• Archives of Pharmacal Research
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• v.20 no.3
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• pp.283-287
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• 1997

In order to identify the structural requirement at 4-position of 1-arylsulfonyl-4-phenyl-4,5-dihydro-2-limidazolones 3 for their cytotoxicity, the corresponding 1-arylsulfonyl-4-cyclohexyl-4,5-dihydro-2-imidazolones 4 were synthesized and their in vitro cytotoxicity against human solid tumor cell lines were measured. Unlike compounds 3a-c, cyclohexyl analogues 4a-c do not show the cytotoxicity. This dramatic loss of activity of these analogues on the volume change with the bulkier cyclohexyl group indicates that the planar structure at 4-position of 1-arylsulfonyl-4-pheny-4,5-dihydro-2-limidazolones 3 is required for their activity as an important pharmacophoric moiety.

• Bulletin of the Korean Chemical Society
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• v.15 no.6
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• pp.442-448
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• 1994

Transition metals tested, $Cu^{2+}$, and $Ni^{2+}$, were found effective in the induction of the cytotoxicity of the quinolones tested, nalidixic acid, oxolinic acid, and pipemidic acid, against L1210 leukemia cells in vitro, whereas the alkaline earth metal, $Mg^{2+}$, was not. The differential effect of the metals on the quinolone cytotoxicity can be explained by their different mode of interaction with the quinolones. Our present difference spectroscopic titration data suggest that the transition metals can form DNA-intercalating agents, with the quinolones, which can cause the cytotoxicity.

• Toxicological Research
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• v.35 no.2
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• pp.201-207
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• 2019

Nanoxel-$PM^{TM}$ (Nanoxel) is a docetaxel-loaded methoxy-poly(ethylene glycol)-block-poly(D,L-lactide) (mPEG-PDLLA). This newly developed and marketed nanoformulation exhibits an improved pharmacokinetic profile, efficacy, and safety. Although the safety of Nanoxel to docetaxel as well as its bioequivalence must be clinically confirmed, all biological activities have not been examined in in vitro or in vivo studies. Here, the toxicity in a cultured cell system and the effects on blood cells were tested with Nanoxel and docetaxel. The in vitro cytotoxicity of Nanoxel was found to be comparable to or slightly lower than that of docetaxel depending on the concentrations tested or the cell types. Neither docetaxel nor Nanoxel induced erythrocytes hemolysis and produced reactive oxygen species up to $100{\mu}M$. However, Nanoxel was able to enhance the aggregatory response of platelets to collagen, whereas docetaxel attenuated such aggregation in a range of $50-100{\mu}M$, while thrombin-induced aggregation was not affected by either of them. Docetaxel or Nanoxel did not alter basal level of $Ca^{2+}$ and 5-hydroxytryptamine-evoked $Ca^{2+}$ transient in vascular smooth muscle cells. These results suggest that the mPEG-PDLLA micellar formulation alters the toxicological properties of docetaxel, and that extra cautions are needed when evaluating the safety of nanomedicine.

• Archives of Pharmacal Research
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• v.19 no.6
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• pp.490-496
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• 1996

Naphtodianthrone hypericin produced a potent antitumor activity in vitro against several tumor cells. However, it did not show any cytotoxicity on normal cells such as Macaccus rheus monkey kidney cells (MA-104) and primary cultured rat hepatocytes up to $500{\mu}M$ concentration. Hypericin added to A431 human epidermoid carcinoma cell membrane inhibited the autophosphorylation of the epidermal growth factor (EGF) receptor and the tyrosine phosphorylation of RR-SRC peptide catalyzed by an EGF-receptor. Similarly, treatment of the A431 cells with hypericin inhibited the tyrosine phosphorylation of EGF-dependent endogenous EGF-receptor by western blotting analysis. Hypericin also inhibited the T cell PTK, $P56^{lck}$, in a dose-dependent fashion with an $IC_{50}=5{\mu}M$. The tyrosine phosphorylation, on RR-SRC peptide and EGF-induced receptor autophosphorylation, either in vitro or in intact cells was inhibited by hypericin at the same concentration as that in A431 cell proliferation. These data suggest that hypericin directly inhibits EGF-receptor and $P56^{lck}$ PTK activity in vitro and can mediate such action in vivo.

• Korean Journal of Microbiology
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• v.36 no.4
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• pp.312-315
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• 2000

Paecilomyces tenuipes DGUM 32001, an entomopathogenic fungus, was examined to evaluate in vitro cytotoxicity against several human cancer cells. The fruiting bodies of P. tenuipes were extracted with methanol and fractioned with some organic solvents i.e. chloroform, ethyl acetate, and butanol. The methanol extracts of P. tenuipes showed significant cytotoxicity against human cancer cell lines; HeLa, HeLa S3, and A-431. Among the fractions tested, the ethyl acetate fraction had the highest cytotoxicity against three cancer cell lines. The $IC_{50}$ values of ethyl acetate fraction against HeLa, HeLa S3, and A-431 were 13, 35, and 30 $\mu$g/ml, respectively. However, cytotoxicity might not be due to apoptosis. The methanol extract of cultured mycelia showed high cytotoxicity against HeLa cell lines.

• The Journal of Korean Medicine
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• v.19 no.2
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• pp.313-325
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• 1998

The effect of Holotrichia on natural killer cell activity in normal mouse were studied. 1. The oral administration of Holotrichia increased spleen weight about 21.1% and also cell numbers of spleen compared to control mice group. 2. The cytotoxicity of effector cell was most effectively induced in a ratio of 50 : 1(effector/target cell). 3. Cytotoxicity of effector cells was. increased about 24% as compared with control group in in vivo test. 4. On the other hand, the administration of Holotrichia original solution showed significant increase the cytotoxicity. The cytotoxicity was increased concentration dependently. 5. The cytotoxicity by $^{3}H-thymidine$ incorporation assay showed similar effect with LDH enzyme method. 6. In the purified NK cells, the cytotoxicity was increased about 31% as compared with control group in in vivo system and the ratio of cytotoxicity was generally more increased than that of partially purified NK cell. 7. In vitro experimet of the purified NK cells, the cytotoxicity was increased 11.8% as compared with control group and the ratio of cytotoxicity was also more increased than that of partially purified NK cell. These results suggest that Holotrichia is administrated to mice with malignant tumors, the increase of NK cell activity may occur and affect tumor cells.

• Journal of the Optical Society of Korea
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• v.18 no.2
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• pp.174-179
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• 2014

Since in vitro neural recording and imaging applications based on a surface plasmon resonance (SPR) technique have expanded dramatically in recent years, cytotoxicity assessment to ensure the biosafety and biocompatibility for those applications is crucial. Here, we report the cytotoxicity of the SPR substrate incorporating a flint glass whose refractive index is larger than that of a conventional crown glass. A high refractive index glass substrate is essential in neural signal detection due to the advantages such as high sensitivity and wide dynamic range. From experimental data using primary hippocampal neurons, it is found that a lead-based flint glass is not appropriate as a neural recording template although the neuron cells are not directly attached to the toxic glass. We also demonstrate that the adhesion layer between the glass substrate and the gold film plays an important role in achieving the substrate stability and the cell viability.

• The Journal of Internal Korean Medicine
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• v.18 no.1
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• pp.48-61
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• 1997

In this study, antineoplastic activity against human hepatocellular carcinoma cell line(Hep G2) was tested in Gleditsiae Spina. Gleditsiae Spina was extracted with water, and the cytotoxic activity was tested using a calorimetric tetrazolium assay(MTT assay), the apoptosis was tested using a DNA electrophoresis and flow cytometry. The nitric oxide production from mouse peritoneal macrophage was tested using a Griess method. Gleditsiae Spina extracts against the proliferation of Hep G2 cells not showed cytotoxicity at the concentration of less than $100{\mu}g/ml$, and Gleditsiae Spina extracts not showed the cytotoxicity of mitomycin C and the cytotoxicity of cisplatin on Hep G2 cells. Gleditsiae Spina extracts aginist the proliperation of BALB/c 3T3 cells not showed cytotoxicity, the proliperation of mouse thymocytes and splenocytes not showed cytotoxicity at the concentration of less than $100{\mu}g/ml$. Gleditsiae Spina extracts not showed nitric oxide production from mouse peritoneal macrophage in vitro. Gleditsiae Spina was administered orally for 7 days at 300mg/kg increased nitric oxide production from mouse peritoneal macrophage.

• Biomedical Science Letters
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• v.16 no.4
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• pp.221-227
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• 2010

To elucidate the invasion mechanism of pathogenic Naegleria fowleri, especially a receptor-ligand recognition, we investigated the in vitro cytotoxicity of pathogenic N. fowleri and nonpathogenic N. gruberi to murine macrophages, RAW 264.7, by adding four kinds of saccharides, ${\alpha}$-fucose, ${\beta}$-galactose, ${\alpha}$-D-mannopyranoside (${\alpha}$-mannose) and xylose. There was not enough of a difference in the cytotoxicity of N. fowleri treated with 10 mM of each saccharide. In particular, the cytotoxicity of N. fowleri was highly inhibited by 100 mM ${\alpha}$-mannose, which was 62.3% inhibition calculated by the analysis of lactate dehydrogenase (LDH) release assay. Although murine macrophages were not significantly destroyed by nonpathogenic N. gruberi under hematoxylin staining, the cytotoxicity of N. gruberi was inhibited from 31.5% to 14.5% (P<0.01) by 100 mM ${\alpha}$-mannose treatment. The binding of N. fowleri to macrophages was inhibited from 33% to 50% by 100 mM ${\alpha}$-mannose. Furthermore, as results of the adhesion assays which were performed to determine whether binding of Naegleria is mediated by saccharides-binding protein, the binding ability of N. fowleri as well as N. gruberi was inhibited by 100 mM ${\alpha}$-mannose.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.749-752
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• 1998

Six 3-dialkylaminomethyl-1-azaanthraquinones and five 4-dialkylaminomethyl-1-azaanthraquinones were synthesized and evaluated in vitro cytotoxicity against four human can cer cell lines. The compounds retained much of their cytotoxic activity against the multi-drug-resistant cell line (KB-V-1) as shown by resistance index.