Aureobasidin作为多药耐药肿瘤细胞中P-糖蛋白的新型抑制剂。

Aureobasidins as new inhibitors of P-glycoprotein in multidrug resistant tumor cells.

作者信息

Kurome T, Takesako K, Kato I

机构信息

Biotechnology Research Laboratories, Takara Shuzo Co., Ltd., Japan.

出版信息

J Antibiot (Tokyo). 1998 Mar;51(3):353-8. doi: 10.7164/antibiotics.51.353.

DOI:10.7164/antibiotics.51.353

PMID:9589072

Abstract

Cyclic depsipeptide antibiotic aureobasidin A (AbA) and its analogs were tested for the inhibitory activity of P-glycoprotein in multidrug resistant cancer cells as well as for the antifungal activity. Some analogs with lower antifungal activity than AbA showed higher inhibition of P-glycoproteins indicating difference of the structure-activity relationships between the two activities. Among AbA analogs tested, [D-beta-hydroxy-methylvalyl9]-AbA newly prepared by chemical synthesis, which had much lower antifungal activity than AbA, showed 10-fold higher inhibitory activity of P-glycoprotein than AbA.

摘要

环缩肽抗生素金担子素A（AbA）及其类似物被测试了对多药耐药癌细胞中P-糖蛋白的抑制活性以及抗真菌活性。一些抗真菌活性低于AbA的类似物对P-糖蛋白的抑制作用更高，这表明两种活性之间的构效关系存在差异。在所测试的AbA类似物中，通过化学合成新制备的[D-β-羟甲基缬氨酸9]-AbA，其抗真菌活性远低于AbA，但对P-糖蛋白的抑制活性比AbA高10倍。