Chen Xiao-Song, Bao Ming-Hong, Mei Xiao-Dong
Department of Respiratory Medicine, Affiliated Provincial Hospital, Anhui Medical University, Hefei, Anhui, 230001, PR China.
Ai Zheng. 2007 Aug;26(8):846-50.
BACKGROUND & OBJECTIVE: Tetrandrine (Tet), a bisbenzylisoquinoline albaloid isolated from the Chinese herb "Hanfangji" (Radix Stephania Tetrandra), could effectively reverse P-glycoprotein-mediated multidrug resistance. This study was to investigate the reversal effect of tetrandrine on multidrug resistance of human epidermoid carcinoma cell line KB-MRP1.
The effects of tetrandrine on the proliferation of KB-3-1 and KB-MRP1 cells were observed by MTT assay. The inhibitory effects of cisplatin (DDP), vincristine (VCR), adriamycin (ADM) and etoposide (VP-16) used alone or in combination with tetrandrine on the proliferation of KB-3-1 and KB-MRP1 cells were evaluated by MTT assay. The effects of tetrandrine on ADM accmulation in KB-MRP1 cells and VCR-induced apoptosis were determined by flow cytometry (FCM).
Tetrandrine at the concentration of 1.5 microg/ml and below showed no significant cytotoxicity to KB-3-1 and KB-MRP1 cells. The resistance of KB-MRP1 cells to VCR, ADM, VP-16 and DDP were 21.23, 38.39, 12.47 and 1.31 folds of that of KB-3-1 cells. When added 1 microg/ml tetrandrine, the chemosensitivity of KB-MRP1 cells to VCR, ADM and VP-16 were increased to 4.96, 5.85 and 4.24 folds, respectively; when added 1.5 microg/ml tetrandrine, the chemosensitivity of KB-MRP1 cells to VCR, ADM and VP-16 were much higher. When treated with 1.5 microg/ml tetrandrine, ADM accumulation in KB-MRP1 cells and the VCR-induced apoptosis were enhanced significantly.
Tetrandrine could moderately reverse the multidrug resistance of KB-MRP1 cells through increasing the accumulation of chemo-drugs in cells and promoting apoptosis.
粉防己碱（Tet）是从中药“汉防己”（粉防己根）中分离得到的一种双苄基异喹啉生物碱，可有效逆转P-糖蛋白介导的多药耐药性。本研究旨在探讨粉防己碱对人表皮样癌细胞系KB-MRP1多药耐药性的逆转作用。
采用MTT法观察粉防己碱对KB-3-1和KB-MRP1细胞增殖的影响。采用MTT法评价顺铂（DDP）、长春新碱（VCR）、阿霉素（ADM）和依托泊苷（VP-16）单独或与粉防己碱联合使用对KB-3-1和KB-MRP1细胞增殖的抑制作用。采用流式细胞术（FCM）检测粉防己碱对KB-MRP1细胞中ADM蓄积及VCR诱导凋亡的影响。
浓度为1.5μg/ml及以下的粉防己碱对KB-3-1和KB-MRP1细胞无明显细胞毒性。KB-MRP1细胞对VCR、ADM、VP-16和DDP的耐药性分别是KB-3-1细胞的21.23、38.39、12.47和1.31倍。加入1μg/ml粉防己碱后，KB-MRP1细胞对VCR、ADM和VP-16的化疗敏感性分别提高到4.96、5.85和4.24倍；加入1.5μg/ml粉防己碱后，KB-MRP1细胞对VCR、ADM和VP-16的化疗敏感性更高。用1.5μg/ml粉防己碱处理后，KB-MRP1细胞中ADM蓄积及VCR诱导的凋亡明显增强。
粉防己碱可通过增加化疗药物在细胞内的蓄积和促进凋亡来适度逆转KB-MRP1细胞的多药耐药性。
