文章基本信息

标题：Mithramycin Represses MDR1 Gene Expression in Vitro, Modulating Multidrug Resistance
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作者：Motoyuki TAGASHIRA ; Takanori KITAGAWA ; Seiji ISONISHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：8
页码：926-929
DOI：10.1248/bpb.23.926
出版社：The Pharmaceutical Society of Japan
摘要：The effect of an aureolic acid, mithramycin (MTM) on multidrug resistance (MDR) was investigated. At a concentration of 0.02-0.1 mg/ml (about 20-90 μM), MTM repressed MDR1 gene transcription of SBC-3/ADM, a MDR-phenotype subline derived from human small cell lung tumor. Under the same conditions, another aureolic acid, chromomycin A₃, showed potent cytotoxicity. FACS analysis revealed that 5 μM MTM depleted the P-glycoprotein (Pgp) and lowered the efflux activity of SBC-3/ADM cells. Furthermore, MTM sensitized the cells against adriamycin^[○!R]. These results suggest that MTM would be a useful modulator of MDR induced by Pgp.
关键词：mithramycin;multidrug resistance;MDR1 gene;P-glycoprotein