• Bulletin of the Korean Chemical Society
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• v.32 no.spc8
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• pp.2997-3002
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• 2011

A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The $IC_{50}$ values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.5{\pm}0.2\;{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $1.52{\pm}0.18\;{\mu}M$.

• Microbiology and Biotechnology Letters
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• v.9 no.4
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• pp.179-183
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• 1981

An extracellular chitinase was purified from the culture fluid of Streptomyces sp. 115-5, and its inhibition mechanism by end product was studied. The activity of chitinase was suppressed by the reducing sugar as the reaction proceeded, and the activity was inhibited by the addition of D-glucose. Besides D-glucose, the rate of chitin hydrolysis was inhibited by D-glucuronic acid, D-sorbitol and D-xylose in the reaction system of the enzyme. it was found that the hydroxyl groups at the C-2, C-3 and C-4 position of D-glucose molecule play an important role in the inhibition of the chitinase activity. D-glucose was found to inhibit the enzyme activity by mixed type of competitive and non-competitive mode.

• BMB Reports
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• v.28 no.6
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• pp.471-476
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• 1995

Acetolactate synthase (ALS) catalyzes the first common step in the biosynthesis of valine, leucine, and isoleucine. ALS is the target enzyme for several classes of structually diverse herbicides. We have synthesized 4,6-dimethoxypyrimidine derivatives as ALS inhibitors, and their inhibitory activities on barley ALS were determined. $IC_{50}$ values for the derivatives are 0.2~200 ${\mu}m$. K11570, the most potent ALS inhibitor with $IC_{50}$ of 0.2 ${\mu}m$, showed mixed-type inhibition with respect to substrate pyruvate, and the progress curves for ALS inhibition by K11570 indicated that the amount of inhibition increased with time. Inhibition-competition experiments were carried out and indicated that three different classes of inhibitors, K11570, a sulfonylurea Ally, and leucine, bind to ALS in a mutually exclusive manner. Chemical modification of tryptophanyl and tyrosyl residues of ALS decreased the sensitivity of ALS to K11570, while cysteine modification did not affect the sensitivity. These results suggest that tryptophanyl and tyrosynyl residues are probably located at or near the inhibitor binding site.

• Bulletin of the Korean Chemical Society
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• v.16 no.5
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• pp.454-458
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• 1995

Inhibiting action of semicarbazide, thiosemicarbazide, sym. diphenylcarbazide towards corrosion of zinc in hydrochloric acid has been investigated. The rate of corrosion depends on the nature of the inhibitor and its concentration. The values of inhibition efficiency from, weight loss, thermometric measurements are in good agreement with those obtained from polarization studies. From the polarization studies, the inhibitors used act as mixed absorption type inhibitors, increased adsorption resulting from an increase in the electron density at the reactive C=S and C=O groups and N-atoms. The thermodynamic parameters of adsorption obtained using Bockris-Swinkels adsorption isotherm reveal a strong interaction of these carbazides on zinc surface.

• Corrosion Science and Technology
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• v.4 no.6
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• pp.231-235
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• 2005

The inhibitive effect of extracts of tamarind seeds and jackfruit seeds, curry leaves and henna leaves on corrosion of mild steel in 1M HCl solution have been studied by weight loss, potentiodynamic polarization and impedance measurements. Results obtained from the electrochemical techniques were in good agreement with weight loss results. From the weight loss data, the values of surface coverage ($\Theta$) and corrosion rate were calculated. The inhibition efficiency (IE) increased with increasing inhibitor concentration in 1M HCl solution. In all the cases the adsorption of the natural product extracts on the mild steel surface from 1M HCl follows the Langmuir adsorption isotherm relationship. Potentiodynamic polarization studies reveal the fact that all the four natural product extracts act as mixed type inhibitors. The decrease in the inhibition efficiency follows the order: Extracts of jackfruit seed>henna leaves>curry leaves>tamarind seed.

• Journal of the Korean Chemical Society
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• v.56 no.2
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• pp.264-273
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• 2012

Five derivatives of phenylthiourea namely: 1-(4-methoxyphenyl)-3-phenylthiourea (1), 1-(4-methylphenyl)-3- phenylthiourea (2), 1-(4-bromophenyl)-3-phenylthiourea (3), 1-(4-chlorophenyl)-3-phenylthiourea (4) and 1-phenylthiourea (5) have been evaluated as new inhibitors for the corrosion of carbon steel in 2 M HCl solution using potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) techniques. Potentiodynamic polarization measurements showed that these derivatives are mixed-type inhibitors. The inhibition efficiency was found to increase with inhibitor concentration and decreases with rise in temperature. The thermodynamic parameters of adsorption and activation were determined and discussed. Nyquist plots showed depressed semicircles with their centre below real axis. The adsorption process of studied derivatives on carbon steel surface obeys Temkin adsorption isotherm. The synergistic effect of these derivatives and some anions is discussed from the viewpoint of adsorption models. The electrochemical results are in good agreement with the calculated quantum chemical HOMO and LUMO energies of the tested molecules.

• Journal of the Korean Chemical Society
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• v.58 no.4
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• pp.359-365
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• 2014

The inhibition effect of cinnamon plant extract as a green corrosion inhibitor for steel in sulfide polluted salt water was studied by potentiodynamic polarization, electrochemical impedance spectroscopy (EIS), and electrochemical frequency modulation (EFM). The results showed that cinnamon plant extract in sulfide polluted salt water is a good corrosion inhibitor with inhibition efficiency reached to 80% at 250 ppm of the plant extract. The adsorption of cinnamon obeys Temkin adsorption isotherm, and acts as a mixed-type of inhibitor but dominantly as a cathodic inhibitor in sulfide polluted salt water.

• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.4
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• pp.693-697
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• 1998

The influence of flavonols from onion skin on xanthine oxidase was investigated. Methanol extract was showed 12.8% of yield, 661.3mg% of flavonoids contents and 88.7% of inhibitory effect on xanthine oxidase F1 and F2 fractions were obtained from the methanol extract by ODS and Sephadex LH-20 chromatography. F1 and F2 fractions flavonols(3-OH free) identified by UV/visible spectroscopy. Inhibitory effect of F1 and F2 on xanthine oxidase were increased with increasing concentration. IC50s of F1 and F2 were 0.95$\mu\textrm{g}$ and 0.67$\mu\textrm{g}$, respectively. To confirm the specificity of F1 and F2 against xanthine oxidase, albumin was added to the reaction mixture. The inhibition of F1 and F2 may be due to specific binding to xanthine oxidase. The modes of their inhibitions were of mixed type with respect to xanthine as a substrate.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.81-86
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• 1986

The effect of imperatorin on hepatic microsomal mixed function oxidases (MF0) was investigated. On acute treatment, imperatorin (30 mg/kg, i.p) caused a significant reduction in activities of hepatic aminopyrine N-demethylase, hexobarbital hydroxylase and aniline hydroxylase as well as cytochrome p0450 content in rats and mice. Kinetic studies on rat liver enzymes revealed that imperatorin appeared to be a competitive inhibitor of aminopyrine N-demethylase (Ki,0.007 mM), whereas a non-competitive inhibitor of hexobarbital hydroxylase (Ki, 0.0148 mM). Imperatorin also inhibited non-competitively aniline metabolism (Ki 0.2 mM). Imperatorin binds to phenobarbital-induced cytochrome p-450 to give a typical type 1 binding sepctrum (max. 388nm, min 422 nm). Multiple administrations of imperatorin (30 mg/kg. i. p. daily for 7 days) to mice shortended markedly the duration of hexobarbital narcosis and increased activities of hepatic aminopyrine N-demethylase and hexobarbital hydroxylase and the level of cytochrome p-450 where as aniline hydroxylase activity was unaffected.

• Journal of the Korean Chemical Society
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• v.41 no.6
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• pp.304-312
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• 1997

Acetolactate synthase(ALS) is the common enzyme in the biosynthetic of valine, leucine, and isoleucine, and is the target of several classes of structually unrelated herbicides, including sulfonylureas, imidazolinones, and triazolopyrimidines. In an effort to develop new and desirable herbicides, we have synthesized 4,6-dimethoxypyrimidine derivatives, and examined their inhibitory activities on pea ALS. The most active compound was found to be K11570 and $IC_{50}$ value for K11570 was 0.2 ${\mu}M.$ The inhibition of pea ALS by K11570 was biphasic, showing increased inhibition with incubation time. The K11570 showed mixed-type inhibition with respect to substrate pyruvate. Dual inhibition analysis of K11570 versus sufonylurea herbicide Ally and feedback inhibitor leucine revealed that three inhibitors were competitive for binding to ALS. The arginine modified enzyme showed decreased inhibition by K11570, sufonylurea Ally, and leucine, in constrast to, tryptophan modification did not affect on the sensitivity of ALS to the inhibitors.