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OBJECTIVE To study the in vitro release behavior and anti-tumor effect of paclitaxel-loaded rhein conjugate (PTX/TPGS-CR) micelles. METHODS The in vitro drug release behavior of PTX/TPGS-CR micelles in different release media was investigated by dialysis method with Taxol® as the control. The cytotoxicity of PTX/TPGS-CR micelles on mouse breast cancer 4T1 cells was evaluated by MTT assay with Taxol® as a control. The effect of PTX/TPGS-CR micelles on the cell cycle and apoptosis of human cervical carcinoma HeLa cells was detected by flow cytometry. The effect of PTX/TPGS-CR micelles on the migration of HeLa and 4T1 cells was investigated by scratch experiments. RESULTS The results of in vitro release assay showed that 50.84% and 71.38% of PTX in PTX/TPGS-CR micelles were released in pH 7.4 phosphate buffer (PBS) within 12 and 72 h, respectively, 79.19% of PTX in PTX/TPGS-CR micelles were released in pH 5.8 PBS which simulated the tumor microenvironment within 12 h, and almost all of PTX in the micelles was released within 72 h. The results of the cytotoxicity assay showed that PTX/TPGS-CR micelles had a strong inhibitory effect on the proliferation of 4T1 cells and displayed a time-and-concentration-dependent characteristic, with IC50 of 0.321 9 nmol·mL-1 at 72 h. PTX/TPGS-CR micelles could induce early apoptosis and late apoptosis in HeLa and 4T1 cells. PTX/TPGS-CR micelles can induce HeLa cells arrest in G2/M phase (arrested by PTX) and G0/G1 phase, which inhibited cell division and proliferation. PTX/TPGS-CR micelles can inhibit the migration of HeLa and 4T1 cells and reduce tumor metastasis. CONCLUSION PTX/TPGS-CR micelles have good pH-responsive drug release characteristics, which can release drugs slowly in the blood environment and rapidly in the tumor microenvironment. PTX/TPGS-CR micelles could inhibit tumor cells proliferation and migration and promote cell apoptosis. PTX/TPGS-CR micelles have a good tumor treatment potential.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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