• Korean Journal of Pharmacognosy
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• v.31 no.2
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• pp.245-248
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• 2000

As a series of the studies on cultivated Korean rhubarb rhizomes (Rheum undulatum), five stilbene derivatives were screened for inhibitory activity against $5{\alpha}-reductase$. Of these, desoxyrhapontigenin, rhapontigenin, and piceatannol exhibited inhibition, whereas, two other stilbene glycosides, rhaponticin and $piceatannol-3'-O-{\beta}-D-glucopyranoside$ did not show the inhibition.

• Archives of Pharmacal Research
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• v.28 no.12
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• pp.1392-1399
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• 2005

This study evaluated the effect of $\alpha$-tocopherol ($\alpha$-TC), ischemic preconditioning (IPC) or a combination on the extent of mitochondrial injury caused by hepatic ischemia/reperfusion (I/R). Rats were pretreated with $\alpha$-TC (20 mg/kg per day, i.p.) for 3 days before sustained ischemia. A rat liver was preconditioned with 10 min of ischemia and 10 min of reperfusion, and was then subjected to 90 min of ischemia followed by 5 h or 24 h of reperfusion. I/R increased the aminotransferase activity and mitochondrial lipid peroxidation, whereas it decreased the mitochondrial glutamate dehydrogenase activity. $\alpha$-TC and IPC individually attenuated these changes. $\alpha$-TC combined with IPC ($\alpha$-TC+IPC) did not further attenuate the changes. The mitochondrial glutathione content decreased after 5 h reperfusion. This decrease was attenuated by $\alpha$-TC, IPC, and $\alpha$-TC+IPC. The significant production of peroxides observed after 10 min reperfusion subsequent to sustained ischemia was attenuated by $\alpha$-TC, IPC, and $\alpha$-TC+IPC. The mitochondria isolated after I/R were rapidly swollen. However, this swelling rate was reduced by $\alpha$­TC, IPC, and $\alpha$-TC+IPC. These results suggest that either $\alpha$-TC or IPC reduces the level of mitochondrial damage associated with oxidative stress caused by hepatic I/R, but $\alpha$- TC combined with IPC offers no significant additional protection.

• The Korean Journal of Physiology and Pharmacology
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• v.9 no.6
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• pp.315-322
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• 2005

In this study, the authors investigated whether death of vascular smooth muscle cell (VSMC) had a pathological pertinence. Conditioned media obtained from rat aorta smooth muscle cell (SMC) that were induced death by expressing FADD in the absence of tetracycline (FADD-SMC) triggered death of normal SMC. DNA fragmentation and caspase-3 activation were observed in dying SMC by conditioned media. FADD-SMC showed transcriptional activation of tumor necrosis factor $(TNF)-{\alpha}$. Conditioned medium contained $TNF-{\alpha}$, indicating secretion of the cytokine from dying FADD-SMC. It was investigated if secreted $TNF-{\alpha}$ was functional. Conditioned medium activated ERK and p38 MAPK pathways and induced MMP-9 expression, whereas depletion of the cytokine with its soluble receptor (sTNFR) remarkably inhibited induction of MMP-9 by conditioned medium. These findings suggest that $TNF-{\alpha}$ in conditioned medium seems to be active. Then, contribution of $TNF-{\alpha}$ on death-inducing activity of conditioned medium was examined. Depletion of $TNF-{\alpha}$ with soluble $TNF-{\alpha}$ receptor decreased the death activity of conditioned medium by 35%, suggesting that $TNF-{\alpha}$ play a partial role in the death activity. Boiling of medium almost completely abolished the death-inducing activity, suggesting that other heat labile death inducing proteins existed in conditioned medium. Taken together, these results indicate that SMC undergoing death could contribute to inflammation by expressing inflammatory cytokines and pathological complications by inducing death of neighboring cells.

• The Korean Journal of Food And Nutrition
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• v.25 no.2
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• pp.246-252
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• 2012

After a mixed carbohydrate diet, inhibition of ${\alpha}$-amylase and ${\alpha}$-glucosidase involved in the digestion and absorption of carbohydrates can significantly decrease the postprandial increase of blood glucose level. In the course of screening these useful enzyme inhibitors, we selected five kinds of bean, using an in-vitro enzyme inhibition assay method. To evaluate the effect of germination process on the functionality of the bean, we investigated the inhibitory activities of the water extracts of non-germinated bean and germinated bean against ${\alpha}$-amylase and ${\alpha}$-glucosidase, relevant to postprandial hyperglycemia. We also investigated the oxygen radical absorbance capacity(ORAC), total phenolics content, and postprandial blood glucose lowering effect in rats(Sprague-Dawley rat model). Most germinated beans showed significantly higher ${\alpha}$-glucosidase inhibitory activity, compared with non-germinated beans. Among germinated beans, Glycine max had the highest ${\alpha}$-glucosidase inhibitory activity(53.3%). The water extract of germinated Phaseolus vulgaris L. had the highest ${\alpha}$-amylase inhibitory activity(95.1%), followed by Glycine max(58.7%), and Glycine max L. Merr(54.1%). Furthermore, the five germinated beans also showed high antioxidant activities in ORAC assay. Results suggested that the germination process may improve and enhance the anti-hyperglycemia potential and antioxidant activity of the bean.

• Journal of Life Science
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• v.17 no.1 s.81
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• pp.45-50
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• 2007

This study investigated biological activity of tumor necrosis factor $(TNF)-\alpha$ secreted from smooth muscle cell (SMC) destined for death by expressing Fas associated death domain containing protein (FADD) (FADD-SMC) when the cells are grown without tetracycline in culture medium. In the absence of tetracycline the FADD-SMC secreted approximately 1000 pg/ml $TNF-\alpha$, whereas hardly detectable amount of the cytokine existed in the presence of tetracycline. The culture medium collected from the FADD-SMC grown in the absence of tetracycline increased phosphorylated form of p38 MAPK and up-regulated nuclear factor kappa B (NF-kB). The medium collected without tetracycline also caused death of L929 cells. Depletion of $TNF-\alpha$ with the soluble TNF receptor (sTNFR) inhibited the phosphorylation of p38 MAPK, the up-regulation of NF-kB activity and the death activity of the medium collected from FADD-SMC in the absence of tetracycline. These results indicate that $TNF-\alpha$ secreted from SMC undergoing death is biologically active and can affect cellular function.

• Biomolecules & Therapeutics
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• v.20 no.3
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• pp.293-298
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• 2012

The purpose of this study was to investigate the modification of expression and functionality of the drug transporter P-glycoprotein (P-gp) by tumor necrosis factor-alpha (TNF-${\alpha}$) and interferon-gamma (IFN-${\gamma}$) at the blood-brain barrier (BBB). We used immortalized human brain microvessel endothelial cells (iHBMEC) and primary human brain microvessel endothelial cells (pHBMEC) as in vitro BBB model. To investigate the change of p-gp expression, we carried out real time PCR analysis and Western blotting. To test the change of p-gp activity, we performed rhodamin123 (Rh123) accumulation study in the cells. In results of real time PCR analysis, the P-gp mRNA expression was increased by TNF-${\alpha}$ or IFN-${\gamma}$ treatment for 24 hr in both cell types. However, 48 hr treatment of TNF-${\alpha}$ or IFN-${\gamma}$ did not affect P-gp mRNA expression. In addition, co-treatment of TNF-${\alpha}$ and IFN-${\gamma}$ markedly increased the P-gp mRNA expression in both cells. TNF-${\alpha}$ or IFN-${\gamma}$ did not influence P-gp protein expression whatever the concentration of cytokines or duration of treatment in both cells. However, P-gp expression was increased after treatments of both cytokines together in iHBMEC cells only compared with untreated control. Furthermore, in both cell lines, TNF-${\alpha}$ or IFN-${\gamma}$ induced significant decrease of P-gp activity for 24 hr treatment. And, both cytokines combination treatment also decreased significantly P-gp activity. These results suggest that P-gp expression and function at the BBB is modulated by TNF-${\alpha}$ or/and IFN-${\gamma}$. Therefore, the distribution of P-gp depending drugs in the central nervous system can be modulated by neurological inflammatory diseases.

• Korean Journal of Food Science and Technology
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• v.18 no.6
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• pp.450-457
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• 1986

For the removal of raffinose and stachyose related to flatulence in soybean, ${\alpha}-Galactosidase$ activity of six commercial enzyme preparations was compared and their enzymatic characteristics were investigated. Among the tested enzymes, one product from Aspergillus niger was shown to be the most potent in ${\alpha}-Galactosidase$ activity. The enzyme characteristics of the selected preparation were shown to be pH 4.0-4.5 for optimum activity, pH 4-5 for optimum stability and $45^{\circ}C$ for optimum activity. Upon reaction on a synthetic substrate, $p-nitrophenyl-{\alpha}-D-galactoside$, Michaelis constant was 2.08 mM and maximum velocity was 435 micromoles of substrate/minute/g enzyme preparation. The enzyme was proved to be essential for SH group for its activity and capable of hydrolyzing raffinose, sucrose and $p-nitrophenyl-{\alpha}-D-galactoside$ almost completely. Thin-layer chromatographic analysis exhibited that the enzyme treatments of raffinose and stachyose were resulted to produce only monosaccharides in 2 hours of hydrolysis. It was, therefore, assumed that the flatulence factor in soybean foods can be easily removed by the use of enzymes showing ${\alpha}-Galactosidase$ activity.

• Preventive Nutrition and Food Science
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• v.15 no.1
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• pp.30-35
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• 2010

The potential biological activities of methanol extract and 5 fractions (hexane, $CH_2Cl_2$, EtOAc, BuOH and water) from roots of Astragalus membranaceus were examined by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, hydroxyl radical (${\cdot}OH$) scavenging activity, reducing power assays, lipid peroxidation inhibitory activity, $\alpha$-amylase and $\alpha$-glucosidase inhibition assays. The EtOAc fraction showed high DPPH free radical scavenging activity ($EC_{50}=170.34\;{\mu}g/mL$), hydroxyl radical scavenging activity ($EC_{50}=32.14\;{\mu}g/mL$), lipid peroxidation inhibitory activity ($EC_{50}=52.46\;{\mu}g/mL$) and a concentration dependence, with OD value ranging from 0.234 to 0.345 (0.1 to 0.5 mg/mL), for reducing power. The EtOAc fraction has the highest total phenolic content ($142.13\;Gal\;{\mu}g/mg$) and the $CH_2Cl_2$ fraction has the highest flavonoid content ($71.63\;Que\;{\mu}g/mg$). Meanwhile, hexane and EtOAc showed certain $\alpha$-amylase and $\alpha$-glucosidase inhibition activities. These results suggest that the methanol extract and fractions from Astragalus membranaceus root have significant antioxidant and anti-diabetes activities, which could be used as a potential source of pharmaceutical materials.

• Korean Journal of Pharmacognosy
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• v.42 no.1
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• pp.61-67
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• 2011

In this study, we evaluated the bioactivities of methanol extract and its solvent fractions of Sonchus asper (L.) Hill. The EtOAc fraction of S. asper exhibited more strong antioxidant activity than other extracts as evidenced by the strongest 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity with a $EC_{50}$ value at $33.55\;{\mu}g/mL$ and reducing power, the total polyphenol (180.71 mg GAE/g) and flavonoid contents (145.86 mg QE/g) of S. asper extract were higher than other extracts. The EtOAc fraction of the S. asper also showed 47.38% mushroom tyrosinase inhibition activity, 56.22% ${\alpha}$-glucosidase inhibition and 46.58% ${\alpha}$-amylase inhibition ratio at 1 mg/mL. Both methylene chloride and EtOAc fractions of methanol extract of S. asper effectively reduced of the 86.34% and 62.03% angiotensin I converting enzyme (ACE) activity at 2 mg/mL, respectively. These findings suggest that the EtOAc fraction of the S. asper could be a potential antioxidant in food additive, medicinal, and industry product.

• Food Science of Animal Resources
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• v.27 no.1
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• pp.102-109
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• 2007

Lactobacillus salivarius subsp. salivarius CNU27 possessed a high level of ${\alpha}$-galactosidase activity. Purified ${\alpha}$-galactosidase was obtained after sonication of harvested cell pellet followed by DEAE-Sephadex A-50 and Mono Q anion exchange chromatography. The specific activity of the purified enzyme was 8,994 units/mg protein which is 17.09 times higher than that in crude extract. The native enzyme was a monomer with a molecular mass of 56,397.1 dalton. The optimum temperature and pH for the enzyme were $40^{\circ}C$ and 6.0, respectively. The enzyme was stable between 25 and $50^{\circ}C$. However, ${\alpha}$-galactosidase activity was lost rapidly below pH 4.5 and above pH 8.5. The enzyme activity decreased to 6.73% and 4.30% of the original activity by addition of $Cu^{2+}$ and $Hg^{2+}$, respectively. Other metal compounds did not affect the enzyme activity significantly. The enzyme liberated galactose from melibiose, raffinose, and stachyose. The rate of substrates hydrolysis was measured by HPLC. Raffinose, stachyose and melibiose were completely decomposed after 24 hr at $40^{\circ}C$.