BIOLOGICAL STUDIES ON THE DEGRADATION PRODUCTS OF 3-[(S)-1'-PHENYLETHYLAMINO]PROPYLAMINOBLEOMYCIN - NOVEL ANALOG (PEPLEOMYCIN)

被引：51

作者：

TAKAHASHI, K ^{[1
]}

EKIMOTO, H ^{[1
]}

AOYAGI, S ^{[1
]}

KOYU, A ^{[1
]}

KURAMOCHI, H ^{[1
]}

YOSHIOKA, O ^{[1
]}

MATSUDA, A ^{[1
]}

FUJII, A ^{[1
]}

UMEZAWA, H ^{[1
]}

机构：

[1] INST MICROBIAL CHEM,SHINAGAWA KU,TOKYO 141,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1979年 / 32卷 / 01期

关键词：

D O I：

10.7164/antibiotics.32.36

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Pepleomycin (PEP), 3-[(S) -l'-phenylethylamino]propylaminobleomycin has potent activity and is less pulmonary toxic than bleomycin (BLM). Biological activity and toxicity of the following degradation products of PEP have been studied in detail : the product of carbamoyl migration (ISO), the product of decarbamylation (DC), the product of ring closure of the side chain on the pyrimidine moiety (RC), the depyruvamide product (DP) and the product of an enzymatic inactivation (DA). These degradation products showed much lower activity than PEP in vitro: antimicrobial and anti-HeLa activities, inhibition of DNA synthesis in AH66 cells and the DNA strand cleavage. Acute toxicity and pulmonary toxicity were tested in mice. Results indicated much lower acute toxicity corresponding to the decreased in vitro activity when compared to PEP. DP and RC did not cause lung fibrosis in mice, while ISO and DC showed 1/2.6 and 1/5.7 degree of pulmonary toxicity, respectively, in comparison with PEP. © 1979, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.

引用

页码：36 / 42

页数：7

共 12 条

[1] PROCEDURE FOR ISOLATION OF DEOXYRIBONUCLEIC ACID FROM MICRO-ORGANISMS [J].