CJ-50002 is an oral vaccine against V.vulnificus infection composed of whole cell lysate of V. vulnificus. The general pharmacological properties of CJ-50002 were evaluated in various animals and in vitro system. CJ-50002 at oral doses of 0.2, 2 and 20 mg/kg had no effect on general behavior in mice, chromo- and electro-convulsions in mice, writhing syndrome induced by acetic acid in mice, body temperature in rats, charcoal meal propulsion in mice and urine and electrolytes excretion in rats. However, oral administration of CJ-50002 at dose of 20 mg/kg prolonged the hexobarbital-inuced sleeping inducing time in mice. In anesthetized dogs, CJ-50002 showed no effect on blood pressure, heart rate and ECG but decreased the respiratory rate and femoral blood flow at dose of 20 mg/kg. p.o. CJ-50002 had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 0.2, 2 and 20 $\mu\textrm{g}$/ml, respectively. Since these pharmacological effects of CJ-500o2 were observed at dose much greater than those in clinical use (approximately 0.16 mg/kg, p.o.), it is likely that this vaccine may be relatively free of undesirable effects in clinical practice.
The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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v.13
no.1
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pp.1-21
/
2000
This experiment was performed to study of Gagambipachungpe-Eum extract solution's effects on acne. Anti-inflammatory edema, anti-histamine, vascular permeability, acne by induced oleic acid, ileum contraction of mice and guinea-pig was measured by oral administration, topical application or both of the sample to the acne of the experimental animals. Dose of samples were taken by 500 and 1,500mg/dl at the experiments. The results were as follows. 1. Gagambipachungpe-Eum on rat hind paw edema induced by $0.5\%$ Carrageenin have statistically significant effects on anti-inflammatory edema at 2, 3(p<0.05) and 4 hours(p<0.01) of the high density 1500mg/kg - oral administration group as compared with sample group. 2. Gagambipachungpe-Eum on rat hind paw edema induced by $1.0\%$ Dextran have statistically significant effects on anti-inflammatory edema at 2 and 4 hours of the high density 1,500mg/kg oral administration group as compared with sample group(p<0.05). 3. Gagambipachungpe-Eum on mouse hind paw edema induced by $1.2\%$% Histamine have statistically significant effects on anti-inflammatory edema at 30, 60 and 90 minutes of the high density 1500mg/kg - oral administration group as compared with sample group(p<0.05). 4. Only high density 1,500mg/kg - oral administration group of Gagambipachungpe-Eum as compared with sample group have significant effects on increased vascular permeability induced by histamine, picryl chloride induced contact dermatitis(p<0.01) and writhing syndrome induced by $0.7\%$ acetic acid(p<0.05) in mice. 5. All of the sample groups, Sample-Ⅰ(orally administered), Sample-Ⅱ(topically administered 500mg/kg), Sample-Ⅲ(topically administered 1,500mg/kg), Sample-Ⅳ(administered simultaneous orally and topically) on acne induced by o1eic acid in rabbit ears has the significant recovery on induced acne after 14 days 6. Gagambipachungpe-Eum have the effects on the motility of the isolated mice ileum, on the contraction induced by acetylcholine chloride and barium chloride in the isolated mice ileum and on the contraction induced by acetylcholine chloride, barium chloride and histamine in the isolated Guinea-pig ileum. According to the about results, it is expected Gagambipachungpe-Eum could be applicable to the treatment of acne.
Gupta, Malaya;Mazumder, UK;Selvan, V Thamil;Manikandan, L;Senthilkumar, GP;Suresh, R;Gomathi, P;Kumar, B Ashok
Advances in Traditional Medicine
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v.8
no.2
/
pp.196-203
/
2008
The methanol extract of the root of Artanema sesamoides Family Scrophuilariaceae (MEAS) was investigated for possible analgesic and anti-inflammatory effects in animals. Three models were used to study the extract effects on nociception, which were acetic acid-induced writhing response, hot-plate method and the tail flick test in mice. The antiinflammatory effects were evaluated using carrageenan, dextran, histamine and serotonin induced rat paw oedema (acute) and cotton pellet induced granuloma (chronic) models in rats. Results of the study revealed that the extract exhibited significant (P < 0.001) analgesic effect at a dose of 50, 100 and 200 mg/kg b.w p.o in mice in all the models. In acute model, the MEAS also exhibited significant (P < 0.001) antiinflammatory effect in all the above mentioned doses. In chronic model (cotton pellet induced granuloma) the MEAS 200 mg/kg and indomethacin 10 mg/kg showed that inhibition of granuloma formation 25.0% and 47.7% respectively (P < 0.001). The MEAS and indomethacin were effectively preventing the transudation of the fluid. Thus, the present study revealed that the methanol extract of the root of Artanema sesamoides exhibited significant analgesic and antiinflammatory activity.
General pharmacological effects of SB-31$^{R}$, the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital- induced sleeping time , rotared performance , electroshock and pentylenetertrazole -induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 m1/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of N $a_{+}$and $K_{+}$at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not pro-duce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.ml/kg.
The general pharmacological properties of EPO were investigated in various animals administering intravenously and in vitro system. The results were as follows. 1. Central nervous system: EPO at doses of 70, 700, 7000 U/kg showed no effect In mice on general behavior, on strychnine- and pentetrazol-induced convulsion and on acetic acid-induced writhing syndrome. The hexobarbital-induced sleeping time in mice was slightly reduced by EPO at a dose of 7000 U/kg but did not change at doses of 70, 700 U/kg. The body temperature in rats was slightly decreased by EPO at doses of 700, 7,000 U/kg but the change was in normal physiological range. 2. Respiratory and cardiovascular system: EPO showed no effect on respiratory rate, blood pressure, heart rate, femoral blood flow, and electrocardiogram in anesthetized dogs at doses of 70, 700, 7000 U/kg. 3. Smooth muscle: EPO at concentrations of 70, 700 U/ml had no effect on the contractile response of isolated guinea pig ileum to histamine and acetylcholine. 4. Water and electrolytes excretion: EPO at dose above 700 U/kg increased urine volume in rats but did not affect the concentrations of $Na^{+},\;K^{+},\;Cl^{-}$ in urine. 5. Gastrointestinal system: EPO(70, 700, 7000 U/kg) had no effect on the intestinal charcoal meal propulsion 6. Blood coagulation system: The administration of EPO(70, 700, 7000 U/kg) had no effect on the plasma prothrombin time(PT) and activated partial thromboplastin time(APTT) in mice. Platelet aggregation induced by ADP and collagen was not influenced by EPO(70 U/ml, 700 U/ml). The overall results obtained indicated that EPO exerts almost no serious pharmacological effect even at a 100-fold clinical dose(7000 U/kg).
This study has been carried out to investigate the effects of Youngyanggaksan (YGS) extract on the anticonvulsive, antipyretic, anlgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. YGS extract prolonged significantly the beginning time to convulsion and time to death induced by strychnine. 2. YGS extract prolonged significantly the time to death induced by electrical shock of ECT unit (3sec, 200F, 25mA). 3. On the experiment of hypothermic effects of YGS extract on the rectal temperature of rats, YGS extract decreased significantly the rectal temperature of rats. 4. On the experiment of antipyretic effects of YGS extract on the febrile induced by the subcutaneous injection of $150{\mu}g/kg$ endotoxin in rats, YGS extract decreased significantly the rectal temperature of rats. 5. On the experiment of analgesic effects of YGS extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1ml/100g in rats, the writhing syndrome was reduced significantly by administration of YGS extract. 6. On the experiment of sedative effects of YGS extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of YGS extract. 7. On the experiment of effects of YGS extract on the activity of GABA-transaminase(GABA-T) in rat brains after 21 days of oral administration of YGS extract, the activity of GABA-T was reduced significantly by administration of YGS extract. 8. On the experiment of effects of YGS extract on the activity concentration of GABA in rat brains after 21 days of oral administration of YGS extract the activity concentration of GABA was reduced significantly by administration of YGS extract. 9. On the experiment of effects of YGS extract on the activity of GAD in rat brains after 21 days of oral adminstration of YGS extract, the activity of GAD was reduced significantly by administration of YGS extract. According to the those results, Youngyanggaksan extract reveals the effects on the anticonvulsive, antipyretic, anlgesic, sedative and GABAergic system.
The analgesic effects of DA-5018, a new caosaucin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the $ED_{50}$ of DA-5018, morphine . HCI, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and crouton oil-induced ear edema test, 2) the AD2 values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprpgin were 1.07 $\pm$ 0. 18, 23.47$\pm$4.46 and 2.97$\pm$0.43 mg/kg in Freund's complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrix-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) In FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP. These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinglammaatory effects to capsaicin cream.
Han Ki-Jung;Choi Seong-Soo;Lee Jin-Young;Lee Han-Kyu;Shim Eon-Jeong;Kwon Min Soo;Seo Young-Jun;Suh Hong-Won
Archives of Pharmacal Research
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v.28
no.2
/
pp.209-215
/
2005
The antinociceptive effect of nicotine administered intracereboventricularly (i.c.v.) or intrathecally (i.t) in several pain models was examined in the present study. We found that i.t. treatment with nicotine (from 5 to 20 g) dose-dependently blocked pain behavior revealed during the second phase, but not during the first phase in the formalin test. In addition, i.c.v. treatment with nicotine (from 0.1 to $10\;{\mu}g$) dose-dependently attenuated pain behavior revealed during both the first and second phases. In addition to the formalin test, nicotine administered i.c.v. or i.t. attenuated acetic acid-induced writhing response. Furthermore, i.c.v. or i.t. administration of nicotine did not cause licking, scratching and biting responses induced by substance P, glutamate, TNF-${\alpha}$(100 pg), IL-$1{\beta}$(100 pg) and INF-${\gamma}$ (100 pg) injectied i.t. The antinociception induced by supraspinally-administered nicotine appears to be more effective than that resulting from spinally administered nicotine. Our results suggest that nicotine administration induces antinociception by acting on the central nervous system and has differing antinociceptive profiles according to the various pain models.
Joo Ji-Hoon;Lim Jong-Min;Koo Kwang-Bon;Yun Jong-Won;Choi Jang Won
Journal of Life Science
/
v.15
no.2
s.69
/
pp.287-292
/
2005
The crude galactomannans (GMs) were obtained from the culture of a newly isolated fungus Trichoderma erinaceum DG-312 and their anti-inflammatory activity was investigated in mice. The maximum concentrations of mycelial biomass and GMs reached 9.44 g/l, 2.72 g/l at day 3 in a 5-l stirred-tank bioreactor, respectively. The results of Sepharose CL-6B gel chromatography and compositional analysis revealed that the crude GMs contain heterogeneous polysaccharides consisting of $74.9\%$ mannose and $24.1\%$ galactose. The GMs was shown to possess a significant anti-inflammatory activity against acetic acid-induced inflammatory mouse model in a dose-dependent manner, when mice were treated with 100 and 200 mg GMs/kg body weight. The inhibition in vascular permeability $(60.6\%)$ and in writhing response $(62.5\%)$ evidenced an anti-inflammatory activity of the GMs. The marked anti-inflammatory and writhing-lowering properties of the GMs suggest its potential therapeutic use.
Previous screening of the pharmacological action of Gastrodia elata (GE) root (Orchidaceae) showed that methanol (MeOH) extracts have significant anti-inflammatory properties. The antiinflammatory agents of GE, however, remain unclear. In this experiment, MeOH extracts of GE were fractionated with organic solvents for the anti-inflammatory activity-guided separation of GE. Eight phenolic compounds from the ether (EtOEt) and ethyl acetate (EtOAc) fractions were isolated by column chromatography: 4-hydroxybenzaldehyde (I), 4-hydroxybenzyl alcohol (II), benzyl alcohol (III), bis-(4-hydroxyphenyl) methane (IV), 4(4'-hydroxybenzyloxy)benzyl-methylether (V), 4-hydroxy-3-methoxybenzyl alcohol (VI), 4-hydroxy-3-methoxybenzaldehyde (VII), and 4-hydroxy-3-methoxybenzoic acid (VIII). To investigate the anti-inflammatory and anti-oxidant activity of these compounds, their effects on carrageenan-induced paw edema, arachidonic acid (AA)-induced ear edema and analgesic activity in acetic acid (HAc)-induced writhing response were carried out in vivo; cyclooxygenase (COX) activity, reactive oxygen species (ROS) generation in rat basophilic leukemia (RBL 2H3) cells and 1,1-diphenyl-2-picryl-hydroazyl (DPPH) scavenging activity were determined in vitro. These phenolic compounds not only had anti-inflammatory and analgesic properties in vivo, but also inhibited COX activity and silica-induced ROS generation in a dose-dependent manner. Among these phenolic compounds, compound VII was the most potent anti-inflammatory and analgesic. Compound VII significantly inhibited silica-induced ROS generation and compound VI significantly increased DPPH radical scavenging activity. Compounds I, II and III significantly inhibited the activity of COX-I and II. These results indicate that phenolic compounds of GE are anti-inflammatory, which may be related to inhibition of COX activity and to anti-oxidant activity. Consideration of the structure-activity relationship of the phenolic derivatives from GE on the anti-inflammatory action revealed that both C-4 hydroxy and C-3 methoxy radicals of benzyl aldehyde play an important role in anti-inflammatory activities.
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