Xu Shu, Ge Hui Ming, Song Yong Chun, Shen Yao, Ding Hui, Tan Ren Xiang
Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, P. R. China.
Chem Biodivers. 2009 May;6(5):739-45. doi: 10.1002/cbdv.200800034.
In addition to the known metabolites cytochalasin H (1), cytochalasin J (2), and epoxycytochalasin H (3), two new 10-phenyl-(11)-cytochalasans, named cytochalasin Z10 and Z11 (4 and 5, resp.) were isolated from the solid substrate culture of Endothia gyrosa IFB-E023, an endophytic fungus residing inside the healthy leaf of Vatica mangachapo (Dipterocarpaceae). The structure determination of 4 and 5 was accomplished through correlative analyses of their spectral data (UV, ESI-MS, IR, (1)H- and (13)C-NMR, COSY, NOESY, HMQC, and HMBC). Metabolites 1-5 were demonstrated to be substantially cytotoxic to the human leukaemia K562 cell line with the IC(50) values of 10.1, 1.5, 24.5, 28.3, and 24.4 microM, respectively, which are comparable to that of 5-fluorouracil (33.0 microM), co-assayed as the positive reference.
除了已知的代谢产物细胞松弛素H(1)、细胞松弛素J(2)和环氧细胞松弛素H(3)外,还从陀螺痂囊腔菌IFB-E023(一种生长在青梅(龙脑香科)健康叶片内的内生真菌)的固体基质培养物中分离出两种新的10-苯基-(11)-细胞松弛素,分别命名为细胞松弛素Z10和Z11(分别为4和5)。通过对它们的光谱数据(紫外光谱、电喷雾电离质谱、红外光谱、氢核磁共振和碳核磁共振、化学位移相关谱、核Overhauser效应谱、异核多量子相干谱和异核多键相关谱)进行关联分析,确定了4和5的结构。已证明代谢产物1-5对人白血病K562细胞系具有显著的细胞毒性,其半数抑制浓度(IC50)值分别为10.1、1.5、24.5、28.3和24.4微摩尔,与作为阳性对照共同检测的5-氟尿嘧啶(33.0微摩尔)相当。