Reversal effects of milbemycins on multidrug resistance in MCF-7/adr cells

Q4 Pharmacology, Toxicology and Pharmaceutics

中国药理学通报 Pub Date : 2013-10-01 DOI:10.3969/J.ISSN.1001-1978.2013.10.019

Aili Gao, Hongsheng Liang, Zhao Wang, Shuai Liu, Qing Wang, Ning Zhao

引用次数: 0

Abstract

Aim To explore the reversal of MDR(multidrug resistance) by nemadectin and milbemycin β1 from the milbemycin family to adriamycin-resistant human breast carcinoma cells(MCF-7 / adr). Methods MTT assay was used to evaluate the cell suppression rates and reversal effects. Intracellular accumulation of adriamycin was determined by HPLC. The accumulation of rhodamine 123(Rh123) was measured with spectrofluorometer. The expressions of P-gp and the MDR1 gene encoding P-gp were tested by flow cytometry and reverse-transcriptase PCR. Results Nemadectin and milbemycin β1at the high dose of 5 μmol·L- 1significantly increased the sensitivity of MCF-7 / adr cells to adriamycin. They also increased the intracellular accumulation of adriamycin and Rh123 in MCF-7 /adr cells in a dose-dependent manner. Expression of both P-gp and MDR1 was down-regulated to different level. Conclusion Nemadectin and milbemycin β1can partly reverse multidrug resistance of MCF-7 / adr,and the effect of nemadectin is better than that of milbemycin β1.

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米贝霉素对MCF-7/adr细胞多药耐药的逆转作用

目的探讨奈马ectin和milbemycin β1对阿霉素耐药人乳腺癌细胞(MCF-7 / adr)的逆转作用。方法采用MTT法测定细胞抑制率和逆转作用。用高效液相色谱法测定阿霉素在细胞内的蓄积。用荧光分光光度仪测定罗丹明123(Rh123)的积累量。采用流式细胞术和逆转录酶PCR检测P-gp及编码P-gp的MDR1基因的表达。结果5 μmol·L- 1高剂量的奈马菌素和米霉素β1显著提高MCF-7 / adr细胞对阿霉素的敏感性。它们还以剂量依赖的方式增加了MCF-7 /adr细胞内阿霉素和Rh123的积累。P-gp和MDR1的表达均不同程度下调。结论奈马连素和米霉素β1能部分逆转MCF-7 / adr的多药耐药，且奈马连素的效果优于米霉素β1。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

中国药理学通报 Pharmacology, Toxicology and Pharmaceutics-Pharmacology

CiteScore

0.80

自引率

0.00%

发文量

11201

期刊介绍： Chinese Pharmacological Bulletin (CPB) is an academic monthly magazine sponsored by the Chinese Association for Science and Technology, the Chinese Pharmacological Society, and Anhui Medical University. Publicly issued domestically and internationally, CN:34:1086/R,ISSN:1001-1978。 The inclusion status of Chinese Pharmaceutical Bulletin (CPB): 1. This journal has been identified as a core medical journal by the China Science Citation Database (CSCD) of the Document Information Center of the Chinese Academy of Sciences (since 1993, there are 909 journals in the core library); 2. Selected as a pharmaceutical core journal by the editor in chief of Peking University Library's "Overview of Chinese Core Journals" (Peking University Core), 1st to 8th editions (1243 scientific and technological journals, including 232 medical and health journals); 3. Designated by the Institute of Science and Technology Information of the Ministry of Science and Technology of China as a source journal for Chinese scientific and technological paper statistics (China Science and Technology Core Journal); 4. Other: Domestic: Chinese Academic Journal Abstracts, Chinese Basic Medical Abstracts, Chinese Pharmaceutical Abstracts, Chinese Biological Abstracts, Chinese Academic Journals (CD version), Wanfang Database, VIP Database, etc; International: Chemical Abstract (USA), Corrective Bulletin on Science and Technology, CBST (Japan), Biological Abstract (USA), Biochemical Abstract (USA), EMBASE/Excerpta Medica (Netherlands), Index Copernicus (Poland), Kunst and Wissen (Germany), WPRIM (World Health Organization Western Pacific Regional Medical Index), Scopus (Netherlands, 2019 CiteScore 0.9), A&I (Netherlands), Centre for Agriculture and Biosciences international (CAB international, UK), Biosis Previews (USA), etc.