• Archives of Pharmacal Research
• /
• 제28권6호
• /
• pp.730-735
• /
• 2005

Nine polymorphic modifications of doxazosin mesylate have been obtained by recrystallization in organic solvents under variable conditions. Different polymorphs of doxazosin mesylate were characterized by powder X-ray crystallography diffractometry (PXRD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TG). Transformation of Form 1 and Form 2 was not occurred in three relative humidities ($0\%$, $51\%$, and $99\%$) at 20$\pm$0.5 for 30 days.

• Archives of Pharmacal Research
• /
• 제12권4호
• /
• pp.295-299
• /
• 1989

Two novel steroidal saponins designated as spicatosides A(1) and B(2) were isolated from the tubers of Liriope spicata and their structures were elucidated as 25(S)-rus-cogenin -1-0- fJ - D-glucopyranosyl (1$\rightarrow$2)- [$\beta$ - D-xylopyranosyl (1$\rightarrow$3)] -$\beta$- D- fucopyranoside (1) and 26-0-$\beta$-D-glucopyranosyI25(S)-22-0-methyl-furost-5-en-l$\beta$, 3$\beta$, 26-trioll-0-fJ -D¬glucopyranosyl (1$\rightarrow$2)- [$\beta$- D-xylopyranosyl (1$\rightarrow$3)] - $\beta$- D- fucopyranoside (2), respectively.

• Archives of Pharmacal Research
• /
• 제27권2호
• /
• pp.173-176
• /
• 2004

Three phenolic compounds, rosmarinic acid (1), methyl rosmarinate (2), ethyl rosmarinate (3), and two flavonoids, luteolin (4), luteolin-7-O-$\beta$-D-glucuronide methyl ester (5) were isolated from the aerial part of Lycopus lucidus (Labiatae). Their structures were determined by chemical and spectral analysis. Compounds 1-5 exhibited potent antioxidative activity on the NBT superoxide scavenging assay. The $IC_{50}$ values for compounds 1-5 were 2.59, 1.42, 0.78, 2.83, and 3.05 $\mu\textrm{g}$/mL respectively. In addition, five compounds were isolated from this plant for the first time.

• Archives of Pharmacal Research
• /
• 제17권4호
• /
• pp.231-235
• /
• 1994

Fluorenecarboxaldehyde hydrazone 9FCH)was synthesized as a new fluorescent reagent for the determination of acidity. FCH had no fluorescence in itself, however, it strongly fluoresced under acidic conditions at excitation maximum of 392 nm and emission maximum of 447 nm, respectively. It showed good correlation with pH in the range from pH 0.60 to pH 3.60 in strong acids. As an application, the acidity of gastric juice in rats and humans was determined. In comparision with pH-metry, the acidity measured by the developed method showed generally increased values of about 0.7-1.3 unit and 0.8-1.2 unit in rats and humans, respectively. However, these results had statistically close correlation with those of pH-metry and the correlation coefficients were 0.887 in rats and humans between two methods.

• Archives of Pharmacal Research
• /
• 제20권2호
• /
• pp.103-109
• /
• 1997

The effects of ginseng total saponins (GTS) on hypoxic damage of primary cultures of astrocytes were studied. Hypoxia was created by placing cultures in an air tight chamber that was flushed with 95% $N_2/5%CO_2$ for 15 min before being sealed. Cultures showed evidence of significant cell injury after 24 h of hypoxia (increased lactate dehydrogenase (LDH) content in the culture medium, cell swelling and decreased glutamate uptake and protein content). Addition of GTS (0.1, 0.3 mg/ml) to the cultures during the exposure to hypoxic conditions produced dose-dependent inhibition of the LDH efflux. GTS (0.1, 0.3 mg/ml) also produced significant inhibition of the increased cell volume of astrocytes measured by $[^3H]$ O-methyl-D-glucose uptake under the hypoxic conditions. Decreased glutamate uptake and protein content was inhibited by GTS. These data suggest that GTS prevents astrocytic cell injury induced by severe hypoxia in vitro.

• Archives of Pharmacal Research
• /
• 제16권2호
• /
• pp.99-103
• /
• 1993

We describe here the conditions of thin layer chromatography (TLC) and high pressures liquid chromatography (HPLC) to improve the analytical method of phosphotyrosine (p-Tyr) in biological sample. TLC was performed on silica plate with the mixture of propanol and water (2.1 : 1 v/v) as a mobile phase and $R_1$ values were 0.42, 0.39 and 0.33 for phosphotyrosine, phosphothreonine and phosphoserine, respectively. HPLC was performed on $NH_2$ column with a mobile phase of potassium biphosphate solution by UV deterction at 192 nm. The optimum condition of HPLC was obtained at 0.01 M, pH 4.5 with a clear separation within 12 min. These procedures have been applied to the analysis of phosphotyrosine obtained from tyrosine-phosphorylated enolase. Both TLC and HPLC methods were suitable to analyze tyrosine-phosphorylated protein without being affected by contaminants from hydrolysates.

• Archives of Pharmacal Research
• /
• 제20권2호
• /
• pp.158-170
• /
• 1997

New HMG-CoA reductase inhibitors, in which 3-substituted 4, 5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor $(11cc, IC_{50}=0.01{\mu}M)$ is 4-fold more potent than lovastatin.

• Archives of Pharmacal Research
• /
• 제23권2호
• /
• pp.151-154
• /
• 2000

Two sesquiterpene endoperoxides, 1S, 4R, 6R-1, 4-endoperoxy-bisabola-2, 10-diene (1), 1R, 4S, 6R-1, 4-endoperoxy-bisabola-2, 10-diene (II), and a sesquiterpene hydroperoxide, 1$\beta$-hydroperoxygermacra-4 (15), 5, 10 (14)-triene (III) were isolated from the aerial parts of Artemisia stolonifera (Compositae). Their chemical structures were assigned by spectral evidences. Compounds I and II exhibited cytotoxicity against five human tumor cell lines with their $\ED_50 values ranging from 0.20 to 5.43 ${\mu}g/m\ell$ and from <0.1 to 0.87 ${\mu}g/m\ell$, respectively.

• Archives of Pharmacal Research
• /
• 제15권1호
• /
• pp.99-103
• /
• 1992

Susceptibility of Psudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis to gentimicin and ceforaxime was affected by salicylaye. In presence of salicylaye (15 mM) and gentamicin (1.0 .mu.g/ml), log efficiency of plating (log E. O. P. s) for the tested bacteria were -1.24, -2.17 and -1.66 respectively. The activity of cefotaxime against Bacillus subtilis was reduced (log E. O. P. = 1.33). The highest potentiating effects of salicylaye were shown when using gentamicin against Staphylococcus aureus, cefotaxime against Ps. aeruginosa, log E. O. P.s were -3.0, and -2.4 respectively. On the other hand, no significant effects were detected with cefotaxime against Staphylococcus aureus (log E. O. P. = -0.04). No significant killing was shown in presence of gentamicin or salicylaye alone. There was no significant effect for salicylaye on MICs (By broth dilution) could be observed except in case of gentamicin against Staphyloccus aureus, which was reduced from 0.02 .mu.g/ml to 0.0012 .mu.g/ml. These results raise the concern that high concentrations of salicylaye in patients might interfere with antibiotic therapies.

• Archives of Pharmacal Research
• /
• 제12권2호
• /
• pp.108-113
• /
• 1989

A new column-switching high performance liquid chromatographic method was developed for the determination of lonazolac in plasma. This method was based on the on-line trace enrichment of lonazolac using a precolumn packed with Amberlite XAD-2. The analysis was complete in 20 min. between injections and the limit of detection was $0.1{\mu}g/ml$ using $100{\mu}l$ of plasma. The method was linear in range of $0.1-10{\mu}g/ml$ with a correlation coefficient of 0.9991. Absolute recovery of lonazolac from the spiked plasma samples ranged from 95.6% to 97.1%. The method was shown to be reproducible over the concentration range studied.