• YAKHAK HOEJI
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• v.35 no.4
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• pp.258-263
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• 1991

Seven drivatives of 2, 3-alkyl substituted aziridinecarboximidates were prepared from alkyl substituted alkene and cyanamide. Their ED$_{50}$ values against L$_{1210}$ cell in vitro were evaluated as 1.5 to 4 $\mu\textrm{g}$/ml.

• Proceedings of the Korean Society of Toxicology Conference
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• 2002.05a
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• pp.115-115
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• 2002

The anti-diarrhea and spasmolytic activities of Soonkijangquebo (SKJQB), a Korean herbal anti-diarrhea formulation, were subjected to pharmacological evaluation. SKJQB, at a dose of 50\ulcorner200 mg/kg, inhibited castor oil-induced diarrhea in mice. The median effective dose (ED50) of the anti-diarrhea effect was 93 mg/kg.(omitted)

• The Plant Pathology Journal
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• v.16 no.4
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• pp.222-226
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• 2000

In disease surveys from 1986 ti 1998, disease incidence of tobacco black shank was gradually increased in burley tobacco from 1996. To study the causes of the disease occurrence, one hundred and fourteen isolates of Phytophthora parasitica var. nicotianae (Ppn) were collected from burley tobacco-growing areas in the southern part of Korea during 1996-1997, and tested in vitro for meatlaxyl sensitivity which was determined by measuring the mycelial growth on corn meal agar (CMA) amended with metalaxyl. Of the tested isolates, 78.1% showed sensitive to metalaxyl, having $\textrm{ED}_{50}$ values less than 1.0 $\mu\textrm{g}/$\textrm{ml}, while 1.7% was resistant weth $\textrm{ED}_{50}$ greater than 100 $\mu\textrm{g}/$\textrm{ml}. Ppn isolates from three provinces, Chungnam, Chonbuk and Chonnam showed similar distributions of metalaxyl sensitivity. Metalaxyl-resistant isolates were not significantly different from metalaxyl-sensitive ones in mycelial growth rate, chlamydospore formation capacity and size of the spore, and pathogenicity on tobacco plant (cv. Burley 21). These results suggest that the metalaxyl-resistant Ppn in burley tobacco may be one of the major factors to cause the higher occurrence of the tobacco black shank in the burley tobacco-growing area.

• Biomolecules & Therapeutics
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• v.11 no.2
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• pp.133-138
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• 2003

The vascular relaxant and antihypertensive effects of newly developed salts of amlodipine-maleate and camsylate-were evaluated on isolated aorta from rats and in spontaneously hypertensive rats, and compared with those of amlodipine besylate, a standard drug. Amlodipine besylate concentration-dependently inhibited $Ca^{2＋}$-induced contraction in depolarised rat aorta($IC_{50}$/: 4.17 nM), with a very slow onset of action. Amlodipine maleate and amlodipine camsylate also showed vascular relaxant effect with a pattern and a potency similar to those of amlodipine besylate($IC_{50}$/: 3.62 and 3.28 nM, respectively). Amloclipine besylate produced a dose-dependent and long-lasting(>10∼24h) antihypertensive effect with a slow onset of action (ED$_{20}$: 2.31 mg/kg) in spontaneously hypertensive rats. Amlodipine maleate and amlodipine camsylate also exerted antihypertensive effects with a pattern and a potency similar to those of amlodipine besylate(ED$_{20}$: 2.09 and 2.21 mg/kg, respectively). These results suggest that amlodipine maleate and amlodipine camsylate are not statistically differ with amlodipine besylate in relaxant effect of $Ca^{2＋}$-induced contraction in depolarised rat aorta and in antihypertensive effect in spontaneously antihypertensive rats.

• Biomedical Science Letters
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• v.6 no.3
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• pp.181-186
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• 2000

Asadisulphide were purified from Ferrula assafoetida by organic solvent extraction and chromatography. Its inhibitory effects on the TPA-induced adherence of HL-60 cells was analyzed. Since ethyl acetate extracts of F. assafoetida has the strongest inhibitory effect on adherence of HL-60 cells, it was re-extracted with ethyl acetate, hexane, and ethyl ether and chromatographed three times to isolate asadisulphide. At the minimum concentration of 2 $\mu\textrm{g}$/ml, asadisulphide inhibited adherence of 98% of HL-60 cells that have been treated with TPA. It also showed anti-cancer effect with no cytotoxity in the ED$_{50}$ value of 20 $\mu\textrm{g}$/ml.

• Natural Product Sciences
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• v.15 no.3
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• pp.130-133
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• 2009

The crude extract of the mycelium of Cladosporium was found to exhibit antimicrobial activity against the Staphylococcus aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus. Bioassayguided fractionation of an organic extract led to the isolation of an acetophenone derivative, clavatol (2',4'-dihydroxy-3',5'-dimethylacetophenone) (1), and a benzodiazepine alkaloid, circumdatin A (2). Compound 1 showed moderate antibacterial activity against S. aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus with minimum inhibitory concentration (MIC) values of 62.5, 62.5, 31.0 $\mu$g/mL, respectively, but compound 2 was inactive. Compounds 1 and 2 exhibited UV-A protection activity with ED$_{50}$ values of 227.0 and 82.0 $\mu$M, respectively, indicating that they were more potent than the positive control, oxybenzone (ED$_{50}$ 350 $\mu$M), a common sunscreen agent.

• Korean Journal of Pharmacognosy
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• v.33 no.3 s.130
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• pp.207-210
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• 2002

The methanol extract from the root of Croton cascarilloides Raeusch. was primarily evaluated for cytotoxic activity in the cultured human lung cancer cell line (A459) and showed cytotoxic potential with $ED_{50}$ value of $5.98\;{\mu}g/ml$. Bioassayguided fractionation of the root extract resulted in 3-acetyl aleuritolic acid, rubiadin-l-methyl ether, and julocrotine. The structures of the compounds were elucidated from the combination of spectroscopic data and references. In addition, the $^{13}C-NMR$ assignments of rubiadin-l-methyl ether were revised.

• Journal of Life Science
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• v.11 no.1
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• pp.62-69
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• 2001

This study was aimed to investigate the effect Chukdamtanggamibang on the vascular systems including changes in blood pressure and regional cerebral blood flow(rCBF) of male Sprague-Dawely rats, contractile force of guinea pig`s tracheal smooth muscle and abdominal aorta and femoral artery in rabbits. Blood pressure was not affected by Chukdamtanggamibang in rats. rCBF was significantly increased by Chukdamtanggamibang in a dose-dependent manner. Contractile force of isolated guinea pig`s tracheal smooth muscle evoked by His ({TEX}$ED_{50}${/TEX}) were inhibited significantly by Chukdamtanggamibang. Propranolol, indomethacin and methylene blue did not significantly alter the inhibitory effect of Chukdamtanggamibang. Contractile force of isolated rabbit`s abdominal aorta and femoral artery evoked by NE ({TEX}$ED_{50}${/TEX}) were inhibited significantly by Chukdamtanggamibang. ODQ and L-NNA significantly attenuated the inhibitory effects of Chukdamtanggamibang in abdominal aorta, whereas propranolol did not significantly alter the inhibitory effect of Chukdamtanggamibang. These results indicate that Chukdamtanggamibang can relax hitamine-induced contraction of guinea pig`s tracheal smooth muscle and that this inhibition involves, in part, the relation to the soluble guanylyl cyclase synthesis and nitric oxide (NO) synthesis.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.423-426
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• 1995

SM-101 is a mixture of metampicillin and sulbactam(2:1). The antibacterial activities of SM-101 were compared with those of metampicillin, piperacillin and Augmentin. It showed powerful antibacterial activities against major strains. Except P. anruginosa and S. marcescens, the in vitro antibacterial activity of SM-101 was higher than those of metampicillin, piperacillin and Augmentin against Staphylococcus spp., Streptococcus spp., Moganella morganii, E. Coil, and Proteus spp. The $ED_{50}$ values of SM-101 were two-fold or greater than those of metampicillin, piperacillin and Augmentin against $\beta-lactamase$ producing strains, p. mirabilis GN79 and M. morganiii MB4-11. The in vivo efficacy of SM-101 was more active than metampicillin and pipeeracillin and similar to Augmentin against S. aureus Smith, E coli MB4-01 and K. pneumoniae MB4-02.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.155-157
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• 1997

An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin analogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells,${\alpha}$-methoxyphenylacetyl-(9), ${\alpha}$-acetoxyphenylacetyl-(13), 3,4-methylenedioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity $(IC_100; value, 4-8{\mu}g/ml)$, while halophenylacetyl- and dimethoxy- or trimethoxyphenylacetyl analogues expressed no activity at $40{\mu}g/ml$, indicating that the presence of a bulky group at $ C^I-{\alpha}$ and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity $(ED_{50})$ of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between $IC_{100}$ values for anti-cell adhesive activity and$ED_{50}$ values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.