• Asian Pacific Journal of Cancer Prevention
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• v.14 no.9
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• pp.4983-4988
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• 2013

Objectives: To establish a taxol-resistant cell line of human ovarian carcinoma (A2780/Taxol) and investigate its biological features. Methods: The drug-resistant cell line (A2780/Taxol) was established by continuous stepwise selection with increasing concentrations of Taxol. Cell morphology was assessed by microscopy and growth curves were generated with in vitro and in vivo tumor xenograft models. With rhodamine123 (Rh123) assays, cell cycle distribution and the apoptotic rate were analyzed by flow cytometry (FCM). Drug resistance-related and signal associated proteins, including P-gp, MRPs, caveolin-1, PKC-${\alpha}$, Akt, ERK1/2, were detected by Western blotting. Results: A2780/Taxol cells were established with stable resistance to taxol. The drug resistance index (RI) was 430.7. Cross-resistance to other drugs was also shown, but there was no significant change to radioresistance. Compared with parental cells, A2780/Taxol cells were significantly heteromorphous, with a significant delay in population doubling time and reduced uptake of Rh123 (p<0.01). In vivo, tumor take by A2780 cells was 80%, and tumor volume increased gradually. In contrast, with A2780/Taxol cells in xenograft models there was no tumor development. FCM analysis revealed that A2780/Taxol cells had a higher percentage of G0/G1 and lower S phase, but no changes of G2 phase and the apoptosis rate. Expression of P-gp, MRP1, MRP2, BCRP, LRP, caveolin-1, PKC-${\alpha}$, Phospho-ERK1/2 and Phospho-JNK protein was significantly up-regulated, while Akt and p38 MARK protein expression was not changed in A2780/Taxol cells. Conclusion: The A2780/Taxol cell line is an ideal model to investigate the mechanism of muti-drug resistance related to overexpression of drug-resistance associated proteins and activation of the PKC-${\alpha}/ERK$ (JNK) signaling pathway.

• Food Science and Preservation
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• v.17 no.5
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• pp.727-732
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• 2010

Activity-guided fractionation of an ethyl acetate (EtOAc)-soluble portion of an ethanolic extract from the leaves of cultivated mountain ginseng, using pancreatic lipase inhibition assay, led to the isolation and identification of three flavonoids of a previously described structure, kaempferol-3-O-sophoroside (I), kaempferol-3-O-${\beta}$-Dglucopyranoside (astragalin, II) and kaempferol (III). All compounds (I.III) showed pancreatic lipase inhibitory activities, with $IC_{50}$ values ranging from $20.3{\pm}2.2$ to $9.1{\pm}1.5$ ${\mu}M$, kaempferol (III) showed the most potent inhibitory activity with an $IC_{50}$ of $9.1{\pm}1.5$ ${\mu}M$. The level of activity may depend on the number of C-3 glucosyl group(s) linked to the kaempferol backbone, and the isolated compounds may have promise as pancreatic lipase inhibitors.

• Applied Biological Chemistry
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• v.51 no.1
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• pp.70-78
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• 2008

Prunus sargentii R. of Rosaceae familiy, has been reported to have radical scavenging activity and anti-inflammatory effect. On these facts, biological activity and safety test were conducted to evaluate biological activities of the extracts of P. sargentii R. as a potential pharmaceutical ingredient. The electron donating ability of its ethanol extracts at a 500 ppm level showed 92%, which was higher than that of hot water extract (59%), the superoxide dismutase (SOD)-like activity of the water extract of P. sargentii R. was about 50%, the ethanol extract of P. sargentii R. was about 40% at 1,000 ppm concentration. Xanthine oxidase inhibition by the water extract of P. sargentii R. was about 40% and that by the ethanol extract was 60% respectively at 500 ppm concentration. From the measurement on lipid oxidation, the $Cu^{2+}$ chelating effect of the ethanol extract was higher than that of hot water extract. The $Fe^{2+}$ chelating effect was also shown to be about 80% at a 500 ppm concentration in both hot water extract and ethanol extract. The tyrosinase inhibition effect related to skin-whitening was 26% by hot water extract and 20% by ethanol extract respectively at a 1,000 ppm. Hyaluronidase inhibition activity related to the anti-inflammation effect was 96% in ethanolic extract at a 500 ppm. Clear zones formed by P. sargentii R. against the human skin-resident micro-flora such as Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Propionibacterium acnes indicated that antimicrobial activity of the ethanol extract was higher than that of the hot water extract.