• The Korean Journal of Physiology and Pharmacology
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• v.9 no.2
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• pp.103-108
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• 2005

To study the direct effect of somatostatin (SS) on calcium channel current ($I_{Ba}$) in guinea-pig gastric myocytes, $I_{Ba}$ was recorded by using whole-cell patch clamp technique in single smooth muscle cells. Nicardipine ($1{\mu}M$), a L-type $Ca^{2+}$ channel blocker, inhibited $I_{Ba}$ by $98{\pm}1.9$% (n=5), however $I_{Ba}$ was decreased in a reversible manner by application of SS. The peak $I_{Ba}$ at 0 mV were decreased to $95{\pm}1.5$, $92{\pm}1.9$, $82{\pm}4.0$, $66{\pm}5.8$, $10{\pm}2.9$% at $10^{-10}$, $10^{-9}$, $10^{-8}$, $10^{-7}$, $10^{-5}$ M of SS, respectively (n=3∼6; $mean{\pm}SEM$). The steady-state activation and inactivation curves of $I_{Ba}$ as a function of membrane potentials were well fitted by a Boltzmann equation. Voltage of half-activation ($V_{0.5}$) was $-12{\pm}0.5$ mV in control and $-11{\pm}1.9$ mV in SS treated groups (respectively, n=5). The same values of half-inactivation were $-35{\pm}1.4$ mV and $-35{\pm}1.9$ mV (respectively, n=5). There was no significant difference in activation and inactivation kinetics of $I_{Ba}$ by SS. Inhibitory effect of SS on $I_{Ba}$ was significantly reduced by either dialysis of intracellular solution with $GDP_{\beta}S$, a non-hydrolysable G protein inhibitor, or pretreatment with pertussis toxin (PTX). SS also decreased contraction of guinea-pig gastric antral smooth muscle. In conclusion, SS decreases voltage-dependent L-type calcium channel current ($VDCC_L$) via PTXsensitive signaling pathways in guinea-pig antral circular myocytes.

• Journal of Korean Society of Environmental Engineers
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• v.30 no.7
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• pp.700-704
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• 2008

Nitrite and free ammonia have been known as substrate inhibitors in anaerobic ammonium oxidation. To reduce inhibitory effect of these substrates, the NH$_3$-N/NO$_2$-N ratio in the influent could be properly controlled in anaerobic ammonium oxidation process. Five kinds of NH$_3$-N/NO$_2$-N ratio were assayed in batch to find optimum NH$_3$-N/NO$_2$-N ratio, curtailing substrate inhibition. As the results of batch test, the highest T-N removal efficiency of 88% was obtained at 1.00 : 1.30 of NH$_3$-N/NO$_2$-N ratio. In addition, rate constants for ammonium and nitrite in zero-order kinetics were found to be the highest values as 7.66 mg/L$\cdot$hr and 11.89 mg/L$\cdot$hr at 1.00 : 1.30 ratio, respectively. However, as for the specific anammox activity, the ratio of NH$_3$-N/NO$_2$-N ratio was recommended as 1 : 1.15 which can maintain the highest SAA during continuous operation and preclude the accumulation of nitrite in the reactor.

• Korean Journal of Weed Science
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• v.17 no.1
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• pp.66-70
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• 1997

LGC-40863(proposed common name ; pyribenzoxim), (benzophenone O-[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxy]benzoyl]oxime) is a new rice herbicide being developed by LG Chemical Ltd. The herbicide is highly selective between rice(Oryza sativa L.) and weeds including barnyardgrass (Echinochloa crus-galli(L.) P. Beauv.), and assumed to inhibit acetolactate synthase(ALS ; EC 4.1.3.18) because other structurally related herbicides inhibit the enzyme. To know inhibitory activity and the mode of inhibition of LGC-40863, $I_{50}$(concentration inhibiting ALS activity by 50%) and inhibition kinetics were investigated using ALS extracted from rice and barnyardgrass. $I_{50}$ values of LGC-40863 were 14 and 16mM in rice and barnyardgrass, respectively. In contrast to imazapyr(2-[4,5-dihydro-4-mythyl-4-(1-methylethyl)-5-oxo-1H-imidazol-2-yl]-3-pyridine-carboxylic acid) which showed an uncompetitive inhibition pattern, LGC-40863 was a noncompetitive inhibitor to ALS with respect to pyruvate similar to chlorsulfuron(2-chloro-N-((4-methoxy-6-methyl-l,3,5-triazin-2-yl) aminocarbonyl)benz-enesulfonamide) in both plants.

• Asian-Australasian Journal of Animal Sciences
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• v.33 no.1
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• pp.127-131
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• 2020

Objective: This study was conducted to determine catalytic properties of wheat phytase with exopolyphosphatase activity toward medium-chain and long-chain inorganic polyphosphate (polyP) substrates for comparative purpose. Methods: Exopolyphosphatase assay of wheat phytase toward polyP75 (medium-chain polyP with average 75 phosphate residues) and polyP1150 (long-chain polyP with average 1150 phosphate residues) was performed at pH 5.2 and pH 7.5. Its activity toward these substrates was investigated in the presence of Mg²⁺, Ni²⁺, Co²⁺, Mn²⁺, or ethylenediaminetetraacetic acid (EDTA). Michaelis constant (K_m) and maximum reaction velocity (V_max) were determined from Lineweaver-Burk plot with polyP75 or polyP1150. Monophosphate esterase activity toward p-nitrophenyl phosphate (pNPP) was assayed in the presence of polyP75 or polyP1150. Results: Wheat phytase dephosphorylated polyP75 and polyP1150 at pH 7.5 more effectively than that at pH 5.2. Its exopolyphosphatase activity toward polyP75 at pH 5.2 was 1.4-fold higher than that toward polyP1150 whereas its activity toward polyP75 at pH 7.5 was 1.4-fold lower than that toward polyP1150. Regarding enzyme kinetics, K_m for polyP75 was 1.4-fold lower than that for polyP1150 while V_max for polyP1150 was 2-fold higher than that for polyP75. The presence of Mg²⁺, Ni²⁺, Co²⁺, Mn²⁺, or EDTA (1 or 5 mM) exhibited no inhibitory effect on its activity toward polyP75. Its activity toward polyP1150 was inhibited by 1 mM of Ni²⁺ or Co²⁺ and 5 mM of Ni²⁺, Co²⁺, or Mg²⁺. Ni²⁺ inhibited its activity toward polyP1150 the most strongly among tested additives. Both polyP75 and polyP1150 inhibited the monophosphate esterase activity of wheat phytase toward pNPP in a dose-dependent manner. Conclusion: Wheat phytase with an unexpected exopolyphosphatase activity has potential as a therapeutic tool and a next-generational feed additive for controlling long-chain polyP-induced inappropriate inflammation from Campylobacter jejuni and Salmonella typhimurium infection in public health and animal husbandry.

• Microbiology and Biotechnology Letters
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• v.41 no.3
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• pp.335-340
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• 2013

The antimicrobial effect of the methanol extract of Inula britannica flowers against methicillin resistant Staphylococcus aureus (MRSA) was investigated. It was confirmed that the methanol extract is mainly composed of quercetin, which has antimicrobial properties. The antimicrobial effect of the methanol extract against 3 MRSA strains was determined by the disc diffusion method. The minimal inhibitory concentrations were ranged from 0.625 mg/ml to 1.25 mg/ml, and the minimum bactericidal concentrations were 2.5 mg/ml. Time kill kinetics revealed bactericidal activities, and the morphological alterations in S. aureus ATCC 33591 treated with the extract were observed using a scanning electron microscope. The methanol extract affected the expression of the resistant genes, mecA, mecI, and mecRI in mRNA. Therefore, the methanol extract of I. britannica flowers clearly demonstrated an antimicrobial effect against MRSA and these results suggest a potential for application as a natural antimicrobial agent.

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.718-723
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• 2002

CKD-602 (7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin) is a recently-developed synthetic camptothecin analogue and currently under clinical development by Chong Kun Dang Pharm (Seoul, Korea). CKD-602 showed potent topoisomerase inhibitory activity in vitro and broad antitumor activity against various human tumor cells in vitro and in vivo in animal models. This study describes the pharmacodynamics of the immediate and delayed cytotoxicity induced by CKD-602 in a human colorectal adenocarcinoma cell line, HT-29, and its intracellular drug accumulation by HPLC. The present study was designed to address whether the higher activity of CKD-602 with prolonged exposure is due to delayed exhibition of cytotoxicity and/or an accumulation of anti proliferative effect on continuous drug exposure. The drug uptake study was performed to determine whether the delayed cytotoxicity is due to a slow drug accumulation in cells. CKD-602 produced a cytotoxicity that was exhibited immediately after treatment (immediate effect) and after treatment had been terminated (delayed effect). Both the immediate and delayed effects of CKD-602 showed a time dependent decrease in 4IC_{50}$ values. Drug uptake was biphasic and the second equilibrium level was obtained as early as at 24hr, indicating that the cumulative and delayed antitumor effects of CKD-602 were not due to slow drug uptake. On the other hand, CKD-602 treatment was sufficient to induce delayed cytotoxicity after 4hr, however, longer treatment (＞24hr) enhanced its cytotoxicity due to the intracellular accumulation of the drug, which requires 24hr to reach maximum equilibrium concentration. In addition, $C^n$$\times$T=h analysis (n=0.481) indicated that increased exposure times may contribute more to the overall antitumor activity of CKD-602 than drug concentration. Additional studies to determine the details of the intracellular uptake kinetics (e.g., concentration dependency and retention studies) are needed in order to identify the optimal treatment schedules for the successful clinical development of CKD-602.

• Applied Biological Chemistry
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• v.47 no.4
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• pp.390-395
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• 2004

In order to characterize ion channels present in tomato roots, microsomes were incorporated into an artificial lipid bilayer arranged for electrophysiological analysis. Of the five different ion channels that could be found, a channel of 450 pS conductance was found most frequently. This channel displayed subconductance states of 450, 257 and 105 pS. All subconductance states showed linear current-voltage relationships. At positive holding potentials, high frequency of transient channel openings was observed; however, at negative potentials, the open times were long and open probability high. Po was 0.83 at -40 mV. When an additional 50 mM $K^+\;or\;Na^+$ was added to the cis side of bilayer, the reversal potentials shifted in the negative direction to near -10 mV. Thus, the 450 pS cation channel selects poorly between $K^+\;and\;Na^+$. In the presence of $100\;{\mu}M$ metal ions, the channel activity was severely inhibited by $La^{3+},\;Ba^{2+},\;and\;Zn^{2+}$, and Po was decreased to 0.2 or even less. However, $Al^{3+}\;and\;Cd^{2+}$ decreased the activity by only 20%. Interestingly, each metal ion showed different kinetics of channel inhibition. While $500\;{\mu}M\;La^{3+}$ inhibited the activities of all subconductance state, 1 mM $Zn^{2+}$ inhibited all except the 105 pS state. $Cd^{2+}$ changed the gating of the channel from a long-opening state to brief transient openings even at negative holding potentials. These data represent that the metal ions may have different binding sites on the channel protein and could be useful modulators and probes to investigate structural characteristics as well as the functional roles of the 450 pS channel on the root physiology.