He Xiangjiu, Tang Jinshan, Qiao Aimin, Wang Guanghui, Jiang Miaomiao, Liu Rui Hai, Yao Xinsheng
Institute of Traditional Chinese Medicine & Natural Products, Jinan University, Guangzhou, China.
Steroids. 2006 May;71(5):392-402. doi: 10.1016/j.steroids.2005.12.003. Epub 2006 Feb 15.
Cinobufagin (1) was one of important cardenolidal steroids and major components of Chan'Su, a famous traditional Chinese medicine. Bioconversion of cinobufagin by the fungi of Mucor spinosus and Aspergillus niger were investigated. Nine bioconversion products were obtained from M. spinosus and seven products from A. niger. Their structures were elucidated by high-resolution fast atom bombardment mass spectroscopy (HR-FAB-MS), extensive NMR techniques, including (1)H NMR, (13)C NMR, DEPT, (1)H-(1)H correlation spectroscopy (COSY), two-dimensional nuclear Overhauser effect correlation spectroscopy (NOESY), heteronuclear multiple quantum coherence (HMQC) and heteronuclear multiple bond coherence (HMBC). The in vitro cytotoxic activities against human hepatoma cells (HepG2, SMMC-7221 and BEL-7402) and human leukemia cells (K562, HL-60 and HEL) of all bioconversion products were determined by the MTT method, and their structure-activity relationships (SAR) were discussed.
华蟾酥毒基（1）是重要的强心甾体类化合物之一，也是著名中药蟾酥的主要成分。研究了棘孢毛霉和黑曲霉对华蟾酥毒基的生物转化。从棘孢毛霉中获得了9种生物转化产物，从黑曲霉中获得了7种产物。通过高分辨快原子轰击质谱（HR-FAB-MS）、广泛的核磁共振技术（包括1H NMR、13C NMR、DEPT、1H-1H相关光谱（COSY）、二维核Overhauser效应相关光谱（NOESY）、异核多量子相干（HMQC）和异核多键相干（HMBC））阐明了它们的结构。采用MTT法测定了所有生物转化产物对人肝癌细胞（HepG2、SMMC-7221和BEL-7402）和人白血病细胞（K562、HL-60和HEL）的体外细胞毒活性，并探讨了它们的构效关系（SAR）。
