• 약학회지
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• 제30권2호
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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 $CL_t$.

• 대한화학회지
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• 제41권12호
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• pp.672-676
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• 1997

쥐의 미크로좀 포스포리파제 D(PLD)를 센 이온세기 상태에서 0.2% taurodeoxycholate를 사용하여 용해시켰다. 포스포리파제 D의 활성은 기질로 방사성 동위원소로 표지 된 dipalmitoylphophatidylcholine을 사용하여 생성된 phosphatidic acid(PA)를 측정하여 결정하였다. 용해된 PLD의 초적 pH와 온도는 각각 6.5와 30$^{\circ}C$로서 용해되기 전 미크로좀 상태의 PLD와 비슷하였다. 올레산의 활성화 효과는 4 mM 농도에서 관찰되었다. PLD 활성도에 미치는 금속이온 영향을 조사한 결과 $Mg^{2+},\; Ca^{2+},\; Sr^{2+}, \;Ba^{2+}$와 같은 알칼리 토금속은 모두 PA 생성을 촉진시킨 반면, $Cu^{2+},\; Cd^{2+},\; Al^{3+},\; Ni^{2+},\; V^{5+}$는 억제하였다.

• Archives of Pharmacal Research
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• 제9권2호
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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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• 제9권1호
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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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• 제16권3호
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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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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• 제23권3호spc1호
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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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• 제10권2호
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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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• 제42권7호
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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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• 제15권3호
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• pp.197-206
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• 1997

목적 : Phospholipase D (PLD)는 phosphatidylcholine을 phosphatidic acid (PA)와 choline으로 가수분해 시키는 효소이다. 최근 이 효소는 다른 phospholipase들과 유사하게 세포 신호전달과정에 관여하는 것으로 알려져 많은 관심의 대상이 되고 있으며, 아울러 발암과정에 관여하리라는 추측을 하게 하고 있다. 이 실험에서는 쥐를 방사선 조사하여 각 조직에서 올레산-PLO에 미치는 영향을 관찰하였다. 방법 : PLD assay를 위한 반응 혼합물에는 $0.1\;\muCi$의 $1,2-di[1^{14}C]palmitoyl$ phosphatidylcholine, 0.5mM phosphatidylcholine, 5mM sodium oleate, $0.2\%$ taurodeoxycholate, 50mM HEPES buffer(pH 6.5), 10mM $CaCl_2$와 25mM KF 를 함께 넣어주었다. 생성된 PA는 TLC로 분리하여 그 방사능을 측정하였다. 사용된 동물은 암컷 Wistar 쥐로서 코발트 60 원격치료 기기를 이용, 조사범위를 $10cm\times10cm$로하여 분당 선량율 2.7Gy로 방사선 조사선랸 l0Gy와 25Gy를 조사 하였다. 결과 : PLD 활성은 폐조직에서 가장 높았으며 신장, 근육, 리, 비장, 골수, 흥선. 간의 순으로 나타났다. 방사선 조사결과 PLD 활성에 변동을 보인 조직은 흥선, 비장, 폐와 골수이며, 특히 흉선과 비장은 PLD의 할성이 각각 2배 이상 증가한 것으로 관찰되었다. 이와는 반대고 골수의 PLD는 $30\%$ 이상 감소한 것으로 나타났다. 한편 PLD 활성값이 가장 낮은 판은 방사선 영향을 거의 받지 않는 것처럼 보였다. 결론 : 동물전신에 방사선 조사시 PLD가 가장 민감한 영향을 받는 조직은 림프양 기관과 조혈 세포인 것으로 보여 PLD가 이들 조직의 생리기능과 밀접한 관계가 있음을 암시해 주고있다. 더 나아가 방사선 긴장 (radiation stress)이 이들 조직의 세포증식내지 괴사현상연구에 중요한 수단을 제공해 줄 수 있을 것이다.