• Title/Summary/Keyword: lipase inhibition

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Biological Activities of Pharbitis nil and Partial Purification of Anticancer Agent from Its Extract (견우자의 생리활성 분석과 추출물로부터 항암 활성물질의 분리)

  • Choi, Hyeun Deok;Yu, Sun Nyoung;Park, Sul-Gi;Kim, Young Wook;Nam, Hyo Won;An, Hyun Hee;Kim, Sang Hun;Kim, Kwang-Youn;Ahn, Soon Cheol
    • Journal of Life Science
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    • v.27 no.2
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    • pp.225-232
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    • 2017
  • This study aimed to evaluate several biological activities of Pharbitis nil and to isolate an anticancer agent from its methanol extract. Pharbitis nil seeds were extracted with methanol (PNM). Then, PNM was fractionated into solvent layers such as ethyl acetate fraction (PNE), butanol fraction (PNB), and water fraction (PNW). The biological activities of the fractions were analyzed for tyrosinase inhibition, lipase inhibition, DPPH-free radical scavenging, and cell growth inhibition. PNM showed strong growth inhibition of prostate cancer PC-3 cells. PNM was subjected to Diaion HP-20 and eluted stepwise with 50%, 80%, and 100% methanol. Then, for activity-guided fraction, each fraction was analyzed for growth inhibition of prostate cancer PC-3 cells by using an MTT assay. Because the 100% fraction showed significantly strong inhibitory activity, the fraction was further separated in the reverse phase C18, which was eluted with 80% and 90% methanol. The 90% fraction was further subjected to Sephadex LH-20 using a mobile solvent of 100% methanol. Finally, the compound PN was partially purified for HPLC analysis. PN showed cell growth inhibitory activity and induced the apoptosis and cell cycle arrest of prostate cancer PC-3 cells, as measured by flow cytometry. The results together suggest that Pharbitis nil possesses various biological activities, especially the inhibitory activity for the proliferation of prostate cancer PC-3 cells, suggesting the possibility of its use as an anticancer agent.

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.

Inhibition of Pancreatic Lipase Activity and Adipocyte Differentiation in 3T3-L1 Cells Treated with Purple Corn Husk and Cob Extracts (자색옥수수 포엽과 속대 추출물의 리파아제 저해활성 및 3T3-L1 지방전구세포에서의 지방분화 억제효과)

  • Lee, Ki Yeon;Hong, Soo Young;Kim, Tae Hee;Kim, Jai Eun;Park, A-Reum;Noh, Hee Sun;Kim, Si Chang;Park, Jong Yeol;Ahn, Mun Seob;Jeong, Won Jin;Kim, Hee Yeon
    • Journal of Food Hygiene and Safety
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    • v.33 no.2
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    • pp.131-139
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    • 2018
  • Our review begins with the maize hybrid for grain, called 'Seakso 1,' which was developed in 2008 by the Gangwon Agricultural Research and Extension Services in Korea, and subsequently registered in 2011. In this study, we aimed to investigate the lipid metabolic enzyme activity and inhibitory effect on the adipocyte differentiation, in 3T3-L1 cells of the identified Seakso 1 corn husk and cob extracts (EHCS). We investigated the pancreatic lipase inhibitory effect and anti-adipogenic effect of EHCS.The lipid accumulation and adipocyte differentiation were measured by the procedure of Oil Red O staining, Real-time PCR and the Western blot analysis. The pancreatic lipase inhibitory activity of EHCS was measured at higher levels than those of the positive control (orlistat) at 100, 500, and $1,000{\mu}g/mL$. In particular, EHCS was noted as being significantly inhibited and including a measured adipocyte differentiation and lipid accumulation, when treated during the adipocyte differentiation process in 3T3-L1 cells. Based on the Oil Red O staining, EHCS inhibited lipid accumulation at 19.19%, 33.30% at $1000{\mu}g/mL$, $2000{\mu}g/mL$, respectively. The real-time PCR and Western blot analysis showed that EHCS significantly decreased in the mRNA expression and protein level of obesity-related factors, such as peroxisome-proliferatorsactivated-receptor-${\gamma}$ ($PPAR{\gamma}$) and CCAAT enhancer-binding-proteins ${\alpha}$ ($C/EBP{\alpha}$). This study potentially suggests that the Saekso 1 corn husk and cob extracts may improve lipid metabolism and reduce lipid accumulation.

호장근 부탄올 분획의 비만 예방 및 치료 효과

  • Kim, Jin-Suk
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2010.10a
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    • pp.7-7
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    • 2010
  • 전 세계적으로 폭발적으로 증가하고 있는 비만은 만병의 근원이다. 동시에 대사성질환의 발병을 증가시키는 결정적인 역할을 하고 있다. 이러한 상황을 극복할 수 있는 안전하고 효능이 우수한 약의 개발이 매우 시급하다. 시판되는 약들은 예견할 수 없는 지방변으로 실제생활을 매우 불편하게 하는 부작용과 우울증 및 자살충동 등의 심각한 부작용을 유발시키고 있다. 특히 생명을 위협하는 약은 시판이 금지되었다. 200여종의 한약재들을 In vitro screening (pancreatic lipase inhibition, PDE inhibition, c-AMP activity), ex vivo screening (lipolytic action on fat pad), short term animal screening(혈중 TG 함량 분석)을 토대로 long term animal model에서비만 예방 및 치료 효능을 검증하기 위하여 호장근 부탄올 분획을 선정하였다. 고지방 사료로 비만을 유도한 rat (Diet induced obesty (DIO) rat)에서 비만 치료 효능이, 고지방 사료로 비만을 유도한 ICR-mice에서 비만 예방 효능이 우수함을 입증하였다 (체중감소, 지방세포의 크기억제, 지방간 예방/치료(간무게, TG함량, 간 색상, 고지혈증 증상억제), 혈중 TNF-a, IL-6, leptin, adponectin 등, 간 조직에서의 pAMPK, SOCS, NF-${\kappa}B$ DNA biding activity, ACC level, FAS expression, CPT-1 activity의 정상화). 호장근 부탄올 분획의 이러한 효능은 AMPK 작용과 CPT-1 작용을 활성화하고 동시에 지방산 합성 억제와 지방산 산화를 촉진함으로 인함임을 규명하였다. 동시에 비만으로 인한 pancreatic beta cell의 파괴를 예방함으로 인슐린 내성을 예방(치료)함을 입증하였다. 이는 AMPK 활성화와 SOCS-3 단백질 억제와 NF-${\kappa}B$-DNA 결합 억제로 인함임을 증명하였다. 3T3-L1 지방 세포주에서 lipogenesis 예방(치료) 및 lipolytic effect에 관여하는 인자들의 변화를 확인하였다. 이는 Multi-compounds-multi-targets에 의한 시너지 효과임을 알 수 있었다.

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Icariin attenuates the severity of cerulein-induced acute pancreatitis by inhibiting p38 activation in mice

  • Dong-Uk Kim;Gi-Sang Bae;Myoung-Jin Kim;Ji-Won Choi;Dong-Gu Kim;Ho-Joon Song;Sung-Joo Park
    • International Journal of Molecular Medicine
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    • v.44 no.4
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    • pp.1563-1573
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    • 2019
  • Acute pancreatitis (AP) is an inflammatory disease of the pancreas. Icariin (ICA), a flavonoid glycoside, has been reported to have several pharmacological effects; however, the anti-inflammatory effects of ICA against AP require further study. Therefore, we aimed to investigate the effect of ICA on cerulein-induced AP. In the present study, AP was induced by intraperitoneally administering a supramaximal concentration of cerulein (50 ㎍/kg/h) for 6 h. ICA was also administered intraperitoneally, and mice were sacrificed 6 h after the final cerulein injection. Blood samples were collected to determine serum amylase and lipase levels. The pancreas and lung were rapidly removed for histological examination, and the analysis of myeloperoxidase activity. In addition, reverse transcription-quantitative polymerase chain reaction was conducted to analyze the expression of inflammatory cytokines in pancreatic tissues. Our results revealed that the administration of ICA prevented an increase in the pancreas weight/body weight ratio of mice and serum digestive enzyme levels. ICA treatment also inhibited cerulein-induced histological injury and neutrophil infiltration of the pancreas and lung. In addition, ICA suppressed the production of pro-inflammatory cytokines, including interleukin (IL)-1β, IL-6 and tumor necrosis factor-α in the pancreas. Furthermore, ICA administration was observed to inhibit p38 activation during cerulein-induced AP. Inhibition of p38 activation resulted in alleviated pancreatitis. Collectively, our results suggested that ICA exhibits anti-inflammatory effects in cerulein-induced AP via the inhibition of p38.

Some Physiological Activity of Phenolic Substances in Plant Foods (식물성 식품중 페놀성 물질의 몇가지 생리활성)

  • Lee, Jung-Hi;Lee, Su-Rae
    • Korean Journal of Food Science and Technology
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    • v.26 no.3
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    • pp.317-323
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    • 1994
  • Nine plant foods (persimmon leaf, perilla seed, Chinese quince, ginger root, walnut, mugwort leaf, arrowroot, buckwheat and sorghum) rich in phenolic substances were examined for their effects on the digestive enzymes, food-poisoning bacteria and mutagenicity/antimutagenicity by Ames test. Among tested samples, Chinese quince significantly inhibited the $\alpha-amylase$ activity (97%), exhibiting an uncompetitive inhibition type. Protease activity was inhibited by Chinese quince (86%), persimmon leaf (51%) and mugwort leaf (20%), in which mugwort extract exhibited a noncompetitive type. Lipase was activated >50% by all samples. The inhibition of $\alpha-amylase$ was highly correlated with the content of condensed tannin (r=0.89) and the inhibition of protease, with total phenolic content (r=0.84). Total phenolies fraction of tested samples showed the growth inhibition toward E. coli. Streptococcus faecalis and Salmonella enteritidis, in which the effect of perilla, sorghum and arrowroot was the highest for E. coli. Standard phenolics and food samples did not show any mutagenicity toward Salmonella typhimurium TA98 and TA100. Tannic acid inhibited the mutation of the two strains by benzo[a]pyrene whereas total phenolics fractions of Chinese quince and walnut exhibited antimutagenicity to a lesser extent.

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Screening of Lactobacilli Derived from Fermented Foods and Partial Characterization of Lactobacillus casei OSY-LB6A for Its Antibacterial Activity against Foodborne Pathogens

  • Chung, Hyun-Jung;Yousef, Ahmed E.
    • Preventive Nutrition and Food Science
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    • v.14 no.2
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    • pp.162-167
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    • 2009
  • Various fermented foods were screened in search of food-grade bacteria that produce bacteriocins active against Gram-negative pathogens. An isolate from a mold-ripened cheese presented antibacterial activity against Gram-positive and Gram-negative bacteria. The most active isolate was identified as Lactobacillus casei by a biochemical method, ribotyping, and membrane lipid analysis, and was designated as OSY-LB6A. The cell extracts of the isolate showed inhibition against Escherichia coli p220, E. coli O157, Salmonella enerica serovar Enteritidis, Salmonella Typhimurium, and Listeria monocytogenes. The antibacterial nature of the cell extract from the isolate was confirmed by eliminating the inhibitory effects of acid, hydrogen peroxide, and lytic bacteriophages. The culture supernatant and cell extract retained antibacterial activity after heating at $60{\sim}100^{\circ}C$ for $10{\sim}20$ min. The activity of the cell extract from Lb. casei was eliminated by pronase and lipase. Finally, the cell extract showed a bactericidal mode of action against E. coli in phosphate buffer solution, but it was bacteriostatic in broth medium and food extracts.

Dlx3 and Dlx5 Inhibit Adipogenic Differentiation of Human Dental Pulp Stem Cells

  • Lee, Hye-Lim;Nam, Hyun;Lee, Gene;Baek, Jeong-Hwa
    • International Journal of Oral Biology
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    • v.37 no.1
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    • pp.31-36
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    • 2012
  • Dlx3 and Dlx5 are homeobox domain proteins and are well-known regulators of osteoblastic differentiation. Since possible reciprocal relationships between osteogenic and adipogenic differentiation in mesenchymal stem cells exist, we examined the regulatory role of Dlx3 and Dlx5 on adipogenic differentiation using human dental pulp stem cells. Over-expression of Dlx3 and Dlx5 stimulated osteogenic differentiation but inhibited adipogenic differentiation of human dental pulp stem cells. Dlx3 and Dlx5 suppressed the expression of adipogenic marker genes such as $C/EBP{\alpha}$, $PPAR{\gamma}$, aP2 and lipoprotein lipase. Adipogenic stimuli suppressed the mRNA levels of Dlx3 and Dlx5, whereas osteogenic stimuli enhanced the expression of Dlx3 and Dlx5 in 3T3-L1 preadipocytes. These results suggest that Dlx3 and Dlx5 exert a stimulatory effect on osteogenic differentiation of stem cells through the inhibition of adipogenic differentiation as well as direct stimulation.

Characterization of degradation of fish wastes using mixed microorganisms (복합미생물을 이용한 수산폐기물의 분해특성)

  • 정해윤;정해윤;김중균
    • Journal of Life Science
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    • v.11 no.1
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    • pp.76-82
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    • 2001
  • Fifteen species of microorganisms were isolate form the intestines of fishes, fish feed, and ferment. Eleven microorganisms except HY4, HY8, HY12, and HY13 were Gram-positive, and HY1, HY2, HY3, HY5, HY6, and HY7 produced lactic acid. The species of HY1, HY2, HY3, HY4, HY5, HY6, HY13, and HY14 showed some growth in the medium containing 1% of NaCl. Except HY6, HY7, HY8, HY12 and HY5, 10 isolates had proteolytic activity, whereas only HY13 and HY14 had lipase activity. From all the results four isolates (HY3, HY4, HY13 and HY14) were chosen for the degradation of fish wastes. There was no mutual inhibition among the microorganisms, and the optimum temperature and pH for the growth of the mixed culture were found to be 3 2$\^{C}$ and 7, respectively. Under the optimum growth conditions the maximum optical density and the maximum specific growth rate were estimated to be 2.35 and {TEX}$0.46h^{-1}${/TEX}, respectively. Major microorganisms in the mixed culture at the log-phase were HY3 and HY4, which occupied 70%. The degrading efficiency of fish waste by the mixed microorganisms was 2.3 times higher, compared to control. The total amount of free amino acids in the degraded products from fish wastes was 39g/100g protein and little odor was produced by the mixed microorganisms after 48 hours.

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Lectin Activity and Chemical Characteristics of Escherichia coli, Lactobacillus spp. and Bifidobacterium spp. from Gastrointestinal Mucosa of Growing Pigs

  • Gao, W.;Meng, Q.X.
    • Asian-Australasian Journal of Animal Sciences
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    • v.17 no.6
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    • pp.863-868
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    • 2004
  • Lectin activities and chemical characteristics of Escherichia coli, Lactobacillus spp. and Bifidobacterium spp. originating from the porcine cecal mucosal layer were studied based on hemagglutination assay (HA) and hemagglutination inhibition assay (HIA). Although all the bacterial strains were able to agglutinate erythrocytes of porcine or rabbit origin, much higher HA titers were consistently observed for Lactobacillus spp. than for E. coli or for Bifidobacterium spp. A remarkable reduction in HA titers occurred by the treatment of E. coli and Lactobacillus spp. with protease or trypsin and of Bifidobacterium spp. with protease, trypsin or periodate. There were no significant effects on the HA titers of the three groups of bacteria after the treatment with lipase. Hemagglutination of E. coli was strongly inhibited by D (+)-mannose and D (+)-galactose; Lactobacillus spp. by $\alpha$-L-rhamnose and methyl-$\beta$-galactopyranoside; Bifidobacterium spp. by D (+)-alactose, $\alpha$-L-rhamnose, $\alpha$-L-fucose, L (+)-arabinose, D (+)-mannose, D (-)-fructose at a relatively low concentration (1.43 to 3.75 mg/ml). These results, combined with the enhanced HA activities of the three bacterial strains by modification of rabbit erythrocytes with neuraminidase and abolished HA activity of E. coli after treatment with $\beta$-galactosidase, indicate that it might be the glycoproteinous substances surrounding the surface of the bacterial cells that are responsible for the adhesions of these microorganisms by recognizing the specific receptors on the red blood cell.