Pettit G R, Kamano Y, Fujii Y, Herald C L, Inoue M, Brown P, Gust D, Kitahara K, Schmidt J M, Doubek D L, Michel C
J Nat Prod. 1981 Jul-Aug;44(4):482-5. doi: 10.1021/np50016a016.
A fifteen year investigation of marine animal components as sources for new and potentially useful cancer chemotherapeutic drugs has led to our discovery of a number of such valuable substance. The especially productive Indian Ocean sea hare Dolabella auricularia has yielded (100 kg leads to or approximately 1 mg each) a series of very potent cell growth inhibitory substances designated dolastatins 1-9. The first member of this new series, dolastatin 1, may represent the most potent anticancer agent so far uncovered with, e.g., a curative response (33%) using a dose of 11 microgram/kg (T/C 240, to T/C 139 at 1.37 microgram/kg) in the National Cancer Institute's murine B16 melanoma. Structural elucidation of the new antineoplastic agents is underway, and recent progress is illustrated with peptide dolastatin 3 (P388 ED 50 2.7 x 10(-7) microgram/ml).
对海洋动物成分作为新型且可能有用的癌症化疗药物来源进行的为期十五年的研究，使我们发现了许多此类有价值的物质。特别高产的印度洋海兔——耳状截尾海兔，已产生（100千克可提取出约1毫克每种）一系列非常有效的细胞生长抑制物质，命名为多拉司他汀1 - 9。这个新系列的首个成员多拉司他汀1，可能是迄今为止发现的最有效的抗癌剂，例如，在国立癌症研究所的小鼠B16黑色素瘤实验中，使用剂量为11微克/千克（T/C为240，在1.37微克/千克时降至T/C 139），有治愈反应（33%）。新型抗肿瘤药物的结构解析正在进行中，最近以肽类多拉司他汀3（P388半数有效剂量为2.7×10⁻⁷微克/毫升）为例说明了进展情况。
