• 생약학회지
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• 제20권3호
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• pp.180-187
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• 1989

Systematic pharmacological studies on powdered whole part of unossified antler obtained from Cervus nippon Temminck var. mantchuricus have been carried out in mice and rats. Powdered antler, with a single oral administration, showed a very weak acute and subacute toxicity; its MLD being >5g/kg orally in mice. On daily oral treatments of the antler for 14 days, it did not cause any significant differences in body weight gain, various organ weights and serum transaminase activities compared to those of the control rats. Powdered antler, with a single oral administration, showed a remarkable analgesic activity as evaluated by writhing syndrome and tail-pressure test, a weak CNS depressant activity as well as a weak immunopotentiating action as evaluated by carbon clearance test in mice. Powdered antler, with repeated treatments, showed a moderate antifatigue effect against immobilized stress and showed significant increases in both adrenal weight and its ascorbic acid content in rats, suggesting that the mode of antifatigue effect of antler is related to adrenal and its components.

• Biomolecules & Therapeutics
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• 제6권2호
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• pp.159-164
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• 1998

General pharmacological properties of recombinant human parathyroid hormone (hPTH) were examined. The administration of hPTH (7, 35 and 175 lU/kg sc) in mice had no effects in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazol solution. hPTH (9 and 44 lU/kg, sc) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration, and it did not influence the responses produced by injection of acetylcholine or epinephrine. It showed no direct effect at 4.4$\times$10$_{-2}$IU/ml in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also showed no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence intestinal propulsion at the doses of 7,35 and 175 lU/kg sc in mice. This drug exhibited no effect on urinary excretion at the doses of 7 and 35 lU/kg sc in rats. However, at a dose of 175 lU/kg sc, it showed a decreased urination along with decreased excretion of potassium, sodium and chloride ion. These results indicate that hPTH does not exert any of serious pharmacological effects except the inhibition of urination at a highest dose used.

• Biomolecules & Therapeutics
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• 제7권1호
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• pp.89-96
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• 1999

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.

• Biomolecules & Therapeutics
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• 제4권2호
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• pp.154-161
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• 1996

General pharmacological properties of LB-00014, an erythropoietin which was produced by recombinant DNA technique in Biotech Research Institute, LG Chemical Ltd. were examined. The administration of LB-00014 (60, 600, 6000 IU/kg, iv) in mice had no effect in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazole solution. LB-00014 (60, 600, 6000 IU/kg, iv) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration rates, and it did not influence the responses produced by injection of acetylcholine or epinephme. The administration of LB-00014 (601, 600, 6000 IU/kg, iv) in rats had no effect on the plasma prothrombin time, activated partial thromboplastin time and hemolytic action. The platelet aggregation induced by collagen in human plasma was not influenced by LB-00014 (10, 100, 1000 lU/kg, iv). It showed no direct effect at 100 and 1000IU/m1 in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also had no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence gastric secretion, pH and acid output at 6000 IU/kg, iv in rats, but showed a significant increase in intestinal propulsion of mice at 6000 IU/kg, iv. Its administration (60, 600, 6000 lU/kg, iv) caused no effect on urine and electrolyte excretion in rats. These results indicate that LB-00014 does not exsert any of serious pharmacological effects.

• 약학회지
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• 제38권5호
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• pp.586-594
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• 1994

The general pharmacological effects of DWQ-013, a new synthetic quinolone antibacterial agent, were examined on the central nervous system in experimentral animals and the following results were obtained. Drug interaction of DWQ-013 with theophylline, fenbufen and nonsteroidal antiinflammatory drugs was also examined. DWQ-013 decreased touch escape effect on the general behavior and decreased body temperature at a concentration of 1000 mg/kg in mice. But DWQ 013 had no effect on the locomotor activity, rotarod perfomance and traction test in mice. Furthermore, DWQ-013 increased pentobarbital-induced sleeping time and affected the onset time in acetic acid-induced writhing test in mice. DWQ-013 reduced onset time and death time on strychnine-induced convulsions and death time on pentylenetetrazole-induced convulsions at a concentration of 1000 mg/kg in mice. But, the drug had no effect on the electroshock. DWQ-013 did not interact with fenbufen and any other NSAIDs but it did interact with theophylline. From these results, it could be suggested that DWQ-013 had less pharmacological effect than other quinolones on the central nervous system.

• Biomolecules & Therapeutics
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• 제18권2호
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• pp.197-204
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• 2010

To establish the anti-inflammatory activity of the total flavonoid fraction of the root barks of Broussonetia papyrifera (EBP) and a new formula, the ethanol extract of the root barks of B. papyrifera was fractionated with ethylacetate, yielding the hydrophobic prenylated flavonoid-enriched fraction. EBP and the ethanol extract of the whole Lonicera japonica (ELJ) plant were then mixed at a ratio of 1:1 (w/w) to give a new preparation (BL) in the hope of obtaining an optimal formula with a higher anti-inflammatory activity. Evaluation of the effects of these preparations on A23187-treated rat basophilic leukemia (RBL-1) cells revealed that EBP potently inhibited 5-lipoxygenase (5-LOX), while ELJ showed weak inhibition. Additionally, the mixture (BL) clearly showed stronger inhibitory effects against 5-LOX than either preparation alone. These preparations also inhibited cyclooxygenase-2-catalyzed $PGE_2$ and inducible nitric oxide (NO) synthase-catalyzed NO production by lipopolysaccharide-treated RAW 264.7 cells. When tested against arachidonic acid-induced mouse ear edema, EBP showed strong inhibitory activity at doses of 5-200 mg/kg when administered orally, but BL had obviously stronger inhibitory effects. When tested against ${\lambda}$-carrageenan-induced paw edema in mice, BL showed a potent and synergistic anti-inflammatory effect. In addition, in the acetic acid-induced writhing test, BL was found to have strong analgesic activity at 50-400 mg/kg. Taken together, these results indicate that each of these preparations exert anti-inflammatory activity in vitro and in vivo. In particular, BL showed stronger anti-inflammatory activity than EBP, and these anti-inflammatory effects were partially related to the inhibition of eicosanoid and NO production. BL may be useful for the treatment of human inflammatory disorders.

• Preventive Nutrition and Food Science
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• 제22권3호
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• pp.157-165
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• 2017

Fruits of Sonneratia apetala (Buch.-Ham.), (English: mangrove apple, Bengali: keora) both seeds and pericarps, are largely consumed as food besides their enormous medicinal application. The fruit seeds have high content of nutrients and bioactive components. The seeds powder of S. apetala was successively fractionated using n-hexane, diethyl ether, chloroform, ethyl acetate, and methanol. The fractions were used to evaluate antibacterial, anti-diarrhoeal, analgesic, and cytotoxic activities. Methanol fraction of seeds (MeS) stronly inhibited Escherichia coli strains, Salmonella Paratyphi A, Salmonella Typhi, Shigella dysenteriae, and Staphylococcus aureus except Vibrio cholerae at $500{\mu}g/disc$. All the fractions strongly inhibited castor oil induced diarrhoeal episodes and onset time in mice at 500 mg extract/kg body weight (P<0.001). At the same concentration, MeS had the strongest inhibitory activity on diarrhoeal episodes, whereas the n-hexane fraction (HS) significantly (P<0.05) prolonged diarrhoeal onset time as compared to positive control. Similarly, HS (P<0.005) inhibited acetic acid induced writhing in mice at 500 mg extract/kg, more than any other fraction. HS and diethyl ether fractions of seed strongly increased reaction time of mice in hot plate test at 500 mg extract/kg. All the fractions showed strong cytotoxic effects in brine shrimp lethality tests. Gas chromatography-mass spectrometry analysis of HS led to the identification of 23 compounds. Linoleic acid (29.9%), palmitic acid (23.2%), ascorbyl palmitate (21.2%), and stearic acid (10.5%) were the major compounds in HS. These results suggest that seeds of S. apetala could be of great use as nutraceuticals.

• 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.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.117-124
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• 1997

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.

• Biomolecules & Therapeutics
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• 제17권3호
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• pp.263-269
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• 2009

4-Hydroxybenzaldehyde, a phenolic compound found in a variety of natural sources, was previously shown to contain anti-inflammatory and related anti-angiogenic and anti-nociceptive activities. The present work was designed to assess some pharmacological activities of 2,4-dihydroxybenzaldehyde (DHD), an analogue of 4-hydroxybenzaldehyde. DHD exhibited a significant inhibition in the chick chorioallantoic membrane (CAM) angiogenesis, and its $IC_{50}$ value was $2.4\;{\mu}g/egg$. DHD also contained in vivo anti-inflammatory activity using acetic acid-induced permeability and carrageenan-induced air pouch models in mice. In the air pouch model, DHD showed significant suppression in exudate volume, number of polymorphonuclear leukocytes and nitrite content. DHD showed an anti-nociceptive activity in the acetic acid-induced writhing test in mice. It also suppressed enhanced production of nitric oxide (NO) and elevated expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. It was able to slightly decrease the level of reactive oxygen species in the stimulated macrophages. DHD at the used concentrations couldn't modulate the viabilities of RAW264.7 cells. Taken together, like 4-hydroxybenzaldehyde, DHD contains anti-angiogenic, anti-inflammatory and anti-nociceptive activities.