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E J Kim

Publications and source records attributed to E J Kim.

At least 55 records · Page 3Linked to original sources
PubMed2001

Baryon rapidity loss in relativistic Au + Au collisions.

An excitation function of proton rapidity distributions for different centralities is reported from AGS Experiment E917 for Au+Au collisions at 6, 8, and 10.8 GeV/nucleon. The rapidity distributions from peripheral collisions have a valley at midrapidity which smoothly change to distributions that display a broad peak at midrapidity for central collisions. The mean rapidity loss increases with increasing beam energy, whereas the fraction of protons consistent with isotropic emission from a stationary source at midrapidity decreases with increasing beam energy. The data suggest that the stopping is substantially less than complete at these energies.

Journal Article↗
PubMed2001

Dose-dependent pharmacokinetics of a new reversible proton pump inhibitor, DBM-819, after intravenous and oral administration to rats: hepatic first-pass effect.

The dose-dependent pharmacokinetic parameters of DBM-819 were evaluated after intravenous (5, 10 and 20 mg/kg) and oral (10, 20 and 50 mg/kg) administrations of the drug to rats. The hepatic first-pass effect was also measured after intravenous and intraportal administrations of the drug, 10 mg/kg, to rats. After intravenous administration, the dose-normalized (based on 5 mg/kg) area under the plasma concentration-time curve from time zero to time infinity, AUC, at 20 mg/kg (27.0 and 45.8 microg min/ml) was significantly greater than that at 5 mg/kg due to saturable metabolism. After oral administration, the dose-normalized (based on 10 mg/kg) AUC(0-12 h) at 50 mg/kg (25.1, 18.3 and 49.2 microg min/ml) was significantly greater than those at 10 and 20 mg/kg again due to saturable metabolism. After oral administration of DBM-819, 10 mg/kg, 2.86% of oral dose was not absorbed and the extent of absolute oral bioavailability (F) was estimated to be 46.7%. After intraportal administration of DBM-819, 10 mg/kg, the AUC was 51.9% of intravenous administration, suggesting that approximately 48.1% was eliminated by liver (hepatic first-pass effect). The considerable hepatic first-pass effect of DBM-819 was also supported by significantly greater AUC of M3 (3.70 and 6.86 microg min/ml), a metabolite of DBM-819, after intraportal administration. The AUCs of DBM-819 were not significantly different (comparable) between intraportal and oral administrations of the drug, 10 mg/kg, suggesting that gastrointestinal first-pass effect of DBM-819 was almost negligible in rats. At 10 mg/kg oral dose of DBM-819, the hepatic first-pass effect was approximately 48.1%, F was approximately 46.7 and 2.86% was not absorbed from gastrointestinal tract in rats.

Administration, Oral↗
PubMed2001

Pharmacokinetics and pharmacodynamics of intravenous bumetanide in mutant Nagase analbuminemic rats: importance of globulin binding for the pharmacodynamic effects.

The importance of plasma protein binding of intravenous furosemide in circulating blood for its urinary excretion and hence its diuretic effects in mutant Nagase analbuminemic rats was reported. Based on the furosemide report, the diuretic effects of another loop diuretic, bumetanide, could be expected in analbuminemic rats if plasma protein binding of bumetanide is considerable in the rats. This was proved by this study. After intravenous administration of bumetanide, 10 mg/kg, to analbuminemic rats, the plasma protein binding of bumetanide was 36.8% in the rats mainly due to considerable binding to alpha- and beta-globulins (this value, 36.8%, was considerably greater than only 12% for furosemide), and hence the percentages of intravenous dose of bumetanide excreted in 6 h urine as unchanged drug was 16.0% in the rat (this value was considerably greater than only 7% for furosemide). After intravenous administration of bumetanide to analbuminemic rats, the area under the plasma concentration-time curve from time zero to time infinity (1012 compared with 2472 microg min/mL) was significantly smaller [due to significantly faster both renal clearance (1.49 compared with 0.275 ml/min/kg) and nonrenal clearance (8.30 compared with 3.71 ml/min/kg)], terminal half-life (9.94 compared with 22.4 min) and mean residence time (4.25 compared with 5.90 min) were significantly shorter (due to faster total body clearance, 9.88 compared with 4.05 ml/min/kg), and amount of 6 h urinary excretion of unchanged bumetanide (559 compared with 261 microg, due to increase in intrinsic renal excretion) was significantly greater than that in control rats. The 6 h urine output and 6 h urinary excretions of sodium, chloride and potassium were comparable between two groups of rats although the 6 h urinary excretion of bumetanide was significantly greater in analbuminemic rats. This could be explained by the following. The amount of urinary excretion of bumetanide was significantly greater in analbuminemic rats than that in control rats only between 0 and 30 min urine collection. In both groups of rats, the urinary excretion rates of bumetanide during 0-30 min reached a upper plateau with respect to urine flow rate as well urinary excretion rates of sodium, potassium and chloride, therefore, the diuretic effects (6 h urine output and 6 h urinary excretions of sodium, potassium and chloride) were not significantly different between two groups of rats.

Acetylglucosaminidase↗
PubMed2001

Inhibitory effect of glycolic acid on ultraviolet-induced skin tumorigenesis in SKH-1 hairless mice and its mechanism of action.

Glycolic acid, an alpha-hydroxy acid derived from fruit and milk sugars, has been used commonly as a cosmetic ingredient since it was discovered to have photoprotective and anti-inflammatory effects and antioxidant effects on ultraviolet (UV)B-irradiated skin. Little is known, however, about the functional role of glycolic acid on UV-induced skin tumorigenesis. In the present study, we examined the effect of glycolic acid on UV (UVA + UVB)-induced skin tumorigenesis and assessed several significant contributing factors in SKH-1 hairless mice. Inbred hairless female mice (15 animals/group) were irradiated for 5 d/wk at a total dose of 74.85 J/cm(2) UVA and 2.44 J/cm(2) UVB for 22 wk. Glycolic acid was applied topically twice a week at a dose of 8 mg/cm(2) immediately after UV irradiation. Glycolic acid reduced UV-induced skin tumor development. The protective effect of glycolic acid was a 20% reduction of skin tumor incidence, a 55% reduction of tumor multiplicity (average number of tumors/mouse), and a 47% decrease in the number of large tumors (larger than 2 mm). Glycolic acid also delayed the first appearance of tumor formation by about 3 wk. The inhibitory effect of glycolic acid on UV-induced tumor development was accompanied by decreased expression of the following UV-induced cell-cycle regulatory proteins: proliferating cell nuclear antigen (PCNA), cyclin D1, cyclin E, and the associated subunits cyclin-dependent kinase 2 (cdk2) and cdk4. In addition, the expression of p38 kinase, jun N-terminal kinase (JNK), and mitogen-activated protein kinase kinase (MEK) also was lower in UV + glycolic acid-treated skin compared with expression in UV-irradiated skin. Moreover, transcription factors activator protein 1 (AP-1) and nuclear factor kappaB (NF-kappaB) activation was significantly lower in UV + glycolic acid-treated skin compared with activation in UV-irradiated skin. These results show that glycolic acid reduced UV-induced skin tumor development. The decreased expression of the cell-cycle regulatory proteins PCNA, cyclin D1, cyclin E, cdk2, and cdk4 and the signal mediators JNK, p38 kinase, and MEK may play a significant role in the inhibitory effect of glycolic acid on UV-induced skin tumor development. In addition, the inhibition of activation of transcription factors AP-1 and NF-kappaB could contribute significantly to the inhibitory effect of glycolic acid.

Animals↗
PubMed2001

Polymeric microspheres composed of pH/temperature-sensitive polymer complex.

A new pH/temperature-sensitive polymer system with transitions resulting both from polymer-water and polymer-polymer interactions has been demonstrated using the mixture of poly(N,N-dimethylamino)ethyl methacrylate (DMAEMA) and polyethyl acrylamide (EAAm). Based on the pH/temperature sensitivity of polymer mixture, the microsphere for pH/temperature-sensitive drug release have been designed and characterized. Hydrocortisone was used as a model drug. This gave the control of hydrocortisone release in an on-off manner without considerable lag time.

Biocompatible Materials↗
PubMed2001

General pharmacology of IY-81149, a new proton pump inhibitor.

IY-81149 (2-[(4-methoxy-3-methyl)-2-pyridinyl]methylsulfinyl -5-(1H-pyrrol-1-yl)-1H-benzimidazole, CAS 172152-36-2) is a new proton pump inhibitor and expected to be an antiulcer drug. Its general pharmacological effects were studied in this paper. The doses given were vehicle control, 0.3, 1, 3, 100, 300 and 1000 mg/kg and were administered orally. The animals used in this study were mouse, rat, guinea pig and beagle dog. IY-81149 decreased spontaneous locomotor activity at 1000 mg/kg and showed a weak effect in motor performance at 300 and 1000 mg/kg. IY-81149 prolonged the hexobarbital-induced sleeping time dose dependently at 100, 300 and 1000 mg/kg. Oral administration of IY-81149 caused a dose-dependent hypothermic effect up to 300 mg/kg and showed analgesic effect at 1000 mg/kg. IY-81149 produced an antisecretory effect in pylorus ligated rats. The total gastric volume and acidity were significantly decreased at doses ranging from 1 to 3 mg/kg. However, IY-81149 had no effects on general behavior, did not show anticonvulsant activity, and did not affect blood pressure and heart rate, LVP (left ventricular peak systolic pressure), LVEDP (left ventricular end diastolic pressure), LVDP (left ventricular developing pressure), DP (double product), HR (heart rate), CFR (coronary flow rate), smooth muscle contraction, respiration, intestinal transport and renal function. These findings demonstrate that IY-81149 possesses weak central nervous system action and inhibitory effects on microsomal enzymes and gastric secretion after single administration. The results suggest that IY-81149 does not exert any notable pharmacological effects on the cardiovascular system, autonomic nerve system or smooth muscle function at all doses tested.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2001

Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo.

The inhibitory effects of IY-81149 (2-[[(4-methoxy-3-methyl)-2- pyridinyl]methyl-sulfinyl]-5-(1H-pyrol-1-yl)-1H-benzimidazole, CAS 172152-36-2), a newly developed proton pump inhibitor (PPI) on gastric acid secretion were investigated in vitro and in vivo. In rabbit parietal cell preparation, IY-81149 irreversibly inhibited H+/K(+)-ATPase in dose-dependent manner with an IC50 of pump inhibitory activity of 6.0 x 10(-6) mol/l and that of omeprazole (CAS 73590-58-6) was 1 x 10(-4) mol/l at pH 7.4. On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of IY-81149 was 9.0 x 10(-9) mol/l and that of omeprazole was 1.9 x 10(-8) mol/l. The inhibition rates of IY-81149 and omeprazole at a concentration of 1 x 10(-9) mol/l in human parietal cells were 137% and 64%, respectively. In pylorus-ligated rats, IY-81149 showed a 2-3 times stronger inhibitory activity than omeprazole against gastric acid secretion. The ED50 of IY-81149 and omeprazole administered intraduodenally was 1.6 mg/kg and 3.8 mg/kg. In the case of oral administration, the ED50 of IY-81149 and omeprazole was 1.94 mg/kg and 5.64 mg/kg, respectively. But after 24 h administration, the anti-secretory activity of IY-81149 was lower than that of omeprazole at all doses tested. In anesthetized rats, IY-81149 dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED50 of IY-81149 and omeprazole was 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED50 of IY-81149 and omeprazole was 3.9 and 4.1 mg/kg, respectively. IY-81149 also significantly inhibited pentagastrin-stimulated gastric secretion. Its ED50 was 2.1 mg/kg and that of omeprazole was 3.5 mg/kg with i.d. administration. In the case of i.v. injection, IY-81149 was equipotent to omeprazole. IY-81149 also inhibited gastric acid secretion strongly in fistular rats. The ED50 of IY-81149 administered intraduodenally was 0.43 mg/kg and that of omeprazole was 0.68 mg/kg. In Heidenhain pouch dogs, the acid output was completely blocked at 0.3 mg/kg, 135 min after i.v. administration. Omeprazole showed a similar effect as IY-81149. The histamine induced increase of acid output in the Heidenhain pouch dog was blocked by 71% 150 min after oral administration of enteric-coated IY-81149 at a dose of 3 mg/kg, and omeprazole showed similar effects. In conclusion, IY-81149 revealed the characteristics as a strong proton pump inhibitor, and its potency against gastric acid secretion was superior to that of the reference drug, omeprazole.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2001

Endoscopic factors predisposing to rebleeding following endoscopic hemostasis in bleeding peptic ulcers.

BACKGROUND AND STUDY AIMS: Various clinical and endoscopic factors have been proposed and used as predictors of endoscopic treatment failure in bleeding peptic ulcers. Recently, several endoscopic factors have been considered to be more significant than various clinical factors, except for shock. Detailed knowledge of which endoscopic factors can be classified as predictors of rebleeding following endoscopic hemostasis is needed. This study describes newly defined endoscopic variables and evaluates their usefulness as predictors of endoscopic treatment failure. PATIENTS AND METHODS: Between January 1996 and April 1999, diagnostic and therapeutic endoscopies were carried out in 143 patients with active bleeding peptic ulcers. Nine clinical and eight endoscopic variables were studied. Endoscopic factors were classified by three types of stigmata bleeding, 14 locations, two ulcer sizes, three ulcer bases, three visible vessel colors, two ulcer depths, two margin shapes, and three endoscopic treatment methods (injection, hemoclipping, and combination). RESULTS: 36 patients experienced rebleeding (25.2 %), 11 patients needed operations (7.7 %) and five deaths occurred (3.5 %). In univariate analysis, rebleeding was significantly related to: i) presence of spurting activity (odds ratio [OR] = 4.91, P = 0.006), ii) ulcer size larger than 2 cm (OR = 2.78, P = 0.017); and iii) location in stomach (OR = 2.81, P = 0.026). Clinical variables including age, shock, and initial hemoglobin levels were not significantly related to rebleeding. In multiple logistic regression using selected significant variables, presence of spurting activity remained a significant independent predictor of rebleeding (adjusted OR = 6.48, P = 0.003). CONCLUSION: Our data support the hypothesis that endoscopic factors are more important than clinical ones when predicting rebleeding of peptic ulcers. Based on statistical analysis of risk factors, the ulcers most likely to rebleed after endoscopic therapy are those which are located in the stomach, are greater than 2 cm in diameter and exhibit oozing or spurting of blood.

Adolescent↗
PubMed2001

Angiogenesis by endothelial cell transplantation.

PURPOSE: Myocardial angiogenesis may improve regional perfusion and perhaps function after cardiac injury. We evaluated the effect of endothelial cell transplantation into a myocardial scar on angiogenesis and ventricular function, as an alternative to angiogenic gene or protein therapy. METHODS AND RESULTS: A transmural myocardial scar was created in the left ventricular free wall of rat hearts by cryoinjury. Allogeneic aortic endothelial cells were injected into the scar 2 weeks after cryoinjury. A cluster of transplanted cells was identified at the site of injection 1 day and 1 week after transplantation, but not after 2 weeks. The size of this cluster of transplanted cells decreased as vascular density in the transplanted scar tissue increased with time. Six weeks after transplantation, vascular density was significantly greater in transplanted hearts than in control hearts. Regional blood flow, by microsphere analysis, was greater in the transplanted rats. Systolic and diastolic ventricular function was similar between groups. In a second series of experiments, syngeneic aortic endothelial cells labeled with bromodeoxyuridine were transplanted 2 weeks after cryoinjury. Vascular density in the transplanted scar was greater than in controls. Labeled transplanted endothelial cells were identified forming part of the newly developed blood vessels. No difference in vascular density was found between allogeneic and syngeneic cell transplantation. Vascular endothelial growth factor was not expressed at greater levels in the transplanted cells or the myocardial scar. CONCLUSION: Transplanted endothelial cells stimulated angiogenesis, were incorporated into the new vessels, and increased regional perfusion in myocardial scar tissue, but did not improve global function in this cryoinjury rat model.

Animals↗
PubMed2001

Interferon-alpha treatment of chronic hepatitis C in children with hemophilia.

BACKGROUND: In children with hemophilia, hepatitis C virus (HCV) is the major cause of chronic liver disease. In this study, long-term efficacy of interferon-alpha was studied to determine the factors that predict a sustained response to interferon therapy in young children with hemophilia who have chronic hepatitis C. METHODS: Seventeen Korean children with hemophilia and chronic hepatitis C were treated with 3.7 million units/m2 of interferon-alpha2a three times weekly for 6 months. Liver biopsy, pretreatment serum HCV RNA quantitation with competitive reverse transcription assay, and HCV genotyping with reverse hybridization assay were performed. RESULTS: Hepatitis C virus genotypes 1a, 1b, and 2a were found in three (18%), five (29%), and six (35%) patients, respectively. Interferon-alpha was well tolerated, and the frequency of bleeding did not increase. Of the 17 patients, 7 (41%) had a sustained response for 3 years after the end of therapy. Patients with a sustained response had lower pretreatment serum HCV RNA levels. One (13%) of eight patients with genotype 1 and five (83%) of six with genotype 2 had a sustained response (P < 0.05). CONCLUSIONS: Interferon-alpha treatment of chronic hepatitis C in children with hemophilia was safe and effective in producing sustained responses. The pretreatment serum HCV RNA level and viral genotype may be predictive factors for sustained response to interferon therapy.

Adolescent↗
PubMed2001

Crystallization and preliminary X-ray diffraction studies of the guanylate kinase-like domain of PSD-95 protein from rat.

The PSD-95 (postsynaptic density-95) protein, one of the members of the MAGUK (membrane-associated guanylate kinase) family, is composed of three PDZ domains, one SH3 domain and one guanylate kinase-like (GK) domain. The GK domain mediates the scaffolding function of PSD-95 by protein--protein interaction. Here, the GK domain was subcloned, expressed as an intein fusion protein, purified without the intein and then crystallized at room temperature by the hanging-drop vapour-diffusion method using PEG 8000 as a precipitant. The complete native data set was collected to a resolution of 2.35 A using flash-cooling. The crystals belong to the primitive tetragonal space group P4(3) (or P4(1)), with unit-cell parameters a = b = 70.03 (4), c = 37.64 (1) A.

Animals↗
PubMed2001

Diffusion-weighted image and MR spectroscopic analysis of a case of MELAS with repeated attacks.

We report the clinical and MR manifestations of an 18 year-old girl with mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS) syndrome. Recurrent status epilepticus caused reversible cytotoxic edema on diffusion-weighted images (DWI). Initial and one month follow-up MR spectroscopy, after seizure control, showed some discrepancies in the ratio of metabolites. N-acetylaspartate (NAA) partially recovered (NAA/creatine (Cr) ratio: 1.27-->1.84). This was because of a normalization of decreased NAA due to cellular dysfunction as a result of status epilepticus. A low ratio of NAA/Cr due to abnormal mitochondria remained in the decreased state. Reversible NAA/Cr ratios in the acute lesion suggested that NAA reflects the neuronal function as well as the level of neuronal structural damage. The altered NAA/Cr ratio better correlated with the abnormal signal intensity area of T2-weighted images (T2WI) and DWI than the lactate (Lac)/Cr ratio. With conservative treatment with anti-epileptics not accompanied by coenzyme Q or sodium dichloroacetate, lactate persistently increased (Lac/Cr ratio: 1.01-->1.21) because of the continued production of lactate in cells with respiratory deficiency, which is the main pathology of MELAS.

Adolescent↗
PubMed2001

What is the best method to diagnose Helicobacter infection in bleeding peptic ulcers?: a prospective trial.

BACKGROUND: It has been debated which diagnostic test should be preferred for the diagnosis of Helicobacter pylori (HP) in patients with peptic ulcer diseases. Several limitations are reported in bleeding peptic ulcers because of intragastric blood and possibility of changed numbers of organisms by medication. This study was designed to find out the best method for diagnosis of HP infection, in aspect of deciding the times of detection and the specific tests in bleeding peptic ulcers. METHODS: We prospectively examined histology, rapid urease test (CLO test), urea breath test (13C-UBT) and serology in HP diagnostics in 32 patients with bleeding peptic ulcers to detect HP infection. Each test was performed two times (four methods at first 24 hours and former three methods at 7th day after initial therapeutic endoscopy). We evaluated the sensitivity of each test, compared the two-times results and evaluated the effect of these tests to an outcome of endoscopic hemostasis. RESULTS: Diagnostic sensitivities of histology, CLO test, 13C-UBT and serology are 75%, 67.8%, 100% and 100% at first endoscopy, and 71.4%, 78.5%, 89.3% at 7th day endoscopy, respectively. Histologic study and CLO test had diagnostic limitation at emergent first endoscopy contrary to UBT (p < 0.01). Histologic study, CLO test and UBT have limitations at 7th day endoscopy. Only 3 patients (9.4%) rebled with subsequent complete endoscopic hemostasis and all diagnostic tests at initial endoscopy did not influence the outcome of hemostasis. CONCLUSION: First day histologic and CLO tests are inadequate methods in detecting HP infection in patients with bleeding peptic ulcers. 7-day histologic, CLO test and UBT have a low sensitivity. First-day UBT can be a standard test to diagnose HP infection in patients with bleeding peptic ulcers.

Biopsy, Needle↗
PubMed2001

A case of mediastinal angiomyolipoma.

Angiomyolipoma is a common tumor of the kidney but has rarely been found in the mediastinum. We report a case of angiomyolipoma of the posterior mediastinum in a 62-year-old woman. She experienced exertional dyspnea and intermittent cough at admission. Computed tomography indicated a tumor located at the left paravertebral and upper posterior mediastinum and MRI imaging demonstrated a mass with low signal intensity in T1-weighted image at T4-5 level. Thoracotomy was done for surgical removal of the tumor and histologic examination revealed a mesenchymal tumor composed of mature fat, capillaries and smooth muscle fibers. The tumor was immunohistochemically positive for CD34 and factor-VIII (for vascular component) smooth muscle actin (for smooth muscle component) and S-100 protein (for fat component). There have been four case reports about mediastinal angiomyolipoma, namely three Japanese cases and one French case. It is suggested that angiomyolipoma could be considered for the differential diagnosis of mediastinal tumors.

Angiomyolipoma↗
PubMed2001

Short report: genetic heterogeneity of Japanese encephalitis virus assessed via analysis of the full-length genome sequence of a Korean isolate.

We determined the full-length genome sequence of Japanese encephalitis virus (JEV) K94P05 isolated in Korea. Sequence analysis showed that the 10,963-nucleotide-long RNA genome of K94P05 was 13 or 14 nucleotides shorter than the genome of other JEV isolates because of a deletion in the 3' noncoding region of K94P05. Compared with sequences of other JEV isolates, the full-length nucleotide sequence showed 89.0-89.6% homology, and the deduced amino acid sequence showed between 96.4-97.3% homology. A region of approximately 60 nucleotides immediately downstream of the open reading frame stop codon of K94P05 showed high sequence variability as compared with other JEV isolates. K94P05 formed a distinct group within a phylogenetic tree established with the full-length genome sequences. Cross-neutralization studies showed that polyclonal antibodies to Korean isolates were 3 times better at neutralizing the Korean isolates than antibodies to Nakayama-NIH. These findings suggest that Korean JEV K94P05 is genetically and antigenically distinct from other Asian JEV isolates.

Amino Acid Sequence↗
PubMed2001

Failure of Bcl-2 to block mitochondrial dysfunction during TRAIL-induced apoptosis. Tumor necrosis-related apoptosis-inducing ligand.

Tumor necrosis (TNF)-related apoptosis-inducing ligand (TRAIL) is a member of the TNF family of cytokines that promotes apoptosis. TRAIL induces apoptosis in a wide variety of tumor cells but not in normal cells. Oncogene Bcl-2 can protect cells from apoptosis induced by various stress stimuli. However, it is not clear whether Bcl-2 can regulate TRAIL-induced apoptosis. The objective of this study was to investigate whether Bcl-2 can regulate apoptosis induced by TRAIL. TRAIL initiates the activation of caspases, the loss of mitochondrial transmembrane potential (Delta psi(m)), and the redistribution of mitochondrial cytochrome c. TRAIL has no effect on Delta psi(m) and apoptosis in Jurkat cells deficient in either FADD or caspase-8, suggesting both FADD and caspase-8 are required for TRAIL signaling. Overexpression of Bcl-2 delays, but does not inhibit, TRAIL-induced Delta psi(m), cytochrome c release from mitochondria and apoptosis, whereas etoposide-induced apoptosis is blocked by Bcl-2. XIAP, cowpox virus CrmA and baculovirus p35 inhibits TRAIL-induced apoptosis. These data suggest that TRAIL can be used to kill Bcl-2 positive cells that can not be killed by other class of chemotherapeutic drugs.

Apoptosis↗
PubMed2001

Stability, blood partition and protein binding of an antifibrotic agent, oltipraz.

The stability, blood partition and factors influencing the binding of oltipraz to 4% human serum albumin (HSA) were evaluated. Oltipraz was relatively stable in various pH (1-12) solutions for up to 48-h incubation, however, it was unstable in pH 13 solution and rat plasma and urine. Oltipraz reached an equilibrium fast (within 30 s mixing manually) between plasma and blood cells o f rabbit blood and the plasma-to-blood cells concentration ratios were independent of initial blood concentrations of oltipraz, 1 and 5 microg/ml; the ratios ranged from 0.908 to 1.004. The binding of oltipraz to 4% HSA was independent of oltipraz concentrations ranging from 1 to 100 microg/ml using an equilibrium dialysis technique: the mean value was 95.0%. However, the binding of oltipraz was dependent on HSA concentrations (the low concentrations, 3, 2, 1 and 0.5% of HSA caused an increase in the unbound fraction of oltipraz by 1.32, 1.98, 3.44 and 5.31 times, respectively, compared with the mean value from 4-6% HSA), incubation temperature (the unbound fractions at 37 degrees C and 22 degrees C increased 1.89 and 1.73 times, respectively, than that at 4 degrees C) and the buffer pHs (the unbound fractions were 6.36, 6.51, 5.60 and 4.63% for buffer pHs of 5.8, 6.4, 7.4 and 8.0, respectively).

Animals↗