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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Biomolecules & Therapeutics
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Journal DOI :
The Korean Society of Applied Pharmacology
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Volume & Issues
Volume 11, Issue 4 - Dec 2003
Volume 11, Issue 3 - Sep 2003
Volume 11, Issue 2 - Jun 2003
Volume 11, Issue 1 - Mar 2003
Selecting the target year
Induction of a systemic IgG and secretory IgA responses in mice by peroral immunization with uropathogenic Escherichia coli adhesin protein coupled to cholera toxin A2B subunits
Lee, Yong-Hwa ; Kim, Byung-Oh ; Rhee, Dong-Kwon ; Pyo, Suh-Kneung ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 157~162
The generation of secretory IgA antibodies(Abs) for specific immune protection of mucosal surfaces depends on stimulation of the mucosal immune system, but this is not effectively achieved by parenteral or even oral administration of most soluble antigens. Thus, to produce a possible vaccine antigen against urinary tract infections, the uropathogenic E. coli (UPEC) adhesin was genetically coupled to the ctxa2b gene and cloned into a pMAL-p2E expression vector. The chimeric construction of pMALfimHIctxa2b was then transformed into E. coli K-12 TB1 and its nucleotide sequence was verified. The chimeric protein was then purified by applying the affinity chromatography. The purified chimeric protein was confirmed by SDS-PAGE and western blotting using antibodies to the maltose binding protein (MBP) or the cholera toxin subunit B (CTXB), plus the N-terminal amino acid sequence was analyzed. The orderly-assembled chimeric protein was confirmed by a modified
-ganglioside ELISA using antibodies to adhesin. The results indicate that the purified chimeric protein was an Adhesin/CTXA2B protein containing UPEC adhesin and the
-ganglioside binding activity of CTXB. This study also demonstrate that peroral administration of this chimeric immunogen in mice elicited high level of secretory IgA and serum IgG Abs to the UPEC adhesin. The results suggest that the genetically linked CTXA2B acts as a useful mucosal adjuvant, and that the adhesin/CTXA2B chimeric protein might be a potential antigen for oral immunization against UPEC.
Pharmacokinetics of a New Antigastritic Agent, Eupatilin, an Active Component of StillenE
, in Rats
Jang, Ji-Myun ; Park, Kyung-Jin ; Kim, Dong-Goo ; Shim, Hyun-Joo ; Ahn, Byung-Ok ; Kim, Soon-Hoe ; Kim, Won-Bae ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 163~168
Pharmacokinetics of eupatilin (an active components of
, a new antigastritic agent) were investigated after both intravenous and oral administration at a dose of 30mg/kg to rats. After intravenous administration, the plasma concentrations of unchanged eupatilin declined rapidly with a mean terminal half-life of 0.101 h. Eupatilin was eliminated fast in rats; the total body clearance was 121 mL/min/kg. Eupatilin was mainly metabolized in rats; the percentage of intravenous dose of eupatilin excreted in 24 h urine and feces as unchanged eupatilin was only 2.5 and 0.919％, respectively. Eupatilin was mainly metabolized to form its glucuronide conjugate; after intravenous administration, 15.9 and 51.7％ of intravenous dose was excreted in 24 h urine and feces, respectively, as eupatilin plus its glucuronide. After oral administration, the absolute bioavailability was only 3.86％ based on
of eupatilin plus its glucuronide. Approximately 68.5％ of oral dose was not absorbed from the entire gastrointestinal tract. Therefore, it could be concluded that the superior effect of eupatilin in experimental animal models of gastric ulcer and inflammatory bowel disease after oral administration could be due to the local action of eupatilin. Further pharmacokinetic studies to elucidate the local action of eupatilin are required.
Inhibition of a Neutral Form of Sphingomyelinase by Alkylthioureido-l,3-propandiols, KY353X Series
Jung, Sang-Mi ; Jeong, Eui-Man ; Jo, Dong-Hwawn ; Chin, Mi-Reyoung ; Jun, Hyung-Jin ; Kim, Yong-Hyun ; Jeon, Hyung-Jun ; Lee, Dong-Hun ; Park, Mi-Ja ; Oh, Mi-Jung ; Yim, Chul-Bu ; Kim, Dae-Kyong ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 169~173
Alkylthioureido-1,3-propandiols (KY353X series) were synthesized and evaluated as inhibitors for neutral sphingomyelinase (N-SMase). To examine whether KY353X series inhibit N-SMase, we purified the N-SMase from bovine brain. The N-SMase was partially purified by sequential chromatographies of DEAE-Cellulose anionic exchange and phenyl-5PW hydrophobic HPLC. These seqeuntial procedures for N-SMase resulted in a 67-fold purification and excluded other isoforms of SMase. Based on in vitro assay, KY353X series inhibited N-SMase activity in time, concentration-dependent manners and completely inactivated N-SMase at 50
M. In particular, KY3535 and KY3536 inhibited more effectively than the others. To further determine the .inhibitory pattern, a Dixon plot was constructed, to showing that the inhibition by KY3535 and KY3536 were competitive. The inhibition constant (Ki) of KY3535 and KY3536 was 1.7
M and 2.5
M in 100 mM Tris-HCl buffer, pH 7.0, respectively.
Protection by Paeonol on Cytotoxicity of Cultured Rat Hepatocytes Exposed to Br-A23187
Bae, Ki-Hwan ; Kim, Young-Ho ; Oh, Ki-Wan ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 174~177
The present experiment was performed to investigate the protective effects of paeonol isolated from Moutan Cortex Radicis on primary cultured rat hepatocytes exposed to Br-A23187 (
ionophore). Br-A23187 is frequently used as a model of cell killing as inducing both necrotic and apoptotic cell death. Hepatocytes were isolated by collagenase perfusion from livers of fasted male Sprague Dawley rats and cultured overnight. Cell viability was determined by propidium iodide using fluorocytometry in Krebs-Ringer-HEPES buffer at pH 7.4. In addition, intracellular calcium was measured by excitation at 340 and 380 nm and emission at 505 nm using a luminescence spectrophotometer. Paeonol (20-100
) inhibited cell killing induced by 10
Br-A23187, in a dose-dependent manner. Paeonol also reduced increased intracellular calcium level when hepatocytes were exposed to Br-A23187. Therefore, the present results suggest that paeonol protects the hepatocytotoxicity induced by Br-A23187, via inhibiting the influx of calcium into into rat hepatocytes.
Optimal Sampling Times of Once Daily Gentamicin in Korean Patients with Urinary Tract Infections
Park, Hyo-Jung ; Sohn, Kie-Ho ; Choi, Kyung-Eob ; Shin, Sang-Yup ; Jung, Sook-In ; Oh, Won-Sup ; Peck, Kyong-Ran ; Song, Jae-Hoon ; Lee, Suk-Hyang ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 178~182
The clinical use of once daily aminoglycoside (ODA) dosing has been increased because of the potential therapeutic advantages of this dosing regimen. To evaluate the optimal sampling times of ODA dosing method in a clinical setting, the study was prospectively conducted in a total of 28 patients with UTI. All of the patients were intravenously administered gentamicin at a dose of 7 mg/kg over 60 minutes and randomly divided into two groups. Blood was collected at 0, 2, and 6 hours in Group A and at 1, 2, and 6 hours in Group B after the end of 1-hour infusion. The pharmacokinetic parameters (Ke, Vd and Cmax) obtained using the 0, 6 hour levels and 2, 6 hour levels in Group A were statistically different while those of 1, 6 hour levels and 2, 6 hour levels in Group B were similar. This finding indicated that the distributional phase of ODA is completed within 1 hour following the end of the I-hour infusion. If we are allowed to collect only two blood samples in ODA considering patients comfort and the analytical cost of drug, the first one should be drawn after 1 hour following the end of infusion to obtain adequate pharmacokinetic information.
General Pharmacology of IH-901
Lim, Wha-Kyung ; Sung, Jong Hwan ; Seong, Yeon Hee ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 183~189
General phannacological properties of IH-901, a new pharmacological composition as an intestinal metabolite formed from ginseng protopanaxadiol saponins, were investigated in experimental animals administered orally and in vitro test system. IH-901 had no effects on general behavior, pentobarbital sleeping time, spontaneous motor activity, motor coordination of mice, normal body temperature, chemoshock produced by pentylenetetrazole and writhing syndromes induced by 0.8％ acetic acid at the dose of 25 and 250 mg/kg. Gastric secretion of rats and intestinal motility in mice were not also influenced by the administration of IH-901 at doses of 25 and 250 mg/kg. IH-901 (25 and 250 mg/kg) did not change the mean arterial blood pressure and heart rate in conscious rats. IH-901 had no effect on the respiratory rate at the same doses when it was given to anesthetized rats. In in vitro experiments, IH-90l at the concentration of 25
/L did not show any direct effect and inhibitory or augmentative action on the histamine-or acetylcholine-induced contractions in the isolated ileum of guinea-pig. Based on these results, it was concluded that IH-901 did not induce any adverse effects in experimental animals.
Genotoxicity Study of AS6, a Triterpenoid Derivatives
Kwon, Jung ; Lee, Michael ; Cha, Kyung-Hoi ; Kim, Jong-Choon ; Han, Jung-Hee ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 190~195
To assess the genotoxicity of AS6, several classical toxicological tests were performed. In Ames test, AS6 did not show any transformation of revertant with or without S-9 metabolic activating system, indicating the lack of mutagenic effect of the compound. To assess clastogenic effect, in vivo micronucleus and in vitro chromosomal aberration assays were performed using male ICR mice and Chinese hamster lung (CHL) fibroblast cells, respectively. Chromosomal aberration was not induced regardless of the presence of S-9 metabolic activating system. In addition, AS6 did not cause any increase in the incidence of micronucleated polychromatic erythrocytes at any of the dose levels, suggesting little clastogenicity in vitro or in vivo. Taken together, these results demonstrate that AS-6 has no mutagenic effect in our test system.
Antioxidative Activities of 60 Plant Extracts
Heo, Chan ; Chung, Ji-Hun ; Jo, Byoung-Kee ; Kim, Hyun-Pyo ; Heo, Moon-Young ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 196~199
The methanol extracts from 60 plant extracts were prepared and evaluated for their antioxidative activity. Arctium lappa, Diospyros kaki, Eugenia caryophyllata, Melia azedarach and Forsythia suspensa showed the inhibitory activity against lipid peroxidation. Caesalpinia sappan, Crataegus pinnatifida, Eugenia caryophyllata, Gleditsia japonica, Osmunda japonica, Rhus javanica and Sanguisorba officinalis showed the highest inhibitory activity against DPPH radical formation. In particular, Eugenia caryophyllata demonstrated strong inhibitory activity on the lipid peroxidation and free radicals. The results suggested that selected plant extracts have a potential as natural antioxidant.
A Single Oral Dose Toxicity Study of Bamboo Leaf Water Extract in Sprague-Dawley Rats
Shin, Dong-Ho ; Jang, Pan-Gu ; Oh, Ki-Seok ; Kim, Jae-Ha ; Chung, Hee-Jong ; Kim, Jong-Choon ;
Biomolecules & Therapeutics, volume 11, issue 3, 2003, Pages 200~203
The present study was carried out to investigate the potential acute toxicity of bamboo leaf water extract by a single oral dose in Sprague-Dawley rats. Twenty male and female rats aged 5 weeks were randomly assigned to four groups of 5 rats each and were administered singly by gavage at dose levels of 0, 1250, 2500, or 5000 mg/kg body weight. Mortalities, clinical findings, and body weight changes were monitored for the l4-day period following the administration. At the end of 14-day observation period, all animals were sacrificed and complete gross postmortem examinations were performed. Throughout the study period, no treatment-related deaths were observed. There were no adverse effects on clinical signs, body weight, and gross finding at any dose tested. The results showed that the single oral administration of bamboo leaf water extract did not induce any toxic effect at a dose level of below 5000 mg/kg in rats and that the minimal lethal dose were considered to be over 5000 mg/kg body weight for both sexes.