Shah A, Naliapara Y, Sureja D, Motohashi N, Kawase M, Miskolci C, Szabo D, Molnár J
Department of Chemistry, Saurashtra University, Rajkot, India.
Anticancer Res. 1998 Jul-Aug;18(4C):3001-4.
Six 6,12-dihydro-1-benzopyrano[3,4-b][1,4]benzothiazin-6-ones and three coumarins were systematically investigated for reversal of multidrug resistance of bacteria and cancer cells in model experiments. 7-Methylcoumarin was able to eliminate the E. coli plasmid significantly; however, the other derivatives were ineffective. Four of 6,12-dihydro-1-benzopyrano[3,4-b] [1,4]benzothiazin-6-ones had a moderate effect on the multidrug resistance efflux pump of mouse lymphoma cells in vitro. Despite of the similarity of resistance mechanisms of bacteria and tumor cells, the reversal of drug resistance in bacteria and in cancer cells is not uniform because the structure-activity requirements are apparently different.
在模型实验中，对六种6,12-二氢-1-苯并吡喃并[3,4-b][1,4]苯并噻嗪-6-酮和三种香豆素进行了系统研究，以探讨其对细菌和癌细胞多药耐药性的逆转作用。7-甲基香豆素能够显著消除大肠杆菌质粒；然而，其他衍生物则无效。六种6,12-二氢-1-苯并吡喃并[3,4-b][1,4]苯并噻嗪-6-酮中的四种对小鼠淋巴瘤细胞的多药耐药外排泵在体外有中等程度的作用。尽管细菌和肿瘤细胞的耐药机制相似，但由于结构-活性要求明显不同，细菌和癌细胞的耐药逆转情况并不一致。
