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海洋生物是抗肿瘤活性物质的重要来源,不同的活性物质因其结构不同而具备不同的生物活性。大环内酯是其中的重要部分,其作用机制主要与结构中的内酯环相关。大多数海洋大环内酯类化合物通过作用于细胞骨架发挥其抗肿瘤活性。细胞骨架包括微丝、微管和中间纤维,微丝和微管分别由肌动蛋白和微管蛋白聚合而成,药物正是通过改变它们的解聚、聚合作用而发挥其抗肿瘤作用。细胞骨架在功能上与细胞结构、胞内运输和细胞分裂密切相关,已成为肿瘤化疗中的新靶点。现综述以细胞骨架为靶点的具有抗肿瘤活性的海洋大环内酯类化合物,以及其作用机制、生物活性的研究进展。
Marine life is an important source of anti-tumor active substances. Different active substances have different biological activities due to their different structures. Macrolides are an important part of it and its mechanism of action is mainly related to the lactone ring in the structure. Most marine macrolides exert their anti-tumor activity by acting on the cytoskeleton. Cytoskeleton includes microfilaments, microtubules and intermediate fibers. Microfilaments and microtubules are polymerized by actin and tubulin respectively. Drugs exert their anti-tumor effect by changing their depolymerization and polymerization. Cytoskeleton is functionally related to cell structure, intracellular trafficking and cell division, and has become a new target in tumor chemotherapy. The review summarizes the antitumor activity of macrolides targeting cytoskeleton, as well as its mechanism of action and biological activity.