• Archives of Pharmacal Research
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• v.15 no.4
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• pp.275-282
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• 1992

The present work was designed to investigate the effects of barzilin on ConAinducedd TCGF release, responsiveness to standardd IL-2, and mitogens-induced proliferation of splenocyte when administered intraperitoneally to 8 week-old C57BL/6 mice for 2 consecutive days. Immunological tests were performed 72 hours after the treatment of brailin. The administration of 50 mg/kg brazilin caused a noticeable increase in TCGF release and responsiveness to standard II-2 but inhibited mitogens-induced proliferation of splenocyte. These results that brazilin is able to modular immunological functions despite of its inhibitory effect on mitogen induced cell proliferation.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.285-288
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• 2002

Four compounds of a coumarin, a steroid and two flavonoids were isolated from the herba of Artemisia apiacea by open column chromatography. Their structures were elucidated as artemicapin C, apigenin, daucosterol and cacticin by chemical and spectroscopic analysis. This is the first report of the isolation of these compounds from this plant.

• Archives of Pharmacal Research
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• v.28 no.2
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• pp.142-150
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• 2005

The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

• Archives of Pharmacal Research
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• v.22 no.4
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• pp.367-371
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• 1999

Effects of several durgs on rabbit renal proximal tubules were examined for the applicability of renal dipeptidase (RDPase, EC 3. 4. 13. 11) release as a model system to study nephrotoxicity. The proximal tubule prepared by the method of Taub (1990) released RDPase spontaneously in the control experiment which was confirmed by Western blotting. RDPase was also released form cisplatin, lipopolysaccardie (LPS), and indomethacin-treated tubules. Gentamicin inhibited RDPase release in a concentration-dependent manner. This RDPase release system may not be a general model to screen nephrotoxicity but could be a useful source of RDPase purification in a simple and inexpensive way.

• Archives of Pharmacal Research
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• v.16 no.4
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• pp.295-299
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• 1993

Human renal dipeptidase (RDPase) was purified from surgically removed kdneys of renal stone aptients by affinity chromatography using its specific inhibitor, cilastain, as the ligand. The partial purified RDPase of 6 mg exhivited specific activity of 99.4 unit/mg with 2, 029 fold purification. it was composed of a slow moving major band (96%) and a fast moving minor band (4%). The minor band was not a contaminant as it showed a dipeptidase-specific activity. The kinetic parameters determined with glycyldehydrophenylalanine (Gdp) as synthetic substrate were Vmax, $322.6\;\mu{mol/min/mg}$ and km, 0.120 mM. This experiment provided biochemical evidences that sugically removed, nonfunctional kidneys in respect of glomerular filtration still retained high activity of renal dipeptidase.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.449-452
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• 2003

Systematic fractionation of Angelica gigas roots led to the isolation of linear furano(pyrano)coumarins such as bergapten (1), decursinol angelate (2), decursin (3), nodakenetin (4) and nodakenin (5). The antibacterial activities of those compounds against pathogenic bacteria were investigated. Among the compounds tested, decursinol angelate (2) and decursin (3) exhibited significant antibacterial activity against Bacillus subtilis with the minimum inhibitory concentrations (MICs) of 50 and $12.5{\;}{\mu}g/mL$, respectively.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.738-741
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• 2004

Three lignans isolated from the roots of A. koreanum (Araliaceae), namely eleutheroside E(1), tortoside A(2), and hemiariensin(4), were evaluated for their ability to inhibit NFAT transcription factor. Of these compounds, compound 4, possessing a diarylbutane skeleton, exhibited potent inhibitory activity against NFAT transcription factor (($IC_{50}$ ： 36.3${\pm}2.5{\mu}\textrm{M}$). However, the activities of 1 (($IC_{50}$：＞500 11M) and 2 (($IC_{50}$： 136.1 ${\pm}9.4\mu\textrm{M}$), which possess bisaryldioxabicy-clooctane skeletons, were lower. As the lignan derivatives of the same skeletons, hinokinin (5) and (-)-yatein (6) with diarylbutane skeletons and(＋)-syringaresinol (3) with a bisaryldioxabicy-clooctane skeleton were also studied for their inhibitory effects on NFAT transcription factor.

• Archives of Pharmacal Research
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• v.27 no.3
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• pp.278-282
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• 2004

A number of 8-arylflavones have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. 8-Arylflavones were obtained from commercially available chrysin via two different synthetic pathways. Most 8-arylflavones exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Functional group replacement at the 8-position of wogonin from methoxy to aryl group caused loss of inhibitory activity. Our present results imply that the functional group at the 8-position of flavones seems to play very important roles for bioactivity.

• Archives of Pharmacal Research
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• v.26 no.5
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• pp.345-350
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• 2003

5,7-Dihydroxyflavones and their Ο-methylated flavone analogs were prepared and evaluated their anti-inflammatory activity to decipher the structure-activity relationships. Most of the analogs were achieved from 2,4,6-trihydroxyacetophenone in 4 steps. 5,7-Dihydroxy-4 -methoxyflavone (4c) and 7-hydroxy-4 ,5-dimethoxyflavone(6c) were prepared following a different synthetic pathway. Among the synthetic flavones tested, 5-hydroxy-7-methoxyflavone analogs (3a-3e) showed moderate inhibitory activities of $PGE_2$ production from LPS-induced RAW 264.7 cells.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.541-545
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• 2001

The evaluation of the anti-inflammatory analgesic and antipyretic activities of loxoprofen sodium given in intramuscular route was investigated as compared to oral application in rats and mice. The intramuscular $ED_{50}$ values of loxoprofen sodium in carrageenan edema and vascular permeability tests are 1.15 and 7.8 mg/kg, respectively, which represent more potent than in case of oral application. Its therapeutic effects in adjuvant arthritis were shown at 6 mg/kg l.m. and 3mg/kg p.o. Analgesic effect was shown to be more potent as given intramuscularly. Similar potency of antipyretic effects was shown in both administration routes. Considerably weak gastric damages were observed in intramuscular application.