• Title/Summary/Keyword: Lipase inhibition

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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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Medicarpin induces lipolysis via activation of Protein Kinase A in brown adipocytes

  • Imran, Khan Mohammad;Yoon, Dahyeon;Lee, Tae-Jin;Kim, Yong-Sik
    • BMB Reports
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    • v.51 no.5
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    • pp.249-254
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    • 2018
  • Natural pterocarpan Medicarpin (Med) has been shown to have various beneficial biological roles, including inhibition of osteoclastogenesis, stimulation of bone regeneration and induction of apoptosis. However, the effect of the Med on lipolysis in adipocytes has not been reported. Here, we show the effect of Med on lipolysis in different mouse adipocytes and elucidate the underlying mechanism. We observed that Med treatment promoted release of glycerol in the media. Differentiated mouse brown adipose tissue cells were treated with Med. RNA-Seq analysis was performed to elucidate the effect of med and subsequently was confirmed by qRT-PCR and western blotting analyses. Med treatment increased both protein and gene expression levels of hormone-sensitive lipase (Hsl) and adipose triglyceride lipase (Atgl), which are two critical enzymes necessary for lipolysis. Mechanistic study showed that Med activates Protein Kinase A (PKA) and phosphorylates Hsl at PKA target position at $Serine^{660}$. Silencing of PKA gene by short interfering RNA attenuated the Med-induced increase in glycerol release and Hsl phosphorylation. The results unveil that Med boosts lipolysis via a PKA-dependent pathway in adipocytes and may provide a possible avenue of further research of Med mediated reduction of body fat.

The Accelerating Action of Lipid Excretion of Immature Citrus Fruits (미숙감귤의 지질배설 촉진작용)

  • Kim, Ki Jung;Ko, Sung Kwon
    • Korean Journal of Pharmacognosy
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    • v.48 no.2
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    • pp.134-140
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    • 2017
  • In a series of investigations to develop a potential anti-obese agent, we prepared a immature Citrus fruits (IMF) and compared its lipid excretion effects to those of Citrus fruits (MF, CP, JP) in an ICR mouse model of obesity induced by a high fat diet. The body weights of IMF fed mice were found to be significantly lower from 2 weeks oral administration, despite the fact that their food intakes were similar to that of the HFD control mice. The fecal cholesterol content showed a significant increase in IMF (52.0 mg/g) at 7 weeks oral administration, and mature Citrus fruits (MF, 41.3 mg/g), immature Citrus peel (CP, 32.2 mg/g), mature Citrus peel (JP, 30.0 mg/g) respectively. And also, the triglyceride content in the feces showed a significant increase in MF (14.6 mg/g), and IMF (14.2 mg/g), CP (10.5 mg/g) and JP (10.0 mg/g), respectively. On the other hand, in the inhibition activity of pancreatic lipase, MF (0.78 nmol/min/ml) showed the greatest decrease in glycerol, CP (0.79 nmol/min/ml), JP, (0.93 nmol/min/ml) and IMF (1.42 nmol/min/ml).

Morphological and Physiological Properties of Interspecific Electrofusants, Bacteriocin Producer, from Lactobacillus sp. JC-7 and Lactobacillus acidophilus 88 (Lactobacillus sp. JC-7과 Lactobacillus acidophilus 88간의 Bacteriocin 생산 세포융합주들의 형태 및 생리학적 성질에 관한 연구)

  • 전홍기;조영배;최현정;배경미
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.26 no.6
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    • pp.1237-1245
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    • 1997
  • Interspecific fusants were made from the cells of two strains of Lactobacillus genus, a streptomycin resistant Lactobacillus sp. JC-7 and a kanamycin resistant L. acidophilus 88. The morphological and physiological properties of the fusants were examined by determining bacteriocin productivity, acid-producing activity, ability of carbohydrates utilization and three important enzyme activities. The fusants produced a bacteriocin against indicator strains and fusant No. 1, 4 exhibited a larger inhibition zone compared to that of L. acidophilus 88. $\beta$-Galactosidase, phospho-$\beta$-galactosidase, lipase activities and resistance to NaCl of Lactobacillus sp. JC-7 were better than those of L. acidophilus 88. Fusant No. 3 and 7 exhibited excellent lipase activities. Protease activity and acid productivity of L. acidophilus 88 were better than those of Lactobacillus sp. JC-7. Proteasse activities of all fusants were higher than those of parental strains, and expecially fusant No. 5 and 7 exhibited excellent proteolysis ability.

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Study of Lipoprotein Lipase Inhibitory Activity of Anti-obesity Herb Extracts (항비만소재의 lipoprotein lipase 억제 작용 연구)

  • Lee, Sung Mee;Kang, Yun Hwan;Kim, Kyoung Kon;Kim, Tae Woo;Choe, Myeon
    • Korean Journal of Food Science and Technology
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    • v.47 no.2
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    • pp.246-253
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    • 2015
  • In this study, we evaluated the lipoprotein lipase (LPL) inhibitory activity of 11 water extracts derived from Cinnamomum cassia Blume, Sarcodon aspratus, Cordyceps militaris, Crataegus pinnatifida Bunge, Corni fructus, Allium cepa, Coix lacryma-jobi, Plantago asiatica L., Lentinus edodes, Rosa rugosa, and Foeniculum fructus. The results of the LPL secretion and activity assay showed Sarcodon aspratus (NE) extract have an LPL secretion inhibitory acitivity. The cause of reduction in LPL secretion after NE treatment was investigated using molecular biology methods. NE treatment affected the LPL content in cells, but did not affect LPL mRNA expression. It also increased the mRNA expression level of sortilin-related receptor LDLR class A (SorLA), a receptor that induces endocytosis and intracellular trafficking of LPL. Finally, cell fractionation revealed that NE treatment induced the expression of CCAAT-enhancer-binding protein beta ($C/EBP{\beta}$), a SorLA transcription factor, in the nuclei of 3T3-L1 adipocytes. These results show that NE's anti-obesity effect involves inhibition of LPL secretion through $C/EBP{\beta}$-mediated induction of SorLA expression.

Comparative Evaluation of Korean Medicine Well-matched with Pork through an Inhibition of Pancreatic Lipase (저육(猪肉)과 잘 어울리는 췌장라이페이즈 억제능을 가진 한약재의 비교평가)

  • Shin, Mi-Rae;Kim, SooHyun;Lee, AhReum;Kim, KyeongJo;Kim, SuJi;Lee, Young Cheol;Roh, Seong-Soo
    • The Korea Journal of Herbology
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    • v.32 no.5
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    • pp.57-63
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    • 2017
  • Objectives : The aim of this study is to search Korean Medicine with the superior inhibitory effect of pancreatic lipase including a possibility as a well-matched sauce material with pork. Methods : We chose 5 samples which have the potent inhibitory effect of pancreatic lipase enzyme among 9 samples. 5 samples were Glycyrrhizae rhizoma, Cinnamomi cortex, Ganoderma lucidum, Syzygium aromaticum, and Schisandra chinensis. Animals were divided into eight groups (n=7). The experimental groups except for normal group were fed 60% high-fat diet. 5 samples were orally administered at a dose of 200 mg/kg body weight and orlistat were orally administrated at a dose of 60 mg/kg body weight for 7 days. Biochemical anaylses of 5 samples were executed based on lipid parameters such as triglyceride (TG) and total cholesterol (TC). Results : Korean Medicines with $IC_{50}$ of below $1mg/m{\ell}$ were Glycyrrhizae rhizoma, Cinnamomi cortex, Ganoderma lucidum, Syzygium aromaticum, and Schisandra chinensis. Body weight change of all drug-treated groups except Glycyrrhizae rhizoma reduced significantly during the experimental period. Orlistat treatment reduced significantly both TG and TC in serum. The significant emission of TG in fece showed in Cinnamomi cortex treatment, whereas Ganoderma lucidum and Syzygium aromaticum showed a tendency to increase without a significance. Besides, Ganoderma lucidum and Schisandra chinensis emitted significantly TC to fece. Conclusions : In conclusion, Cinnamomi cortex may exert anti-obesity effect by directly inhibiting pancreatic lipase, which would prevent the absorption of lipid from the small intestine. Accordingly, Cinnamomi cortex may suggest a high possibility as a well-matched sauce material with pork.

Inhibition of Adipogenesis in 3T3-L1 Adipocytes with Magnolia officinalis Extracts (후박 추출물의 지방세포 분화 억제 효능에 관한 연구)

  • Kim, Hyun-Ju;Lee, Yeo-Myeong;Kim, Yeon-Hyang;Won, Sun-Im;Choi, Sung-A;Choi, Shin-Wook
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.2
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    • pp.117-123
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    • 2009
  • Magnolia extract, prepared from the Chinese herb Magnolia officinalis, is known for its potent anti-oxidative and anti-inflammatory effects. In this report, we showed that Magnolia extract inhibits adipocyte differentiation, as evidenced by reduced triglyceride (TG) accumulation. Also, Magnolia extract increased hormone sensitive lipase (HSL) protein level, and decreased the adipogenic transcription factor peroxisome proliferator activated receptor (PPAR)-${\gamma}$ protein and their corresponding mRNA. Our results suggest a potential apllication of Magnolia extract as anti-obesity agents inhibits adipocyte differentiation through the down-regulation of adipogenic transcription factors and other adipocyte-specific genes.

Investigation of Antioxidant, Hypoglycemic and Anti-Obesity Effects of Euphorbia Resinifera L.

  • Benrahou, Kaoutar;El Guourrami, Otman;Mrabti, Hanae Naceiri;Cherrah, Yahia;My El Abbes, Faouzi
    • Journal of Pharmacopuncture
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    • v.25 no.3
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    • pp.242-249
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    • 2022
  • Objectives: The aim of this work is to evaluate the in vitro antioxidant, hypoglycemic, and antiobesity effects of Euphorbia resinifera extracts and investigate the phenolic constituents and the toxicity of these extracts. Methods: Phytochemical screening was performed to detect polyphenols and flavonoids. Antioxidant activity was evaluated by four methods (DPPH, ABTS, H2O2, and xanthine oxidase inhibition). The hypoglycemic effect was determined by the inhibition of α-amylase and α-glucosidase enzymes in vitro and via a starch tolerance study in normal rats. The antiobesity effect was estimated by in vitro inhibition of lipase. Results: Phytochemical screening revealed that the ethanolic extract was rich in polyphenols (99 ± 0.56 mg GEA/g extract) and tannins (55.22 ± 0.17 mg RE/g extract). Moreover, this extract showed higher antioxidant activity in different tests: the DPPH assay (IC50 = 53.81 ± 1.83 ㎍/mL), ABTS assay (111.4 ± 2.64 mg TE/g extract), H2O2 (IC50 = 98.15 ± 0.68 ㎍/mL), and xanthine oxidase (IC50 = 10.26 ± 0.6 ㎍/mL). With respect to hypoglycemic effect, the aqueous and ethanolic extracts showed IC50 values of 119.7 ± 2.15 ㎍/mL and 102 ± 3.63 ㎍/mL for α-amylase and 121.4 ± 1.88 and 56.6 ± 1.12 ㎍/mL for α-glucosidase, respectively, and the extracts lowered blood glucose levels in normal starch-loaded rats. Additionally, lipase inhibition was observed with aqueous (IC50 = 25.3 ± 1.53 ㎍/mL) and ethanolic (IC50 = 13.7 ± 3.03 ㎍/mL) extracts. Conclusion: These findings show the antioxidant, hypoglycemic, and hyperlipidemic effects of E. resinifera extracts, which should be investigated further to validate their medicinal uses and their pharmaceutical applications.

Antioxidative and digestion enzyme inhibitory activity of Ganoderma lucidum depends on the extraction solvent (추출용매에 따른 영지버섯(Ganoderma lucidum)의 항산화 및 소화효소 저해활성)

  • Joo, Ok Soo;Hwang, Chung Eun;Hong, Su Young;Sin, Eui Cheol;Nam, Sang Hae;Cho, Kye Man
    • Food Science and Preservation
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    • v.25 no.1
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    • pp.124-135
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    • 2018
  • This study investigated the nutritional properties and biological activities of Ganoderma lucidum (GL). The round type of GL contained higher carbohydrate content, while the Nokgak type of GL contained higher crude ash, crude fat, and crude protein content. The most abundant amino acid, fatty acid, mineral, and soluble vitamin observed were valine (round type: 11.90 mg/g and Nokgak type: 17.18 mg/g), linoleic acid (round type: 47.56% and Nokgak type: 75.68%), potassium (round type: 116.50 mg/100 g and Nokgak type: 184.36 mg/100 g), and vitamin B3 (round type: 1.78 mg/100 g and Nokgak type: 1.81 mg/100 g), respectively. In addition, the ${\beta}$-glucan content were 34.15 g/100 g (round type) and 30.07 g/100 g (Nokgak type). The GL 70% ethanol extract at $40^{\circ}C$ showed higher radical scavenging as well as carbohydrate and lipid enzyme inhibition than other conditions. At 1 mg/mL of treatment with the 70% ethanol extract at $40^{\circ}C$ of round type GL, the DPPH, ABTS, hydroxyl radical scavenging, and ${\alpha}$-glucosidase, ${\alpha}$-amylase, and pancreatic lipase inhibition activities obtained were approximately 92.85, 99.74, 58.09, 89.68, 44.68, and 67.56%, respectively.

Anti-Obese Effects of Mixture Contained Pine needle, Black Tea and Green Tea Extracts (솔잎, 홍차 및 녹차 추출물 함유 조성물의 항비만 효과)

  • Jeon, Jeong-Ryae;Kim, Jong-Yeon;Lee, Kyung-Mi;Cho, Duck-Hyung
    • Applied Biological Chemistry
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    • v.48 no.4
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    • pp.375-381
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    • 2005
  • The aims of this study were to evaluate the anti-obese effects of pine needle, black tea and green tea in rats and overweight people. Supplementation of 1, 2, 4 and 8% amount to the control diet of pine needle extract and mixture groups significantly decreased body weight gain and visceral fat mass compared with that of control diet group. Supplementation of 1, 2 and 4% amount to the control diet of black and green tea extracts groups significantly decreased body weight gain and visceral fat mass compared with that of control diet group. Anti-obese effect in body weight gain and visceral fat mass of mixture group was higher than in other groups. In human study, extracts mixture supplementation to overweight subjects significantly decreased both body weight and body fat compared with placebo control group. In vitro study, black and green tea extracts significantly inhibited both the pancreatic lipase and ${\alpha}-amylase$ activities dose dependently. In conclusion, the anti-obese effects of pine needle, black, and green teas in rats were found. In overweight human subjects, extracts mixture decreased body weight and body fat compared with placebo control group. Anti-obese effect in black and green tea groups might be from an decrease in carbohydrate and fat digestions via inhibition of pancreatic ${\alpha}-amylase$ and lipase activities in part.