动力霉素非二炔类和氮杂蒽醌类的细胞毒性及DNA结合特性。

Cytotoxicity and DNA-binding property of non-diynene class of dynemicins and aza-anthraquinones.

作者信息

Shirai R, Shimazawa R, Shichita M, Takahashi M, Hashimoto Y, Iwasaki S

机构信息

Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.

出版信息

Nucleic Acids Symp Ser. 1995(34):151-2.

PMID:8841597

Abstract

Dynemicin A is a potent antibacterial and antitumor antibiotic having a striking hybrid structure of both anthraquinone as a DNA intercalator and diynene as a DNA strand breaker. We have investigated the DNA-binding property and cytotoxicity of non-diynene class of dynemicins (H, L, M, O and Q) and several related synthetic tri- and pentacyclic aza-anthraquinones 1a-3a (R = H) and 1b-3b (R = CH3). Among them, dynemicin H, L, M, O, Q, 1a, 1b and 2b exhibited DNA-binding property. All non-diynene class of dynemicins investigated exhibited intercalative binding activity, however, synthetic aza-anthraquinones 1a-3a did not show such ability. Dynemicin H, Q, 2a, 2b and 3b showed cytotoxicity against HL-60 and K-562 cell lines.

摘要

力达霉素A是一种强效抗菌和抗肿瘤抗生素，具有独特的杂合结构，它同时含有作为DNA嵌入剂的蒽醌和作为DNA链断裂剂的二炔结构。我们研究了非二炔类力达霉素（H、L、M、O和Q）以及几种相关的合成三环和五环氮杂蒽醌1a - 3a（R = H）和1b - 3b（R = CH3）的DNA结合特性和细胞毒性。其中，力达霉素H、L、M、O、Q、1a、1b和2b表现出DNA结合特性。所有研究的非二炔类力达霉素均表现出嵌入结合活性，然而，合成氮杂蒽醌1a - 3a却没有这种能力。力达霉素H、Q、2a、2b和3b对HL - 60和K - 562细胞系表现出细胞毒性。