Research on “unification of medicines and excipients” nanosystem comprising tea polyphenol and melittin for antitumor therapy / 中草药

ABSTRACT

Objective: To prepare nanocomplex comprising tea polyphenol and melittin (EMN) with synergistic effect for antitumor therapy. Methods: Poly-epigallocatechin gallate (polyEGCG) was synthesized by Bayer reaction and characterized by 1H-NMR and MS spectra. The preparation process of EMN was optimized by orthogonal test, and the in vitro release of EMN was conducted at different medium with different pH. The cell uptake of FITC-labeled Mel and EMN was measured by flow cytometry. The synergistic antitumor effect of polyEGCG and Mel was investigated using B16F10 and A549 cells by MTT assay. Results: The structure of polyEGCG was confirmed by 1H-NMR and MS. The optimized preparation process of EMN was as follws 0.5 mg/mL polyEGCG solution was added dropwise to 1 mg/mL equal volume of Mel solution, and then incubated at room temperature for 30 min. In vitro release studies showed that acidic environment could accelerate the release of Mel. Cell uptake experiments showed that the cell uptake of Mel and EMN was comparable. MTT assay results showed the combination index (CI) of polyEGCG and Mel was less than 1, which intimated the synergistic effect when combined therapy with polyEGCG and Mel. Conclusion: EMN was prepared by a self-assembly method, which has a simple preparation process, a suitable particle size, and synergistic antitumor effect, and it is worthy of further studies.