Kameyama T, Takahashi A, Matsumoto H, Kurasawa S, Hamada M, Okami Y, Ishizuka M, Takeuchi T
Institute of Microbial Chemistry, Tokyo, Japan.
J Antibiot (Tokyo). 1988 Nov;41(11):1561-7. doi: 10.7164/antibiotics.41.1561.
Thrazarine, O-[(3R)-2-diazo-3-hydroxybutyryl)]-L-serine, is a new antitumor antibiotic produced by Streptomyces coerulescens MH802-fF5. Thrazarine was isolated from culture filtrate by Sephadex LH-20 column chromatography and reversed phase HPLC. Thrazarine induced cytolysis of tumor cell lines co-cultured with nonactivated macrophages. This effect was tumor specific because the nontumorigenic cells were not lysed by macrophages in the presence of thrazarine. Thrazarine inhibited DNA synthesis and growth of tumor cells directly. It showed neither antimicrobial activity nor the inhibition of transamidation reactions in contrast to azaserine. Toxicities of thrazarine were much weaker than those of azaserine.
噻嗪菌素，O-[(3R)-2-重氮-3-羟基丁酰基]-L-丝氨酸，是由天蓝色链霉菌MH802-fF5产生的一种新型抗肿瘤抗生素。噻嗪菌素通过Sephadex LH-20柱色谱和反相高效液相色谱从培养滤液中分离得到。噻嗪菌素可诱导与未活化巨噬细胞共培养的肿瘤细胞系发生细胞溶解。这种作用具有肿瘤特异性，因为在噻嗪菌素存在的情况下，非致瘤细胞不会被巨噬细胞裂解。噻嗪菌素直接抑制肿瘤细胞的DNA合成和生长。与重氮丝氨酸相比，它既没有抗菌活性，也没有抑制转酰胺反应。噻嗪菌素的毒性比重氮丝氨酸弱得多。
