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        Anti-Inflammatory Mode of Isoflavone Glycoside Sophoricoside by Inhibition of Interleukin-6 and Cyclooxygenase02 in Inflammatory Response

        김병학,EunYongChung,Jae-ChunRyu,Sang-HunJung,KyungRakMin,YoungsooKim 대한약학회 2003 Archives of Pharmacal Research Vol.26 No.4

        Soy, high dietary intake for the oriental population, is a main source of isoflavonoids. Sophoricoside (SOP) an isoflavone glycoside was isolated from immature fruits of Sophora japonica (Leguminosae family) and its inhibitory effect on chemical mediators involved in inflammatory response was investigated in this study. SOP inhibited the interleukin (IL)-6 bioactivity with an IC50 value of 6.1 mM whereas it had no effects on IL-1b and TNF-a bioactivities. SOP was identified as a selective inhibitor of cyclooxygenase (COX)-2 activity with an IC50 value of 4.4 mM, but did not show inhibitory effect on the synthesis of COX-2. However, SOP had no effect on the production of reactive oxygen species including superoxide anions and nitric oxide. These results revealed that in vitro anti-inflammatory action of SOP is significantly different from that of genistein known as a phytoestrogen of soy products. This experimental study has documented an importance of dietary soy isoflavonoids as multifunctional agents beneficial to human health, and will help to clarify protective mechanisms of SOP against inflammatory conditions.

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        Quantitative Analysis of Tiropramide in Human Blood by Gas Chromatography with Nitrogen-Phosphorus Detedtor

        Oh-SeungKwon,Young-JinPark,Jae-ChunRyu,YounBokChung 대한약학회 2003 Archives of Pharmacal Research Vol.26 No.5

        The analytical method of antispasmodic agent tiropramide {(±)a-(benzoylamino)-4-[2-(diethylamino) ethoxy]- N, N-dipropylbenzenepropanamide hydrochloride} was developed by gas chromatography/ nitrogen-phosphorus detector (GC/NPD) in human plasma. Two kinds of tiropramide tablets were orally administered to volunteers by Latin square crossover design, and blood was withdrawn as designed schedule. The plasma of 1 mL was loaded on Sep-pak C18 cartridge and eluted with methanol after washing with 30% methanol. The residue dissolved in 100 mL of methanol after evaporation was analyzed by GC/NPD. Precision (CV%) of intra-day was located within 2.6% and accuracy was less than 9.7%. Inter-day precision was below 8.7% and accuracy was relatively good as less than 14%. Plasma samples obtained from human volunteers were analyzed for the determination of tiropramide concentration by using this method. The method was sensitive, rapid and suitable enough to be applied for pharmacokinetic and bioequivalence studies of tiropramide in human volunteers.

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        Identification of New Urinary Metabolites of Byakangelicin, a Component of Angelicae dahuricae Radix, in Rats

        권오승,송윤선,Kuk-HyunShin,Jae-ChunRyu 대한약학회 2003 Archives of Pharmacal Research Vol.26 No.8

        Byakangelicin, 9-(2,3-dihydroxy-2-methylbutoxy)-4-methoxy-7H-furo[3,2-g][l]benzopyran-7-one (BKG), a component of Angelicae dahuricae Radix, is considered to be an inhibitor of aldose reductase for the treatment of diabetic cataract. An analytical method for the isolation of BKG developed by high-performance liquid chromatography has been reported. No literature on the metabolism of BKG, however, has been found. With the purpose of identifying new metabolites of BKG, BKG (100 mg/kg) was orally administered to Sprague-Dawley rats via a gavage. Using a metabolic cage, urine was collected for 24 h, and the urine samples were extracted by liquid-liquid extraction. For structural identification of new urinary metabolites of BKG, various instrumental analyses were conducted by gas-chromatography/mass spectrometry, high-performance liquid chromatography/diode array detector, liquid chromatography/mass spectroscopy with thermospray interface and 1H nuclear magnetic resonance spectroscopy. Two metabolites produced from the O-demethylation or O-dealkylation of BKG were newly identified, and another new but unknown metabolite was assumed to be the hydroxylated form of BKG. These results indicate that the major metabolic products of BKG are formed by O-demethylation or O-dealkylation of BKG side chains. ODemethylation,

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