Kunze B, Jansen R, Sasse F, Höfle G, Reichenbach H
GBF, Gesellschaft für Biotechnologische Forschung mbH, Abteilung Naturstoffbiologie, Braunschweig, Germany.
J Antibiot (Tokyo). 1998 Dec;51(12):1075-80. doi: 10.7164/antibiotics.51.1075.
A novel macrolide, apicularen A, was produced by several species of the genus Chondromyces. Initially it was discovered by bioassay-guided RP-HPLC-fractionation of culture extracts of Chondromyces robustus, strain Cm a13. Apicularen A showed no antimicrobial activity, but was highly cytotoxic for cultivated human and animal cells, with IC50 values ranging between 0.1 and 3 ng/ml. A cometabolite of apicularen A, the N-acetylglucosamine glycoside apicularen B, was distinctly less cytotoxic with IC50 values between 0.2 and 1.2 microg/ml, and showed weak activity against a few Gram-positive bacteria. Apicularen A is chemically closely related to the salicylihalamides A and B from the marine sponge Haliclona sp.
一种新型大环内酯类化合物——顶枝孢菌素A，由几种顶枝孢属的物种产生。最初它是通过对强壮顶枝孢菌株Cm a13的培养提取物进行生物测定引导的反相高效液相色谱分级分离而发现的。顶枝孢菌素A没有抗菌活性，但对培养的人和动物细胞具有高度细胞毒性，半数抑制浓度（IC50）值在0.1至3纳克/毫升之间。顶枝孢菌素A的一种共代谢产物，N-乙酰葡糖胺糖苷顶枝孢菌素B，细胞毒性明显较低，IC50值在0.2至1.2微克/毫升之间，并且对一些革兰氏阳性细菌表现出微弱活性。顶枝孢菌素A在化学上与来自海洋海绵Haliclona sp.的水杨酰卤酰胺A和B密切相关。
