• Title/Summary/Keyword: Lipase inhibition

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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.

Identification of Bacteriocin-producing Lactic Acid Bacteria from Kimchi and Partial Characterization of their Bacteriocin

  • Ha, Duk-Mo;Cha, Dong-Soo
    • Journal of Microbiology and Biotechnology
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    • v.4 no.4
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    • pp.305-315
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    • 1994
  • Nineteen strains of bacteriocin-producing lactic acid bacteria were isolated from 432 Kimchi samples, and identified by the comprehensive biochemical and morphological tests verifying their cellular fatty acid composition. Using partially purified bacteriocins from these isolates, their inhibitory activities against other lactic acid bacteria and some pathogens, and sensitivity to enzyme and heat treatments were tested. The isolates were identified as Lactobacillus plantarum (2 strains), L curvatus (2 starins), L brevis (2 strains), Enterococcus faecium (6 strains), Leuconostoc mesenteroides subsp. mesenteroides (1 strain) and Lactobacillus sp. (6 strains). The bacteriocins produced by E. faecium strains provided the broadest spectrum of inhibition, affecting against other Gram-positive bacteria including lactic acid bacteria and health-threatening bacteria such as Clostridium perfringens and Listeria monocytogenes. The bacteriocins of Lactobacillus sp., L plantarum and L brevis strains were capable of inhibiting many strains of the lactic acid bacteria, whereas those of L curvatus and L mesenteroides subsp. mesenteroides strains were only inhibitory to a few strains. Generally, the inhibitory activities of both E. faecium and Lactobacillus sp. strains were greater than those of other producer strains. The bacteriocins from the isolates were sensitive to several proteolytic enzymes, and those of L curvatus and L mesenteroides subsp. mesenteroides were also sensitive to lipase and $\alpha$-amylase as well as to proteolytic enzymes. The bacteriocins from the strains of Lactobacillus sp. and a strain of L. brevis were resistant to autoclaving.

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Properties of the Fusants of Lactobacillus acidophilus 88 and Lactobacillus casei subsp. casei KCTC 1121

  • Jo, Young-Bae;Heo, Kyeong;Kim, Sung-Koo;Baik, Hyung-Suk;Jun, Hong-Ki
    • Journal of Microbiology and Biotechnology
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    • v.7 no.1
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    • pp.25-31
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    • 1997
  • Protoplast fusion between L. casei KCTC 1121 and L. acidophilus 88 was attempted to obtain improved strains. The fusants produced a bacteriocin against indicator strains, making a smaller inhibition zone compared to that of L. acidophilus 88. After culturing for 2 months on selective medium, the selected fusants were still stable without segregation. Fusants showed higher lipase activity compared to those of the two parent strains. Fusant No.4, 11, and 15 exhibited excellent lactic acid productivity. Fusant No.4 and 15 exhibited improved proteolysis ability compared to the two parent strains. Whereas L. casei possessed both ${\beta}-galactosidase$ and $phospho-{\beta}-galactosidase$ activities, and L. acidophilus 88 had only ${\beta}-galactosidase$ activity, the fusants had both the intermediate enzyme activities. Cell size of the fusants was greater than that of the parents.

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Anti-obese effects of mulberry (Morus alba L.) root bark through the inhibition of digestive enzymes and 3T3-L1 adipocyte differentiation (소화효소 저해 및 지방세포 분화 억제활성에 의한 상백피의 항비만 효능)

  • Wu, Yong-Xiang;Kim, You-Jeong;Li, Sha;Yun, Myung-Chul;Yoon, Jin-Mi;Kim, Jin-Young;Cho, Sung-Il;Son, Kun-Ho;Kim, Taewan
    • Food Science and Preservation
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    • v.22 no.1
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    • pp.27-35
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    • 2015
  • Anti-obese effects of mulberry (Morus alba L.) root bark was investigated in vitro by measuring its inhibitory effect against 3T3-L1 preadipocyte differentiation and digestive enzymes such as ${\alpha}$-amylase, ${\alpha}$-glucosidase and pancreatic lipase. Ethanol extract of mulberry root bark (MRE) showed the potent inhibitory activities on ${\alpha}$-amylase, ${\alpha}$-glucosidase and pancreatic lipase with $IC_{50}$ values of $7.86{\pm}0.36$, $0.12{\pm}0.03$ and $7.93{\pm}0.11mg/mL$, respectively. Furthermore, MRE significantly suppressed cellular lipid accumulation in 3T3-L1 cells in a dose-dependent manner. To elucidate the mechanism of MRE, we performed qRT-PCR and Western blotting for the expression of genes related with adipogenesis and lipogenesis. Treatment of MRE markedly suppressed the protein expression of $PPAR{\gamma}$, $C/EBP{\alpha}$ and SREBP-1c, as well as FAS and ACC, which are the key transcription factors and metabolic enzymes in adipogenesis and lipogenesis. In addition, qRT-PCR analysis indicated that the anti-adipogenesis effect of MRE might be due to its inhibition at transcription levels. These results demonstrate that MRE can effectively suppress adipocyte differentiation and inhibit key enzymes related to obesity. Our findings suggest that mulberry root bark may have a potential benefit in preventing obesity.

Antioxidant and Anti-obesity Effects of Mulberry (Morus alba L) Fermented withLactobacillus plantarum JCM 1149 or Pichia kudriavzevii Atz-EN-01 (Lactobacillus plantarum JCM 1149와 Pichia kudriavzevii Atz-EN-01를 이용한 오디 발효액의 항산화 및 항비만 효과)

  • Ji-Young Lee;Su-Bin Oh;So-Yoon Joo;Sang-Kyu Noh;Dae-Ook Kang
    • Journal of Life Science
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    • v.33 no.10
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    • pp.797-807
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    • 2023
  • To improve the functionality of mulberry, samples were fermented with Lactobacillus plantarum JCM 1149 (LP) or Pichia kudriavzevii Atz-EN-01 (PK), and their antioxidant and anti-obesity activities were compared to those of unfermented mulberry. After fermenting for 60 hr, the total polyphenol and flavonoid content of the PK-fermented mulberry (PKFM) and LP-fermented mulberry (LPFM) was 1.5-fold and 2-fold higher, respectively, while the total anthocyanin content was 1.3-fold and 1.5-fold higher in the PKFM and LPFM, respectively. DPPH radical scavenging activity was found to be 16.3% higher (86% vs. 100%) after PK fermentation and 8.1% higher (86% vs. 93%) after LP fermentation. The lipase inhibitory activity of the LPFM and PKFM was 62.9% and 52.5%, respectively. 3T3-L1 preadipocytes were treated with unfermented mulberry, LPFM, or PKFM at 200, 400, or 800 ㎍/ml and stained with oil-red-O. A slight difference in the staining was observed in samples treated with 400 ㎍/ml. However, treatment with 800 ㎍/ml significantly reduced staining compared to the control, and the LPFM exhibited relatively higher adipogenesis inhibitory activity than the PKFM. Blood triglyceride content increased by 9.5% in the high-fat diet group, but decreased by 17.1% in the control group, 37.1% in the LPFM group, and 41.6% in the PKFM group. The blood triglyceride content of the LPFM group decreased by 43.1% and 21.4% compared to the high-fat diet group and the control group, respectively, and that of the PKFM group decreased by 48.6% and 28.9% compared to the same groups. In conclusion, the results indicate that fermented mulberry has increased antioxidant activity, lipase inhibitory activity, and adipogenesis inhibition activity, and decreased blood triglyceride content compared to unfermented mulberry.

Immunostimulatory and Anti-Obesity Activity of Lonicera insularis Nakai Extracts in Mouse Macrophages RAW264.7 Cells and Mouse Adipocytes 3T3-L1 Cells (섬괴불나무(Lonicera insularis Nakai) 추출물의 면역자극 및 항비만 활성)

  • Yu, Ju Hyeong;Yeo, Joo Ho;Choi, Min Yeong;Lee, Jae Won;Geum, Na Gyeong;An, Mi-Yun;Jeong, Jin Boo
    • Korean Journal of Plant Resources
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    • v.35 no.4
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    • pp.417-427
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    • 2022
  • In this study, we investigated in vitro immuno-stimulatory and anti-obesity activity of fruit (LIF), leaves (LIL) and stems (LIS) from Lonicera insularis Nakai in mouse macrophages RAW264.7 cells and mouse pre-adipocytes 3T3-L1 cells. LIF, LIL and LIS increased the production of immunostimulatory factors such as nitric oxide (NO), inducible nitric oxide synthase (iNOS), interleukin-1β (IL-1β), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α) and activated phagocytosis in RAW264.7 cells. Inhibition of toll-like receptor 2/4 (TLR2/4) partly blocked LIF, LIL and LIS mediated production of immunostimulatory factors. In addition, inhibition of mitogen-activated protein kinases (MAPK) signaling attenuated the production of immunostimulatory factors induced by LIF, LIL and LIS. Based on these results of this study, LIF, LIL and LIS is thought to activate macrophages the production of immunostimulatory factors and phagocytosis through toll-like receptor 2/4 (TLR2/4) and MAPKs signaling pathway. In anti-obesity study, LIF reduced the lipid accumulation in 3T3-L1 cells. LIF increased the protein phosphorylation expressions such as AMP-activated protein kinase (AMPK), hormone sensitive lipase (HSL), adipose triglyceride lipase (ATGL) related to the lipolysis of the adipocytes. In addition, LIF increased the expression of proteins involved in energy metabolism and brown adipose tissues differentiation such as peroxisome proliferator-activated receptor gamma coativator 1α (PGC-1α) and PR domain-containing16 (PRDM16). These results suggest that LIF is involved in lipid accumulation inhibition through expressing the proteins such as lipolysis and differentiation of white adipocytes to brown adipocytes.

Bioconversion of nutrient and phytoestrogen constituents during the solid-state fermentation of soybeans by mycelia of Tricholoma matsutake (송이버섯 균사체를 이용한 대두 고체발효 중 영양성분과 식물성 에스트로겐 성분의 생물전환)

  • Hee Yul Lee;Kye Man Cho;Ok Soo Joo
    • Food Science and Preservation
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    • v.30 no.6
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    • pp.1012-1028
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    • 2023
  • The findings of this study confirmed the alteration of β-glucosidase activity, nutritional constituents, isoflavones, antioxidant activities, and digestive enzyme inhibition activities in soybeans during solid-state fermentation times with mycelia of Tricholoma matsutake. After nine days, the highest activity level was observed for β-glucosidase (3.90 to 38.89 unit/g) and aglycones (163.03 to 1,074.28 ㎍/g). The sum of isoflavones showed a significant decrease (3,489.41 to 1,325.66 ㎍/g) along with glycosides (2,753.87 to 212.43 ㎍/g) for fermentation, while fatty acids showed a slight increase and amino acids showed a marked increase. Total phenolic and flavonoid contents showed a corresponding increase according to fermentation times (5.58 to 15.09 GAE mg/g; 0.36 to 1.58 RE mg/g). Antioxidant and enzyme inhibition activities also increased; in particular, the highest level of scavenging activities was observed for ABTS (up 60.13 to 82.08%), followed by DPPH (up 63.92% to 71.98%) and hydroxyl (up 36.01 to 52.02%) radicals. Of particular interest, α-glucosidase (6.69 to 83.49%) and pancreatic lipase inhibition (1.22 to 77.43%) showed a marked increase. These results demonstrated that fermentation of soybeans with the mycelia of T. matsutake enhanced the nutritional and functional constituents, and the biological activities of soybeans. Thus, this fermentation technology can be used to produce a novel functional materials from soybeans.

Antioxidant and Antiobesity Activities of Various Color Resources Extracted from Natural Plants (천연식물로부터 추출한 색소성분의 항산화 및 항비만 활성)

  • Hwang, Cho-Rong;Kang, Min Jung;Shim, Hye Jin;Suh, Hwa Jin;Kwon, Oh Oun;Shin, Jung-Hye
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.2
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    • pp.165-172
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    • 2015
  • The objective of this study was to investigate the antioxidant and antiobesity activities of various color resources extracted from natural plants such as, clove, persimmon, gall nut, amur cork, gardenia, safflower, and annatto. Total phenolic content was the highest in gall nut extract (2,441.45 mg/kg) followed by clove extract (1,346.48 mg/kg). DPPH, and ABTS radical scavenging activities and ferric reducing antioxidant power (FRAP) were also higher in gall nut extract. ${\alpha}$-Glucosidase inhibitory activity ($IC_{50}$) was highest in persimmon extract ($22.83{\mu}g/mL$) followed by gall nut extract. ${\alpha}$-Amylase and lipase inhibitory activities were also higher in persimmon extract (49.45% and 61.01%, respectively). Lipid accumulation in 3T3-L1 cells was lower in persimmon, clove, and annatto extracts (81.54%, 83.36%, and 85.70% at $20{\mu}g/mL$, respectively). Triglyceride content in 3T3-L1 cells was lowest in clove extract (66.11%) followed by persimmon extract (88.88%). The results of this study suggest that gall nut extract has the highest antioxidant activity, whereas persimmon and clove extract show the antiobesity activities by inhibition of digestive enzymes and fat accumulation in 3T3-L1 cells. These extracts are useful materials for the development of antioxidant and antiobesity functional foods.

Development of Anti - obesity Dietary Supplement Decreasing Nutrient Absorption by Digestive Enzyme Inhibition in Gut (장내 소화 효소 활성 저해를 통한 섭취 영양소의 흡수 억제와 이를 이용한 비만 개선용 식이조성물의 개발)

  • Yun, Yu-Sik;Park, Yun-Sin;Hong, Jeong-Mi;Choe, Seon-Mi;Lee, Hong-Seok;Hong, Seong-Gil
    • Journal of the Korean Dietetic Association
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    • v.8 no.2
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    • pp.199-205
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    • 2002
  • In this study, we found a new food additive as an natural herbal extracts against lipid digestion enzymes for the regulation of fatty acid absorption and weight control. The Water extracts of Platycodon grandiflorum and Solanum melongena. inhibited lipase activity and decresed serum total cholesterol and triglyceride concentration in mouse fed lipid emulsion. Twenty three volunteers were subjected to the intake of the herbal extracts plus the egg yolk IgY that inhibit carbohydrate digestion enzymes in gut 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 natural herbal extract and egg yolk IgY improve the obesity by the decrement of body weight and body fat mass.

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Determination and Characterization of Thermostable Esterolytic Activity from a Novel Thermophilic Bacterium Anoxybacillus gonensis A4

  • Faiz, Ozlem;Colak, Ahmet;Saglam, Nagihan;Canakci, Sabriye;Belduz, Ali Osman
    • BMB Reports
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    • v.40 no.4
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    • pp.588-594
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    • 2007
  • A novel hot spring thermophile, Anoxybacillus gonensis A4 (A. gonensis A4) was investigated in terms of capability of tributyrin degradation and characterization of its thermostable esterase activity by the hydrolysis of p-nitrophenyl butyrate (PNPB). It was observed that A. gonensis A4 has an esterase with a molecular weight of 62 kDa. The extracellular crude preparation was characterized in terms of substrate specificity, pH and temperature optima and stability, kinetic parameters and inhibition/activation behaviour towards some chemicals and metal ions. Tributyrin agar assay showed that A. gonensis A4 secreted an esterase and $V_{max}$ and $K_m$ values of its activity were found to be 800 U/L and 176.5 ${\mu}M$, respectively in the presence of PNPB substrate. The optimum temperature and pH, for A. gonensis A4 esterase was $60-80^{\circ}C$ and 5.5, respectively. Although the enzyme activity was not significantly changed by incubating crude extract solution at $30-70^{\circ}C$ for 1 h, the enzyme activity was fully lost at $80^{\circ}C$ for same incubation period. The pH-stability profile showed that original crude esterase activity increased nearly 2-fold at pH 6.0. The effect of some chemicals on crude esterase activity indicated that A. gonensis A4 produce an esterase having serine residue in active site and -SH groups were essential for its activity.