) 중(中) 효소활성변화(酵素活性變化))

  • Lee, Sang-Yeol;Min, Young-Kyoo;Park, Kwan-Hwa
    • Korean Journal of Food Science and Technology
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    • v.15 no.2
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    • pp.101-107
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    • 1983
  • The four varieties of Korean soybeans were allowed to undergo natural fermentation for seven days at ambient temperature. The average pH of the product was 3.93 and titratable acidity was 1.94%. For all varieties of soybeans the content of riboflavin increased from 98 to $309.4{\mu}g/100g$ dry-matter, relative nutritive value from 78.66 to 94.59% and available lysine from 6.56 to 7.38 mg/gN, respectively. During fermentation, the activities of protease and lipase increased, while lipoxygenase and trypsin inhibitor activity decreased markedly. The capacity of water sorption of fermented soybean flour was increased with progress of proteolysis during fermentation. The cookie and noodle prepared with 20:80 mixture of fermented soybean flour and wheat flour were in the 'like' category, but it was desirable to neutralize the sour taste produced by fermentation. Among five kinds of products prepared from the fermented soybean flour pan cake was liked most by rural consumers.

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