洛哌丁胺，一种美国食品药品监督管理局批准的抗腹泻药物，能有效逆转多药耐药 MCF-7/MDR1 人乳腺癌细胞对阿霉素诱导的细胞毒性的耐药性。
Loperamide, an FDA-approved antidiarrhea drug, effectively reverses the resistance of multidrug resistant MCF-7/MDR1 human breast cancer cells to doxorubicin-induced cytotoxicity.
机构信息
Department of Oral Pathology, Howard University, Washington, DC, USA.
出版信息
Cancer Invest. 2012 Feb;30(2):119-25. doi: 10.3109/07357907.2011.640653.
Abstract
Loperamide is an FDA-approved antidiarrhea drug which acts on the μ-opioid receptors in the mesenteric plexus of large intestine and exhibits limited side effects. We hypothesized that loperamide might reverse the multidrug resistance (MDR) of human cancer cells to chemotherapeutic agents. MCF-7/MDR1 cells express high level of MDR1 and are resistant to doxorubicin. We found that loperamide significantly enhanced the cytotoxicity of doxorubicin to MCF-7/MDR1 cells in a dose-dependent manner. In conclusion, loperamide reversed the resistance of MCF-7/MDR1 cells to doxorubicin, suggesting that chemotherapy in combination with loperamide may benefit patients with MDR tumors once applied in clinic.
摘要
洛哌丁胺是一种获得 FDA 批准的抗腹泻药物，它作用于大肠肠系膜丛中的 μ-阿片受体，表现出有限的副作用。我们假设洛哌丁胺可能逆转人癌细胞对化疗药物的多药耐药性（MDR）。MCF-7/MDR1 细胞表达高水平的 MDR1 并对阿霉素耐药。我们发现洛哌丁胺以剂量依赖性方式显著增强阿霉素对 MCF-7/MDR1 细胞的细胞毒性。总之，洛哌丁胺逆转了 MCF-7/MDR1 细胞对阿霉素的耐药性，表明化疗联合洛哌丁胺一旦在临床上应用，可能使 MDR 肿瘤患者受益。
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