OBJECTIVE: To study the reversal effect of matrine and its derivatives on drug resistance of human nasopharyngeal carcinoma cell line HONE1/DDP.METHODS: The drug-resistant cell line was established by the human nasopharyngeal carcinoma cells HONE1 with gradually increasing concentration of cisplatin. The matrine and its derivatives were added into the HONE1/DDP according to different concentrations to measure their cytotoxicity. MTT assay was used to measure the reversal effect on the drug resistance of the non-toxic doses of matrine and its derivatives. Cell cycle was measured by flow cytomety. The expression level of MRP1, BAX, BCL-2 was assayed by Western blot.RESULTS: HONE1/DDP indicated drug resistantance. When the non-toxic doses of matrine and its derivatives were used to HONE1/DDP with 24h, the resistance of HONE1/DDP was down-regulated, the reversal fold was 1.45 and 1.77. The cell number of G0/G1-phase increased in matrine group while S phase decreased in matrine derivatives group compared with HONE1/DDP. Compared with HONE1/DDP group, the MRP1 expression levels in HONE1 cells were reduced (P < 0.05), and Matrine group and matrine derivatives group were enhanced (P < 0.05). The expression of BAX was lower while the expression of BCL-2 was higher.CONCLUSION: The resistance of HONE1 cells to DDP is able to increase the expression of MRP1; Matrine and its derivatives can reverse the drug resistance of HONE1/DDP to DDP, its activity may be related to change cell cycle distribution, the inhibition of MRP1 expression and down-regulation of BAX/BCL-2.
Alkaloids Antineoplastic Agents