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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 7, Issue 4 - Dec 1999
Volume 7, Issue 3 - Sep 1999
Volume 7, Issue 2 - Jun 1999
Volume 7, Issue 1 - Mar 1999
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Role of Nitric Oxide in Pepsinogen Secretion from Rat Gastric Chief Cells
Sung, Dae-Suk ; Seo, Dong-Wan ; Choi, Don-Woong ; Ahn, Seong-Hoon ; Hong, Sung-Youl ; Lee, Hoi-Young ; Han, Jeung-Whan ; Lee, Hyang-Woo ;
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 105~111
Nitric oxide (NO), a cellular messenger synthesized from L-arginine by NO synthase (NOS, EC.184.108.40.206), is considered to be a regulator of gastric secretion. In the present study, the role of NO in the regulation of exocrine secretion was investigated in rat gastric chief cells. Treatment of chief cells with carba-chol resulted in an increase in the arginine conversion to citrulline, the amount of
, the release of pepsine-gen, and the level of cGMP Especially, carbachol-stimulated increase of arginine to citrulline transformation, the amount of
, cGMP level and the release of pepsinogen were partially reduced by the natural NOS inhibitor,
-monomethyl-L-arginine (MMA) and
-dimethyl-L-arginine (DMA). Furthermore, MMA- and DMA-induced decrease of pepsinogen secretion showed dose-dependent patters. Activation of NOS is one of the early events in receptor-mediated cascade of reactions in gastric chief cells and NO, not completely, but partially mediates gastric secretion. Agonist-stimulated pepsinogen secretion in chief cells has been considered to be mediated in adenosine 3',5'-cyclic monophosphate pathway and/or guanosine 3', 5'-cyclic monophosphate (cGMP) pathway. Taken together, the above results suggest that partial decrease of exocrine secretion following treatment of NOS inhibitor may result from the inactivation of NOS and subsequent guano- late cyclase, and NO/cGMP pathway may play a pivotal role in exocrine secretion.
Differential Antioxidant Effects of Ambroxol, Rutin, Glutathione and Harmaline
Kim, Hyun-Ho ; Jang, Yoon-Young ; Han, Eun-Sook ; Lee, Chung-Soo ;
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 112~120
The protective actions of ambroxol, rutin, glutathione and harmaline on oxidative damages of various tissue components were compared. The mechanisms by which they prevent oxidative tissue damages were explored. Lipid peroxidation of liver microsomes induced by combinations of
and ascorbate or
, ADP and NADPH was inhibited by
of rutin, ambroxol, harmaline and glutathione. Ambroxol (
) inhibited the degradation of hyaluronic acid by
and ascorbate, and it was greater than that of harmaline, whereas hyaluronic acid degradation was not prevented by rutin and glutathione. The compounds used (
) did not protect the degradation of cartilage collagen by xanthine and xanthine oxidase. Rutin, glutathione and harmaline decreased the degradation of IgG by xanthine and xanthine oxidate, while ambroxol did not attenuate degradation of IgG. Glutathione showed a scavenging action on
. The compounds all showed scavenging actions on hydroxyl radical. Ambroxol and harmaline exhibited quenching effects en singlet oxygen. In conclusion, ambroxol, rutin, glutathione and harmaline may exert protective effects differently on tissue components against oxidative attack depend on kind of tissue component and free radical.
Effects of Hyperbaric Oxygen Treatment on the Malondialdehyde Level and Activities of Catalase and Superoxide Dismutase in the Kidney of the Rats Exposed to Carbon Monoxide
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 121~126
In an attempt to define the effects of hyperbaric oxygen treatment on the lipid peroxidation and oxygen free radical reactions in rats exposed to carbon monoxide, we studied malondialdehyde (MDA) level and activities of catalase and superoxide dismutase in the kidney of the rats exposed to carbon monoxide. Male Sprague-Dawley albino rats weighing 240 to 260 gm were used. Experimental groups consist of Control group (=breathing with air), HBO group (=exposed to hyperbaric oxygen 〔HBO, 3ATA, 100%〕 after air breath), CO group (=exposed to CO〔3,970 ppm〕after air breath), CO-Air group (=exposed to CO after air breath followed by air breath) and CO-HBO group (=exposed to CO after air breath followed HBO treatment). The CO group showed significantly higher MDA level, catalase activity and SOD activity as compared to that of control group. The CO-HBO group showed significantly lower MDA level as compared to that of CO group, and did not show significantly lower catalase activity and SOD activity as compared to that of CO group. These results suggest that the excessive oxygen free radicals is an important determinant in pathogenesis of CO-induced nephrotoxicity and HBO inhibits the lipid peroxidation caused by excessive oxygen free radicals in the kidney of the rats exposed to carbon monoxide.
Immunosuppressive Activity of Simazine
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 127~132
Triazine herbicide has been reported to directly suppress the immune response. In the present study, the effect of simazine on the immune response was investigated. Splenic lymphocytes were treated withmitogen (lipopolysaccaride, concanavalin A) in the presence of simazine. When simazine(300 mg/kg, 600 mg/kg) was administrated every day for 3 weeks or 4 weeks, respectively, the number of plaque forming cells (PFC) was decreased. Antibody production of IgM and IgG class was significantly decreased in splenic cells from simazine-treated animals. In addition, when animals were exposed to simazine, the susceptibility of virus infection as well as the growth of tumor cells was increased. These data suggest that simazine affected the immune function and humoral immunity impaired by simazine treatment contributed to pathological process.
Inhibitory Effects of Eugenia caryophyllate, Ephedra sinica and Cinnamomum cassia on the Replication of HBV in HepG2 2.2.15 Cells
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 133~137
This study was undertaken to test for anti-Hepatitis B virus (HBV) activity of the aqueous extracts prepared from Eugenia caryophyllate, Ephedra sinica, Cinnamomum cassia. Aqueous extracts were assayed for the inhibition of HBV replication by measurement of HBV DNA and surface antigen (HBsAg) levels in the extracellular medium of HePG2 2.2.15 cells. All extracts decreased the levels of extracellular HBV virion DNA at concentrations ranging from 128 to 256
g/ml and inhibited the production of HBsAg dose-dependently. Our findings suggest that these three hebal medicinal plants may have potential to develop as specific anti-HBV drugs in the future.
Inhibitory Effects of Devazepide on the Pancreatic Exocrine Function of Ginseng Saponin in Rats
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 138~144
Recent studies have suggested that Panax ginseng saponins may stimulate pancreaticobiliary secretion. However, the precise mechanisms underlying the alterations in pancreaticobiliary function associated with ginseng saponins remain uncertain. We studied the effects of ginseng saponins and devazepide, cholecys-tokinin receptor antagonist, on pancreaticobiliary secretion in male Sprague-Dawley rats. The saponins tested were crude saponin (TS) and panaxatriol saponin (PTS). After single or two weeks administration of saponins, pancreaticobiliary juice of rats was collected for 8hrs. Single administration of TS and PTS did not change the volume of pancreaticobiliary juice compared with control group. In contrast, the pretreatment of devazepide significantly increased the volume of pancreaticobiliary juice. The amylase activity was significantly increased by acute TS treatment, but this increase was inhibited by devazepide pretreatment. In animals with two weeks administration of TS and PTS, the volume of pancreaticobiliary juice was not increased as compared to the control group. However, the volume of pancreaticobiliary juice was significantly increased by devazepide treatment. The amylase activity was significantly increased by two weeks administration TS and PTS respectively. This increase was inhibited by devazepide treatment. Our findings suggest that ginseng saponins, especially panaxatriol, increase the amylase activity in pancreaticobiliary juice, and this is, in part, caused by release of endogenous cholecystokinin.
Studies on the Anti-inflammatory Activity of Ginseng Total Saponin, Protopanaxadiol and Protopanaxatriol
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 145~152
In an attempt to elucidate the anti-inflammatory action of ginseng total saponin, protopanaxadiol and protopanaxatriol, the anti-inflammatory activity of three compounds was investigated under various acute and chronic inflammatory models. The blood vessel permeability was slightly inhibited by total saponin and protopanaxatriol treatments. Granuloma formation induced by 2% carrageenan was inhibited by total saponin and protopanaxatriol. The cotton-pellet granuloma formation was significantly inhibited by intraperitoneal injection of total saponin. Total saponin and protopanaxadiol inhibited leukocyte emigration and protein exudation in CMC-induced pouch but protopanaxauiol increased leukocyte emigration. The swelling of rat hind paw induced by 1% carrageenan was significantly inhibited by total saponin, protopanaxadiol and protopanaxatriol both single and 2 weeks treatments. Total saponin, protopanaxadiol and protopanaxatriol decreased the anti-inflammatory activity in adrenalectomized rat. Our results suggest that total saponin, protopanaxadiol and protopanaxatriol have potent anti-inflammatory activity, this may be mediated in part through stimulation of adrenal glands.
Anticancer Effects of Natural Medicinal Plant Extracts on Oral Carcinoma Cells
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 153~157
The anticancer effect of medicinal plants against two oral carcinoma cells, A253 and SCC-25 were investigated in this study. Methanol extracts from 63 medicinal plants, which have anticancer activities against other cancers such as stomach, hepatocellular or colon carcinomas, were prepared and screened for their anti- oral cancer activity by using MTT assay. Thirty one samples showed anti-oral cancer activity against either cell line used, however, other 32 samples had no anti-oral cancer activity. Among these samples methanol extract of Caesalpinia sappan revealed the strongest anti-oral cancer activity. The
/ values of this extract against A253 and SCC-25 cells were 16 and 25
g/m1, respectively. Fractions of n-hexane, dichloromethane, ethylacetate, n-buthanol and water were prepared from methanol extracts of Caesalpinia sappan, Anthriscus sylvestris, Rhus japonica, Curcuma arowatica, Inula helenium, Sinoarnudinaria reticulata, and Polygonum cuspidatum, respectively. Among these 35 fractions the n-hexane fraction of Inula helenium showed the strongest anti-oral cancer activity, the
/ value was 1.6
/ml. Ten other fractions showed
/ values lower than 10
Antiherpetic Activities of Natural Quercitrin Alone and in Combinations with Nucleoside Antiherpetic Agents
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 158~163
In order to find less toxic antiherpetic agents, antiviral activities of quercitrin against two strains of pathogenic viruses such as herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) were determined in Vero cells using plaque reduction assay in vitro. Quercitrin showed a concentration-dependent decrease in plaque formation of HSV-1 and HSV-2. It also exhibited more potent antiherpetic activity on HSV-1 with 50% effective concentration (EC
) of 20.4
g/ml than on HSV-2 with EC
g/ml. The combined antiherpetic effects of quercitrin with nucleoside antiherpetic agents, acyclovir and vidarabine, were examined on the multiplication of these two strains of herpesviruses in Vero cells by the combination assay. The results of combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combinations of quercitrin with acyclovir and vidarabine on HSV-1 showed more potent synergism with CI values of 0.27-0.81 for 50%, 70%, 90% effective levels than those on HSV-2 with CI values of 1.03~2.20..20.
Synthesis and Antimicrobial Activity of N-Substituted Glycyl Derivatives of Norfloxacin
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 164~169
The synthesis and antimicrobial activity of N-substituted glycol derivatives of Norfloxacin were described. Norfloxacin was treated with chloroacetyl chloride to yield chloroacetyl norfloxacin (1). This compounds was reacted with alkyldiamines to afford bivalent ligand quinolone carboxylic acids (2-6), which was added to pivaloyloxymethyl chloride to give bivalent ligand pivaloyloxymethyl quinolone carboxylates (7-11). Chloroacetyl norfloxacin (1) treated with alkylamines to obtain monovalent ligand quinolone carboxylic acids (12-15), which was reacted with pivaloyloxymethyl chloride to get monovalent ligand pivaloyloxymethyl quinolone carboxylates (16-19). Free carboxylic quinolones (2-6, 12-15) showed little stronger activities to their pivaloyloxymethyl esters (7-11, 16-19). In monovalent ligand quinolone analogues, longer a1kyl chain com-pounds showed stronger activities than shorter one.
General Pharmacology of PEG-Hemoglobin SB1
Kim, Eun-Joo ; Lee, Rae-Kyong ; Bak, Ji-Yeong ; Choi, Gyu-Kap ;
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 170~177
PEG-hemoglobin SB1 (SB1), which is a hemoglobin-based oxygen carrier, is intended to use as a safe blood substitute against brain ischemia and stroke. The general pharmacological profiles of SB1 were studied. The doses given were 0, 5, 10, 20 ml/kg and drugs were administered intravenously. The animals used for this study were mouse, rat and guinea pig. SB1 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital sleeping time, anticonvulsant activity, analgesic activity, blood pressure and heart rate, left ventricular peak systolic pressure, left ventricular end diastolic pressure, left ventricular developing pressure, double product, heart rate, coronary flow rate, smooth muscle contraction using guinea pig ileum, gastrointestinal transport, gastric secretion, urinary volume and electrolyte excretion at all doses tested except the decrease of body temperature. These findings demonstrated that SB1 possesses no general pharmacological effects at all doses tested.
Pharmacological Evaluation of Bamboo Salt
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 178~184
Bamboo salt has been used for the purpose of precaution and treatment of certain diseases including cancer. Therefore, present study was carried out to ascertain the effects of bamboo salt upon anti-cancer, anti-hypertensive, and anti-diabetic activities as well. To examine the anti-cancer activity of bamboo salt, ICR mice implanted with 1
cells of sarcoma 180 intraperitoneally had been treated daily with bamboo salt A, crude salt, and reagent-grade NaCl (0.2, 1.0, and 2.0 g/kg, p.o.) for 60 days using adriamycin (2 mg/kg) as a positive control. Neither survival rate nor body weight had been significantly influenced by all the treatments indicating that bamboo salt A did not exert the anti-cancer effect on ICR mice. Anti-hypertensive activity was examined in spontaneously hypertensive rats (SHR) which had been administered with bamboo salt A, crude salt, and reagent-grade NaCl (0.1, 0.5, and 1.0% in drinking water) for 28 days using hydralazin (2 mg/kg) as a positive control. Blood pressure and heart rate were measured at 1, 3, and 4 weeks after the starting date. Significant anti-hypertensive activity was not observed in any treated group compared to the positive control group. In order to determine if bamboo salt had anti-diabetic activity, rats in which diabetes had been induced by streptozotocin (45 mg/kg, i.m.) were treated daily with bamboo salt A, crude salt, and reagent-grade NaCl (0.2, 1.0, and 2.0 g/kg, p.o.) for 28 days using insulin (50 U/kg, s.c..) as a positive control. Blood samples were taken and analyzed at 1,2, and 4 weeks after the starting date. Bamboo salt did not cause any decreasing effect on the blood glucose levels. These results clearly demonstrated that bamboo salt A did not exert anti-cancer, anti-hypertensive, or anti-diabetic activities in the present experimental animals.
Acute Oral Toxicity Studies of 1:1 mixture of Phellodendron amurense cortex and Arabia elata cortex P55A in SD Rats and Beagle Dogs
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 185~190
The current study was performed to determine the acute oral toxicity of P55A, a crude extract of 1 : 1 mixture of Phellodendron amurense cortex and Aralia elata cortex, in SD rats and beagle dogs. 5 rats of each sex were treated with a single dose of P55A orally at doses of 0 and 5,000 mg/kg respectively. Also 2 dogs of each sex were treated with a single dose of P55A orally at doses of 0 and 2,000 mgAg, respectively. After the treatment, clinical signs, and body weight change were observed for 14 days. All rats survived during the study and did not show any clinical sign. Body weight gain showed no significant difference between the control and treated rats. Grossly, no lesion was observed in the rats. All dogs survived during the study. In clinical signs, dark stool was observed in the 2,000 mg/kg treated dogs at day 1 after administration. The animals recovered from general signs at day 2 after administration. Body weight gain showed no significant difference between the control and treated dogs. Grossly, no lesion was observed in the dogs. It is suggested that the LD
of P55A by oral administration was estimated to be over 5,000 mg/kg in both sexes of rats and 2,000 mg/kg in both sexes of beagle dogs.s.
Drug Screening for the Formulation of Topical Antiblister Preparations
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 191~197
The effects of various drugs on the alleviation of the symptoms of chemical bums were evaluated in mice to formulate topical antiblister preparations. After a chemical bum was induced on the mouse dorsal skin with 2-chloroethylethyl sulfide, the drug was applied on the disease site. The effectiveness of the drug was evaluated by determining blister size, necrosis score of skin and appearance of the chemical burns induced. It showed that steroids and aminoglycoside antibiotics had a tendency to protect skin cell, and antihistamines decreased the size of chemical bums. While oleaginous base resulted in deleterious effect, hydrophilic base didn't show a significant difference on the alleviation of the chemical burn symptoms compared to the control.
Anti-inflammatory and Analgesic Activities, and Plasma Concentration of Loxoprofen Sodium Plasters
Biomolecules & Therapeutics, volume 7, issue 2, 1999, Pages 198~203
Loxoprofen-Na (sodium 2-〔4-(2-oxocyclopentylmethyl)pheny)propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will be a new type of drug for controlling the various local pain or inflammation.