• Title/Summary/Keyword: Co-inhibition

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Study on the Antioxidative Activities and Anti-Inflammatory Effect of Kaempferol and Kaempferol Rhamnosides (Kaempferol 및 Kaempferol Rhamnosides의 항산화 활성 및 항염 효과에 관한 연구)

  • Lee, Keun-Ha;Cho, Young-Long;Joo, Chul-Gue;Joo, Yeon-Jeong;Kwon, Sun-Sang;Ahn, Soo-Mi;Oh, Su-Jin;Rho, Ho-Sik;Park, Chung
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.3
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    • pp.257-264
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    • 2011
  • In this study, to evaluate the antioxidative activities and anti-inflammatory effects of kaempferol and its rhamnosides, we performed the free radical scavenging assay, ROS inhibition assay and TARC (thymus and activation-regulated chemokine) assay. Also, we studied physiological activity of kaempferol and its rhamnosides (${\alpha}$-rhamnoisorobin, afzelin, kaempferitn) by structure-activity relations. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities were determined with kaempferol (62.5 ${\mu}M$) and ${\alpha}$-rhamnoisorobin (50.0 ${\mu}M$) but afzelin and kaempferitrin did not show free radical scavenging activities. Kaempferol showed a 97.5, 57.8, 47.8 % inhibition of ROS (reactive oxygen species) generated at concentrations of 10, 50 and 100 ${\mu}M$, compared to control (100 %). ${\alpha}$-rhamnoisorobin showed a 93.1, 59.1 and 41.4 % inhibition of ROS at the same concentration. We investigated the inhibitory effects of kaempferol and its rhamnosides on TARC expression. Kaempferol showed a 48.8, 5.5 and 4.4 % inhibition of TARC generated at 10, 50 and 100 ${\mu}M$, compared to control. ${\alpha}$-Rhamnoisorobin showed a 88.1, 19.0 and 1.0 % inhibition of TARC generated at the same concentration. In conclusion, these results indicate that kaempferol and ${\alpha}$-rhamnoisorobin have good antioxidative activities and anti-inflammatory effects that could be applicable to new functional cosmetics for anti-aging and anti-inflammation.

Screening of 3-Hydroxy-3-Methylglutaryl-Coenzyme A Reductase Inhibitors In Vitro and Its Application to Pullets (HMG-CoA Reductase의 저해제 탐색과 가금의 콜레스테를 저하 효과)

  • Moon, Young-Ja;Yeom, Keum-Hee;Sung, Chang-Keun
    • The Korean Journal of Food And Nutrition
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    • v.15 no.4
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    • pp.307-313
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    • 2002
  • The primary objective of these studies was to screen the materials showing inhibitions of HMG-CoA reductase in vitro. The secondary objective was to determine the effect of garlic, lovastatin and copper on cholesterol concentrations in plasma, liver and breast tissues in pullets. The degree of inhibition of the selective samples on HMG-CoA reductase activity was determined in vitro. The inhibition ratios of water soluble garlic extracts, lovastatin (methanol extracts) and copper to HMG-CoA reductase activity were 51.3%, 87.5%, and 82.0%, respectively. Control diet (basal diet) and experimental diets, garlic powder (3% in diet), lovastatin (300mg/Kg of diet) and copper (200mg/Kg of diet) were fed to pullets in order to investigate the changes of cholesterol concentration in plasma and tissues. Total cholesterol, HDL- and LDL-cholesterol in blood plasma were significantly reduced in pullets fed diet containing 3% garlic powder. However, copper significantly increased total cholesterol compared to control and lovastatin did not affect plasma cholesterol concentration. Total cholesterol and triglyceride of liver and breast tissues in pullets were not affected by adding the cholesterol-lowering materials to diets. The data suggests that it is not easy for HMG-CoA reductase inhibitors to reduce cholesterol levels in body due to complication of cholesterol metabolism. However, garlic administration can lower the levels of plasma cholesterol in pullets.

Long-Term Effects of ACE Inhibitors in Post-Tuberculosis Emphysema

  • Kim, Myung-A;Lee, Chang-Hoon;Kim, Deog-Kyeom;Chung, Hee-Soon
    • Tuberculosis and Respiratory Diseases
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    • v.69 no.6
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    • pp.418-425
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    • 2010
  • Background: Little is known about the long-term effects of angiotensin-converting enzyme (ACE) treatment on post-tuberculosis emphysema. This study evaluated the effects of ACE inhibition on cardiac function and gas exchange in patients with post-tuberculosis emphysema. Methods: At baseline and at 6 months after initiation of ACE inhibition therapy, patients underwent pulmonary function testing, arterial blood gas analysis, and echocardiography, both at rest and post exercise. Cardiac output (CO) and right ventricular ejection fraction (RVEF) were measured at those time points as well. Results: After ACE inhibition; resting and post-exercise RVEF ($Mean{\pm}SEM,\;61.5{\pm}1.0,\;67.6{\pm}1.2%$, respectively) were higher than at baseline ($56.9{\pm}1.2,\;53.5{\pm}1.7%$). Resting and post-exercise CO ($6.37{\pm}0.24,\;8.27{\pm}0.34L/min$) were higher than at baseline ($5.42{\pm}0.22,\;6.72{\pm}0.24L/min$). Resting and post-exercise $PaO_2$ ($83.8{\pm}1.6,\;74.0{\pm}1.2mmHg$, respectively) were also higher than at baseline ($74.2{\pm}1.9,\;66.6{\pm}1.6mmHg$). Post-exercise $PaCO_2$($46.3{\pm}1.1mmHg$) was higher than at baseline ($44.9{\pm}1.1;\; Resting\;42.8{\pm}0.8\;vs.\;42.4{\pm}0.9mmHg$). Resting and post-exercise A-a $O_2$ gradient ($12.4{\pm}1.4,\;17.8{\pm}1.5 mmHg$) were lower than at baseline ($22.5{\pm}1.5,\;26.9{\pm}1.6mmHg$). Conclusion: In post-tuberculosis emphysema, RVEF and CO were augmented with a resultant increase in peripheral oxygen delivery after ACE inhibition. These findings suggest that an ACE inhibitor may have the potential to alleviate co-morbid cardiac conditions and benefit the patients with post-tuberculosis emphysema.

Emerging Co-signaling Networks in T Cell Immune Regulation

  • Jung, Keunok;Choi, Inhak
    • IMMUNE NETWORK
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    • v.13 no.5
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    • pp.184-193
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    • 2013
  • Co-signaling molecules are surface glycoproteins that positively or negatively regulate the T cell response to antigen. Co-signaling ligands and receptors crosstalk between the surfaces of antigen-presenting cells (APCs) and T cells, and modulate the ultimate magnitude and quality of T cell receptor (TCR) signaling. In the past 10 years, the field of co-signaling research has been advanced by the understanding of underlying mechanisms of the immune modulation led by newly identified co-signaling molecules and the successful preclinical and clinical trials targeting co-inhibitory molecules called immune checkpoints in the treatment of autoimmune diseases and cancers. In this review, we briefly describe the characteristics of well-known B7 co-signaling family members regarding the expression, functions and therapeutic implications and to introduce newly identified B7 members such as B7-H5, B7-H6, and B7-H7.

Fatty acid uptake and oxidation in skeletal muscle

  • Yun, Hea-Yeon;Tamura, Tomohiro;Lim, Kiwon
    • Korean Journal of Exercise Nutrition
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    • v.16 no.1
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    • pp.1-9
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    • 2012
  • Long chain fatty acids (LCFAs) are transported into cells via plasma transporters, are activated to fatty acyl-CoA by fatty acyl-CoA synthase (ACS), and enter mitochondria via the carnitine system (CPT1/CACT/CPT2). The mitochondrial carnitine system plays an obligatory role in β-oxidation of LCFAs by catalyzing their transport into the mitochondrial matrix. Fatty acyl-CoAs are oxidized via the β-oxidation pathway, which results in the production of acetyl-CoA. The acetyl-CoA can be imported into the tricarboxylic acid (TCA) cycle for oxidation in the mitochondrial matrix or can be used for malonyl-CoA synthesis by acetyl-CoA carboxylase 2 (ACC2) in the cytoplasm. In skeletal muscle, ACC2 catalyzes the carboxylation of acetyl-CoA to form malonyl-CoA, which is a potent endogenous inhibitor of carnitine palmitoyltransferase 1 (CPT1). Thus, ACC2 indirectly inhibits the influx of fatty acids into the mitochondria. Fatty acid metabolism can also be regulated by malonyl-CoA-mediated inhibition of CPT1.

Effect of Paeonia lactiflora Extracts on ${\alpha}-Glucosidase$

  • Lee, Sung-Jin;Ji, Seung-Tack
    • Natural Product Sciences
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    • v.10 no.5
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    • pp.223-227
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    • 2004
  • This study was carried out to investigate inhibitory effect of extracts from the root of Paeonia lactiflora on postprandial hyperglycemia. Organic solvent (hexane, ethyl acetate, butanol, aqueous) extracts from the crude drug were fractionated by high performance liquid chromatography. These fractions were examined to evaluate ${\alpha}-glucosidase$ (EC 3. 2. 1. 20) inhibition by microplate colorimetric assay. Among the fractions examined, the ethyl acetate fraction from the roots of Paeonia lactiflora showed potent inhibitory effects on ${\alpha}-glucosidase$. Therefore, further fractionation of the fraction was carried out to isolate the active principles. Finally, we isolated and Purified 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) as a active principle by activity-guided fractionation. These results suggest that the extract from the root of Paeonia lactiflora can be used as a new nutraceutial for inhibition on postprandial hyperglycemia and PGG might be a candidate for developing an ${\alpha}-glucosidase$ inhibitor.

Anti-Diabetic Activities of Fucosterol from Pelvetia siliquosa

  • Lee, Yeon-Sil;Shin, Kuk-Hyun;Kim, Bak-Kwang;Lee, Sang-Hyun
    • Archives of Pharmacal Research
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    • v.27 no.11
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    • pp.1120-1122
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    • 2004
  • Fucosterol isolated from Pelvetia siliquosa was tested for its anti-diabetic activity in vivo. Fucosterol, when administered orally at 30 mg/kg in streptozotocin-induced diabetic rats, was caused a significant decrease in serum glucose concentrations, and exhibited an inhibition of sorbitol accumulations in the lenses. Fucosterol, when administered orally at 300 mg/kg in epinephrine-induced diabetic rats, was also caused an inhibition of blood glucose level and glycogen degradation. These results demonstrated that fucosterol is a main anti-diabetic principle from the marine algae P. siliquosa.

Evaluation of Adverse Drug Properties with Cryopreserved Human Hepatocytes and the Integrated Discrete Multiple Organ Co-culture (IdMOCTM) System

  • Li, Albert P.
    • Toxicological Research
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    • v.31 no.2
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    • pp.137-149
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    • 2015
  • Human hepatocytes, with complete hepatic metabolizing enzymes, transporters and cofactors, represent the gold standard for in vitro evaluation of drug metabolism, drug-drug interactions, and hepatotoxicity. Successful cryopreservation of human hepatocytes enables this experimental system to be used routinely. The use of human hepatocytes to evaluate two major adverse drug properties: drug-drug interactions and hepatotoxicity, are summarized in this review. The application of human hepatocytes in metabolism-based drug-drug interaction includes metabolite profiling, pathway identification, P450 inhibition, P450 induction, and uptake and efflux transporter inhibition. The application of human hepatocytes in toxicity evaluation includes in vitro hepatotoxicity and metabolism-based drug toxicity determination. A novel system, the Integrated Discrete Multiple Organ Co-culture (IdMOC) which allows the evaluation of nonhepatic toxicity in the presence of hepatic metabolism, is described.

Effects of Ginkgo biloba Extract (EGb 761) on the Enalapril-induced ACE Inhibition in SHRs (SHR에 있어 Enalapril의 ACE억제효과에 대한 Ginkgo biloba Extract(EGb 761)의 영향)

  • 이영미;염윤기;신완균;손의동;안형수
    • YAKHAK HOEJI
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    • v.45 no.1
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    • pp.93-100
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    • 2001
  • Drug inetraction between of enalapril-induced angiotensin converting enzym) inhibitory effect and Ginkgo biloba Ext.-induced antioxidant action was evaluated in spontaneously hypertensive rats. Combination treatment of enalapril (20 mg/kg/day p.o.) and Ginkgo biloba Ext. (60 mg/kg/day, p.o.) for 6 weeks in drinking water to SHRs resulted the inhibition of ACE activity in lung tissue, angiotensin I-induced pressure response and plasma angiotensin II concentration as similar to enalapril alone treatment. But these effects were sustained after 1 week withdrawal of enalapril and Ginkgo biloba Ext. co-administeration. Also, coadministered group did not increase the concentration of bradykinin in lung tissue, which were different from enalapril alone treated group. Co-administration of enalapril and Ginkgo biloba Ext. inhibited the hemolysis induced by UV B type, even Ginkgo biloba Ext. alone treated group did not. These results suggested that Ginkgo biloba Ext. sustained ACE inhibitory effect and reduced the inhibitory effect of bradykinin inactivation induced by enalapril, meanwhile, enalapril increased the antioxidant effect of Ginkgo biloba Ext.

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