• The Korean Journal of Pharmacology
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• v.26 no.1
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• pp.35-49
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• 1990

A highly purified $(Na^+,\;K^+)-ATPase$ from the rectal gland of Squalus acanthias and from the electric organ of Electrophorus electricus has been used to raise antibodies in rabbits. The 97,000 dalton catalytic subunit and glycoprotein derived from the rectal gland of spiny shark were also used as antigens. The two $(Na^+,\;K^+)-ATPase$ holoenzymes and the two shark subunits were antigenic. In Ouchterlony double diffusion experiments, these antibodies formed precipitation bands with their antigens. Antibodies prepared against the two subunits of shark holoenzyme also formed precipitation bands with their antigens and shark holoenzyme, but not with eel holoenzyme. These observations are in good agreement with inhibitory effect of these antibodies on the catalytic activity of $(Na^+,\;K^+)-ATPase$ both from the shark and the eel, since there is very little cross-reaction between the shark anticatalytic subunit antibodies and the eel holoenzyme. The maximum antibodies titer of the anticatalytic subunit antibodies is found to be 6 weeks after the initial single exposure to this antigen. Multiple injections of the antigen increased the antibody titer. However, the time required to produce the maximum antibody titer was approximately the same. These antibodies also inhibit catalytic activity of $(Na^+,\;K^+)-ATPase$ vesicles reconstituted by a slow dialysis of cholate after solubilization of the enzyme in a presonicated mixture of cholate and phospholipid. In these reconstituted $(Na^+,\;K^+)-ATPase$ vesicles, effects of these antibodies on the fluxes of $Na^+$, $Rb^+$, and $K^+$ were investigated. Control or preimmune serum had no effect on the influx of $^{22}Na^+$ or the efflux of $^{86}Rb^+$. Immunized sera against the shark $(Na^+,\;K^+)-ATPase$ holoenzyme, its glycoprotein or catalytic subunit did inhibit the influx of $^{22}Na^+$ and the efflux of $^{86}Rb^+$. It was also demonstrated that these antibodies inhibit the coupled counter-transport of $Na^+$ and $K^+$ as studied by means of dual labeling experiments. However, this inhibitory effect of the antibodies on transport of ions in the $(Na^+,\;K^+)-ATPase$ vesicles is manifested only on the portion of energy and temperature dependent alkali metal fluxes, not on the portion of ATP and ouabain insensitive ion movement. Simultaneous determination of effects of the antibodies on ion fluxes and vesicular catalytic activity indicates that an inhibition of active ion transport in reconstituted $(Na^+,\;K^+)-ATPase$ vesicles appears to be due to the inhibitory action of the antibodies on the enzymatic activity of $(Na^+,\;K^+)-ATPase$ molecules incorporated in the vesicles. These findings that the inhibitory effects of the antibodies specific to $(Na^+,\;K^+)-ATPase$ or to its subunits on ATP and temperature sensitive monovalent cation transport in parallel with the inhibitory effect of vesicular catalytic activity by these antibodies provide direct evidence that $(Na^+,\;K^+)-ATPase$ is the molecular machinery of active cation transport in this reconstituted $(Na^+,\;K^+)-ATPase$ vesicular system.

• Biomedical Science Letters
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• v.11 no.2
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• pp.175-183
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• 2005

The two major isoflavones in soy, genistein and daidzein, are well known to prevent hormone-dependent cancers by their anti estrogenic activity. The exact molecular mechanisms for the protective action are, however, not provided yet. It has been reported that genistein and daidzein have a potential anticancer activity through their antiproliferative effect in many hormone-dependent cancer cell lines. Transforming growth $factor-\beta1(TGF-\beta1)$ has also been found to have cell growth inhibitory effect, especially in mammary epithelial cells. This knowledge led to a hypothetical mechanism that the soy isoflavones-induced growth inhibitory effect can be derived from the regulation of $TGF-\beta1$ and $TGF-\beta$ receptors. In order to test this hypothesis, the effects of the soy isoflavones at various concentrations and periods on the expression of $TGF-\beta1$and $TGF-\beta$ receptors were investigated by using Northern blot analysis in human breast carcinoma epithelial cell lines, an estrogen receptor positive cell line (MCF-7) and an estrogen receptor negative cell line (MDA-MB-231). As a result, only genistein has shown a profound dose-dependent effect on $TGF-\beta1$ expression in the $ER^+$ cell line within the range of doses tested, and the expression levels are correspondent to their inhibitory activities of cell growth. Moreover, daidzein showed down-regulated $TGF-\beta1$ expression at a low dose, the cell growth proliferation was promoted at the same condition. Therefore, antiproliferative activity of the soy isoflavones can be mediated by $TGF-\beta1$ expression, and the effects are mainly, if not all, occurred by ER dependent pathway. The expression of $TGF-\beta$ receptors was induced at a lower dose than the one for $TGF-{\beta}1$ induction regardless of the presence of ER, and the expression patterns are similar to those of the cell growth inhibition. These results indicated that the regulation of $TGF-\beta$ receptor expression as well, prior to $TGF-\beta1$ expression, may be involved in the antiproliferative activity of soy isoflavones. Little or no expression of $TGF-\beta$ receptors was found in the MCF-7 and MDA-MB-231 cells, suggesting refractory properties of the cells to growth inhibitory effect of the $TGF-\beta$. The soy isoflavones can seemingly restore the sensitivity of growth inhibitory responses to $TGF-\beta1$ by re-inducing $TGF-\beta$ receptors expression. In conclusions, our findings presented in this study show that the antitumorigenic activity of the soy isoflavones could be mediated by not only $TGF-\beta1$induction but $TGF-\beta$ receptor restoration. Thus, soy isoflavones could be good model molecules to develop new nonsteroidal antiestrogenic chemopreventive agents, associated with, regulation of $TGF-\beta$ and its receptors.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.6
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• pp.840-845
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• 2012

This research was done to verify the inhibitory activity of water extracts from Ecklonia cava (WE-EC) against trypsin and the effects on various temperature and pH conditions. The WE-EC showed high trypsin inhibitory activity of 76, 62 and 60% at concentrations of 5, 2.5 and 1 mg/mL, respectively. In all heat treatments excepted for two conditions, such as $100^{\circ}C$ for 20 min and $121^{\circ}C$ for 15 min, the inhibitory activity was stable compared with the untreated group. With regard to pH stability, the WE-EC showed no significant changes at pH 2~8, but somewhat decreased inhibitory activity was revealed at pH 10. Therefore, the WE-EC could be used in the food industry as a natural trypsin inhibitor.

• Applied Biological Chemistry
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• v.33 no.2
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• pp.109-115
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• 1990

This study was carried out to investigate the effect of L-cysteine and sodium sulfite on heat inactivation of soybean trypsin inhibitor(STI) and to determine cultivar difference in the inhibitory activity of STI. Effect of L-cysteine and sodium sulfite at different concentrations, pH's, and lengths of treatment on inactivation of STI were studied. The inactivation of STI was spectrophotometrically determined by measuring the rate of production of p-nitroaniline from synthetic substrate, N-benzoyl-DL-arginine-p-nitroanilide. Addition of L-cysteine and sodium sulfite increased magnitude of heat inactivation and greatly inhibited the re-activation of STI. There was no difference STI inactivation in among soybean cultivars employed. The trypsin inhibitory activity of STI of the soybean cultivars ranged from 64.7 to 86.4 TIU(trypsin inhibitor unit) per gram soyflour and the decreasing order of the TIU was Jangback>Hill>Jangyeab, Kwangkyo> Danyeab>Dangkyung>Paldal, Saeal, Duckyu>Hwangkeum. Inhibitory activity of STI was correlated with cysteine $content(r=0.6568^*)$ and with $digestivility(r=-0.7695^{**})$, but there was no correlation between the protein content and the inhibitory activity of STI.

• Journal of Life Science
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• v.23 no.7
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• pp.913-918
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• 2013

The applicability of the ultrasonic wave method to the extraction of useful components from seaweeds was investigated. Extracts from freeze-dried Ecklonia cava powder were prepared with hot water ($65^{\circ}C$), water ($24^{\circ}C$), 50% ethanol, and 100% ethanol, and ultrasonic extraction was also performed. The content of phenolic compounds and the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and tyrosinase inhibitory activity of the extracts were analyzed, and differences in the data obtained by the ultrasonic extraction and the traditional extraction methods were compared. The phenolic content in the E. cava extract by ultrasonic extraction (142.80 mg/g) was approximately 14 times higher than the phenolic content in the hot water extract (10.03 mg/g). The DPPH radical scavenging and the tyrosinase inhibitory activities of the ultrasonic extract were approximately 4 times and 14 times higher than the hot water extracts, respectively. The correlation between the phenolic content and the DPPH radical scavenging activity ($R^2$=99.47) and between the phenolic content and the tyrosinase inhibitory activity ($R^2$=99.99) was very high. These results indicate that ultrasonic extraction is more suitable than traditional extraction for the extraction of useful components from E. cava.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.856-859
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• 2002

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dosedependent manner, and the $IC_{50}$ values of compounds 1-3 were 74.6, 63.7 and 89.1 uM, respectively.

• 한국생물공학회:학술대회논문집
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• 2003.04a
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• pp.663-665
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• 2003

For the screening of anti-inflammation and antioxidative activities, ethanolic extract of 40 species of traditional herbal medicines were examined in vitro their hyaluronidase inhibitory effect and radical scavenging activity. Astragali Radix, Eucommia Cortex, Schizandrae Fructus, Scutellaria Radix and Moutan Radicis Coritex showed more than 50% hyaluronidase inhibitory effects. Moutan Radicis Cortex, Paeoniae Radix Alba, Plantaginis Semen and Sorbus commixta Hedl. showed more than 90% in electron donating activity. The scavenging effects of ethanolic extracts on hydroxyl radical showed significantly activity.

• KSBB Journal
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• v.27 no.4
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• pp.222-226
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• 2012

In this study, the effect of gamma irradiation on the microbial contamination and biological activities of tuna cooking juices was investigated. Tuna cooking juice was by-produced during the canning processing, and had various functional components. But, it was shown that the tuna cooking juice was seriously contaminated. Gamma irradiation effectively reduced the microbial population in tuna cooking juice. Also, 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging activity, tyrosinse inhibitory activity, and ACE inhibitory activity of tuna cooking juices were all increased as a result of gamma irradiation. These results suggest that wasted tuna cooking juices can be used as a functional component in the food and cosmetic industries if the irradiation technology were applied.

• Mycobiology
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• v.43 no.2
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• pp.150-156
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• 2015

2',4'-Dihydroxychalcone (2',4'-DHC) was identified from a heat shock protein 90 (Hsp90)-targeting library as a compound with Hsp90 inhibitory and antifungal effects. In the presence of 2',4'-DHC ($8{\mu}g/mL$), radial growth of Aspergillus fumigatus was inhibited 20% compared to the control, and green pigmentation was completely blocked. The expression of the conidiation-associated genes abaA, brlA, and wetA was significantly decreased (approximately 3- to 5-fold) by treatment with 2',4'-DHC. The expression of calcineurin signaling components, cnaA and crzA, was also significantly reduced. The inhibitory effects of 2',4'-DHC on metabolic activity and mycelial growth were significantly enhanced by combination treatment with itraconazole and caspofungin. Docking studies indicated that 2',4'-DHC bind to the ATPase domain of Hsp90. These results suggest that 2',4'-DHC act as an Hsp90-calcinurin pathway inhibitor.

• Biomolecules & Therapeutics
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• v.11 no.1
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• pp.5-7
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• 2003

The purpose of this study was to evaluate tyrosinase inhibitory activity of plant for extracts for cosmetic use. When 80 plant extracts were tested, the methanol extracts of Allium thunbergi, Asparagus oligoclonos, Ixeris dentate, Salvia plebeia, Sophora flavescens and Sophora japonica showed more than 30% inhibition of mushroom tyrosinase activity at 100 $\mu\textrm{g}$/mL. Although less active than the reference compound, kojic acid ($IC_{50}$=7.0-16.3 $\mu\textrm{g}$/mL), these plant extracts may be used as tyrosinase inhibitors in cosmetics.