Reversal of P-Glycoprotein Mediated Multidrug Resistance in K562 Cell Line by a Novel Synthetic Calmodulin Inhibitor, E6(Pharmacology)

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概要

• 論文の詳細を見る

• The overexpression of P-glycoprotein (P-gp) is associated with multidrug resistance (MDR) of tumor cells to a number of chemotherapeutic drugs. P-gp inhibitors have been shown to effectively reverse P-gp-mediated MDR in both in vitro and in vivo. Our previous studies demonstrated that E6, a novel synthetic calmodulin inhibitor, exhibited potent inhibitory effect on P-gp in rat brain microvessel endothelial cells (RBMECs). In the present study, the effect of E6 on MDR in a K562 MDR cell line (K562/DOX) highly expressing P-gp was studied and compared with that of a conventional P-gp inhibitor, verapamil (VER). E6 at concentrations of 1, 3, 10, 30μM reduced the IC_<50> value of doxorubicin in K562/DOX cells from 79.19μm to 35.18, 21.86, 6.31 and 1.97μM, respectively. However, the IC_<50> value of doxorubicin in K562 sensitive subline was not significantly changed by E6. Using a DNA content analysis and an annexin V binding assay, the effects of E6 on doxorubicin-induced apoptosis were also examined. The results indicated that E6 effectively reversed the resistance to doxorubicin-induced apoptosis in K562/DOX cells. In addition, co-treatment of E6 and doxorubicin resulted in a remarkably G2/M blocking effect in K562/DOX cells. Furthermore, the treatment of K562/DOX cells with 10μM E6 led to increased intracellular accumulation and decreased efflux of doxorubicin. Overall, the pharmacological effects of E6 on P-gp-mediated MDR is much stronger than that of positive control drug VER. These results suggested that E6 is a novel and potent MDR reversal agent and may be a potential adjunctive agent for tumor chemotherapy.

• 公益社団法人日本薬学会の論文
• 2005-10-01

著者

• GUO Qing-Long

  Department of Physiology, China Pharmaceutical University

• Guo Qing-long

  中華人民共和国

• Guo Qing-long

  Department Of Physiology No. 24 Tong Jia Xiang China Pharmaceutical University

• Wang Jun

  Department Of Electrical Electronic And Information Engineering Osaka University

• Wang Jun-sheng

  米国

• ZHU Hao

  Department of Pharmaceutical Sciences, Medical University of South Carolina

• GUO Qing

  Department of Physiology, China Pharmaceutical University

• JIANG Yan

  Department of Pharmacology, China Pharmaceutical University

• LIU Guo

  Department of Pharmacology, China Pharmaceutical University

• Wang Jun

  Department Of Chemistry Faculty Of Science And Engineering Saga University

• Zhu Hao-jie

  Department Of Pharmaceutical And Biomedical Sciences Medical University Of South Carolina

• Zhu Hao

  Department Of Pharmaceutical Sciences Medical University Of South Carolina

• Guo Qing

  Department Of Physiology China Pharmaceutical University

• Jiang Yan

  Department Of Pharmacology China Pharmaceutical University

• Guo Qing

  Department Of Dermatology And Venerology The Second Affiliated Hospital Of Sun Yat-sen University

• Wang Jun

  Department Of Automation And Computer-aided Engineering The Chinese University Of Hong Kong

• Wang Jun-Sheng

  Department of Psychiatry and Behavioral Sciences, Medical University of South Carolina

• JIANG Yan

  Department of Endocrinology, Key Laboratory of Endocrinology, Ministry of Health, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences

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