塔利索霉素，一种与博来霉素相关的新型抗肿瘤抗生素复合物。V. 新型生物合成塔利索霉素衍生物塔利索霉素S10b的生产、特性及抗肿瘤活性

Tallysomycin, a new antitumor antibiotic complex related to bleomycin. V. Production, characterization and antitumor activity of tallysomycin S10b, a new biosynthetic tallysomycin derivative.

作者信息

Miyaki T, Numata K, Nishiyama Y, Tenmyo O, Hatori M, Imanishi H, Konishi M, Kawaguchi H

出版信息

J Antibiot (Tokyo). 1981 Jun;34(6):665-74. doi: 10.7164/antibiotics.34.665.

DOI:10.7164/antibiotics.34.665

Abstract

Tallysomycin S10b is a biosynthetic derivative of tallysomycin B obtained by precursor amine-feeding fermentation. Tallysomycin S10b contains 1,4-diaminobutane as the terminal amine moiety in place of spermidine of tallysomycin B, and its assigned structure was verified by carbon-13 NMR spectrum. The antitumor activity of tallysomycin S10b was comparable to that of tallysomycin A against sarcoma 180 but less active than the latter against leukemia P388. Tallysomycin S10b was less toxic than tallysomycin A in terms of acute and subacute LD50 values. The nephrotoxic potential of tallysomycin S10b in rats was less than that of tallysomycin A.

摘要

塔利索霉素S10b是通过前体胺进料发酵获得的塔利索霉素B的生物合成衍生物。塔利索霉素S10b含有1,4 - 二氨基丁烷作为末端胺部分，取代了塔利索霉素B中的亚精胺，其指定结构通过碳-13核磁共振光谱得到验证。塔利索霉素S10b对肉瘤180的抗肿瘤活性与塔利索霉素A相当，但对白血病P388的活性低于后者。就急性和亚急性半数致死量值而言，塔利索霉素S10b的毒性低于塔利索霉素A。塔利索霉素S10b在大鼠中的肾毒性潜力小于塔利索霉素A。