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Review Article

斑鳖素及其类似物抗癌作用的研究进展

卷 30, 期 18, 2023

发表于: 27 December, 2022

页: [2006 - 2019] 页: 14

弟呕挨: 10.2174/0929867330666221103151537

价格: $65

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摘要

背景：斑蝥素（CTD）是一种剧毒物质，可用于治疗多种癌症。然而，由于其严重的副作用，临床应用受到限制。近年来，筛选其类似物、探索其作用机制以及使用某些物质的联合治疗被认为是减少副作用并提高CTD治疗活性的可行方法。该综述旨在描述CTD类似物的SAR（构效关系）、CTD诱导机制和联合治疗探索。 方法：我们通过输入数据库搜索关于CTD的研究。有目的地筛选和提取重要信息，包括SAR、机制、方法等。 结果：一些在C-5和C-6位具有咪唑鎓盐或双键的CTD类似物显示出良好的抗癌活性。通过在C-1或C-4位置引入甲基和乙酰氧基，PP的抑制作用减弱甚至失活。去除C-2和C-3的两个甲基可以减少副作用并提高疗效。用氟取代甲基也可以提高活性并降低毒性。通过打开五元酸酐环形成羧酸、盐、酰胺和酯衍生物，可以提高水溶性和生物利用度。抗癌机制可分为以下几个方面，包括抑制细胞侵袭和转移、诱导细胞凋亡、调节细胞周期和增强免疫力。CTD及其类似物（脂质体、纳米粒子和胶束）的合理配方可以提高癌症的靶向性，减少毒副作用。CTD联合抗血管生成药物（人参皂苷Rg3、贝伐单抗、阿帕替尼和Endostar）显示出额外的抗胰腺癌症作用。 结论：发现其潜在机制与多通道和多靶点相互作用密切相关，为后续探索新的临床治疗应用提供了指导方向。然而，一些详细的机制仍然不清楚，需要更多的证据来验证。此外，提高CTD及其类似物治疗潜力的新方法在未来仍需进行更多的临床试验。这一前景非常广阔，值得进一步研究。

关键词: 斑鳌素，毒性，抗癌，副作用，构效关系，联合治疗。

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