Shao Rong-guang, Zhen Yong-su
Institute of Medicinal Biotechnology, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, China.
Anticancer Agents Med Chem. 2008 Feb;8(2):123-31. doi: 10.2174/187152008783497055.
The enediyne antibiotics, the potent anticancer agents that contain diyne-ene functional groups, are appreciated for their novel molecular architecture, their remarkable biological activity and their fascinating mechanism of action. Their anticancer activity is apparently due to their ability to damage DNA through radical-mediated hydrogen abstraction. The enediyne antibiotics show markedly cytotoxicities against cancers in vitro and in vivo. Lidamycin is a member of the enediyne anticancer antibiotic family. This review examines lidamycin with particular emphasis on the discovery, the biological properties and its structure-activity relationships. In addition, the possible mechanisms of action of lidamycin are described. Recent progress, particularly in the areas of biosynthesis, and immunoconjugates are highlighted. Finally, the pharmacological applications of lidamycin in cancer therapy and its potential use as anticancer agents are also discussed.
烯二炔类抗生素是一类含有二炔-烯官能团的强效抗癌药物，因其新颖的分子结构、卓越的生物活性和迷人的作用机制而备受关注。它们的抗癌活性显然归因于其通过自由基介导的氢提取来损伤DNA的能力。烯二炔类抗生素在体外和体内对癌症均表现出显著的细胞毒性。力达霉素是烯二炔类抗癌抗生素家族的一员。本综述对力达霉素进行了研究，特别强调了其发现、生物学特性及其构效关系。此外，还描述了力达霉素可能的作用机制。重点介绍了近期的进展，特别是在生物合成和免疫缀合物领域。最后，还讨论了力达霉素在癌症治疗中的药理学应用及其作为抗癌药物的潜在用途。
