• Archives of Pharmacal Research
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• v.25 no.3
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• pp.306-312
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• 2002

Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in the diabetic complication. The inhibitors of aldose reductase, therefore, would be potential agents for the prevention of diabetic complications. To evaluate active principles for the inhibition of aldose reductase from the rhizomes of Belamcanda chinensis, twelve phenolic compounds were isolated and tested for their effects on rat lens aldose reductase. As a result, isoflavones such as tectorigenin, irigenin and their glucosides were found to show a strong aldose reductase inhibition. Tectoridin and tectorigenin, exhibited the highest aldose reductase inhibitory potency, their $IC_{50}$ values, being $1.08{\times}10^{-6}{\;}M{\;}and{\;}1.12{\times}10^{-6}{\;}M$, respectively, for DL-glyceraldehyde as a substrate. Both compounds, when administered orally at 100 mg/kg for 10 consecutive days to streptozotocin-induced diabetic rats, caused a significant inhibition of sorbitol accumulation in the tissues such as lens, sciatic nerves and red blood cells. Tectorigenin showed a stronger inhibitory activity than tectoridin. From these results, it is suggested that tectorigenin is attributed to be a promising compound for the prevention and/or treatment of diabetic complications.

• Corrosion Science and Technology
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• v.19 no.1
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• pp.8-15
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• 2020

In this paper, the efficiency and the inhibition mechanisms of cobalt salts (cobalt nitrate and cobalt-exchange silica Co/Si) for the corrosion protection of AA2024 were investigated in a neutral aqueous solution by using the electrochemical impedance spectroscopy (EIS) and polarization curves. The experimental measurements suggest that cobalt cation plays a role as a cathodic inhibitor. The efficiency of cobalt cation was important at the concentration range from 0.001 to 0.01 M. The formation of precipitates of oxides/hydroxides of cobalt on the surface at low inhibitor concentration was confirmed by the Scanning Electron Microscopy/Energy Dispersive X-Ray Spectroscopy (SEM/EDS) analysis. EIS measurements were also conducted for the AA2024 surface covered by water-based epoxy coating comprising Co/Si salt. The results obtained from exposure in the electrolyte demonstrated the improvement of the barrier and inhibition properties of the coating exposed in the electrolyte solution for a lengthy time. The SEM/EDS analysis in artificial scribes of the coating after salt spray testing revealed the release of cobalt cations in the coating defect to induce the barrier layer on the exposed AA2024 substrate.

• Archives of Pharmacal Research
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• v.19 no.2
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• pp.126-131
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• 1996

The effects of various synthetic benzimidazole derivatives on gastric H^+/K^+$ATPase activity in vitro were examined. The results showed that the effects of substituents on the benzimidazole ring were not significant. However, replacement of sulfoxide connecting two ring systems to sulfide resulted in a completely inactive compound in vitro, suggesting the essential role of sulfoxide group in the inhibition. In addition, compounds with 5 or 6-membered oxacyclic substituents attached to the pyridine ring displayed the most effective inhibitory activity. Among these derivatives, AU-47 was the most potent, and detailed mechanistic studies with the compound were carried out. AU-47 inhibited gastricH^+/K^+$ATPase in a concentration and time dependent manner with 50% inhibition at $6\muM$. The presence of sulfhydryl reducing agents or substrate analogue protected H^+/K^+$ATPase from the inactivation. The inhibition by AU-47 was potentiated by acid pretreatment of the compound, suggesting the structural conversion of AU-47 into a more active intermediate which was favored in acidic condition. Consistent with in vitro results, AU-47 inhibited in vivo gastric acid secretion. The results suggest that AU47 is a relevant candidate for the development of new antiulcer agent.

• Food Science and Biotechnology
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• v.15 no.4
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• pp.516-522
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• 2006

This study was to assess the antimicrobial action of 2-hydroxyethyl ${\beta}$-undecenate purified from cumin (Cuminum cymium L.) seed against the oral anaerobe, Streptococcus mutans, which is associated with gingivitis, specifically focusing on the catabolic effect. 2-Hydroxyethyl ${\beta}$-undecenate inhibited the acid production and growth of S. mutans after 30 hr incubation at 50 mM. The glycolysis of S. mutans with glucose as substrate was similarly sensitive to 2-hydroxyethyl ${\beta}$-undecenate, with 70% inhibition of glucose utilization at 5 mM and 90% inhibition at 50 mM. In addition, this substance potently inhibited the glycolysis enzyme, glyceraldehyde-3-phosphate dehydrogenase (GADP); the phosphoenolpyruvate, glucose phosphotransferase (Glucose-PTS); and membrane ATPase, in a concentration dependent manner. The $IC_{50}$ values for inhibition of GADP, Glucose-PTS, and ATPase were 1, 0.9, and 5 mM, respectively. Furthermore, 2-hydroxyethyl ${\beta}$-undecenate inhibited teeth calcium ion elution by 80% at 50 mM. These results suggest that 2-hydroxyethyl ${\beta}$-undecenate is a potent inhibitor of carbohydrate metabolism and the growth of S. mutans JC-2.

• Korean Journal of Metals and Materials
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• v.47 no.7
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• pp.423-432
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• 2009

In the galvanizing coating process, the effects of the silicon content on the coatability and wettability of molten zinc were investigated on Dual-Phase High Strength Steels (DP-HSS) with various Si contents using the galvanizing simulator and dynamic reactive wetting systems. DP-HSS showed good coatability and a well-developed inhibition layer in the range of Si content below 0.5 wt%. Good coatability was the results of the mixed oxide $Mn_{2}SiO_{4}$, being formed by the selective oxidation on the surface, with a low contact angle in molten zinc and a large fraction of oxide free surface that provided a sufficient site for the molten zinc to wet and react with the substrate. On the other hand, with more than 0.5 wt%, DP-HSS exhibited poor coatability and an irregularly developed inhibition layer. The poor coatability was due to the poor wettability that resulted from the development of network-type layers of amorphous ${SiO}_{2}$, leading to a high contact angle in molten zinc, on the surface.

• Applied Biological Chemistry
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• v.42 no.3
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• pp.252-255
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• 1999

Inhibition activities$(pI_{50})$ of chalcone derivatives as substrate with farnesyl protein transferase(FPTase) were determined in vitro. The structure activity relationships(SAR) between the activity and physicochemical parameters of X & Y-substituents on the phenyl groups were analyzed by Free-Wilson and Hansch method. X-substituents on the benzoyl group have the more important role to inhibition activity than Y-substituents on the styryl group. Among them, none substituent, 8 showed the highest FPTase inhibition activity$(pI_{50}=4.30)$. Particularly, the SAR equation could be formulated, showing a parabolic relationship between the activity and hydrophobicity(logP) where the optimal value$({\Sigma}logP)_{opt}$ was 3.915. And also the activity depends on the steric effect(Es > 0) with X-substituent and the resonance effect(R < 0) with electron donating Y-substituents. Based on the results of SAR analyses, the interactions between substrates and receptor, FPTase, could be assumed.

• Korean Journal of Medicinal Crop Science
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• v.24 no.1
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• pp.7-13
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• 2016

Background : Ginger has been extensively used in foods and traditional medicines in Asian countries. Despite its frequent consumption in daily life, the mechanism of potential interactions between ginger components-drug has not been examined. To elucidate the mechanism of governing the effects of 6-shogaol, a primary constituent of dried ginger, on human cytochrome P450 (CYP) isoenzymes an incubation studies were carried out using pooled human liver microsome (HLM). Methods and Results : CYP isoenzyme specific substrate was incubated with multiple concentrations of inhibitor, HLM and cofactors. 6-shogaol showed a potent inhibitory effect on CYP2C9, CYP1A2 and CYP2C19 with half maximal inhibitory concentration ($IC_{50}$) values of 29.20, 20.68 and $18.78{\mu}M$ respectively. To estimate the value of the inhibition constant ($K_i$) and the mode of inhibition, an incubation study with varying concentrations of each CYP isoenzyme-specific probe was performed. 6-shogaol inhibited CYP2C9 and CYP2C19 noncompetitively ($K_i=29.02$ and $19.26{\mu}M$ respectively), in contrast, the inhibition of CYP1A2 was best explained by competitive inhibition ($K_i=6.33{\mu}M$). Conclusions : These findings suggest that 6-shogaol may possess inhibitory effects on metabolic activities mediated by CYP1A2, CYP2C9 and CYP2C19 in humans.

• Corrosion Science and Technology
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• v.11 no.1
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• pp.9-14
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• 2012

The formation of the Fe-Al inhibition layer in hot-dip galvanizing is a confusing issue for a long time. This study presents a characterization result on the inhibition layer formed on C-Mn-Cr and C-Mn-Si dual-phase steels after a short time galvanizing. The samples were annealed at $800^{\circ}C$ for 60 s in $N_{2}$-10% $H_{2}$ atmosphere with a dew point of $-30^{\circ}C$, and were then galvanized in a bath containing 0.2 %Al. X-ray photoelectron spectroscopy (XPS) and transmission electron microscopy (TEM) was employed for characterization. The TEM electron diffraction shows that only $Fe_{2}Al_{5}$ intermetallic phase was formed. No orientation relationship between the $Fe_{2}Al_{5}$ phase and the steel substrate could be identified. Two peaks of Al 2p photoelectrons, one from metallic aluminum and the other from $Al^{3+}$ ions, were detected in the inhibition layer, indicating that the layer is in fact a mixture of $Fe_{2}Al_{5}$ and $Al_{2}O_{3}$. TEM/EDS analysis verifies the existence of $Al_{2}O_{3}$ in the boundaries of $Fe_{2}Al_{5}$ grains. The nucleation of $Fe_{2}Al_{5}$ and the reduction of the surface oxide probably proceeded concurrently on galvanizing, and the residual oxides prohibited the heteroepitaxial growth of $Fe_{2}Al_{5}$.

• Archives of Pharmacal Research
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• v.11 no.1
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• pp.33-40
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• 1988

Two new nitro analogs of tranylcypromine, (E)-2-(p-nitrophenyl)cyclopropylamine ((E)-p-NTCP) and (E)-2-(m-nitrophenyl)cyclopropylamine ((E)-m-NTCP) were synthesized in order to examine the effect of aromatic nitro substitution on the MAO-inhibitory activity of 2-phenylcyclopropylamines. The compounds were obtained by treating t-butyl (E)-2-(p-nitrophenyl) cyclopropanecarbamate and t-butyl (E)-2-(m-nitrophenyl)cyclopropanecarbamate with p-toluenesulfonic acid in $CH_3$CN. Inhibitions of rat brain mitochondrial MAO-A and B by the compounds were examined using serotonin and benzylamine as the substrate at both in vitro and ex vivo levels. It was found from in vitro measurements that (E)-p-NTCP at $6.0{\times}10^{-5}M$ elicited merely 22.5% inhibition against MAO-B without any effect on MAO-A. In contrast, (E)-m-NTCP showed fair degrees of inhibitions of MAO-A and B with $IC_{50}$ values, $2.5{\times}10^{-7}M\;and\;1.4{\times}10^{-6}M$, respectively. It was also noted from (E)-m-NTCP that m-nitro substitution caused a shift of selectivity of the inhibition toward MAO-A. According to ex vivo measurements at 1.5, 3, 6, and 12 hr following the administration of a dose of 0.015 mmol/kg, i.p. to the rats, the inhibition percents of MAO-A by (E)-m-NTCP were 58.6, 63.7 63.6, and 46.6%, slightly lower than those observed by tranylcypromine. Whereas, (E)-m-NTCP at the same dose level did not show significant inhibitions against both MAO-A and MAO-B. Possible reasons for the difference in potencies between (E)-m-NTCP and (E)-p-NTCP were sought in relation to differing electron withdrawing effects of m- and p-substituents which will influence electron density of the side chain amino functions and the partitions.

• KSBB Journal
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• v.8 no.4
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• pp.341-350
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• 1993

As an effort to develop an alternative transportation fuel, the production of methanol from methane gas was studied using the resting cells of an obligatory methanotroph, Methylosinus trichosporium OB3b. The reaction was carried out in high concentration phosphate buffer solutions with the flask-grown cells containing the exclusively cytoplasmic methane monooxygenase (sMMO) activity. The methanol accumulation rate was observed to be 79nmo1/mg·min during the initial 4.5hr. Phosphate-dependent inhibition was found for both sMMO and methanol dehydrogenase (MDH) activities, and the inhibition constants were 185mM and 42mM, respectively. The inhibition mode was noncompetitive. Methanol was found to be very inhibitory to the sMMO activity and the inhibition constant (noncompetitive) was 21mM when propylene was used as substrate. The sMO activity in the resting cells was declined very fast and the rate became very high during the methanol production. These results indicate that the use of M. trichosporium OB3b as a biocatalyst for the methanol production is heavily dependent on the stable maintenance of the whole-cell SMO activity as well as the effective alleviation of product inhibition.