Newman David J, Cragg Gordon M
Natural Products Branch, Developmental Therapeutics Program, NCI-Frederick, P.O. Box B, Frederick, Maryland 21702, USA.
J Nat Prod. 2004 Aug;67(8):1216-38. doi: 10.1021/np040031y.
The marine environment has proven to be a very rich source of extremely potent compounds that have demonstrated significant activities in antitumor, antiinflammatory, analgesia, immunomodulation, allergy, and anti-viral assays. Although the case can and has been made that the nucleosides such as Ara-A and Ara-C are derived from knowledge gained from investigations of bioactive marine nucleosides, no drug directly from marine sources (whether isolated or by total synthesis) has yet made it to the commercial sector in any disease. However, as shown in this review, there are now significant numbers of very interesting molecules that have come from marine sources, or have been synthesized as a result of knowledge gained from a prototypical compound, that are either in or approaching Phase II/III clinical trials in cancer, analgesia, allergy, and cognitive diseases. A substantial number of other potential agents are following in their wake in preclinical trials in these and in other diseases.
海洋环境已被证明是极具活性化合物的丰富来源,这些化合物在抗肿瘤、抗炎、镇痛、免疫调节、抗过敏和抗病毒试验中表现出显著活性。尽管有人认为阿糖腺苷(Ara-A)和阿糖胞苷(Ara-C)等核苷是从对具有生物活性的海洋核苷的研究中获得的知识衍生而来,但尚无直接来自海洋来源(无论是分离的还是全合成的)的药物在任何疾病领域进入商业市场。然而,正如本综述所示,现在有大量非常有趣的分子来自海洋来源,或者是由于从原型化合物获得的知识而合成的,它们正在或即将进入癌症、镇痛、过敏和认知疾病的II/III期临床试验。大量其他潜在药物也在这些疾病和其他疾病的临床前试验中紧随其后。