• Bulletin of the Korean Chemical Society
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• 제33권12호
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• pp.4023-4027
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• 2012

Cytotoxicity assessment of silver nanoparticles (AgNPs) was performed using MTT-based microfluidic image cytometry (${\mu}FIC$). The $LC_{50}$ value of HeLa cells exposed to AgNPs in the microfluidic device was estimated as 46.7 mg/L, which is similar to that estimated by MTT-based IC for cells cultured in a 96 well plate (49.9 mg/L). These results confirm that the ${\mu}FIC$ approach can produce cytotoxicity data that is reasonably well-matched with that of the conventional 96 well plate system with much higher efficiency. This ${\mu}FIC$ method provides many benefits including ease of use and low cost, and is a more rapid in vitro cell based assay for AgNPs. This may aid in speeding up data acquisition in the field of nanosafety and make a significant contribution to the quantitative understanding of nanoproperty-toxicity relationships.

• Journal of Microbiology and Biotechnology
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• 제31권1호
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• pp.33-42
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• 2021

Due to the potential of antioxidants to scavenge free radicals in human body, it is important to be able to prepare antioxidant peptides that meet the industrial requirements for cosmetics and food. Here, we determined in vivo/in vitro activities of antioxidant peptide from P. fucata (PFAOP) prepared by bio-fermentation method. The antioxidant property test results showed the DPPH, hydroxyl, superoxide radical-scavenging, and cellular antioxidant activity. EC50 values of PFAOPs were 0.018 ± 0.005, 0.126 ± 0.008, 0.168 ± 0.005, and 0.105 ± 0.005 mg/ml, respectively, exhibiting higher antioxidant activities than glutathione (p < 0.05). Moreover, anti-proliferation and cytotoxicity activity results illustrated PFAOP has a potent anti-proliferative activity against HepG2, Caco-2, and MCF-7 carcinoma cells with no cytotoxicity. Moreover, the protocols we developed in this work demonstrated several excellent advantages in PFAOP preparation compared to enzymatic hydrolysis or chemical synthesis methods and provide a theoretical foundation for higher-value application of marine-derived functional peptides.

• Macromolecular Research
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• 제15권6호
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• pp.513-519
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• 2007

Self-assembled nanoparticles have great potential to act as vehicles for hydrophobic drug delivery. Understanding nanoparticle cellular internalization is essential for designing drugs intended for intracellular delivery. Here, the endocytosis and exocytosis of fluorescein isothiocyanate (FITC)-conjugated glycol chitosan (FGC) self-assembled nanoparticles were investigated by flow cytometry and confocal microscopy. The cellular internalization of FGC nanoparticles was initiated by nonspecific interactions between nanoparticles and cell membranes. Although adsorptive endocytosis of the nanoparticles occurred quickly, significant amounts of FGC nanoparticles were exocytosed, particularly in the early stage of endocytosis. The amount of exocytosed nanoparticles was dependent on the pre-incubation time with nanoparticles, suggesting that exocytosis is dependent on the progress of endocytosis. FGC nanoparticles internalized by adsorptive endocytosis were distributed in the cytoplasm, but not in the nucleus. In vitro cell cycle analysis demonstrated that FGC nanoparticles delivered paclitaxel into the cytoplasm and were effective in arresting cancer cell growth.

• Archives of Pharmacal Research
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• 제19권4호
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• pp.286-291
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• 1996

Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$, bibenzyl, $2,2^I-dimethylbibenzyl$, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.

• 약학회지
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• 제35권4호
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• pp.283-287
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• 1991

Seven derivatives of 2,3-alkyl substituted N-cyanoaziridine were stereoselectively prepared from alkyl substituted alkenes and cyanamide. NMR spectral property and conformation of N-cyanoaziridine were analysed. Protons(3.34 ppm) at 2,3 position of N-cyanoaziridines are significantly deshielded in case of cyclopentyl fused N-cyanoaziridine. These protons are getting more anisotropically shielded with increasing the fused carbocycle size of N-cyanoaziridine. Therefore chemical shift for these protons are upfield shifted to 2.80 ppm in case of cyclooctyl fused N-cyanoaziridine. Their ED$_{50}$ values aganist L$_{1210}$, cell in vitro were evaluated as 0.5~8.0 $\mu$g/ml. Conformation of carbocycle of fused N-cyanoaziridine is more important to their cytotoxicity than the increment of the strain energy of 3-membered ring.

• 대한한의학회지
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• 제30권1호
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• pp.64-75
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• 2009

Objective: This study was designed to investigate the effect of Samultang (SMT) under hippocampus cells ischemia both in vitro and in vivo. Methods: In the in vitro study, HT22 cells, predominantly detected in the cytoplasm, which coincides with the location of the mitochondria, were used as indicators. In the in vivo study, permanent middle cerebral artery occlusion (MCAO) was induced on rats. SMT was given orally 2 h before induction of permanent focal brain ischemic injury. Result: In the in vitro study, SMT had protective effects in glutamate-induced cytotoxicity, which was revealed as apoptosis characterized by chromatic condensation and the loss of mitochondrial membrane potential in HT22 cells. In the in vivo study, TTC (2,3,5-triphenyltetrazolium chloride) staining showed a marked ischemic injury in blood supply territory of the middle cerebral artery (MCA) such as the cerebral cortex and striatum. However, treatment with SMT significantly reduced infarcted volume. SMT increased marked survival of HT22 cells against glutamate-induced cytotoxicity in MTT assay. Conclusion: These results suggest that water extract of SMT provides neuroprotection against ischemic or oxidative injury by inhibition of apoptotic cell death.

• 약학회지
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• 제42권4호
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• pp.408-413
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• 1998

To establish prediabetes in vitro/ model concerning the etiology of Insulin Dependent Diabetes Mellitus (IDDM) in cellular level we have designed experimental prediabefic model in pancreatic beta cells. RINm5F, HIT-T15 and isolated rat islets were chosen as pancreatic beta cells. Since interleukin-$1{\beta}$-induced beta cell cytotoxicity has been implicated in the autoimmune cytotoxicity of IDDM, we used inteleukin-$1{\beta}$ as diabetogenic agent. For establishment of prediabetic in vitro model, the degree of beta cell deterioration was determined by cell proliferation, insulin release and morphological appearance. Cell proliferation, insulin release and morphology were changed dose-dependently in condition that inteleuldn-$1{\beta}$ was exposured to pancreatic beta cells. The concentration and exposure time of interleukin-$1{\beta}$ to set up prediabetic model in beta cell lines and isolated rat islets were 100${\sim}$1000U/ml, 48hr. And 25${\sim}$100U/ml, 48hr, respectively.

• Toxicological Research
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• 제19권2호
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• pp.147-152
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• 2003

We investigated antitumor activities of the ethanol extract from mushroom Phellinus linteus and Phellinus baumii on mulberry, oak and elm. in vitro test, the ethanol extract of mushroom cultivated on oak of Phellinus linteus showed highest activities about SK-OV-3, HCT15, XF498, SK-MEL-2 and A549. SK-OV-3 cell line showed 100% cytotoxicity in 100 $\mu\textrm{g}$/ml and HCT15 (98.39%), XF498 (89.62%), SK-MEL-2 (84.07%) and A549 (79.92%) cytotoxicity respectively. Also $IC_{50}$ showed 3.99 $\mu\textrm{g}$/ml to SK-OV-3 cell line and HCT15 (4.37 $\mu\textrm{g}$/ml), A549 (5.48 $\mu\textrm{g}$/ml), SK-MEL-2 (6.72 $\mu\textrm{g}$/ml), XF 498 (6.88 $\mu\textrm{g}$/ml). As those results, cultivated oak of Phellinus linteus showed a very low $IC_{50}$ value against SK-OV-3, HCT15, XF498, SK-MEL-2 and A549 cancer cell lines.

• Bulletin of the Korean Chemical Society
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• 제35권7호
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• pp.1933-1938
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• 2014

Despite increasing importance of in vitro cell-based assays for the assessment of nanoparticles (NPs) cytotoxicity, their suitability for the assessment of NPs toxicity is still in doubt. Here, limitations of widely used cell viability assay protocol (i.e., MTT asssay) for the cytotoxicity assessment of P25 $TiO_2$ NPs were carefully examined and an alternative toxicity assessment method to overcome these limitations was proposed, where the artifacts caused by extracellularly formed formazan and light scattered by agglomerated NPs were minimized by measuring only the intracellular formazan via image cytometric methods.

• Mycobiology
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• 제29권3호
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• pp.170-172
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• 2001

The methanolic extract of fruiting body of Paecilomyces tenuipes DGUM 32001 showed significant cytotoxicity against human cancer cells: HepG2 and MCF-7. The methanolic extract was further fractionated with organic solvents such as chloroform and ethyl acetate in that order. Among the fractions tested, the ethyl acetate fraction showed the highest cytotoxicity against the carcinoma tested. The $IC_{50}$ values of ethyl acetate fraction against HepG and MCF-7 were 40 and 9.6 ${\mu}g/ml$, respectively.