Schoettler Sylvia, Bascope Marcelo, Sterner Olov, Anke Timm
Department of Biotechnology, University of Kaiserslautern, Paul-Ehrlich-Str. 23, D-67663 Kaiserslautern, Germany.
Z Naturforsch C J Biosci. 2006 May-Jun;61(5-6):309-14. doi: 10.1515/znc-2006-5-601.
In the course of a screening for compounds inhibiting the growth of two human breast cancer cells lines, two highly cytotoxic compounds were isolated from fermentations of Myrothecium roridum. The elucidation of their structures revealed that they are macrocyclic trichothecenes of the verrucarin type, 16-hydroxyverrucarin A (1), reported here as a natural product for the first time, and verrucarin X (2), a new compound. Both 1 and 2 exhibit moderate antifungal activity and pronounced cytotoxic activity, with IC50 values in the nanomolar (1) and micromolar (2) range. Both compounds preferentially inhibit in vivo protein biosynthesis.
在对抑制两种人乳腺癌细胞系生长的化合物进行筛选的过程中,从绿核菌的发酵产物中分离出了两种具有高度细胞毒性的化合物。对其结构的解析表明,它们是疣孢菌素型的大环单端孢霉烯族毒素,16 - 羟基疣孢菌素A(1),此为首次作为天然产物报道,以及疣孢菌素X(2),一种新化合物。化合物1和2均表现出中等程度的抗真菌活性和显著的细胞毒性活性,其半数抑制浓度(IC50)值分别在纳摩尔(1)和微摩尔(2)范围内。这两种化合物均优先抑制体内蛋白质生物合成。