• Title/Summary/Keyword: Lipase Inhibitor

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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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Adipocyte Differentiation Inhibitor Isolated from the Barks of Phellodendron amurense (황백(Phellodendri Cortex)으로부터 분리한 지방세포 분화 저해물질)

  • Kim, Kyung-Hee;Ahn, Soon-Cheol;Lee, Myung-Sun;Kweon, Oh-Song;Oh, Won-Keun;Kim, Min-Soo;Sohn, Cheon-Bae;Ahn, Jong-Seog
    • Korean Journal of Food Science and Technology
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    • v.35 no.3
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    • pp.503-509
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    • 2003
  • For the development of the anti-obesity natural drug, the inhibitor of adipocyte differentiation was screened from Korean traditional medicinal plants. Phellodendri Cortex was selected as a candidate of adipocyte differentiation inhibitor. An inhibitory compound PC-4 was purified from the methanol (MeOH) extract of Phellodendri Cortex using silica gel and ODS RP-18 column chromatography and HPLC. PC-4 was obtained as yellow powder; UV ${\lambda}_{max}$ (MeOH): 230, 260, 340 and 430 nm. The chemical structure of PC-4 was determined as an isoquionoline alkaloid, berberine, on the basis of various NMR experiments including $^1H-\;and\;^{13}C-NMR$. The PC-4 inhibited the differentiation of preadipocyte NIH-3T3 L1 cells at a concentration of $1\;{\mu}g/mL$.

Pharmacological Therapies of Obesity: A Review of Current Treatment Options

  • Bacher, H.Peter;Shepherd, Gillian M.;Legler, Udo F.
    • Biomolecules & Therapeutics
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    • v.17 no.4
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    • pp.348-352
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    • 2009
  • Over the last decade, the incidence of overweight and obesity has nearly doubled in many countries and is considered a pandemic. Obesity was identified as a major risk factor for cardiovascular disease as the same level as smoking and diabetes. Visceral fat is considered one of the key contributors to outcome and certain ethnic groups such as Asians seem to be more affected than others. Weight reduction through lifestyle changes was found to be impactful to improve overall health, but weight loss and maintenance thereof is limited and difficult to sustain. Surgical intervention demonstrated a greater weight loss in the severely obese and was associated with improved all-cause mortality. Despite numerous pharmacological targets and a high medical need, only few drugs have been successfully developed. Earlier studies with amphetamine-derived compounds showed significant weight loss but their critical safety profiles led to market withdrawals and disappointment. More recent compounds; orlistat - a lipase inhibitor, rimonabant - a cannaboid-1-receptor antagonist, and sibutramine - a combined serotonin/norepinephrine re-uptake inhibitor, all demonstrated similar significant efficacy; however, they carry specific safety profiles making them unsuitable for every patient. The main limitation of pharmacotherapy is the absence of clear benefit-risk assessments through outcome studies. Such a study - the SCOUT trial - was designed to compare sibutramine versus placebo and the effect on morbidity and mortality in nearly 10,000 obese patients with additional risk factors. Such studies could provide new scientific evidence for obesity treatment and may support future pharmacological approaches.

A study of the lipoprotein lipase inhibitory mechanism of Poncirus trifoliata water extracts (탱자 (Poncirus trifoliata)의 lipoprotein lipase 억제메커니즘)

  • Lee, Sung Mee;Kang, Yun Hwan;Kim, Kyoung Kon;Kim, Tae Woo;Choe, Myeon
    • Journal of Nutrition and Health
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    • v.48 no.1
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    • pp.9-18
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    • 2015
  • Purpose: Poncirus trifoliata has been reported to have anti-inflammatory, antioxidant, and immune activities. However, its anti-obesity activity and the mechanism by which the water extract of dried, immature fruit of Poncirus trifoliata (PF-W) acts are not clear. This study suggests a potential mechanism associated with the anti-obesity activity of PF-W. Methods: We measured the effect of PF-W on lipoprotein lipase (LPL) regulation using enzyme-linked immunosorbent assay (ELISA) and an activity assay. The LPL regulation mechanism was examined by reverse transcription polymerase chain reaction (RT-PCR) to measure the mRNA expression of biomarkers related to protein transport and by western blot for analysis of the protein expression of the transcription factor CCAAT-enhancer-binding protein ($C/EBP{\beta}$). Results: The total polyphenol and flavonoid content of PF-W was $52.15{\pm}4.02$ and $6.56{\pm}0.47mg/g$, respectively. PF-W treatment decreased LPL content in media to $58{\pm}5%$ of that in control adipocyte media, and increased LPL content to $117{\pm}3.5%$ of that in control adipocytes, but did not affect the mRNA expression of LPL. PF-W also increased the mRNA expression of sortilin-related receptor (SorLA), a receptor that induces endocytosis and intracellular trafficking of LPL, in a concentration- and time-dependent manner. Finally, cell fractionation revealed that PF-W treatment induced the expression of $C/EBP{\beta}$, a SorLA transcription factor, in the nuclei of 3T3-L1 adipocytes. Conclusion: The LPL secretion and activity assay showed PF-W to be an LPL secretion inhibitor, and these results suggest the potential mechanism of PF-W involving inhibition of LPL secretion through $C/EBP{\beta}$-mediated induction of SorLA expression.

Development of an anti-obesity dietary supplement inhibiting the digestion of carbohydrate and lipid (비만 개선 효과를 지닌 탄수화물 및 지방 흡수 억제 기능성 식이조성물 개발)

  • 윤유식;최선미;홍순복;홍정미;김정원;이홍석;홍성길
    • Korean journal of food and cookery science
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    • v.18 no.3
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    • pp.319-324
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    • 2002
  • In a previous study, we developed a new food additive as an egg yolk antibody (IgY) against carbohydrate digestion enzymer for the regulation of blood glucose level and weight control. The IgY delayed and decreased the increment if blood glucose level after administration of sucrose in human being by 30% in 20∼30 min. We also developed a lipase inhibitor as a water extract of two kinds of herb, Platycodon grandiflorum and Solanum Melongena, Twenty three volunteers were subjected to the intake of the egg yolk IgY Plus the herbal extracts for 50 days. In average, the treated subjects appeared to lose 1.96 kg of body weight and 3.4 kg of body fat mass during the treated period. Furthermore, Panniculus adiposus and breech size were significantly decreased during the experimental period. Above results suggested that the administration of the dietary additives composed of egg yolk IgY and natural herbal extract improve the obesity by the decrement of body weight and body fat mass.

An Efficient Synthesis of γ-Aminobutyric Acid-Derived Phospholipase A2 Inhibitors from Acyl Cyanophosphoranes and Amine Derivatives (아실 시아노포스포레인과 아민 유도체로 부터 γ-아미노부틸산에서 유도된 포스포리파제 A2 저해제의 효과적인 합성)

  • Lee, Kie-Seung;Kim, Dae-Keun
    • Journal of the Korean Chemical Society
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    • v.48 no.2
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    • pp.161-170
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    • 2004
  • A series of ${\gamma}$-aminobutyric acid-derived, potent human cytosolic phospholipase A$_2$ inhibitors have been prepared from acyl cyanophosphoranes and amine derivatives in a convergent manner. The ${\alpha}$-keto amide functionalities in the inhibitors have been introduced as electrophilic fragments via direct coupling reactions between the labile ${\alpha},{\beta}$-diketo nitriles and ${\gamma}$-aminobutyric acid t-butyl ester derivatives at -78 $^{\circ}C$ in moderate to good yields.

Pancreatico-pleural Fistula: A Rare Cause of Hemorrhagic Pleural Effusion - A case report - (췌흉강루에 의한 혈성 흉수의 치험 - 1예 보고 -)

  • Yu, Jeong-Hwan;Kang, Shin-Kwang;Kim, Yong-Ho;Yu, Jae-Hyeon;Lim, Seung-Pyung;Lee, Young;Chun, Kwang-Sik
    • Journal of Chest Surgery
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    • v.42 no.2
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    • pp.263-267
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    • 2009
  • A pancreatico-pleural fistula (PPF), caused by rupture of a pancreatic pseudocyststectomy or obstruction of the pancreatic duct, is a rare condition. A 48-year-old man with chronic alcoholism was admitted with a massive pleural effusion. Pleural fluid studies revealed elevated amylase and lipase. A PPF complicated by a ruptured pancreatic pseudocyststectomy was diagnosed by computerized tomography scan. Although the symptoms improved with conservative management, (chest tube drainage, NPO, total parenteral nutrition, and a pancreatic secretion inhibitor), a distal pancreatectomy, including a pseudocystectomy and thoracotomy, were performed for an increasing size of the hemorrhagic pancreatic pseudocyststectomy and a recurrent hemorrhagic pleural effusion. There were no post-operative complications and the patient was discharged on post-operative day 27.

$17{\beta}$-estradiol Prevents the Expression of $CEBP{\alpha}$-mediated Adipocyte Marker Genes in Female Ovariectomized C57BL/6 Mice

  • Yoon, Mi-Chung;Jeong, Sun-Hyo
    • Biomedical Science Letters
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    • v.14 no.3
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    • pp.131-137
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    • 2008
  • Adipogenesis is a complex sequence of events that culminates in the differentiation of fibroblast-like preadipocytes into specialized lipid-filled adipocytes and also involves a cascade of expression of many transcription factors such as peroxisome proliferator-activated receptor ${\gamma}(PPAR{\gamma})$ and CCAAT/enhancer-binding proteins (C/EBPs). $PPAR{\gamma}$ and C/EBPs transcriptionally transactivate adipocyte specific genes, including fatty acid transport protein (FAT/CD36) and leptin. To determine whether $17{\beta}$-estradiol modulates $C/EBP{\alpha}$ actions on adipogenesis in high fat diet-fed female ovariectomized (OVX) C57BL/6 mice, mice were treated with $17{\beta}$-estradiol for 7 days and the effects of $17{\beta}$-estradiol on adipose tissue mass and expression of adipocyte specific gene as well as $C/EBP{\alpha}$ were measured. Compared to vehicle-treated OVX control mice, OVX mice treated with $17{\beta}$-estradiol for 7 days had lower adipose tissue weights that were similar to weights in high fat diet-fed sham-operated (Sham) mice. OVX mice showed the increased expression of $C/EBP{\alpha}$ mRNA compared with Sham mice. However, $17{\beta}$-estradiol treatment in OVX mice inhibited OVX induced-$C/EBP{\alpha}$ activation, indicating that $17{\beta}$-estradiol may act as an inhibitor of $C/EBP{\alpha}$ action. Moreover, $17{\beta}$-estradiol decreased mRNA levels of adipocyte marker genes, such as lipoprotein lipase, FAT/CD36 and leptin, to levels in Sham mice. These results suggest that down-regulation of adipogenesis by $17{\beta}$-estradiol may be due to reduced adipose $C/EBP{\alpha}$ activities in female OVX C57BL/6 mice.

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Epigallocatechin Gallate Activates Phospholipase D in Glioma Cells (교세포에서 Epigallocatechin Gallate에 의한 포스포리파제 D의 활성화)

  • Kim, Shi-Yeon;Kim, Joonmo;Min, Do-Sik
    • Journal of Life Science
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    • v.13 no.6
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    • pp.924-932
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    • 2003
  • Epigallocatechin-3 Gallate (EGCG), a major constituent of green tea, has attracted increasing interest because of its many reported health benefits. Here we demonstrate for the first time that EGCG stimulates phospholipase D (PLD) activity in U87 human astroglioma cells. EGCG-induced PLD activation was abolished by the phospholipase C (PLC) inhibitor and a lipase inactive PLC-\gama1$ mutant, and was dependent on intracellular $Ca^{ 2+}$, and possibly involved $Ca^{ 2+}$ calmodulin-dependent protein kinase II (CaM kinase II). Interestingly, EGCG induced translocation of PLC-\gama1$ from the cytosol to the membrane and PLC-\gama1$interaction with PLD1. Taken together, these results demonstrate for the first time that in human astroglioma cells, EGCG regulates PLD activity via a signaling pathway involving a PLC-\gama1$ (inositol 1,4,5-trisphosphate-$Ca^{ 2+}$)-CaM kinase II-PLD pathway.

Effects of Local Pancreatic Renin-Angiotensin System on the Microcirculation of Rat with Severe Acute Pancreatitis

  • Pan, Zhijian;Feng, Ling;Long, Haocheng;Wang, Hui;Feng, Jiarui;Chen, Feixiang
    • The Korean Journal of Physiology and Pharmacology
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    • v.19 no.4
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    • pp.299-307
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    • 2015
  • Severe acute pancreatitis (SAP) is normally related to multiorgan dysfunction and local complications. Studies have found that local pancreatic renin-angiotensin system (RAS) was significantly upregulated in drug-induced SAP. The present study aimed to investigate the effects of angiotensin II receptors inhibitor valsartan on dual role of RAS in SAP in a rat model and to elucidate the underlying mechanisms. 3.8% sodium taurocholate (1 ml/kg) was injected to the pancreatic capsule in order for pancreatitis induction. Rats in the sham group were injected with normal saline in identical locations. We also investigated the regulation of experimentally induced SAP on local RAS expression in the pancreas through determination of the activities of serum amylase, lipase and myeloperoxidase, histological and biochemical analysis, radioimmunoassay, fluorescence quantitative PCR and Western blot analysis. The results indicated that valsartan could effectively suppress the local RAS to protect against experimental acute pancreatitis through inhibition of microcirculation disturbances and inflammation. The results suggest that pancreatic RAS plays a critical role in the regulation of pancreatic functions and demonstrates application potential as AT1 receptor antagonists. Moreover, other RAS inhibitors could be a new therapeutic target in acute pancreatitis.