• Title/Summary/Keyword: MCF-7/ADR cell

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Preparation and Characterization of Tributyrin Sub-micron Emulsion as Carrier for Paclitaxel

  • Fei, Xiang;Xu, Wenting;Yue, Yuan;Lee, Mi-Kyung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.5
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    • pp.295-300
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    • 2011
  • Paclitaxel is a well known anticancer agent and has been a pharmaceutical challenge because of its extremely poor water-solubility and susceptibility to the p-glycoprotein (p-gp)-mediated efflux in multi-drug resistant (MDR) cancer cells. Tributyrin (TB), a triglyceride with relatively short fatty acid chains, was chosen as solubilizing vehicle for paclitaxel based on the solubility study (26.6 mg/mL). Tributyrin (10%) o/w emulsion containing paclitaxel (5%), egg phosphatidylcholine (5%) and pegylated phospholipid (0.5%) was prepared by high pressure homogenization to obtain submicron-sized emulsion. The mean particle size of the resultant TB emulsion was 395.5 nm. Paclitaxel in TB emulsion showed higher anticancer activity against human breast cancer cell line, MCF-7, than free form delivered in DMSO solution. On the other hand, its anticancer activity was significantly reduced in MCF-7/ADR, a MDR variant cancer cell line of MCF-7, and recovered by the presence of verapamil, suggesting of the susceptibility to the p-gp mediated efflux even though paclitaxel was encapsulated into emulsion. The TB emulsion showed great potential as a promising vehicle for water-insoluble anticancer agent, paclitaxel.

P-Glycoprotein Inhibitory Activity of Indonesian Medicinal Plants in Human Breast Cancer Cells

  • Kim, Hyang-Rim;Chung, Soo-Yeon;Jeong, Yeon-Hee;Go, Eun-Jung;Han, Ah-Reum;Kim, Na-Hyung;Sung, Min-Kyung;Song, Gi-Na;Jang, Jung-Ok;Nam, Joo-Won;Lee, Hwa-Jeong;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • v.10 no.6
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    • pp.268-271
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    • 2004
  • In order to examine their effects on the P-glycoprotein (P-gp) activity in human breast cancer cells, MCF-7/ADR, one hundred Indonesian plant extracts were screened. Among them, the five chloroform extracts of Calotropis gigantea, Curcuma aeruginosa, Merremia mammosa, Sindora sumatrana, and Zingiber cassumunar, showed the most potent P-gp inhibitory activity. When each of these extracts was treated together with the anticancer agent, daunomycin, they increased the cytotoxic activity of daunomycin up to $IC_{50}$ values of less than $6.62\;{\mu}M$, which is a value with a positive control, verapamil. Also, other 15 plant extracts exhibited significant P-gp inhibitory activity with $IC_{50}$ values between 6.62 and $13.20\;{\mu}M$. These prospective samples will be subjected to further laboratory phytochemical investigation to find active principles.

Effect of ${\alpha}$-Glycosidase Inhibitor in Multidrug Resistant Cell Lines

  • Paek, Nam-Soo;Namgung, Jun;Lee, Jung-Joon;Choi, Yong-Jin;Kim, Tae-Han;Kim, Kee-Won
    • BMB Reports
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    • v.31 no.3
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    • pp.269-273
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    • 1998
  • The objective of this study was to evaluate the reversal of multi drug resistance of human cell lines by specific inhibitors of ${\alpha}-glycosidase$ and mannosidases that had been reported to be involved in N-linked oligosaccharide processing of glycoproteins. N-methyldeoxynojirimycin, I-deoxynojirimycin, and castanospermine, which were known to be potent inhibitors of both ${\alpha}-glycosidase$ I and II, showed no activity against the multidrug resistant phenotype of the cell lines of SNU1DOX, KB-V1, and MCF-7/ADR. In contrast, I-deoxymannojirimycin, an inhibitor of mannosidase I, resulted in a slight reversal for the vinblastine resistance of the KB-V1 cell line, but did not show any activity toward the other cell lines. Parallel experiments with tunicamycin, an inhibitor of N-linked glycosylation, also resulted in no significant changes in multidrug resistant (MDR) phenotype of the cell lines tested in this work. These observations suggest that the unglycosylation of P-glycoprotein associated with the inhibitor treatments might not be correlated with the reversal of multidrug resistance of the cell lines tested in this study.

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