• Archives of Pharmacal Research
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• v.10 no.4
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• pp.260-261
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• 1987

The UV-pattern of several flavones, theier cytotoxicities against L1210 cell and their Inhibiting effects on ATPase from the cell seem to be correlated. 5.2'-Dihydroxy 6, 7, 8, 6'-tetramethoxyflavone ($ED_{50}$ = 2.3 ug/ml) and 5,2',6'-trihydroxy-6, 7, 8 trimethoxy flavone ($ED_{50}$ = 4.5 ug/ml), the most active flavones studied, have shown a narrow range of the absorbance ratio, Log $\varepsilon$ II/Log $\varepsilon$ I = 1.073 -1.109. They have inhibited the ATPase-activity to the greatest extent. These finding ssuggest that a certain angle between the flavone rings B and C plays an important role for the inhibition of the enzyme activity and thus the cytotoxicity.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.288-301
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• 2000

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.302-309
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• 2000

Based on (-)-neplanocin A with the 5'-hydroxyl substituted with fluoro, azido, or amino group, the corresponding xylo- and arabino derivatives were synthesized from D-ribose using the Mit-sunobu reaction as a key step. None of the final nucleosides did show either significant antiviral activities or cytotoxicities.

• Archives of Pharmacal Research
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• v.27 no.6
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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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• v.17 no.6
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• pp.420-423
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• 1994

Various N'-substituted anilino-N-methyl-N'-nitrosoureas(2a-n) were easily prepared from the reaction of substituted phenylhydraines $(3, 4-CH_3, {\;} 3-, {\;} 4-OCH_3, {\;} 3-, {\;} 4-F, {\;} 3, {\;} 4-Cl, {\;} 4-Br, {\;} 2-, {\;} 3-, {\;} 4-NO_2, 4-(NO_2)_2)$ with methyl isocyanate, followed by the nitrosation with 99% HCOOH and dry sodium lnitrite powder. Surprisingly, of these series of analogus, the anilino-nitrocosureas substituted with eletron-withdrawing nitro groups (2k-a) showed significantly low $ED_{30}$ values of $1.4-3.4 {\mu}g/ml.$ In addition, none of these copounds subtituted with electron-donating groups exhibited cytotoxicities.

• Archives of Pharmacal Research
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• v.16 no.3
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• pp.254-256
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• 1993

For the evaluation of the role of .alpha., .betha.-unsaturated ketone portion of ar-tumerone for its activity, the structural variation of this structural unit was performed to omit its alkylating propery. Thus compounds 2, 3, and 4 were prepared and their cytotoxicities were determined against three different leukemiz cell lines (HL-60, K-562, and $L_{1210})$ in vitro. The biological inactivity against three different cell lines of these analogues implies that the $\alpha, \beta$-unsaturated ketone of ar-tumerone is the essential pharmacophore for its activity.

• Bulletin of the Korean Chemical Society
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• v.30 no.2
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• pp.339-342
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• 2009

In this study, a hydrogenated lecithin-containing liposome was prepared using a sonicator and microfluidizer at high shear. The surface tension, particle size, turbidity, and transition temperature ($T_c$) of the liposome were investigated and compared with the commercially available standard surfactant Tween-60. The cytotoxicities were characterized using the MTT method. The surface tension of hydrogenated lecithin was found to be higher than that of Tween-60. The particle size prepared at above $T_c$ was smaller than that prepared below $T_c$. The results of the cytotoxicity experiment indicated that Lecinol 10 exhibits the highest I$C_{50}$ value, which shows its high safety in this study.

• Bulletin of the Korean Chemical Society
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• v.26 no.8
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• pp.1209-1213
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• 2005

Nuclear membrane is one of the main barriers in intracellular delivery of genetic materials. The previous report showed that glucocorticoid receptor dilated the nuclear pore to 60 nm in the presence of a ligand. It was also suggested that the transport of genetic material to nucleus might be facilitated by glucocorticoid. In this study, the effect of glucocorticoid preincubation in the polymeric gene delivery was investigated. The cells were preincubated with dexamethasone, a potent glucocorticoid, and transfection assays were performed with polyethylenimine (PEI) and polyamidoamine (PAMAM) dendrimer. As a result, the transfection efficiency of PEI or PAMAM to the cells in the presence of dexamethasone was enhanced, compared to the cells without dexamethasone. This effect was not observed in the cells preincubated with cholesterol. The polymer/DNA complex was stable in the presence of dexamethasone. In addition, the cytotoxicities of the polymeric carriers to the cells were observed in the presence of dexamethasone. In conclusion, dexamethasone enhances the transfection efficiency of polymeric carriers and may be useful in the development of polymeric gene carriers.

• YAKHAK HOEJI
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• v.32 no.2
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• pp.125-128
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• 1988

Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

• YAKHAK HOEJI
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• v.32 no.2
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• pp.137-140
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• 1988

To investigate polyacetylene compounds isolated from petroleum ether extract of panax ginseng effect on the macromolecule synthesis, lympoid lukemia L1210 cell was incubated with them at 4, 8, 12,16 hours. Panaxydol, panaxynol and panaxytriol as cytotoxic substances inhibited the synthesis of macromolecule such as DNA, RNA and protein. Panaxydol which had the most potent cytotoxicity among these three compounds showed the strongest inhibitory effect on DNA, RNA and protein synthesis. For DNA and RNA synthesis, panaxynol and panaxytriol decreased the rate of inhibition with the incubation time but panaxydol had a strongest inhibitory effect at 16 hour incubation time. Protein synthesis was markedly inhibited by all these polyacetylene compounds. It was obserbed that there is a relationship between cytotoxicities of polyacetylene compounds and the inhibition of macromolecule synthesis.