• Natural Product Sciences
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• v.18 no.1
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• pp.47-51
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• 2012

Among 38 Vietnamese medicinal plant extracts investigated for their ${\alpha}$-glucosidase inhibitory activity, 35 extracts showed $IC_{50}$ values below $250{\mu}g/mL$. The MeOH extracts of the heartwood of Oroxylum indicum, the seeds of Caesalpinia sappan, and the fruits of Xanthium strumarium exhibited strong ${\alpha}$-glucosidase inhibitory activity with $IC_{50}$ values less than $50{\mu}g/mL$. Fractionation of the MeOH extract of the heartwood of O. indicum led to the isolation of oroxylin A (1), oroxyloside (2), hispidulin (3), apigenin (4), ficusal (5), balanophonin (6), 2- (1-hydroxymethylethyl)-4H,9H-naphtho[2,3-b]furan-4,9-dione (7), salicylic acid (8), p-hydroxybenzoic acid (9), protocatechuic acid (10), isovanillin (11), and ${\beta}$-hydroxypropiovanillon (12). Compounds 1 - 3, 5, 6, 8, 10, and 12 showed more potent activities, with $IC_{50}$ values ranging from 2.13 to $133.51{\mu}M$, than a positive control acabose ($IC_{50}$, $241.85{\mu}M$). The kinetic study indicated that oroxyloside (2) displayed mixed-type inhibition with inhibition constant (Ki) was $3.56{\mu}M$.

• The Korean Journal of Zoology
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• v.23 no.3
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• pp.137-148
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• 1980

The effects of divalent cations, $Hg^{2+}, Cu^{2+}, Pb^{2+}, Cd^{2+}$, and $Mn^{2+}$ on the total ATPase activity of the fragmented sarcoplasmic reticulum isolated from rabbit skeletal muscle were investigated. The inhibitory effects of the cations on the enzyme activity increased as the concentrations of the ions increased with the order of efficiency of $Hg^{2+}$ > $Cu^{2+}$ > $Pb^{2+}$ > $Cd^{2+}$ > $Mn^{2+}$ in the concentration range between 10 and 500$\mu$M. The 50% inhibition for each ion was almost identical with the inhibition constant (Ki) value for each ion. The Ki's were 10, 30 130, and 350$\mu$M for $Hg^{2+}, Cu^{2+}, Pb^{2+}, and Cd^{2+}$, respectively. $Mn^{2+}$ seemed to be an activator at lower concentrations and an inhibitor at higher concentrations. The presence of the cations did not change the Km values, suggesting that the ions act as a reversible noncompetitive inhibitor on the FSR ATPase. The energy of activation of the enzyme was aproximately 19 Kcal/mole. The presence of the ions decreased the value slightly. A possible mechanism for the reversible noncompetitive inhibitory effect of the cations was discussed.

• Food Science and Biotechnology
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• v.14 no.6
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• pp.727-731
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• 2005

Synthesized Ile-Ala-Val-Pro (IAVP) peptide, which has the highest hypocholesterolemic effect among a number of synthesized derivatives of Ile-Ala-Val-Pro-Gly-Glu-Val-Ala (IAVPGEVA) isolated from 11S globulin of soy protein by pepsin digestion, was selected for investigation in the present study. Using a recombinant Syrian hamster 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR), we studied in detail the inhibition of this enzyme by IAVP and compared the action of this peptide to that of lovastatin, a known competitive inhibitor of this enzyme. The concentration of IAVP required for 50% inhibition ($IC_{50}$) of HMGR activity in given experimental conditions was $340\;{\mu}M$. Kinetic analysis revealed that the studied peptide is a competitive inhibitor of HMGR with respect to both 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) and nicotinamide adenine dinucleotide phosphate (NADPH), with an equilibrium constant of inhibitor binding ($K_i\;=\;[E][I]/[EI]$) of $61{\pm}1.2\;{\mu}M$ and $157{\pm}4.4\;{\mu}M$, respectively. At the same conditions, $K_i$ and $IC_{50}$ for lovastatin were $2.2{\pm}0.1\;nM$ and 12.5 nM, respectively. Thus, the given peptide interacts with HMGR as a bisubstrate, consequently blocking access of both substrates to the active sites. The achieved results suggest the design of new peptide sequences having a higher relative affinity to binding sites of this enzyme and an enhancement of their hypocholesterolemic properties.

• Archives of Pharmacal Research
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• v.28 no.8
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• pp.923-929
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• 2005

Methanol extracts of domestic plants of Korea were evaluated as a potential inhibitor of neutral pH optimum and membrane-associated 60 kDa sphingomyelinase (N-SMase) activity. In this study, we partially purified N-SMase from bovine brain membranes using ammonium sulfate. It was purified approximately 163-fold by the sequential use of DE52, Butyl-Toyopearl, DEAE-Cellulose, and Phenyl-5PW column chromatographies. The purified N-SMase activity was assayed in the presence of the plant extracts of three hundreds species. Based on the in vitro assay, three plant extracts significantly inhibited the N-SMase activity in a time- and concentration-dependent manner. To further examine the inhibitory pattern, a Dixon plot was constructed for each of the plant extracts. The extracts of Abies nephrolepis, Acer tegmentosum, and Ginkgo biloba revealed a competitive inhibition with the inhibition constant (Ki) of $11.9 {\mu}g/mL,\;9.4{\mu}g/mL,\;and\;12.9{\mu}g/mL$, respectively. These extracts also inhibited in a dose-dependent manner the production of ceramide induced by serum deprivation in human neuroblastoma cell line SH-SY5Y.

• Archives of Pharmacal Research
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• v.28 no.3
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• pp.330-334
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• 2005

The effect of a new hepatoprotective agent, YH-439, on the hepatobiliary transport of a model organic cation (OC), TBuMA (tributylmethylammonium), was investigated. The area under the plasma concentration-time curve (AUC) from time zero to 4 h following iv administration of TBuMA (6.6 $\mu$mol/kg) was increased significantly when YH-439 in corn oil (300 mg/kg) was orally administered to rats 24 h prior to the experiment. Nevertheless, the cumulative biliary excretion of TBuMA remained unchanged. As a consequence, the apparent biliary clearance ($CL_b$) of TBuMA was decreased significantly as a result of YH-439 pretreatment, consistent with the fact that the in vivo excretion clearance of TBuMA across the canalicular membrane ($CL_{exc}$) was not changed by the pretreatment. The in vitro uptake of TBuMA into isolated hepatocytes was decreased by one half by the pretreatment, owing to a decrease in the apparent V$_{max}$ and $CL_{linear}$, but the $K_m$ for the process remained constant. Most interestingly, however, the sinusoidal uptake of glucose, a nutrient, into hepatocytes was not influenced by the pretreatment, suggesting the YH-439 pretreatment specifically impaired the sinusoidal uptake of OCs. Thus, the OC-specific inhibition of hepatic uptake, without influencing the uptake of glucose, a nutrient, appeared to be associated with the hepatoprotective activity of YH-439.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.31 no.1
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• pp.1-11
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• 2018

Objectives : The purpose of this study is to investigate the effect of Shinsuwisaengtang (SSWST) extracts on antioxidant activity and inhibition of phototoxicity as a medicine for skin damage due to ultra violet stimulation. Methods : To determine the cytotoxicity of Hs68 cells from SSWST extracts, we investigated cell viability by MTT assay. To determine the protective effect of phototoxicity, we investigated cell viability after UVB radiation. The DPPH radical scavenging activity was examined to determine the antioxidant effect of SSWST extracts. Hoechst 33258 staining was performed to observe the protective effect of SSWST on UVB. Results : The cytotoxicity of SSWST extracts in Hs68 cells was not appeared significantly in all concentration. SSWST extracts significantly increased the viability of UVB-stimulated Hs68 cells at a concentration of 25, 50 and $100{\mu}g/ml$. SSWST extract showed higher DPPH radical scavenging than the control group. It was observed that SSWST extracts inhibited the apoptosis of the UVB-stimulated Hs68 cells through a fluorescence microscope. Conclusions : It was observed that SSWST did not induce cytotoxicity at a constant concentration and had a protective effect on phototoxicity and an antioxidant effect. Thus, it is considered that it maybe used as a medicine to cure skin damage caused by UVB and photoaging changes in the future.

• Journal of Electrochemical Science and Technology
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• v.3 no.3
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• pp.123-134
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• 2012

The electrochemical performance of positive pole grids of lead-acid batteries made of Pb-0.08%Ca-1.1%Sn alloys without and with 0.1 wt% of each of Cu, As or Sb and with 0.1 wt% of Cu, As and Sb combined was investigated by electrochemical methods in 4.0 M $H_2SO_4$. The corrodibility of alloys under open-circuit conditions and constant current charging of the positive pole, the positive pole gassing and the self-discharge of the charged positive pole were studied. All impurities (Cu, As, Sb) were found to decrease the corrosion resistance, $R_{corr}$ after 1/2 hour corrosion, but after 24 hours an improvement in $R_{corr}$ was recorded for Sb containing alloy and the alloy with the three impurities combined. While an individual impurity was found to enhance oxygen evolution reaction, the impurities combined significantly inhibition this reaction and the related water loss problem was improved. Impedance results were found helpful in identification of the species involved in the charging/discharging and the self-discharge of the positive pole. Impurities individually or combined were found to increase the self-discharge during polarization (33-68%), where Sb containing alloy was the worst and impurities combined alloy was the least. The corrosion of the positive pole grid in the constant current charging was found to increase in the presence of impurities by 5-10%. Under open-circuit, the self-discharge of the charged positive grids was found to increase significantly (92-212%) in the presence of impurities, with Sb-containing alloy was the worst. The important result of the study is that the harmful effect of the studied impurities combined was not additive but sometimes lesser than any individual impurity.

• Journal of Life Science
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• v.22 no.11
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• pp.1451-1455
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• 2012

The study was conducted to investigate the effect of Maillard reaction products (MRPs) on enzymatic browning of crown daisy (Chrysanthmum coronarium var. spatiosum). The MRPs prepared by heating various amino acid and sugar at $90^{\circ}C$ caused a strong inhibitory effect on crown daisy polyphenol oxidase (PPO, ${\sigma}$-diphenol oxygen oxidoreductase, EC 1.10.3.1). As the reaction time of the solution containing glycine and glucose increased at $90^{\circ}C$, the production of MRPs was increased, whereas the amounts of glycine and glucose were decreased. Accordingly, the inhibitory effect of crown daisy PPO activity by MRPs was increased as the amounts of synthesized MRPs were increased. The MRPs synthesized from the various amino acids and sugars significantly reduced the PPO activity, particularly MRPs prepared by glutamine and xylose. The Michealis-Menten constant value ($K_m$) of crown daisy PPO with catechol as a substrate was 22.0 mM, and MRPs were a noncompetitive inhibitor against crown daisy PPO.

• Korean Journal of Food Science and Technology
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• v.33 no.1
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• pp.7-11
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• 2001

The influence of temperature and calcium concentration on the gelation kinetics of purified Aigeok system has been investigated by small deformation oscillatory measurement. DE(degree of esterification) of the present sample was indicated of low methoxyl Aigeok polysaccharide by FT-IR. The calcium induced gelation of Aigeok has been studied. Both moduli reached the saturation value during the period of experiments. Rate constant increased with increasing calcium concentration, however above 4.08 mM calcium chloride caused a sudden drop in gel strength. The experimental result that the decrease in gel strength at high calcium concentration was seems to be phase separation or competitive inhibition between calcium ions. The storage and loss shear moduli decreased with increasing temperature. The rate constant of Aigeok system remarkably dropped above $35^{\circ}C$. Thus hydrogen bonding is prior to hydrophobic interaction for Aigeok molecule.

• Journal of the Korea Organic Resources Recycling Association
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• v.2 no.2
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• pp.3-17
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• 1994

The inhibitory effect of sodium ion on the anaerobic degradation of food waste was studied by an anaerobic batch toxicity assay and inhibition model. The anaerobic degradation activity of food waste spiked with over $2g\;Na^+/L$ of sodium ion was severely inhibited at the initial stage of the exposure. The inhibition response of anaerobic microorganisms on the sodium ion estimated from the methane production was differed according to the concentration of sodium ion. The relative acclimation time(RAT) and methanation rate(RMR), defined as the ratios of initial lag time and maximum methane production rate of the sample spiked with sodium ion to the control. respectively, were used to evaluate the acclimation and inhibitory effects quantitatively on the anaerobic microorganisms. When sodium ion was increased from $2g\;Na^+/L$ to $20g\;Na^+/L$, the RAT was exponentially increased from 18.9 to 90. but the RMR was linearly decreased from 0.97 to 0.02. The effects of sodium ion for the maximum methanation rate, first order kinetic constant and ultimate methane production were well evaluated by a generalized nonlinear expression model. it could be described by the uncompetitive inhibition mode. The sodium ion concentration causing 50% inhibition of methanation activity was about $11g\;Na^+/L$, and the critical sodium ion beyond to compelete inhibition was 20 to $21g\;Na^+/L$. The presented results could be used to obtain the design or operation parameters of the anaerobic process treating food waste of high salt.