• 대한약리학회지
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• 제30권2호
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• pp.227-242
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• 1994

The general pharmacological effects of a new anthracycline anticancer agent, DA-125 $[7-0-(2,\;6-dideoxy-2-fluoro-{\alpha}-L-talopyranosyl)-adriamycinone-14-{\beta}-alaninate{\cdot}HCI]$ were investigated in mice, rats, guinea pigs, rabbits and dogs. Intravenous administration of DA-125 presented no significant effects on the central and peripheral nervous systems of ICR mice except a decrease in the numbers of acetic acid-induced writhing response at a dose of 10 mg/kg. In anesthetized rats and dogs, DA-125 produced a transient depression of blood pressure and an increase in heart rate, but did not affect the peripheral blood flow in the isolated ear vessels of rabbits and the mechanical functions of the isolated hearts of guinea pigs. No significant effects were observed on the gastrointestinal functions and the contractilities of smooth muscle preparations obtained from guinea pig trachea, rabbit ileum, pregnant and non-pregnant uterus and vas deferens of rats. DA-125 Increased the contractility of the isolated ileum of guinea pigs in a dose range of $10^{-6}{\sim}10^{-9}g/ml$, and also increased, but weaker than adriamycin, the vascular permeability in rat skin. DA-125 had no effect on the kallikrein-induced increase in permeability and the permeability of the visceral organs. DA-125 did not adversely affect the liver function and the blood coagulation system, and did not induce hemolysis in vitro. It is concluded from the results that the general pharmachological effects of DA-125 are similar to or weaker than those of adriamycin, and that little adverse effects are anticipated with a therapeutic dose range.

• 대한한방내과학회지
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• 제18권1호
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• pp.69-85
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• 1997

This study was designed to elucidate the anti-inflammatory, cardiovascular, anti-thrombotic and analgesic effects of Shintongchugeotang. The anti-inflammatory effect was measured by the method of carragenin induced edema, protein leakage test using CMC-pouch, and the analgesic effect was measured by the acetic acid method and hot plate method, and the effect of Shintongchugeotang on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit, and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity was observed for the measurement of the anti-coagurative effect of Shintongchugeotang. The result was as follows : 1. After the administration of Shintongchugeotang extract, Carragenin induced edema and CMC-pouch protein leakage were significantly decreased. 2. The slight analgesic effect of Shintongchugeotang extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time. 3. The drug increased the auricular blood flow in rabbit. 4. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 5. The drug inhibited the death rate of mouse which was led to thromboembolism by serotonin and collagen. 6. The drug inhibited the platelet aggregation in rat. 7. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable.

• 대한한방내과학회지
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• 제20권1호
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• pp.57-72
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• 1999

This study was designed to elucidate the anti-inflammatory, cardiovascular, anti-thrombotic, and analgesic effect of Whalrakdan. The anti-inflammatory effects was measured by the method of carrageenin induced edema, protein leakage test using CMC-pouch, and the effect of Whalrakdan on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit. and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity, antithrombin activity was observed for the measurement of the anti-thrombotic effect of Whalrakdan, and the analgesic effect was measured by the acetic acid method and hot plate method. The result was as follows: 1. After 2 or 3hour of Whalrakdan administration, carrageenin induced edema and CMC-pouch protein leakage was significantly decreased. 2. The slight anagesic effect of Whalrakdan extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time. 3. The droplet of Ringer solution increased according to the increase of concentration of Whalrakdan extract, and the vasoconstriction decreased dependantly to the concentration of Whalrakdan extract. 4. The anti-thrombotic effect of Whalrakdan was observed by the decrease of death rate, the inhibition of platelet aggregation, and the increase of anti-thrombin activity.

• Biomolecules & Therapeutics
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• 제10권1호
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• pp.19-24
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• 2002

The effects of a newly synthesized $H^+/K^+$ ATPase inhibitor,1-(2-methyl-4-methoxypheny)-4-[(3-hy-droxypropyl)amino] -6-methyl-2,3-dihydropyrrolo (3,2-c) quinoline (DBM-819) , on the central nervous system, isolated smooth muscle, cardiovascular and digestive systems and renal function were investigated in various experimental animals. Oral administration of DBM-819 had no effect on the central nervous system except body temperature of mice slightly decreased at doses of 15 and 50 mg／kg. DBM-819 produced a moderate analgesic effect in acetic acid-induced writhing test in mice at 50 mg／kg (p.o.). In conscious rats, DBM-819 (15 and 50 mg／kg, p.o.) showed a slight increase in blood pressure and a small decrease in heart rate. DBM-819 had an significant effect on agonist-induced contraction of guinea pig ileum at $1.5{\times}10^{-5}g/ml.$ No significant effect of DBM-819 (5 and 15 mg／kg, i.p) on urinary volume or urinary excretion of $Na^+,\;K^+$ and Cl- was observed in rats. DBM-819 had no significant effect on intestinal transport of a semisolid meal in mice at 15 and 50 mg／kg (p.o.). These findings suggest that DBM-819 exerts no significant pharmacological effects on the central nervous system and renal function at 15 mg／kg (p.o.), but produces some effects on the smooth muscle and circulatory system.

• Advances in Traditional Medicine
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• 제6권4호
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• pp.355-360
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• 2006

Plants have been used in traditional medicinal system for centuries. Bangladeshi medicinal plants have received considerable attention from the researchers for evaluation of their bioactivity. As a part of our ongoing research of screening the Bangladeshi medicinal plants, the ethanolic extract of Dendrophthoe falcata have been chosen for the present study. The ethanolic extract of the leaves of the plant have been assessed for their antioxidant, antinociceptive, and general toxicity. The extract showed potent antioxidant activity ($IC_{50}5.1{\mu}g/ml$) using DPPH radical scavenging assay, which is comparable to the standard ascorbic acid ($IC_{50}4.6{\mu}g/ml$). The extract significantly and dose dependently inhibited the acetic acid induced writhing in mice (71.2%, P < 0.001 and 28.0%, P < 0.05 for 500 and 250 mg/kg body weight, respectively). A general toxicity was assessed by a simple and low cost assay using brine shrimp lethality as an indicator. The extract showed low level of toxicity ($LC_{50}100{\mu}g/ml$). Using different chromatographic techniques, quercitrin (quercetin 3-O-${\alpha}$-rhamnoside) was separated as the major component from the extract. The structure was elucidated by detailed 1D and 2D NMR and mass spectral analysis.

• 대한한방소아과학회지
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• 제10권1호
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• pp.323-349
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• 1996

Gamitonggyutang has been used for treatment of rhinitis in oriental medical science. It is reported that Gamitonggyutang has a good effect on sinusitis in clinical medicine. So this study analysed the effect of Gamitonggyutang on anti-inflammatory, analgenic, anti-Allergic effect and Antibacterial Activity. The result were summerised as follows; 1. Gamitonggyutang extract decreased the edema indused by Carregennin at 200mg/kg and 400mg/kg. 2. Gamitonggyutang extract decreased the protein exudation indused by CMC-pouch at 200mg/kg and 400mg/kg. 3. Gamitonggyutang extract showed the ataralgesia at 800mg/kg by measurement of writhing syndrome, paw licking time and escape time induced by the i.p. infection of acetic acid and hot plate. 4. Gamitonggyutang extract decreased the effluent of vascular permeability indused by Evans blue at 600mg/kg and 800mg/kg. 5. Gamitonggyutang extract decreased the acute edema indused by Carregennin about 2 and 4 hours but didn't show useful effect. 6. Gamitonggyutang extract decreased the death rate, resulted from the effect of active systemic anaphylaxis reaction indused by CGG, but didn't show useful effect.. 7. Gamitonggyutang extract showed the growth inhibitory effect of each bacterias at $52mg/m{\ell}$. 8. Gamitonggyutang extract suppressed the growth of Streptococcus mutans 10449, and showed the supression of acid fabrication in case of 1:10 more than 1:100.

• 약학회지
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• 제34권2호
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• pp.126-132
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• 1990

To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, Ibu-P.A., and Ibu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The $LD_{50}$ was 495 mg/kg for ibuprofen, 187 mg/kg for Ibu-M.P., and over 1250 mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life($t_{1/2}$) were 0.74($hr^{-1}$) and 0.94(hr) for ibuprofen, and 0.72 ($hr^{-1}$) and 0.96 (hr) respectively for Ibu-M.P..

• 한국식품영양과학회지
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• 제28권5호
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• pp.1113-1123
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• 1999

The purpose of this study was to see the effect of anti inflammatory and analgesic action of the glucosamine hydrochloride(GA HCl) or taurine. Male Sprague Dawley rats(100~250g) and ICR mice(20 ~30g) were used. Experimental groups were divided into seven groups, one control group given as saline and six groups given as oral administration of GA HCl or taurine; GA HCl 250mg/kg, b.w group, taurine 250mg/kg, b.w group, GA HCl 250mg/kg, b.w＋taurine 250mg/kg, b.w group, GA HCl 500mg/kg, b.w group, taurine 500mg/kg, b.w group, GA HCl 500mg/kg, b.w＋taurine 500mg/kg, b.w group. Carrageenan induced edema test were shown to be significantly inhibited in the GA HCl 250mg/kg group and taurine 250mg/kg group compared to the control group, but the GA HCl 500mg/kg＋taurine 500mg/kg group were significantly inhibited than the control group. Capillary permeability test were shown to be sig nificantly inhibited in the taurine 500mg/kg group, but the GA HCl 500mg/kg＋taurine 500mg/kg group were significantly inhibited than the control group. Leucocyte emigration test were shown to be significantly inhibited in the GA HCl 250mg/kg＋ taurine 250mg/kg group and GA HCl 500mg/kg＋taurine 500mg/kg group compared to the control group. Acetic acid, Phenyl p benzoquinone writhing syndrome were shown to be significantly inhibited in the GA HCl 500mg/kg＋taurine 500mg/kg group compared to the control group. Inhibitory action against COX 1 and COX 2 were not significantly inhibited in the experimental group. These results suggest that the combined administration of the GA HCl and taurine have potential action in anti inflammatory and analgesic action.

• 대한한방내과학회지
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• 제19권2호
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• pp.88-106
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• 1998

This study was designed to elucidate the antiinflammatory, cardiovascular, antithrombotic, and analgesic effect of Sambitang. The antiinflammatory effects was measured by the method of carrageenin induced edema, protein leakage test using CMC-pouch, and the effect of Sambitang on the cardiovascular system was observed by the change of flow rate of Ringer solution in the vascular system in the ear of rabbit, and the contraction and dilatation of rat tail artery. Death rate, platelet aggregation, plasma coagulation activity was observed for the measurement of the anticoagurative effect of Sambitang, and the analgesic effect was measured by the acetic acid method and hot plate method. The result was as follows: 1. Sambitang administration, edema and protein leakage was significantly decreased. 2. The drug increased the auricular blood flow in rabbit. 3. The drug relaxed the artery contraction by pretreated norepinephrine in rat. 4. The drug inhibited the death rate of mouse which was led to thromboembo- lism by serotonin and collagen. 5. The drug inhibited the platelet aggregation in rat. 6. The drug prolonged the prothrombin time and activated partial thromboplastin time on the test of plasma coagulation factor activity in rat, but was not valuable. 7. The slight anagesic effect of Sambitang extract was confirmed by the observation of writhing syndrome, paw licking time, and escape time.

• 대한약침학회지
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• 제17권1호
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• pp.74-79
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• 2014

Objectives: This study was conducted to clarify the analgesic effect of toad cake and toad-cake-containing herbal drugs. Methods: We counted the writhing response of mice after the intraperitoneal administration of acetic acid as a nociceptive pain model and the withdrawal response after the plantar surface stimulation of the hind paw induced by partial sciatic nerve ligation of the mice as a neuropathic pain model to investigate the analgesic effect of toad cake and toad-cake-containing herbal drugs. A co-treatment study with serotonin biosynthesis inhibitory drug 4-chloro-DL-phenylalanine methyl ester hydrochloride (PCPA), the catecholamine biosynthesis inhibitory drug ${\alpha}$-methyl-DL-tyrosine methyl ester hydrochloride (AMPT) or the opioid receptor antagonist naloxone hydrochloride was also conducted. Results: Analgesic effects in a mouse model of nociceptive pain and neuropathic pain were shown by oral administration of toad cake and toad-cake-containing herbal drugs. The effects of toad cake and toad-cake-containing herbal drugs disappeared upon co-treatment with PCPA, but not with AMPT or naloxone in the nociceptive pain model; the analgesic effect of toad-cake-containing herbal drugs also disappeared upon co-treatment with PCPA in the neuropathic pain model. Conclusion: Toad cake and toad-cake-containing herbal drugs have potential for the treatments of nociceptive pain and of neuropathic pain, such as post-herpetic neuralgia, trigeminal neuralgia, diabetic neuralgia, and postoperative or posttraumatic pain, by activation of the central serotonin nervous system.