烯二炔类抗肿瘤抗生素的研究进展

Research Advances in The Antitumor Antibiotics of Enediyne

烯二炔类抗生素由稀有放线菌产生,其新颖结构中含有双烯双炔共轭大环,通过形成苯型游离基的方式直接氧化破坏肿瘤细胞DNA分子链,具育抗瘤谱广,强烈的生物学活性和作用机制独持的特点。

The enediyne antibiotics were produced from the culture supernatant of an actinomyces. The antitumor antibiotics of the Esperamicin .Calicheamicin .Dynemicin ,C-1027 .Kedarcidin families have aroused considerable interest owing to their exceptional potency, the potent inhibitory activity against a wide range of tumor cells , the stract ural novelty of their 1, 5-diyne -3-ene core, and their intriguing mode of action. The key mechanism of activation of these compounds toward DNA cleavage is a Bergman cyclization of the encdiyne core triggered by an intramolecular conjugate. The enquisite positioning of the benzyne moiety in the minor groove of DNA has been postulated to lead to double - strand scission by synchronous homolytic hydrogen abstractions.