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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Biomolecules and Therapeutics
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Journal DOI :
The Korean Society of Applied Pharmacology
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Volume & Issues
Volume 3, Issue 4 - Dec 1995
Volume 3, Issue 3 - Sep 1995
Volume 3, Issue 2 - Jun 1995
Volume 3, Issue 1 - Mar 1995
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Effects of Panax ginseng on Morphine-induced Immune Suppression
Lee, Shee-Yong ; Kim, Ae-Young ; Kim, Young-Ran ; Kim, Kyeong-Man ;
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 177~181
To investigate the possibility of Panax ginseng as a therapeutic agent for the immune suppression, ginseng total saponin (GTS) extracted from korean red ginseng was tested on immune functions from morphine-induced immune suppressed mice. To study how immune functions are affected by morphine and also to test whether GTS can be an useful therapeutic agent for morphine toxicity, several parameters were employed, body weight, immune organ weight, B cell functions, and T cell function. Morphine impaired the development of body weight and immune organ weight such as spleen and thymus. Morphine also depressed a B-cell function, antibody production. T-cell functions studied by type IV hypersensitivity test were most markedly affected by morphine treatment. GTS restored most of morphine-induced immune suppression. GTS restored the morphine-induced decrease in spleen weight to body weight ratio in a dose dependent manner, but not the body weight decrease. Also all of the morphine-induced impairments of B cell functions and cellmediated immunity were fully recovered by GTS. These results suggest that ginseng product could be very helpful for the treatment of immune suppression occurring in morphine abusers.
The Evaluation of Genotoxicities of Antifungal 6-[(N-Halophenyl)amino]-7- Chlore-5,8-Quinolinediones
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 182~187
The clastogenecity and mutagenicity of antifungal 6-[(N-halophenyl)amino]-7-chloro-5, 8-quinolinedione (RCK 3, 7, 13, 14, and 15) had been evaluated. Salmonella typhimurium reversion assay (Ames test) was used to test the mutagenicity of RCKs. RCK14 was mutagenic in S. typhimurium(TA98 and TA100) with and without rat liver microsomal activation. Whereas RCK3, 7, 13 and 15 were negative in Ames test with Salmonella typhimurium(TA98 and TA100), The clastogenecity was tested on the RCKs with in vivo mouse micronucleus assay. All of RCKs tested did not show any clastogenic effect in mouse peripheral blood. Thus RCKs were not supposed to cause any chromosomal damage termed micronuclei. These results indicate that RCK 3, 7, 13 and 15 have no genotoxic potential under these experimental condition.
NO Formation of the PMA and LPS-activated Rat Kupffer- and Endothelial Cells in vitro
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 188~191
The Present study was undertaken to indicate the major source of NO by liver cells in vitro. Even at early stages of induction or low LPS concentrations, NO was produced at high rates by LPS(Lipopolysaccharide) on the isolated rat kupffer cells. PMA(phorbol 12-myristate 13-acetate) induced NO formation at low rates in the same cells. IFN-
) alone had not induced NO formation but it stimulated the effects of LPS. Calcium ionophore A23187 caused no stimulatory effect. It suggests that LPS has especially strong NO inducer on the kupffer cells and its mechanism is related to those on macrophage in other organs. In other nonparenchymal liver cells, sinusoidal endothelial cells were not stimulated to produce NO either by inducers of aortic endothelium(A23187, ATP and ADP) or by effectors of macrophages(LPS, IFN-
. This results suggest that rat liver kupffer cells appear to be the major source of NO by liver cells in vitro. But in vivo, liver endothelial cells may still be capable of producing NO. Furthermore, kupffer cells may produce factors that facilitate NO production by the endothelial cells.
Effect of Mequitazine on the Muscarinic Receptors
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 192~198
The affinity of mequitazine, a non-sedating antihistamine, for muscarinic receptors was evaluated in the guinea-pig ventricle and ileum by in vitro binding techniques and functional studies. In binding studies, [
H]quinuclidinyl benzilate (QNB) identified a single class of muscarinic receptors with similar apparent
value of about 100 pM in two tissues. Mequitazine inhibited [
H]QNB binding to muscarinic receptors competitively. Analysis of the mequitazine inhibition curve of [
H]QNB binding to ventricular microsome and ileal homogenate indicated the presence of a single homogeneous binding site with Ki value of 25 nM and 18 nM, respectively. In functional studies, mequitazine caused parallel rightward shifts of concentration-response curves for carbachol and histamine in the isolated guinea-pig ileum. The slope values obtained from Schild plot analysis for the antagonistic action of mequitazine on muscarinic and histamine
-receptors were not significantly different from unity. The p
values of mequitazine for muscarinic and histamine
-receptors were about 7.6 (
= 25.1 nM) and 8.88 (
= 1.32 nM), respectively. These results indicate that the muscarinic receptor blocking action of mequitazine is 15 times less potent than the
receptor blocking action, but high concentration of this drug may cause the peripheral muscarinic receptor blocking effect.t.t.t.
Effect of the Ether Fraction of Gastrodia elata Methanol Extract on the Pentylenetetrazole-induced Seizures
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 199~204
Gastrodia elata is a medicinal plant which has been used as anticonvulsant in Korea, Japan and China. This study was conducted to examine the action mechanism of Gastrodia elata centering around the change of GABA and glutamic acid level in brain while observing the anticonvulsive effect in PTZ-induced seizure model. Seizures were reduced effectively by pretreatment of ether soluble part of methanol extract of Gastrodia elata. The pretreatment of ether soluble part inhibited not only the decrease of brain GABA level but also the increase of brain glutamic acid level observed in PTZ model of convulsive dose. Although there was not any change in glutamic acid level, the same development was also observed in the model of subconvulsive dose. From above results, it seems that the anticonvulsive component of Gastrodia elata is lipophilic, and its action mechanism is originated from both control action of GABA level and inhibition of glutaminergic neurotransmission.
Studies on the Mechanism of Action of the Gastric
ATPase Inhibitor KH 3218
Cheon, Hyae-Cyeong ; Kim, Hyo-Jung ; Yum, Eul-Kgun ; Cho, Sung-Yun ; Kim, Do-Yeob ; Yang, Sung-Il ;
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 205~209
The novel compound KH 3218 was synthesized and evaluated for its ability to inhibit the gastric H
ATPase activity in vitro as well as to lessen gastric acid secretion in vivo. KH 3218 inhibited rabbit gastric H
ATPase in a concentration and time dependent manner.
/ value was estimated to be about 15
M. The inhibition of the H
ATPase by KH 3218 was blocked by sulfhydryl reducing agents, dithiothreitol or
-mercaptoethanol. The inhibition of the enzyme was not reversible by 50 fold dilution of the incubation mixtures, suggesting the irreversible nature of the inactivation. In the pylorus-ligated rift, KH 3218 reduced the total acid output as compared with the control. In addition, KH 3218 was capable of inhibiting H. pylori urease activity. These data suggest that KH 3218 is a potent inhibitor for H
ATPase activity as well as for gastric acid secretion, and has a potential to be developed as a novel antiulcer agent.
Inhibition of HIV-1 Replication by the Water-soluble Extract Mixture of Ricini Semen and Coptidis Rhizoma
Kim, Kyong-Tai ; Park, Se-Young ; Hong, Eun-Kyung ; Han, Yong-Bok ; Kim, Jong-Bae ;
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 210~216
Partially purified water-soluble extract mixture from Ricini and Coptidis (named as RIC) showed to be a potent inhibitor of human immunodeficiency virus-1 (HIV-1) replication. RIC was evaluated for in vitro anti-HIV activity using SupTl and H9 cells infected by a recombinant virus (pSVCAT) containing chloramphenicol acetyltransferase (CAT) gene substituted for nef gene in the HIV-1 genome. RIC inhibited syncytiaformation of SupTl cells with a half maximal effective concentration,
/, of 2.5
/mι and showed marked inhibition of CAT activity in the infected H9 cells and also suppressed reverse transcriptase (RT) activity in the supernatant of the infected H9 culture. However, RIC did not inhibit the activity of reverse transcriptase directly when it was mixed with the enzyme or with viral particles. Berberine, one of components of RIC, also showed similar anti-HIV activity as RIC did. The data suggest that there are active ingredients which mediate anti-HIV activity in RIC.
Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 217~222
Several acyclonucleoside analogues of pyrimidine base and N
-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.
Effects of Biphenyldimethyl Dicarboxylate(DDB) on the Lipid Peroxidation and Oxygen Free Radical Scavenging Enzyme Activities in Mercuric Chloride-induced Hepntotoxic Rats
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 223~228
In an attempt to define the effects of biphenyldimethyl dicarboxylate (DDB) on the lipid peroxidation and oxygen free radical scavenging enzymes activities in mercuric chloride-induced hepatotoxic rats, we studied malondialdehyde (MDA) level and the activities of catalase and superoxide dismutase (SOD) in liver of the rats at 24 hr after the injection of mercuric chloride. Sprague-Dalwey albino rats were injected subcutaneously with mercuric chloride (5 mg/kg) only and mercuric chloride (5 mg/kg) plus. DDB (200 mg/kg/day, p.o) is administered for 4 days prior to 3 days from the injection of mercuric chloride. The group treated with mercuric chloride showed significantly higher MDA level and lower catalase and SOD activities as compared with that of control group. The group treated with mercuric chloride plus DDB showed significantly lower MDA level and catalase activity and higher SOD activity as compared with that of mercuric chloride-treated group. These results suggest that the excessive oxygen free radicals resulting from the depression of superoxide dismutase activity is an important determinant in the pathogenesis of mercuric chloride-induced hepatotoxicity and DDB has antioxidant effects.
Effects of Glycyrrhizae Radix on Acetaminophen-induced Hepatotoxicity in Mice
Aree Moon ; Lee, Mi-Kyung ; Kim, Chang-Ok ;
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 229~232
In order to study if Glycyrrhizae Radix (GR) has protective effects on hepatotoxicity of acetaminophen in mouse, one of the species which are sensitive to acetaminophen-induced hepatotoxicity, effects of GR on liver weight to body weight ratio, serum alanine and aspartate transaminase (ALT and AST) activities, hepatic UDP-GT2 activity, and histopathologic changes were determined in acetaminophen-treated mice. Liver weight to body weight ratio and UDP-GT2 activity in mouse liver were not altered by GR. However, GR pretreatment lowered serum ALT and AST activities by 77% and 90% respectively, and diminished the degree of centrilobular necrosis caused by acetaminophen in liver as determined by histopathologic observation. These results suggest a possible protective effect of GR against the acetaminophen-induced hepatotoxicity in mice.
Growth Effects of Recombinant Human Growth Hormone
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 233~237
The growth effects of newly developed recombinant human growth hormone (rHGH), were compared with those of Biotropine. For the effective evaluation, we examined the increasing rate of body weight and the thickness of tibial epiphysis as criteria of growth effects on hypophysectomised female rats treated with varing concentration of rHGH for 4 days. rHGH treated groups showed significant body weight gain which was less evident in Biotropine and vehicle treatment group. In tibial epiphyseal test, rHGH also showed clear effects compared to Biotropine and vehicle treatment group. Above findings indicate that newly developed rHGH has better effects of growth stimulation on female rats than Biotropine does.
Effect of Piperidinopyrimidine Derivatives on the Blood Pressure in Rats
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 238~241
To investigate the effects of N-4-salicyloamide-2-amino-6-piperidinopyrimidine 3-oxide (SALMI) on the blood pressure, this study was carried out in rats, using ethanol as vehicle. When Salmi and its salt were administered into the rat by oral administration or i.v. injection, both of them decreased blood pressure. But when Salmi was administered not more than 200 mg/kg(oral) and 30 mg/kg(i.v.) and Salmi·HC1 was administered not more than 100 mg/kg(oral), they did not significantly influence on the depressor effects of blood pressure.
In vitro Alternatives to Skin Irritation Test
Shin, Dae-Sup ; Kim, Dai-Byung ; Ryu, Seung-Rel ; Lee, Sun-Hee ; Koh, Jae-Sook ; Park, Won-Sae ; Kim, Pu-Young ;
Biomolecules and Therapeutics, volume 3, issue 3, 1995, Pages 242~244
In vitro cell culture system has been proposed as a promising alternative model to in vivo skin irritation test. These studies were performed to screen the cytotoxicity effects of surfactants using normal human skin fibroblasts. Cell membrane integrity assessed by the leakage of lactate dehydrogenase (LDH) and mitochondrial integrity by MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromides reduction test were affected in a dose dependent manner. The irritation potential of surfactants to human skin patch test, and the changes of capillary permeability by rabbit intradermal safety test were assessed as in vivo methods. Our results suggest that LDH leakage assay and MTT reduction test using cultured human fibroblasts could be predictive for the irritancy of various surfactants in human, and LDH assay is superior correlated with in vivo test (r=0.886) to MTT test with in vivotest (r=0.757).