• The Korean Journal of Physiology and Pharmacology
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• v.7 no.2
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• pp.59-63
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• 2003

The medial vestibular nucleus (MVN) neurons are controlled by excitatory synaptic transmission from the vestibular afferent and commissural projections, and by inhibitory transmission from interneurons. Spontaneous synaptic currents of MVN neurons were studied using whole cell patch clamp recording in slices prepared from 13- to 17-day-old rats. The spontaneous inhibitory postsynaptic currents (sIPSCs) were significantly reduced by the $GABA_A$ antagonist bicuculline ($20{\mu}M$), but were not affected by the glycine antagonist strychnine ($1{\mu}M$). The frequency, amplitude, and decay time constant of sIPSCs were $4.3{\pm}0.9$ Hz, $18.1{\pm}2.0$ pA, and $8.9{\pm}0.4$ ms, respectively. Spontaneous excitatory postsynaptic currents (sEPSCs) were mediated by non-NMDA and NMDA receptors. The specific AMPA receptor antagonist GYKI-52466 ($50{\mu}M$) completely blocked the non-NMDA mediated sEPSCs, indicating that they are mediated by an AMPA-preferring receptor. The AMPA mediated sEPSCs were characterized by low frequency ($1.5{\pm}0.4$ Hz), small amplitude ($13.9{\pm}1.9$ pA), and rapid decay kinetics ($2.8{\pm}0.2$ ms). The majority (15/21) displayed linear I-V relationships, suggesting the presence of GluR2-containing AMPA receptors. Only 35% of recorded MVN neurons showed NMDA mediated currents, which were characterized by small amplitude and low frequency. These results suggest that the MVN neurons receive excitatory inputs mediated by AMPA, but not kainate, and NMDA receptors, and inhibitory transmission mediated by $GABA_A$ receptors in neonatal rats.

• Advances in Traditional Medicine
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• v.7 no.5
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• pp.477-484
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• 2008

The present study was aimed at investigating the hypouricemic and xanthine oxidase inhibitory activities of the various fractions of the hydromethanolic extract of the leaves of Coccinia grandis L. Voigt (Cucurbitaceae). The leaves of this species was used in traditional medicinal system for the treatment of gout, rheumatism, jaundice, bronchitis, fever, skin eruptions, wounds, etc. The degree of xanthine oxidase inhibition was determined in vitro by measuring the increase in absorbance at 295 nm associated with uric acid formation. Among the fractions tested, the chloroform fraction exhibited highest potency ($IC_{50}$ $17.8\;{\mu}g/ml$). This was followed by the pet-ether ($IC_{50}$ $29.7\;{\mu}g/ml$), ethyl acetate ($IC_{50}$ $41.2\;{\mu}g/ml$) and residual ($IC_{50}$ $47\;{\mu}g/ml$) fractions. The $IC_{50}$ value of allopurinol was $6.1\;{\mu}g/ml$. In addition, the hypouricemic and hepatic xanthine oxidase (XO)/xanthine dehydrogenase (XDH) inhibitory activities of the fractions were examined in vivo using oxonate (280 mg/kg, i.p.) induced hyperuricemic mice. At a dose of 200 mg/kg orally for 7 days, the pet-ether, chloroform and ethyl acetate fractions produced a significant (P < 0.01) reduction in serum urate level and also inhibited hepatic XO/XDH activities when compared to hyperuricemic mice. These inhibitory effects were weaker than that observed for the standard drug, allopurinol (10 mg/kg, p.o.). Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type. These results suggest that the use of Coccinia grandis leaves for the treatment of gout could be attributed to its XO inhibitory activity.

• Korean Journal of Medicinal Crop Science
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• v.28 no.1
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• pp.21-28
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• 2020

Background: Owing to its high efficiency in lipid and protein production, peanut (Arachis hypogaea L.) is considered one of most important crops world-wide. The kernels of peanuts are undoubtedly the most important product this plant, whereas the skin is almost completely neglected in nutraceutical terms. However, peanut skin contains potentially health-promoting phenolics and dietary fiber, and there is considerable potential for commercial exploitation. In this study, we evaluated the α-glucosidase inhibitory activity of an extract of peanut skin (PS). Methods and Results: The α-glucosidase inhibitory effects of 80% ethanol extracts of peanut (A. hypogaea L. 'Sinpalkwang') skin were evaluated and found to have a half-maximal inhibitory concentration (IC₅₀) value of 1.2 ㎍/㎖. Progress curves for enzyme reactions were recorded spectrophotometrically, and the inhibition kinetics revealed time-dependent inhibition with enzyme isomerization. Furthermore, using ultra-high performance liquid chromatography combined with quadrupole-orbitrap mass spectrometry, we identified 26 compounds in the peanut skin extract, namely, catechin, epicatechin, and 24 proanthocyanidins. Conclusions: The results suggest that peanut skin can be utilized as an effective source of α-glucosidase inhibition in functional foods and nutraceuticals.

• Archives of Pharmacal Research
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• v.17 no.4
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• pp.218-222
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• 1994

The natural product, spirostanol glycoside dioscin, was shown to directly inactivate human pleural fluid phospholipase $A_2{\;}(PLA_2)$ Inactivation was dose, and time dependent. The $IC_{50}$ was estimated at 18 .mu.M and virtually complete inactivation of the enzyme occurred at 50 .mu.M. Using Michaelis-Menten kinetics, dioscin inactivated the enzyme by a competitive inhibitory manner, the apparent Ki value was $6.9{\times}10_{-4}$. Reversibility was studied directly by dialysis method, the inhibition was reversible. Additioin of excess $Ca^{2+}$ concentration up to 8 mM did not antagonize the inhibitory activity of dioscin. Inactivation of several kinds of $PLA_2$ by dioscin is due to interaction with the active site of $PLA_2$ and may be a useful adjunt in the theraphy of inflammatory diseases.

• Korean journal of food and cookery science
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• v.26 no.6
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• pp.848-852
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• 2010

This study investigated the antibacterial activities of extracts and fractions of Sasa borealis against eight bacteria (Bacillus cereus, Bacillus subtilis, Listeria monocytogenes, Staphylococcus aureus, Psedomonas aerginosa, Salmonella choleraesuis, Serratia marcescens and Vibrio vulnificus) by broth dilution assay. Using survival curves, the kinetics of bacterial inactivation upon exposure to the extracts and fractions were followed for 24 h. In this same manner, MIC (minimum inhibitory concentration) values were determined by broth microdilution assay and then confirmed to be the extract concentrations that inhibited bacterial growth. Sasa borealis extracts showed antibacterial activities against all tested bacteria. In particular, all tested fractions of Sasa borealis had stronger activities than 70% ethanol extract. MIC of Sasa borealis extract was determined to be 5 mg/mL against Salmonella choleraesuis. All fractions of Sasa borealis extract had extremely strong antibacterial activities. MIC of fractions were determined to be 0.03~2.5 mg/mL. These results suggest that the extracts and fractions of Sasa borealis effectively inhibited bacterial growth and thus are useful as natural antibacterial agents.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.742-750
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• 2004

This paper for the first time reports the isolation of 5 compounds from Phellinus linteus. A sphingolipid (1) and two tyrosinase inhibitory compounds (2, 3) along with two carboxylic acids (4, 5), were isolated from the fruiting body of Phellinus linteus (Berk ＆ Curt) Aoshima. The structure of compound 1 was identified as 1-O-$\beta$-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-[(2R)-2-hydroxyhexadecanoylamino]-9-methyl-4,8-octadecadiene-1,3-diol, known as cerebroside B, based on spectroscopic methods such as 1D and 2D NMR as well as by acid hydrolysis. Compounds 2-5 were identified as protocatechualdehyde (2), 5-hydroxymethyl-2-furaldehyde (HMF) (3), succinic acid (4), and fumaric acid (5) based on the spectroscopic evidence. Compounds 2 and 3 inhibited the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with an $IC_{50}$ of 0.40 and 90.8 $\mu\textrm{g}$/mL, respectively. The inhibitory kinetics, which were analyzed by the Lineweaver-Burk plots, were found to be competitive and noncompetitive inhibitors with a $K_{j}$ of 1.1 $\mu\textrm{m}$ and 1.4 mM, respectively.

• Microbiology and Biotechnology Letters
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• v.20 no.6
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• pp.693-698
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• 1992

The resistant effect of several heavy metal ions to Serratia marcescens strain P was studied by the method of minimal inhibitory concentration(MIC), and testing for their metal biosorption. S. marcescens strain P showed a good survival in the presence of high concentrations of some metal ions, namely cadmium, lead, iron, magnesium, and manganese. Copper had the most inhibitory effect among tested. The MIC value was ranged from 0.79 to 1.58 mM. Cells of S. marcescens strain P exhibit an abnormally long lag phase when incubated in high concentrations of zinc and cadmium. Pigment production was reduced by zinc and cadmium, but enhanced by lead and iron. S. marcescens strain P was resistant to ampicillin, tetracycline, cefamandole and chloramphenicol with minimal inhibitory concentration of 128 $\mu$g/ml, 32 $\mu$g/ml, 256 $\mu$g/ml, and 8 $\mu$g/ml, respectively. The kinetics study of biosorptive uptake by S. marcescens strain P revealed that 16.59% of cadmium and 35.38% of lead were eliminated from the media.

• Natural Product Sciences
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• v.10 no.2
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• pp.80-84
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• 2004

Rosmarinic acid and its methyl ester, isolated from the ethyl acetate soluble fraction of the methanolic extract of Salvia miltiorrhiza Bunge (Labiatae), were found to inhibit the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with the $IC_{50}$ values of 16.8 and $21.5\;{\mu}M$, respectively. It was comparable with kojic acid, a well-known tyrosinase inhibitor, with an $IC_{50}$ of $22.4\;{\mu}M$. The inhibitory kinetics analyzed by the Lineweaver-Burk plots, were found rosmarinic acid and its methyl ester to be competitive inhibitors with $K_i\;of\;2.4{\times}10^{-5}\;and\;1.5{\times}10^{-5}\;M$, respectively.

• YAKHAK HOEJI
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• v.33 no.1
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• pp.64-71
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• 1989

Since time-dependent inactivation of MAO was found to be complete in a few minutes when high concentration ratios of tranylcypromine to MAO were used, a method to obtain kinetic parameters was sought suitable to the conditions in which concentrations of tranylcypromine analogs did not exceed that of MAO. For the purpose, kinetic equations were derived and the method applied to the kinetic studies of tranylcypromine enantiomers. It was found that (E)-(+)-2-phenylcyclopropylamine inhibited MAO by the mechanism following bimolecular reaction scheme with $\tilde{K}_i$ of $2.0\;{\times}\;10^6M^{-1}min^{-1}$. Whereas, MAO-inhibitory pattern of the (-)-enantiomer was to be interpreted by suicide inhibition scheme and measured $k_{in}\;and\;\tilde{K}'$ were $0.457\;min^{-1}\;and\;$5.4{\mu}M$, respectively.

• Journal of Korean Society on Water Environment
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• v.18 no.3
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• pp.271-282
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• 2002

The sonochemical process has been applied as a treatment method to investigate its effect on the decomposition of humic substances (HS). The reaction kinetics and mechanisms in the process of sonochemical treatment for humic substances in wastewater have also been discussed. It was observed that the metal ions such Fe(II) and Mn(II) showed catalytic effects, while Al(III), Ca(II), and Mg(II) had inhibitory effects on the decomposition of humic substances in sonochemical reaction with hydrogen peroxide. Experimental results also showed factors such as hydrogen peroxide dose affected the formation of disinfection by-products. Two trihalomethanes, chloroform and dichlorobromomethane were formed as major disinfection by-products during chlorination. The depolymerization and the radical reaction of HS radicals appear to occur simultaneously. The final step of the reaction is the conversion of organic acids to carbon dioxide.