• Archives of Pharmacal Research
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• 제27권6호
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• pp.581-588
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• 2004

A series of 2, 5-dihydroxychalcones and related compounds were synthesized, and their cyto-toxicities against tumor cell lines and human umbilical venous endothelial cells (HUVEC） eval-uated. It was found that chalcones, with electron-withdrawing substituents on an A ring, exhibited significant cytotoxicities. Among the synthesized compounds, 2'-chlbro-2, 5-dihydrox-ychalcone (9） was most potent, with an $IC_{50}$ value as low as $0.31{\;}{\mu\textrm{g}}/mL$. This compound also exhibited a significant cytotoxic selectivity toward HUVEC.

• Archives of Pharmacal Research
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• 제29권1호
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• pp.64-66
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• 2006

The methanolic extract of the aerial parts of Centipeda minima was found to show inhibitory activity on farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of 6-O-angeloylprenolin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the $IC_{50}$ value of 6-O-angeloylprenolin was 18.8 ${\mu}M$.

• Archives of Pharmacal Research
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• 제26권10호
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• pp.816-820
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• 2003

The chloroform extract of the aerial part of Limnophila geoffrayi showed antimycobacterial and antioxidant activities. Bioassay-guided fractionation has led to the isolation of the flavones nevadensin (5,7-dihydroxy-6,8,4'-trimethoxyflavone, 1) and isothymusin (6,7-dimethoxy-5,8,4'-trihydroxyflavone, 2). Both compounds 1 and 2 exhibited inhibition activity against Mycobacterium tuberculosis, with equal MIC value of $200{\;}\mu\textrm{g}/mL$. Only compound 2 exhibited antioxidant activity against the radical scavenging ability of DPPH, with the $IC_{50}$ value of $7.7{\;}\mu\textrm{g}/mL$. The crude hexane, chloroform and methanol extracts as well as the pure compounds 1 and 2 did not exhibit mutagenic activity in the Bacillus subtilis recassay.

• Archives of Pharmacal Research
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• 제28권11호
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• pp.1224-1227
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• 2005

Here we report the cytotoxic activity of three known compounds isolated for the first time from Corydalis pallida (Papaveraceae). An isoquinoline alkaloid, berberine, exhibited cytototoxic activity against two human cancer cell lines, HT-1080 (human fibrosarcoma) and SNU-638 (human stomach adenocarcinoma), with $IC_{50}$ values of 3.2 and 3.4 $\mu$g/mL, respectively. N­trans-feruloyltyramine and N-trans-feruloylmethoxytyramine were also isolated from this plant but were inactive.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.186-189
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• 2005

Anti-estrogenic activity of (-)-sesamin (1), helioxanthin (2), savinin (3), taiwanin C (4), and 3­(3,4-dimethoxybenzyl)-2-(3,4-methylenedioxybenzyl)butyrolactone (5) isolated from the root of Acanthopanax chiisanensis was tested using Ishikawa cells. Among them, compound 3 exhibited anti-estrogenic activity ($IC_{50}\;=\;4.86\;{\mu}M$).

• Archives of Pharmacal Research
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• 제22권1호
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• pp.9-12
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• 1999

A new glycoprotein was purified from the aqueous methanolic extract of the root bark of Morus alba which has been used as a component of antidiabetic remedy in Oriental Medicine. SDS-PAGE result shows that the molecular weight of the glycoprotein was approximately 20 kDa. This new glycoprotein was named as Moran 20K. The protein lowered blood glucose level in streptozotocin-induced hyperglycemic mice model and it also increased the glucose transport in cultured epididymis fat cells. The amino acid composition of the protein was analyzed, and the protein contained above 20% serine and cysteine such as insulin. The actual molecular weight of the protein was determined as 21.858 Da by MALDI-TOF mass spectroscopy.

• Archives of Pharmacal Research
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• 제26권5호
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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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• 제27권10호
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• pp.1037-1042
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• 2004

Study of the effects of the methanolic extract of Tagetes patula roots on blood pressure led to the isolation of well known citric (1) and malic acid (7) as hypotensive, and pyridine hydrochloride (4) as hypertensive constituents of the plant along with a new constituent, 2-hydroxy, 5- hydroxymethyl furan (9). Citric acid and malic acid caused 71% and 43% fall in Mean Arterial Blood Pressure (MABP) of rats at the doses of 15 mg/kg and 30mg/kg respectively while pyridine hydrochloride produced 34% rise in the MABP of rats at the dose of 30mg/kg. $LD_{50}\;and\;LD_{100}$ of citric acid in mice have been determined as 545 mg/kg and 1000 mg/kg, respectively.

• Archives of Pharmacal Research
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• 제8권4호
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• pp.213-220
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• 1985

From olibanum, acetylboswellic acid (I) and boswellic acid (II) were isolated as mixed crystals of $\alpha$-and $\alpha$-forms in the ratio of 1 to 2 and 1 to 4, respectively. And acetyl-11-keto$\beta$-boswellic acid (III) and 11-keto-$\beta$-boswellic acid (IV) were also isolated and their $\alpha$-forms were not found in olibanum by GC/selected ion monitoring MS technique. Contents of four compounds were determined.

• Archives of Pharmacal Research
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• 제16권4호
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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.