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芳基萘类木脂素鬼臼毒素是从不同鬼臼属植物根茎中提取的树脂中的主要成分,具有显著的抗肿瘤活性。但是由于毒性大限制了其作为抗肿瘤药物的应用,因此对鬼臼毒素开展了大量结构修饰工作。依托泊苷(VP-16)和替尼泊苷(VM-26)作为鬼臼毒素衍生物,现已广泛用作抗肿瘤的临床治疗。然而,临床应用发现依托泊苷和替尼泊苷水溶性差,易产生多药耐药和严重的胃肠道功能紊乱,为了克服上述缺陷,寻找更有效的鬼臼毒素类衍生物显得尤为迫切。本文对鬼臼毒素抗肿瘤作用机制、结构修饰和构效关系进行了总结,为新鬼臼毒素衍生物的合成提供参考。
Arylnaphthalene Lignophyll Podophyllotoxin is a major component of resin extracted from rhizomes of different Podophyllum plants and has significant anti-tumor activity. However, due to its high toxicity limit its application as an anticancer drug, a large amount of structural modification has been carried out on podophyllotoxin. Etoposide (VP-16) and teniposide (VM-26), as podophyllotoxin derivatives, are now widely used as anti-tumor clinical treatments. However, clinical application of etoposide and teniposide found that water solubility is poor, prone to multi-drug resistance and serious gastrointestinal disorders, in order to overcome these shortcomings, looking for more effective podophyllotoxin derivatives is particularly urgent. In this paper, the anti-tumor mechanism of podophyllotoxin, structural modification and structure-activity relationship were summarized for the synthesis of new podophyllotoxin derivatives provide a reference.