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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Biomolecules and Therapeutics
Journal Basic Information
Journal DOI :
The Korean Society of Applied Pharmacology
Editor in Chief :
Volume & Issues
Volume 10, Issue 4 - Dec 2002
Volume 10, Issue 3 - Sep 2002
Volume 10, Issue 2 - Jun 2002
Volume 10, Issue 1 - Mar 2002
Selecting the target year
Taurine in Bone Formation and Alleviation of Its Diseases
;Ramesh C. Gupta;;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 137~141
Taurine, amino acid, chemically known as 2-amino ethane sulphonic acid was discovered more than two hundred years ago from ox bile. it is widely distributed in both mammals and nonmammals. It is found in considerably high amount in hUl11an: a normal adult of 70 kgs contains about 70 grams of taurine. Taurine with this much concentration, is involved in almost all life processes. Its deficiency causes several abnormalities in major organs like brain, eye and heart. Taurine-bone interaction is latest addition to its long list of actions. In bone cells, taurine is also found in high concentration. Taurine is found to help in enhancing the bone tissue formation which is evidenced by increased matrix formation and collagen synthesis. Besides stimulating the bone tissue formation, it also inhibits the bone loss through inhibiting the bone resorption and osteoclast formation. Thus, taurine acts as a double agent. In addition to these two major actions of taurine in bone, it also has beneficial effect in wound healing mld bone repair. Taurine possess radioprotective properties, too. As it is a naturally available molecule, it can be used as a preventive agent. Taurine has a potential to replace bisphosphonates which are currently in use for the inhibition of bone loss but this needs in depth study. As taurine is involved in bone formation and inhibition of bone loss, a detailed study can make it a single marker of bone metabolism. All these taurine-bone interaction is a symbol of their deep involvement but still require further extension to make taurine as a choice for tile sound bone health.
Influence of Apamin on Catecholamine Secretion from the Rat Adrenal Medulla
Lee, Eun-Sook ; Park, Hyeon-Gyoon ; Lim, Dong-Yoon ;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 142~151
The present study was attempted to investigate the effect of apamin on catecholamine (CA) secretion evoked by ACh, high
, DMPP, McN-A-343, cyclopiazonic acid and Bay-K-8644 from the isolated perfused rat adrenal gland and to establish the mechanism of its action. The perfusion of apamin (1 nM) into an adrenal vein for 20 min produced greatly potentiation in CA secretion evoked by ACh (5.32
), DMPP (
M for 2 min), McN-A-343 (
M for 2 min), cyclopiazonic acid (
M for 4 min) and Bay-K-8644 (
M for 4 min). However, apamin itself did fail to affect basal catecholamine output. Furthermore, in adrenal glands preloaded with apamin (1 nM) under the presence of glibenclamide (
M), an antidiabetic sulfonylurea that has been shown to be a specific blocker of ATP-regulated potassium channels (for 20 min), CA secretion evoked by DMPP and McN-A-343 was not affected. However, the perfusion of high concentration of apamin (100 nM) into an adrenal vein for 20 min rather inhibited significantly CA secretory responses evoked by ACh, high
, DMPP, McN-A-343, cyclopiazonic acid and Bay-K-8644. Taken together, these results suggest that the low concentration of apamin causes greatly the enhancement of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. These findings suggests that apamin-sensitive SK (
) channels located in rat adrenal medullary chromaffin cells may play an inhibitory role in the release of catecholamines mediated by stimulation of cholinergic nicotinic and muscarinic receptors as well as membrane depolarization. However, it is thought that high concentration of apamin cause the inhibitory responses in catecholamine secretion evoked by stimulation of cholinergic receptors as well as by membrane depolarization from the rat adrenal gland without relevance with the SK channel blockade.
Effects of Harmaline and Harmalol on Dopamine Quinone-induced Brain Mitochondrial Dysfunction
Han, Eun-Sook ; Lee, Chung-Soo ;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 152~158
The present study elucidated the effect of
-carbolines (harmaline and harmalol) on brain mitochondlial dysfunction caused by the tyrosinase-induced oxidation of dopamine. Harmaline, harmalol and antioxidant enzymes (SOD and catalase) attenuated the dopamine-induced alteration of membrane potential, cytochrome c release and thiol oxidation in mitochondria. In contrast, antioxidant enzymes failed to reverse mitochondrial dysfunction induced by dopmnine plus tyrosinase.
-Carbolines decreased the damaging effect of dopamine plus tyrosinase against mitochondria, except no effect of harmalol on thiol oxidation. Antioxidant enzymes decreased the melanin formation from dopamine in the reaction mixture containing mitochondria but did not reduce the formation of dopamine quinone caused by tyrosinase. Both harmalol and harmaline inhibited the formation of reactive quinone and melanin. Harmalol being more effective for quinone formation and vise versa. The results indicate that compared to MAO-induced dopamine oxidation, the toxic effect of dopamine in the presence of tyrosinase against mitochondria may be accomplished by the dopamine quinone and toxic substances other than reactive oxygen species.
-Carbolines may decrease the dopamine plus tyrosinase-induced brain mitochondrial dysfunction by inhibition of the formation of reactive quinone and the change in membrane permeability.
Effects of Polymerized Basic Amino Acids Under 50mer Range of Degree of Polymerization on Physiological and Stimulated Mucin Release from Cultured Hamster Tracheal Surface Epithelial Cells
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 156~164
In the present study, we tried to investigate whether polymerized basic amino acid e.g. poly-L-lysine (PLL) which has the degree of polymerization under 50mer significantly affects the physiological and stimulated mucin release from cultured hamster tracheal surface epithelial cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with
-glucosamine for 24 hr and chased for 30 min in the presence of either PLLs or adenosine triphosphate (ATP) and PLL to assess the effects on basic or ATP-stimulated
-mucin release. Possible cytotoxicities of PLLs were assessed by measuring lactate dehydrogenase (LDH) release from HTSE cel1s during treatment. The results were as follows: PLLs significantly inhibited basic mucin release from cultured HTSE cells in a dose-dependent manner from the range of 46mer to 14mer; PLL 46mer significantly inhibited the stimulated mucin release by ATP from cultured HTSE cells; there was no significant release of LDH from cultured HTSE cells during treatment. We conclude that PLLs inhibit both physiological and stimulated mucin release from airway epithelial cells without significant cytotoxicity and PLL lost its activity under the range of 14mer. This finding suggests that polymer of basic amino acid like PLL might function as a regulator for hypersecretion of mucus manifested in various respiratory diseases.
Hepatoprotective and Anti-diabetic Effects of Pelvetia siliquosa, a Marine Algae, in Rats
Lee, Yeon-Sil ; Jung, Sang-Hoon ; Lee, Sang-Hyun ; Choi, Yong-Jo ; Shin, Kuk-Hyun ;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 165~169
The effects of various fractions from the whole plant of Pelvetia siliquosa Tseng et Chang (Fucaceae) on the
-induced hepatotoxicity as well as on streptozotocin (STZ)-induced diabetes in rats were investigated. The ether fraction exhibited a potent rat lens aldose reductase (RLAR) inhibition in vitro and showed a significant inhibition of not only serum glucose concentrations but also sorbitol accumulations in the lens, red blood cells and sciatic nerves in the STZ-induced diabetic rats. When administered orally in Sprague-Dawley rats,
fraction was found to cause a significant inhibition of the rise in the serum transaminase activities in
-intoxicated rats. These results suggested that this plant might possess constituents with hepatoprotective, anti-diabetic effects and those effects on diabetic complications.
Local Irritation Test of HM10411 (rhG-CSF) in Rabbits
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 170~174
The local irritation study (skin and occular irritation tests) of HM10411, a rhG-CSF (recombinant human granulocyte-colony stimulating factor) was carried out in New Zealand White rabbits. HM10411 was applied to the bare skin at a dose of 2.5 mg/rabbit (5.0 mg/ml, 0.5 ml) and to the conjunctival sac of eye at a dose of 0.5 mg/rabbit (5.0 mg/ml, 0.1 ml) , respectively. In this study, there were no clinical signs which were related to HM10411 compared with those of control group. From above results, HM10411 has not any irritating activity to skin and eye in rabbits.
Neutralizing Effects of Antiserum by Repeated Subcutaneous Administration of Recombinant Human Growth Hormone (rhGH)
Song, Yeon-Jung ; Park, Shin-Hye ; Park, Seung-Kook ; Yeon, Je-Deuk ;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 175~179
Human growth hormone (hGH) forms antibody by repeated administration. The present study investigated to confirm formation of antibody by repeated subcutaneous administration of hGH for two months in rats and dogs. In this result, hGH-injected sera were significantly higher than control sera by 1:1,000,000 of dilution factor. After antibody formed sera (anti-hGH sera) and control sera were added to 30
/ml hGR, the complex incubated for overnight at
. Anti-hGH sera decreased hGH contents about 90% compared to control sera. Also, body weight gain conducted decreased about 67% compared to control sera in hypophysectomised rat. Inconclusion, repeated administration of hGH formed antibody because hGH was foreign protein to rats and dogs. And formed antibody of hGH was blocked and decreased many efficacy of hGH, the antibody was proved to be neutralizing antibody. Thus, because neutralizing antibodies were decreased pharmacological effects of hGH, administration more than two months were no significance.
Bioequivalence Assessment of Triamcinolone Tablets in Healthy Male Human Volunteers
Pyo, Hee-Soo ; Jang, Moon-Sun ; Chung, Youn-Bok ; Kwon, Oh-Seung ;
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 180~185
The bioequivalence of two 4 mg triamcinolone tablets (Dong-Kwang Triamcinolone
vs. Wyeth Korea Ledercoat
) was assessed in healthy male volunteers after oral administration of 16mg triamcinolone in a randomized crossover study. Blood samples were collected at specified time intervals, and plasma was analyzed for triamcinolone using a validated HPLC method. The pharmacokinetic parameters of
were determined from plasma concentration-time profile of two formulations. The pharmacokinetic parameters were statistically compared to evaluate bioequivalence between two formulations, according to Korea Food and Drug Administration Guideline. The analysis of variance did not show any significant difference between the two formulations and 90% confidence limits fell within the acceptable range (80-120%) for bioequivalence. Based on these data it was concluded that the two products showed comparable pharmacokinetic profiles and that the Dong-Kwang triamcinlone
tablet is bioequivalent to the Wyeth Korea Ledercoat
Assay of Human Chorionic Gonadotropin in Urine of Athletes and Evaluation of Assay Kit Performance
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 186~192
Special attention has been paid to human chorionic gonadotropin (hCG) for athlete doping control because it stimulates the endogenous production of testosterone and epitestosterone without increasing the T/E ratio which is a doping indicator for the exogenous administration of testosterone. Even though the IOC banned the use of hCG, a detection method has not been decided upon since there are a variety of immunoassay kits available on the market. We evaluated three kits in terms of their performance characteristics. The assay value of the control sample varied depending on the kit, resulting in 198 mIU/ml for the MAIA kit, 172mIU/ml for the IRMA kit, and 143 mIU/ml for the MEIA kit. Considering the IOC inter-lab distribution of results(55-312 mIU/ml) using 27 different kits and the mean value (178
56 mIU/ml), all three kits are within the range of －15.8% - ＋5.6% of the mean value, which proves them useful for the hCG assay. The MEIA kit resulted in lower hCG values because it detects only intact hCG molecules, in contrast to the other two kits which detect intact hCG and
10% of the mean values, and an specimens tested negative with hCG values less than the detection limit of 2 mIU/ml.
Relationships between Dapsone Metabolic Activity and Polymorphism of Arylamine N-acetyltransferase 2 in the F2 Hybrid Rats
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 193~199
The arylamine N-acetyltransferases (NATs) are a family of enzymes that N-acetylate mylhydrazines and arylamines through transfer of an acetyl group from acetyl coenzyme A. This activity was found to vary among individuals as a Mendalian trait and the basis of the genetic differences in human NAT activity is one of the best of the genetic studied examples of pharmacogenetic variation. The classical N-acetylation polymorphism is regulated at the NAT2 locus, which segregates individuals into rapid, intermediate, and slow acetylator phenotypes. In this study, the relationship between NAT2 activity phenotype using HPLC:UV assay for the determination of dapsone and monoacetyldapsone in plasma and NAT2 genotype by PCR-RFLP (polymerase chain reaction-restriction fragment length polymorphism) was investigated in the F2 hybrid (Fischer 344 vs Wistar-Kyoto) rats. Three Common mutant alleles at the NAT2 gene locus have been identified in the F2 generation progeny of Fischer 344 rats as raid acetylator and Wistar-Kyoto rats as slow acetylator segregated into three modes (low, intermediates, and high) with simple Mendelian inheritance. The metabolic activity of NAT2 of the intermediate and rapid acetylators is significant1y greater than slow acetylator, but the metabolic activity of rapid acetylator is not significantly different from Intermediate type. Therefore, we could observe that complete trimodal NAT2 genotypic alleles and incomplete trimodal NAT2 metabolic phenotypic distribution in tile F2 hybrid rats. These observations suggest that the relationships between NAT2 genotype and metabolic phenotype exists and F2 hybrid (Fischer 344: Wistar-Kyoto) animal models about NAT2 polymorphism might be applied in the toxicity and pharmacogenetic studies of arylamine drugs and carcinogens.
Therapeutic Effect of the GODEX on the Liver Chirrosis Induced by CCl
and Ethanol in the Rat
Biomolecules and Therapeutics, volume 10, issue 3, 2002, Pages 202~207
The hepato-protective activity of the GODEX (Hepadif-s capsule) has been studied in the rats against
-ethanol induced liver toxicity. The rats were oral1y treated with
1:1, 1 mg/kg). And one week passes,
(0.4 mg/kg) administered two times a week for 7 weeks. The drugs have been administered every two days for 4 weeks after
injection. The experimental groups have consisted of the GODEX (250 mg/kg), Hepadif (200 mg/kg), DDB complex (DDB 50 mg/kg and garlic oil powder 50 mg/kg), DDB (50 mg/kg), and vehicle control respectively. There was a significant decrement on the serum level of aspartate aminotransferase (AST), alanine aminotransferase (ALT) and total bilirubin in all treated groups. Specially, ALT level of GODEX and Hepadif only treated groups was decreased c1early. Also, serum albumin level was significantly enhanced in GODEX treated group compared with control and DDB treated groups. In histological results, hepatocellular vacuolar degeneration, lobular restructure and necrosis of bile duct were severely showed in control. But other treated groups showed centerilobular degeneration and mild hyper-plasia. Hepadif or DDB has a effects of the recovery on serum parameters and structure ill liver injury. When it was compared GODEX to Hepadif alone or DDB complex or DDB, it suggested to have the best activity of the liver recovery.