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Archives of pharmacal research : a publication of ... 19건

  1. [국내논문]   S-Nitrosylation of Sulfhydryl Groups in Albumin by Nitrosating Agents  

    Park, Jeen-Woo (Department of Biochemistry, College of Natural Sciences, Kyungpook National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 1 - 5 , 1993 , 0253-6269 ,

    초록

    The reaction of sulfhydryl groups in human serum ablumin with bacteriostatic and hypotensive notrosating agents such as sodium nitorprusside and sodium nitrite has been examined. The low reactivity of sodium nitroprusside to sulfhydral groups in albumin has been observed and the sterical inaccessilibility of the agent site which sulfhydryl group resides was implicated. The reaction of sodium nitrite with albumin was highly influenced by pH and little reactivity was observed at physiological pH. On the other hand, the reaction between albumin and S-nitrosoglutatione, an intermediate induced from the reaction of glutathione and nitrosating agents, resulted in the rapid decrease of free sulfhydryl groups in albumin. S-Nitrosylation of the sulfhydryl group by S-nitrosoglutathione and the subsequent production of mixed disulfide is the probable route of modification. In the physiological system, S-nitroso-glutathione may act as an active intermediate in expressing reacivity of nitrosating agents to sulfhydryl groups in albumin.

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  2. [국내논문]   The Effects of KR-10876, a new Quinolone Antimicrobial Agent, on the Central Nervous System  

    Kim, Eun-Joo (Korea Research Institute of Chemical Technology ) , Cha, Shin-Woo (Korea Research Institute of Chemical Technology ) , Shin, Hwa-Sup (Korea Research Institute of Chemical Technology ) , Roh, Jung-Koo (Korea Research Institute of Chemical Technology ) , Park, Myoung-Whan (Korea Research Institute of Chemical Technology ) , Kim, Wan-Joo (Korea Research Institute of Chemical Technology)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 6 - 12 , 1993 , 0253-6269 ,

    초록

    To evaluate KR-10876, a new fluoroquinolone antibacterial agent, its effects on the central nervous system(CNS) were investigated in mmice as part of phamacological study, and the results were compared with those for ciprofloxacin and ofloxacin, two prototypes of quinolone antiabctrial agents. All the parameters indicative of CNS function and acute toxicity were measured by close observation of the animals at regular time intervals after oral treatment of test compounds. KR-10876 did not have any effect on the parameters measured at lower does (100, 300 mg/kg, p.o.), it caused ptosis, suppressed spontaneous locomotor activity, hypothemia, and prolonged hexobarbital-induced sleeping time. KR-10876 also had a slight effect on motor coordination only at high dose. Simialr to ciprofloxacin, KR-10876 did not protect mice from pentylenetetrazol-strychnine-, and electroshock-inducedl convulsions at doses tested. These findings demonstrate that KR-10876 affects CNS functions only at high doses. The rank order for effects is ofloxacin $\le$ KR-10876>ciprofloxacin.

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  3. [국내논문]   Effects of naturally occurring furanocoumarins on lipid peroxidation and carbon tetrachloride induced hepatotoxicity in mice  

    Shin, Kuk Hyun , Woo, Won Sick , Moon, Ki Ho , Yoo, Seung Jo
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 13 - 17 , 1993 , 0253-6269 ,

    초록

    To evaluate KR-10876, a new fluoroquinolone antibacterial agent, its effects on the central nervous system(CNS) were investigated in mmice as part of phamacological study, and the results were compared with those for ciprofloxacin and ofloxacin, two prototypes of quinolone antiabctrial agents. All the parameters indicative of CNS function and acute toxicity were measured by close observation of the animals at regular time intervals after oral treatment of test compounds. KR-10876 did not have any effect on the parameters measured at lower does (100, 300 mg/kg, p.o.), it caused ptosis, suppressed spontaneous locomotor activity, hypothemia, and prolonged hexobarbital-induced sleeping time. KR-10876 also had a slight effect on motor coordination only at high dose. Simialr to ciprofloxacin, KR-10876 did not protect mice from pentylenetetrazol-strychnine-, and electroshock-inducedl convulsions at doses tested. These findings demonstrate that KR-10876 affects CNS functions only at high doses. The rank order for effects is ofloxacin $\le$ KR-10876>ciprofloxacin.

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  4. [국내논문]   Effects of Natrually Occurring Furanocoumarins on Lipid Peroxidation and Carbon Tetrachloride Induced Hapatotoxicity in Mice  

    Shin, Kuk-Hyun (Natural Products Research Institute, Seoul National University ) , Woo, Won-Sick (Natural Products Research Institute, Seoul National University ) , Moon, Ki-Ho (Natural Products Research Institute, Seoul National University ) , Yoo, Seung-Jo (College of Pharmacy, Sungkyukwan University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 13 - 17 , 1993 , 0253-6269 ,

    초록

    Several naturally occurring furanocoumarins significantly inhibited microsomal lipid peroxidation not only mediated by endogeneous iron and NADPH but also initiated by $CCL_4$ metabolites, phellopterin, a potent inhibibitor of cytochrome p-450, exhibited an almost complete inhibition of $CCL_4$ -induced hepatotoxicity as measured by sGPT activity 24 hr after $CCL_4$ intoxication, whereas other furanocoumarins such as imperation, byakangelicin and oxypeucedanin methanolate exerted no protective effect. When compared with other cytochrome P-450 inhibitors(SKF-52A, AIA) and silymarin given at the same dose level $(ED_{50})$ , phellopterin still showed a significant inhibition of hepatotoxicity which was even stronger than that of AIA, known as a typical suicide inhibitor. Phellopterin was partially effective when given 30 min after $CCL_4$ treatment. Repeated administrations of phellopterin, however, resulted in a complete loss of the protection against $CCL_4$ -induced hepatotoxicity.

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  5. [국내논문]   Antiinflammatory Activity of Flavonoids:Mouse Ear Edema Inhibition  

    Kim, Hee-Kee (College of Pharmacy, Kangweon National University ) , Namgoong, Soon-Young (College of Pharmacy, Kangweon National University ) , Kim, Hyun-Pyo (College of Pharmacy, Kangweon National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 18 - 24 , 1993 , 0253-6269 ,

    초록

    In this inverstigation, the various flavonoid aglycones were evaluated for their inhibitory activities against croton-oil or arachidonic acid induced mouse ear edema by oral or topical administration. The compounds tested were thirteen derivatives of flavan-3-ol(catechin and epicatechin), flavanone (flavanone and naringenin), flavone (flavone, chrysin and apigenin), flavonol(favonol, galangin, quercetin and morin) and isoflavone (biochanin A and 2-carbethoxy-5,7-dihydroxy-4'-methoxyisoflavone), along with hydrocortisone, indomethacin, 4-bormophenacyl bromide, nordihydroguaiaretic acid and phenidone as positive controls. A(isoflavone) were found to show broad inhibitoty activities (14-52%) against croton-oil or arachidonic acid induced ear edema by oral or topical application at the dose of 2 mg/mouse, although they showed less activity than hydrocortisone (26-88%) or indomethacin (36-80%). Flavonoid agtlycones tested showed higher activity when aplied topically than by the oral administration. It was also found that they inhibited arachidonic acid induced edema more profoundly than croton-oil induced edema by topical application. In arachidonic acid induced edema when applied topically, flavone derivatives such as flavone, chrysin and apigenin were revealed to be the good inhibitory agents in addition to flavonols and isoflavones. When quercetin and biochanin. A were selected for evaluating in carrageenan induced rat pleurisy and biochanin both flavonoids showed antiinflammatory activity at the dose of 70 mg/kg by the oral adminis-tration. All of these results revealed that flavonoid aglycones, especially 5,7-dihydroxy-flavonols having hydroxyl group(s) in B-ring and biochanin A (isoflavone) possessed in vivo antiinflammatory activity.

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  6. [국내논문]   Antiinflammatory Activity of Naturally Occurring Flavone and Flavonol Glycosides   피인용횟수: 1

    Lee, Song-Jin (College of Pharmacy, Kangweon National University ) , Son, Kun-Ho (Dept. Food and Nutrition, Andong National University ) , Chang, Hyeun-Wook (College of Pharmacy, Yeongnam University ) , Do, Jae-Chul (College of Pharmacy, Yeongnam University ) , Jung, Keun-Young (College of Pharmacy, Yeongnam University ) , Kang, Sam-Sik (Natural Products Research Institute, Seoul National University ) , Kim, Hyun-Pyo (College of Pharmacy, Kangweon National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 25 - 28 , 1993 , 0253-6269 ,

    초록

    Our previous report demonstrated that certain flavonoid aglycones such as apigenin (flavone), quercetin, morin (flavonols), and biochanin A (isoflavone) showed in vivo antiinflammatory activity via topical and oral routes of adminstation. As a continual study, the various flavonoid glycosides have been evaluated in mouse ear edema assay using archidonic acid or croton-oil as a inflammagen. Flavonoids were orally administered (2 mg/mouse) and ear edema inhibition was measured. Significant antiinflammatory activities were found esepcially in flavone and flavonol glycosides (15-29% inhibition) although the flavonoid derivatives tested showed less antiinflammatory activity than hydrocortisone or indomethacin. Chalcone and flavanone derivatives were not significantly active. And in general, flavonol glycosides of kaempferol-type were found to have a higher oral antiinflammatory activity than that of flavonol glycosides of quercetin-type in mice.

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  7. [국내논문]   Antiinflammatory Principle of Bupleurum longiradiatum Roots  

    Woo, Won-Sick (Natural Products Research Institute, Seoul National University ) , Choi, Jae-Soo (Department of Nutrition and Food Science, National Fisheries University of Pusan)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 29 - 31 , 1993 , 0253-6269 ,

    초록

    A methanol extract of the roots of bupleurum longiradiatum (Umbelliferar) showed antiinflammatory activity in rats. Hexane, chloroform, butanol, and aqueous fractions from the methanol extract were tested with the result that only the hexane fraction exhibited positive activity. Fractionation of the hexane extract resulted in isolation of arborinone as an active principle.

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  8. [국내논문]   Triterpenoids from the Roots of Dipsacus asper  

    Jung, Keun-Young (College of Pharmacy, Yeungnam University ) , Son, Kun-Ho (Department of Food and Nutrition, Andong National University ) , Do, Jae-Chul (College of Pharmacy, Yeungnam University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 32 - 35 , 1993 , 0253-6269 ,

    초록

    Four titerpenoids were isolated from the roots of Dipsacus asper. On the basis of chemical and spectral evidence, the structures of these compounds have been elucidated to be hederagenin(1), hederagenin $3-O-\alpha-L-$ arabinoside(2). $3-O-\alpha-$ L-arabinopyranosyl hederagenin $2B-O-\beta$ -D-glucopyranosyl ester(3) and hederagenin $28-O-\beta$ -D-glucopyranosyl(1->6)- $\beta$ -D-glucopyranosyl ester(4). The new glycoside, 4, was named dipsacus saponin A.

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  9. [국내논문]   Toxic Components of Auricularia polytricha  

    Kim, Ha-Won (Department of Microbial Chemistry, College of Pharmacy, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 36 - 42 , 1993 , 0253-6269 ,

    초록

    To find biologically active components of the higher fungi of Korea, the carpophores of Auricularia polytricha, a well-known edible mushroom, were extracted with 0.14 M NaCl solution. The extract was successively fractionated by adding ammonium sulfate at various concentrations, and the respective precipitates were separated by centrifugation, then dialyzed and freeze-dried. When a does of 60 mg/kg of each was injected i.p. into ICR mice, the fraction which precipitated at 20% ammonium sulfate showed the highest toxicity, killing seven out of seven mice within two days. The fraction obtained at 40% ammonium sulfate showed the second highest toxicity. The two fractions were named auritoxin I and II after the genus name. However, they Nere shown to have nearly identical composition by physicochemical and 6.8% protein. The polysaccharide moiety was found to have 12.3% $\alpha$ -linkage and 87.7% $\beta$ -linkage and to be a heteromannoglucan consisting of 45.1% glucose, 435 mannose and 11.0% xylose. The protein moiety contained ten amino adids. The molecular weight of the toxin was $1.5\times10^6$ dalton by Sepharose CL-4B gel filtration. The modian lethal doses of auritoxin in mice were 56.4, 157.2 and 454.6 mg/kg by i.p., s.c. and p.o.administrations, respectively. The signs of intrxication were convulsion during the first 30 minutes after the injection, coma or sleeping within an hour, termor, lacrimation, nasal bleeding congestion, and death in 24 hours. Smong the various organs, the spleen was found to be enlarged remarkably. Human platelet aggregation was inhibited by the addition of auritoxin. The activity of malic dehydrogenase in vitro was inhibited by the toxin.

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  10. [국내논문]   Studies on Controlled Release of Indomethacin from PVA Hydrogel  

    Lee, Chi-Ho (College of Pharmacy, Pusan National University ) , Lee, Kyoung-Jin (College of Pharmacy, Pusan National University ) , Park, Ae-Jin (College of Pharmacy, Pusan National University ) , Shin, Young-Hee (College of Pharmacy, Kyoungsung University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.16 no.1 ,pp. 43 - 49 , 1993 , 0253-6269 ,

    초록

    The polyvinyl alcohol (PVA) hydrogel containing 1-methy-2-pymolidinone (MP) and sorbitol was preapred by the freeze and thaw method. The release rate of indomethacin from PVA hydrogel was used as a criterion for deciding the optimum formula of hydrogel using the computer optimization technique. The hydrogel of optimum formula was composed of PVA (10 w/v%), MP (0 w/v%) and sorbitol (40 w/v%) and the release rate of indomethacin was 1.981 $\mu$ g/ml $\cdot{min}^{1/2}$ .

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