Pettit George R, Hoffmann Holger, McNulty James, Higgs Kerianne C, Murphy Alison, Molloy David J, Herald Delbert L, Williams Michael D, Pettit Robin K, Doubek Dennis L, Hooper John N A, Albright Leslie, Schmidt Jean M, Chapuis Jean-Charles, Tackett Larry P
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona 85287-2404, USA.
J Nat Prod. 2004 Mar;67(3):506-9. doi: 10.1021/np0204592.
By use of bioassay (murine P388 lymphocytic leukemia cell line) guided isolation procedures, extracts of the Republic of Singapore marine sponge Hymeniacidon sp. were found to contain demethyloxyaaptamine (1) and aaptamine (3) as prominent cancer cell growth inhibitory constituents accompanied by the trace, albeit more active, component isoaaptamine (4). The isolation, X-ray structure elucidation, and antineoplastic and antimicrobial activities of isoaaptamine (4) have been summarized. Because of instability, isoaaptamine (4) was converted to a stable sodium phosphate prodrug designated hystatin 1 (7).
通过生物测定法（小鼠P388淋巴细胞白血病细胞系）指导的分离程序，发现新加坡共和国海洋海绵 Hymeniacidon sp. 的提取物含有去甲基氧化海兔胺（1）和海兔胺（3）作为显著的癌细胞生长抑制成分，同时伴有痕量但活性更高的成分异海兔胺（4）。异海兔胺（4）的分离、X射线结构解析以及抗肿瘤和抗菌活性已作了总结。由于异海兔胺（4）不稳定，将其转化为一种稳定的磷酸钠前药，命名为抑癌素1（7）。
