BACKGROUND Paclitaxel, a natural diterpenoid compound, has anti-tumor effect by acting on tubulin, whereas coumarin, another kind of natural product, has anti-tumor effect, along with some other effects, such as anti-bacterial-., Moreover, it also possesses fluorescence. OBJECTIVE Multi targeting is an effective strategy in drug design to combat tumor. Therefore, a combination of paclitaxel with other active molecular drugs for exploring the novel lead with multi-functions is in demand. MATERIALS AND METHODS To synthsize paclitaxel-coumarin conjugate via click chemistry and to investigate anticancer activity by MTT assay and the scratch test. RESULTS AND DISCUSSION The results of MTT assay showed that compared tothe paclitaxel, the anti-tumor activity of the conjugate was significantly improved. The results of flow cytometry showed that the conjugate had a stronger ability to induce apoptosis. The scratch test results showed that the conjugate had better anti- metastasis ability than paclitaxel. CONCLUSION These findings indicated that paclitaxel and coumarin had a synergistic effect, which paved the way for the development of paclitaxel through fluorescence.

中文翻译：

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紫杉醇-香豆素偶联物的合成和抗癌活性。

背景技术紫杉醇是一种天然的二萜类化合物，通过作用于微管蛋白而具有抗肿瘤作用，而另一种天然产物香豆素具有抗肿瘤作用，同时具有抗菌等其他作用。也有荧光。目的多靶向是药物设计中对抗肿瘤的有效策略。因此，需要紫杉醇与其他活性分子药物的组合，以探索具有多功能的新型先导药物。材料与方法通过点击化学合成紫杉醇-香豆素偶联物，并通过MTT法和划痕试验研究抗癌活性。结果与讨论MTT法结果表明，与紫杉醇相比，偶联物的抗肿瘤活性显着提高。流式细胞术结果表明偶联物具有较强的诱导细胞凋亡能力。划痕试验结果表明，该偶联物比紫杉醇具有更好的抗转移能力。结论这些发现表明紫杉醇和香豆素具有协同作用，这为紫杉醇的荧光开发铺平了道路。