Synthesis and anticancer activity of paclitaxel-coumarin conjugate.

Abstract

BACKGROUND\nPaclitaxel, a natural diterpenoid compound, has anti-tumor effect by acting on tubulin; coumarin, another kind of natural product, has anti-tumor, antibacterial effects and so on. Moreover coumarin has fluorescence.\n\n\nOBJECTIVE\nMulti target to combat tumor is an effective strategy in drug design. Therefore, combination of paclitaxel with other acticive moleculer to explore the novel lead with multi-functons is in demand.\n\n\nMATERIALS AND METHODS\nTo synthsize paclitaxel-coumarin conjugate via click chemistry and to investigate anticancer activity by MTT assay and the scratch test.\n\n\nRESULTS AND DISCUSSION\nThe results of MTT assay showed that compared with paclitaxel, the anti-tumor activity of the conjugate was significantly improved. The results of flow cytometry showed that the conjugate had stronger ability to induce apoptosis. The scratch test results showed that the conjugate had better anti- metastasis ability than paclitaxel.\n\n\nCONCLUSION\nThese findings indicated that paclitaxel and coumarin had synergistic effect, which provided a new idea for the development of paclitaxel monitored by fluorescence.