Selenorhodamine photosensitizers for photodynamic therapy of P-glycoprotein-expressing cancer cells.

Selenorhodamine photosensitizers for photodynamic therapy of P-glycoprotein-expressing cancer cells.
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DOI:
10.1021/jm501259v
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发表时间:
2014-10-23
影响因子:
7.3
通讯作者:
Detty MR
Detty MR
中科院分区:
医学1区
文献类型:
--
作者:
Hill JE;Linder MK;Davies KS;Sawada GA;Morgan J;Ohulchanskyy TY;Detty MR

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We examined a series of selenorhodamines with amide and thioamide functionality at the 5-position of a 9-(2-thienyl) substituent on the selenorhodamine core for their potential as photosensitizers for photodynamic therapy (PDT) in P-glycoprotein (P-gp) expressing cells. These compounds were examined for their photophysical properties (absorption, fluorescence, and ability to generate singlet oxygen), for their uptake into Colo-26 cells in the absence or presence of verapamil, for their dark and phototoxicity toward Colo-26 cells, for their rates of transport in monolayers of multidrug-resistant, P-gp-overexpressing MDCKII-MDR1 cells, and for their colocalization with mitochondrial specific agents in Colo-26 cells. Thioamide derivatives 16b and 18b were more effective photosensitizers than amide derivatives 15b and 17b. Selenorhodamine thioamides 16b and 18b were useful in a combination therapy to treat Colo-26 cells in vitro: a synergistic therapeutic effect was observed when Colo-26 cells were exposed to PDT and treatment with the cancer drug doxorubicin.
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