Deoxycholic acid derivatives as inhibitors of P-glycoprotein-mediated multidrug efflux

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• 作者：Luc Rocheblave^a ; ^{luc.rocheblave@univ-lyon1.fr} ; Marc Rolland de Ravel^b ; Elodie Monniot^a ; Jeremy Tavenard^a ; Claude-Yves Cuilleron^a ; Catherine Grenot^a ; Sylvie Radix^a ; Eva-Laure Matera^b ; Charles Dumontet^b ; Nadia Walchshofer^a ; ^{nadia.walchshofer@univ-lyon1.fr}
• 关键词：Multidrug resistance ; P-glycoprotein inhibitors ; Deoxycholic acid derivatives
• 刊名：Steroids
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：116
• 期：Complete
• 页码：5-12
• 全文大小：618 K
• 卷排序：116

文摘

Deoxycholic acid derivatives were identified as P-glycoprotein modulators. All derivatives were evaluated through daunorubicin accumulation in K562/R7 cells. All derivatives were evaluated through potentiation of doxorubicin in K562/R7 cells. Intrinsic toxicity of all derivatives was evaluated on K562 cells. Some deoxycholic acid derivatives are more active and less toxic than cyclosporine A.