Using rhodamine 123 accumulation in CD8 + cells as a surrogate indicator to study the P-glycoprotein modulating effect of cepharanthine hydrochloride in vivo

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Abstract

The purpose of this study was the use of rhodamine 123 (Rho123) accumulation in peripheral blood CD8 + cells as a surrogate indicator to evaluate the modulating effect of P-glycoprotein (P-gp) inhibitors in the multidrug resistance (MDR) tumor-bearing mouse model. Rho123 was administered to mice, and the fluorescence level in CD8 + cells was measured. Cepharanthine hydrochloride (CH) and verapamil (VER), two P-gp inhibitors, were administered to mice 1 hour prior to Rho123 administration in vivo or added to peripheral blood 1 hour prior to Rho123 addition ex vivo. The tumor inhibition effect of 5-fluorouracil/adriamycin/cisplatin (FAP) protocol plus CH was also investigated. A concentration- or dose-response relationship was shown between the concentration and dose of CH and Rho123 accumulation or the antitumor activity. In conclusion, the measurement of Rho123 accumulation in CD8 + cells provides a surrogate assay for the screening of candidate P-gp inhibitors in preclinical trials, and CH is effective in modulating P-gp-mediated MDR in vivo. Copyright © 2011 Han Li et al.

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Qing-Duan, W., Li, H., Yan, Z., Ning, W., Xiao-Juan, G., Cai-Hong, Z., … Fang, M. (2011). Using rhodamine 123 accumulation in CD8 + cells as a surrogate indicator to study the P-glycoprotein modulating effect of cepharanthine hydrochloride in vivo. Journal of Biomedicine and Biotechnology, 2011. https://doi.org/10.1155/2011/281651

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