• Archives of Pharmacal Research
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• v.16 no.1
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• pp.43-49
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• 1993

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$\cdot{min}^{1/2}$.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.782-784
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• 1998

Ginseng total saponin (GTS) can modulate dopaminergic activity at both presynaptic and postsynaptic dopamine receptors (Kim et al, 1998). The present study investigated t he effect of GTS on the bovine adrenal tyrosine hydroxylase (TH), which catalyze L/tyrosine to DOP. GTS inhibited the bovine adrenal TH by 42.4, 51.5 and 55.3% at concentrations of 40, 80 and 100${\mu}g$/ml, respectively. The IC50 value of GTS was 77.5${\mu}g$/ml. GTS exhibited noncompetitive inhibition with a substrate L-tyrosine. The Ki value was 155${\mu}g$/ml.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.734-737
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• 1998

The hexane fractions from methanolic extracts of Anetheum graveolens L. (Umbelliferae) and Acorus gramineus Soland. (Araceae) revealed potent inhibitory activities against the resistance of multi-drug resistant Staphylococcus aureus SA2 when combined with ampicillin (Am) or chloramphenicol (Cm). As active principles, carvone and the liquid mixture containing carvone from Anetheum graveolens L. and a liquid mixture mainly consisting of benzoic acid phenyl-methyl ester (benzyl benzoate) from Acorus gramineus Soland. were identified. They showed resistance inhibition at the level of 20-50${\mu}g$/ml when combined with 100 or ${\mu}g$/ml of Am or Cm, respectively.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.729-733
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• 1998

The crude extract of Streptomyces sp. strain KM86-9B, isolated from a marine sponge, displayed significant inhibition on topoisomerase I activity. Investigation of the ca usative components by bioactivity-directed fractionation resulted in the isolation of a series of iso- and anteiso-fatty acids.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.718-722
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• 1998

Scopoletin (7-hydroxy-6-methoxycoumarin), a coumarin, was isolated from the aerial part of Solanum lyratum Thunb. by the activity-guided fractionation employing carbon te trachloride-intoxicated primary cultured rat hepatocytes as a screening system. Its hepatoprotective activity was first evaluated by measuring the release of glutamic pyruvic transaminase and sorbitol dehydrogenase from carbon tetrachloride-intoxicated rat hepatocytes into the culture medium. Scopoletin significantly reduced the releases of glutamic pyruvic transaminase and sorbitol dehydrogenase from the carbon tetrachloride-intoxicated primary cultured rat hepatocytes by 53% and 58%, respectively, from the toxicity in a dose-dependent manner over concentration ranges of 1mcM to 50mcM. Further studies revealed that at the concentration of 10mcM, scopoletin significantly preserved glutathione content by 50% and the activity of superoxide dismutase by 36% and also inhibited the production of malondialdehyde to the degree as seen in the control.

• Archives of Pharmacal Research
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• v.23 no.1
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• pp.26-30
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• 2000

The enantiomers of the bronchodilator terbutaline were separated by reversed-phase high performance liquid chromatograhy after derivatization with 2,3,4,6-tetra-O-acetyl-\beta-D-glucopyranosyl isothiocyanate(GITC) reagent. The derivatization proceeded quantitatively within 1 h at room temperature. The corresponding diastereomeric thiourea derivatives were well resolved on an ODS column with acetonitrile-acetate buffer as a mobile phase. Elution orders of the diastereomers were confirmed by derivatization of R-(-)-terbutaline and S-(+)-terbutaline which were collected by semi-preparative chiral HPLC using Sumichiral OA-4700 column. The native fluorescence of terbutaline was quenched by derivatization with GITC. The detection limit was 25ng when monitored at UV 278 nm.

• Archives of Pharmacal Research
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• v.23 no.6
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• pp.626-632
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• 2000

Brazilin, an active principle of Caesalprenia sappan, was examined for its immunopotentiating effects in multiple low dose streptozotocin (MLD-STZ) induced type diabetic mice. Brazilin was intraperitoneally administered for 5 consecutive days to MLD-STZ induced type 1 diabetic mice. Delayed type hypersensitivity, Con A-induced proliferation of splenocytes and mixed lymphocyte reaction, which had been decreased in diabetic mice, were significantly recovered by the administration of brazilin. Brazilin increased IL-2 production without affecting suppressor cell activity. Con A-induced and IL-2-induced expression of high affinity IL-2 receptors were also enhanced by brazilin. These results indicate that brazilin augments cellular immune responses, which are suppressed in the MLD-STZ induced type I diabetic mice, by increasing IL-2 production and responsiveness of immune cells to IL-2.

• Archives of Pharmacal Research
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• v.23 no.6
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• pp.592-598
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• 2000

A lectin (agglutinin, VCA) from Korean mistletoe (Viscum album L. coloratum) was isolated by affinity chromatograpy on a asialofetuin-Sepharose 4B. The molecular weights of A- and B-chains of VCA were different from those of VAAS. The VCA recognized the antibody of VAAs in the Western blot analysis and ELLA system. We also investigated the synergistic effects of the components in mistletoe by dividing the extract into different molecular weight fractions.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.831-836
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• 2002

A new and two known lupane-triterpene glycosides were isolated from the hot MeOH fraction of the leaves of Acanthopanax gracilistylus W. W. Smith. Based on the physical properties and spectroscopic data, their chemical structures were determined as acankoreoside A (1), acankoreoside D (2), and $3{\alpha}-hydroxy-lup-23-al-20(29)-en-28-oic$ acid $28-O-{\alpha}-L-rhamnopyranosyl-(1{\rightarrow}4)-{$beta}-D-glucopyranosyl-(1{\rightarrow}6)-{\beta}-D-glucopyranosyl$ ester (3), respectively. To our best knowledge, compand 3 appears to be novel, which was named as wujiapioside A.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.532-534
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• 2003

Kojic acid dimethyl ether (1), and the known kojic acid mono methyl ether (2), kojic acid (3) and phomaligol A (4) have been isolated from the organic extract of the broth of the marine-derived fungus Altenaria sp. collected from the surface of the marine green alga Ulva pertusa. The structures were assigned on the basis of comprehensive spectroscopic analyses. Each isolate was tested for its tyrosinase inhibitory activity. Kojic acid (3) was found to have significant tyrosinase inhibitory activity, but compounds 1, 2, and 4 were found to be inactive.