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首页> 外文期刊>Biochemistry >STEROID TRANSPORT, ACCUMULATION, AND ANTAGONISM OF P-GLYCOPROTEIN IN MULTIDRUG-RESISTANT CELLS
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STEROID TRANSPORT, ACCUMULATION, AND ANTAGONISM OF P-GLYCOPROTEIN IN MULTIDRUG-RESISTANT CELLS

机译：多药耐药细胞中P-糖蛋白的类固醇转运，积累和拮抗作用

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摘要

According to multiple reports, progesterone is not transported by P-glycoprotein (Pgp), which mediates multidrug resistance through active drug efflux. However, progesterone has been shown to block Pgp-mediated efflux of other drugs. To extend these observations, and to examine the effect of modulating Pgp phosphorylation, the accumulation of progesterone and 14 other steroids in untreated and calphostin C-treated multidrug-resistant human colon carcinoma SW620 Ad300 cells was compared to the accumulation in parental SW620 cells. The accumulation of progesterone in untreated multidrug resistant cells expressing Pgp was not reduced compared to parental cells. However, the accumulation of more hydrophilic steroids was reduced by as much as 50%. Progesterone and progesterone-like compounds, however, were potent inhibitors of Pgp-mediated vinblastine efflux; increased antagonism correlated with increased steroid hydrophobicity. Treatment with calphostin C, a PKC inhibitor which decreases Pgp phosphorylation, increased progesterone efflux, modulated Pgp antagonism by steroids, and inhibited photoaffinity labeling of Pgp by progesterone. These results extend previous observations that Pgp can mediate the transport of, and be antagonized by, a variety of steroids and that these properties vary with both a steroid's hydrophobicity and the phosphorylated state of Pgp.
机译：根据多份报告，孕酮不被P-糖蛋白（Pgp）转运，P-糖蛋白通过活性药物外流介导多药耐药性。然而，黄体酮已被证明可以阻断Pgp介导的其他药物外排。为了扩展这些观察结果，并检查调节Pgp磷酸化的作用，将未经处理和钙磷蛋白C处理的多药耐药人结肠癌SW620 Ad300细胞中的孕酮和14种其他类固醇的积累与亲代SW620细胞中的积累进行了比较。与亲本细胞相比，未处理的表达Pgp的多药耐药细胞中孕酮的积累没有减少。但是，亲水性类固醇的积累减少了多达50％。然而，孕酮和类孕激素化合物是Pgp介导的长春碱流出的有效抑制剂。拮抗作用增加与类固醇疏水性增加有关。用钙磷蛋白C（一种减少Pgp磷酸化，增加黄体酮外排，通过类固醇调节Pgp拮抗作用以及抑制黄体酮对Pgp的光亲和性标记）处理的钙磷蛋白C。这些结果扩展了先前的观察结果，即Pgp可以介导多种类固醇的运输并被其拮抗，并且这些性质随类固醇的疏水性和Pgp的磷酸化状态而变化。

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