Yi S N, Wass J, Vincent P, Iland H
Kanematsu Laboratories, Royal Prince Alfred Hospital, Camperdown, NSW, Australia.
Leuk Res. 1991;15(10):883-6. doi: 10.1016/0145-2126(91)90163-n.
Mylabris, the dried body of the Chinese blister beetle, has been used as a Chinese medicinal for over 2000 years. Its active constituent, cantharidin, has antitumor properties and causes leukocytosis. Norcantharidin (NCTD), the demethylated form of cantharidin, is easier to synthesize and is less toxic. NCTD irreversibly reduced the clonogenic efficiency of parental and drug-resistant K562 sublines, with drug-resistant sublines showing greater susceptibility to NCTD than parental cells. NCTD inhibited DNA synthesis by blocking cells at the G2/M phase of the cell cycle. The data suggest that NCTD may be suitable in the treatment of drug-resistant leukemia.
斑蝥，即中国芫菁的干燥虫体，作为一味中药已使用了两千多年。其活性成分斑蝥素具有抗肿瘤特性并可引起白细胞增多。去甲斑蝥素（NCTD）是斑蝥素的去甲基化形式，更容易合成且毒性较小。NCTD不可逆地降低了亲本及耐药K562亚系的克隆形成效率，耐药亚系对NCTD的敏感性高于亲本细胞。NCTD通过将细胞阻滞在细胞周期的G2/M期来抑制DNA合成。这些数据表明NCTD可能适用于耐药白血病的治疗。
