• YAKHAK HOEJI
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• v.30 no.2
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• pp.68-72
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• 1986

Effect of sodium taurodeoxycholate (TDC) on the pharmacokinetics of methylene blue (MB) was investigated in the rats of experimental hepatic failure induced by $CCI_4$. Intravenous infusion of TDC increased the distribution volume of central compartment ($Vd_1$) and the total body clearance ($CL_t$) of MB. Increased lipophilicity through ion-pair formation with TDC seemed to be the probable cause of increased $Vd_1$ and $CL_t$.

• Journal of the Korean Chemical Society
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• v.41 no.12
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• pp.672-676
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• 1997

Microsomal phospholipase D (PLD) in rat brain was solubilized employing 0.2 % taurodeoxycholate in high ionic strength. Phopholipase D activity was determined by measuring product phophatidic acid (PA) using isotope-labelled dipalmitoylphophatidylcholine as a substrate. The solubilized PLD showed an optimal pH of 6.5 and the highest activity at 30$^{\circ}C.$ These properties were similar to those of microsomal PLD before solubilization. The stimulatory effect of oleic acid was observed at the concentration of 4 mM. When effects of metal ions on PLD activity were examined, alkaline earth metals such as $Mg^{2+},\; Ca^{2+},\; Sr^{2+}, \;Ba^{2+}$ promoted the PA production but $Cu^{2+},\; Cd^{2+},\; Al^{3+},\; Ni^{2+},\; V^{5+}$ showed inhibitory effects.

• Archives of Pharmacal Research
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• v.9 no.2
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• pp.111-114
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• 1986

Bretylium tosylate is a quaternary ammonium compound used for the treatment of ventricular fibrilation in humans. It is advantageous to other cationic compound in the study of biliary excretion in that negligible amount is bound to plasma protein and metabolite is not likely is to be formed. Some researchers reported that the formation of ion-pair complex caused to increase the lipothilicity of cationic compound. The partition of bretylium between water and organic phase was increased with the addition of sodium taurodeoxycholate. Also sensitive gas chromatographical assay procedure using flame ionization detector was studied. This procedure can detect as low as 0.1 mg/ml using 0.1 ml biological sample, but contamination by previous injection is the major problem of this method.

• Archives of Pharmacal Research
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• v.9 no.1
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• pp.49-54
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• 1986

Effect of sodium taurodeoxycholate (TDC) infused intravenously on the pharmacokinetics of methylene blue (MB) was studied in the rat to investigate the role of ion-pair complexation in the body on drug elimination and disposition. Distribution volume (Vd) of MB was increased significantly (p< 0.05) by TDC infusion. Considering together with the fact that apparent partition coefficient (APC) of MB between phosphate buffer (pH 7.4) and n-octanol was increased markedly by TDC, the increase in Vd seemed to be the result of decreased polarity of MB by ion-pair formation with TDC. But total body clearance (CLt) and biliary excretion clearance (CLbil) of MB were not increased significantly by TDC.

• Journal of Pharmaceutical Investigation
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• v.16 no.3
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• pp.110-117
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• 1986

Plasma disappearance of amaranth (AM), a model compound of organic anionic drugs, was retarded by intravenous infusion of taurodeoxycholate (TDC), a representative bile acid, in the rat. Biliary excretion accounted for 30-60% of the systemic excretion of AM. AM seemed to be metabolised in the hepatocyte to form a compound that is excreted more rapidly into the bile than AM itself, considering apparent biliary clearance, $CL_{bil}$, is much larger than systemic clearance, $CL_s$. Decrease in $CL_{bil}$ by TDC infusion might be due to elevated plasma level rather than decreased biliary excretion of AM. Decreased distribution or urinary excretion of AM by TDC was supposed to be one of the probable reasons of elevated plasma level. Competitive inhibition between AM and TDC on tissue distribution and urinary excretion might explain the mechanism. The effect of TDC on the $CL_{bil}$ of methylene blue, a cationic dye, was quite different from that of AM, as reported previously by us. More intensive study would be necessary to elucidate the difference of biliary excretion between organic anions and cations.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.179-179
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• 1993

1. PS및 CP의 flux는 전류의 새기 및 donor의 약물농도에 비래하였다. 2. pH의 flux는 pH가 증가할수록 증가하였으나, CP(pKa=9.2)의 flux는 pH=2에서 최대치를 보였다. 이는 약물의 해리 정도와 H$^{＋}$이온의 mobility, 또 피부의 permselectivity의 balance에 의해 결정된 것으로 생각된다. 3. donor cell에 NaCl을 첨가하면 두 약물 공히, 그러나 특히 PS의 flux가 저하되었다. 이는 두 약물의 이온과 $Na^{＋}$의 mobility차이에 기인한다고 생각된다. 4. PS의 경우 taurodeoxycholate(TDC)같은 음이온을 donor cell에 공존시키면 flux가 감소하였다. 이는 PS와 TDC가 전기적으로 중성인 ion-pair complex를 형성함으로써 PS이온의 유효농도가 감소하기 때문으로 생각된다.

• Journal of Pharmaceutical Investigation
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• v.23 no.3
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• pp.41-50
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• 1993

The iontophoretic delivery across rat skin of quaternary ammonium salts (isopropamide: ISP, pyridostigmine: PS), which are positively charged over a wide pH range, was measured ill vitro. The study showed that: (a) iontophoresis significantly enhanced delivery of ISP and PS compared to respective passive transport; (b) delivery of ISP and PS was directly proportional to the applied continuous direct current density over the range of $0-0.69\;mA/cm^2;$ (c) delivery of ISP and PS was also proportional to the drug concentration in the donor compartment over the range of $0-2{\time}l0^{-2}M:$ (d) sodium ion in the donor compartment inhibited the drug transport possibly due to decreasing the electric transference number of the drug; (e) delivery of ISP and PS increased as the pH of the donor solution increased over the pH range 2-7 suggesting permselective nature of the epidermis, and inhibition of the transference number of the drugs by hydronium ion; (f) some organic anions such as taurodeoxycholate, salicylate and benzoate which form lipophilic ion-pair complexes with ISP inhibited the delivery of ISP. The degree of inhibition by the organic anions was linearly proportional to the extraction coefficient $(K_e)$ of ISP from the partition system with each counteranion between phosphate buffer (pH 7.4) and n-octanol. For PS, however, taurodeoxycholate, but not salicylate and benzoate inhibited the iontophoretic delivery. It suggests that not only sodium ion and hydronium ion but also the counteranions which form lipophilic ion-pairs with quaternary ammonium drugs are not favorable components in formulating the donor solution of the drugs to achieve an effective iontophoretic delivery.

• Journal of Ginseng Research
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• v.10 no.2
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• pp.209-217
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• 1986

Yeast alcohol dehydrogenates and ginseng saponin interaction has been investigated to understand the non-specific enzyme stimulating effect of the saponin of Panax ginseng C.A. Meyer. It was confirmed that several amphiphiles such as sodium dodecyl sulfate(SDS), Triton X-100, sodium taurodeoxycholate (Na-TDC) as well as ginseng saponin mixture and purified ginseng glycosides lowered Km values of yeast alcohol dehydrogenase (ADH) for ethanol and NAD in the presence of the above amphiphiles suggesting that the surface activity of the amphiphiles might play a significant role in the ADH catalyzed reactions. Conformational change of yeast alcohol dehydrogenase in the presence of the above amphiphiles at their optimal concentration for the maximum activity was studied. Circular dichroism (C.D) spectrum of yeast ADH showed that the conformational change of the enzyme occurred in the presence of above amphiphiles. Fluorescence data also showed that the hydrophobic area increased in the presence of above amphiphiles. Examination of the interaction between ADH and ginseng saponin using radioactive saponin showed that there might be a very weak interaction between them. From the above results, it was concluded that the non-specific enzyme stimulating effect of the saponin might be due to the change of polarity of the enzyme solution in the presence of the saponin.

• BMB Reports
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• v.42 no.7
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• pp.462-466
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• 2009

Lipopolysaccharide (LPS), found in the outer membrane of Gram negative bacteria, only exerts its toxic effects when in free form. LPS has three major parts, lipid A, the toxic component, along with a core polysaccharide and O-specific polysaccharide. LPS monomers are known to have molecular masses between 10 to 30 kDa. Under physiological conditions, LPS exists in equilibrium between monomer and vesicle forms. LPS removal by 100 kDa ultrafiltration was more efficient (99.6% of LPS removed) with a low concentration of protein (2.0 mg/ml) compared to a high concentration (20.1 mg/ml). In the presence of different detergents (0.5% Tween 20, 1.0% taurodeoxycholate and 1.0% Triton X-100), LPS removal was more efficient at low protein concentrations (2.0 mg/ml) compared to high protein concentrations (20.1 mg/ml).

• Radiation Oncology Journal
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• v.15 no.3
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• pp.197-206
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• 1997

Purpose : Phospholipase D (PLD) catalyzes the hydrolysis of phosphatidylcholine to phosphatidic acid (PA) and choline. Recently, PLD has been drawing much attentions and considered to be associated with cancer Process since it is involved in cellular signal transduction. In this experiment, oleate-PLD activities were measured in various tissues of the living rats after whole body irradiation. Materials and Methods : The reaction mixture for the PLD assay contained $0.1\;\muCi\;1,2-di[1-^{14}C]palmitoyl$ phosphatidylcholine 0.5mM phosphatidylcholine, 5mM sodium oleate, $0.2\%$ taurodeoxycholate, 50mM HEPES buffer(pH 6.5), 10mM $CaCl_2$, and 25mM KF. phosphatidic acid, the reaction product, was separated by TLC and its radioactivity was measured with a scintillation counter. The whole body irradiation was given to the female Wistar rats via Cobalt 60 Teletherapy with field size of 10cmx loom and an exposure of 2.7Gy per minute to the total doses of 10Gy and 25Gy. Results : Among the tissues examined, PLD activity in lung was the highest one and was followed by kidney, skeletal muscle, brain, spleen, bone marrow, thymus, and liver. Upon irradiation, alteration of PLD activity was observed in thymus, spleen, lung, and bone marrow. Especially PLD activities of the spleen and thymus revealed the highest sensitivity toward $\gamma-rar$ with more than two times amplification in their activities In contrast, the PLD activity of bone marrow appears to be reduced to nearly $30\%$. Irradiation effect was hardly detected in liver which showed the lowest PLD activity. Conclusion : The PLD activities affected most sensitively by the whole-body irradiation seem to be associated with organs involved in immunity and hematopoiesis. This observation s1ron91y indicates that the PLD is closely related to the physiological function of these organs, Furthermore, radiation stress could offer an important means to explore the phenomena covering from cell Proliferation to cell death on these organs.