一株内生真菌米曲霉中分离得到的新型细胞毒三萜烯大环内酯。
A new cytotoxic trichothecene macrolide from the endophyte Myrothecium roridum.
机构信息
Medical College, Yangzhou University, Yangzhou, P. R. China.
出版信息
Planta Med. 2010 Jul;76(10):1004-6. doi: 10.1055/s-0029-1240897. Epub 2010 Mar 1.
A new cytotoxic roridin-type trichothecene macrolide named roritoxin E(1) was characterized from the solid culture of Myrothecium roridum IFB-E091 (residing originally inside Artemisia annua root), together with the known compounds lumichrome (2), (22 E,24 S)-cerevisterol (3), and (22 E,24 R)-6 beta-methoxy-ergosta-7,22-diene-3 beta,5 alpha-diol (4). The structure of the new macrolide (1) was elucidated by a combination of spectroscopic (UV, IR, MS, and 1D and 2D NMR) analyses. Compound 1 was demonstrated to be inhibitory in vitro against the gastric carcinoma SGC-7901 and hepatocarcinoma SMMC-7721 cell lines, with IC (50) values of 0.26 and 10.54 microg/mL, respectively. 5-Fluorouracil co-assayed as a positive control had an IC (50) value of 6.66 microg/mL against SGC-7901 cells, and it demonstrated only a 9.98 % growth inhibition against SMMC-7721 cells at 10 microg/mL.
从内生在青蒿（Artemisia annua）根部的米黑毛霉（Myrothecium roridum）IFB-E091 的固体发酵物中，分离得到了一个新型细胞毒素罗托毒素 E（1），同时还分离得到了已知化合物色胺酮（2）、（22E，24S）-酵母甾醇（3）和（22E，24R）-6β-甲氧基-麦角甾-7，22-二烯-3β，5α-二醇（4）。通过光谱（UV、IR、MS 以及 1D 和 2D NMR）分析，鉴定了新大环内酯（1）的结构。1 体外显示对胃癌 SGC-7901 和肝癌 SMMC-7721 细胞株具有抑制活性，IC50 值分别为 0.26 和 10.54μg/mL。阳性对照 5-氟尿嘧啶的 IC50 值为 6.66μg/mL，对 SGC-7901 细胞的生长抑制率为 9.98%，在 10μg/mL 时对 SMMC-7721 细胞的生长抑制率仅为 9.98%。
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