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五味子甲素逆转多药耐药相关蛋白1多药耐药机制的研究 被引量:5

Reversal effect of Schisandrin A on MRP1-mediated multidrug resistance
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摘要 目的:探讨五味子甲素对表达多药耐药相关蛋白1的肿瘤耐药细胞株的逆转耐药作用及相关机制。方法:FCM测定不同浓度五味子甲素对柔红霉素抑制HL60/ADR生长及同一浓度五味子甲素对不同化疗药物抑制HL60/ADR和HL60/MRP细胞生长的影响;五味子甲素作用前后,HL60/ADR和HL60/MRP细胞内化疗药物柔红霉素和MRP1特异性底物二醋酸羧基荧光素积聚的变化。结果:25μmol/L五味子甲素可有效降低HL60/ADR、HL60/MRP对柔红霉素、长春新碱和依托泊甙的半数抑制浓度,逆转倍数分别是5,11,16和3,3,13倍;五味子甲素能够增加柔红霉素和MRP1特异性底物二醋酸羧基荧光素在细胞内的积聚。结论:五味子甲素可以逆转不同化疗药物对MRP1介导的耐药,其逆转机制与增加化疗药物的积聚能力有关。 Objective To investigate the reversal effect of Schisandrin A(Schisandrin A) on MRP cell lines and its possible mechanisms. Methods Susceptibility of DNR, VCR and VP16 enhanced by Schisandrin A in HL-60/ADR and HL-60/MRP cell lines, were evaluated with flow cytometry. The intracellular concentrations of DNR and CFDA, and a specific fluorescent substrate for MRP1 were detected also with flow cytometry. Results Schisandrin A could increase the drug susceptibility of HL 60/ADR and HL-60/MRP cells to DNR, VCR and VP16 at the concentrations of 25 μM and the reversal folds were 5-, 11-, 16- and 3-, 3 , 13-fold, respectively. Meanwhile, Schisandrin A could significantly increase the intracellular accumulation of DNR in the two cell lines when detected by flow cytometry. Conclusion Schisandrin A could reverse multidrug resistance of different drugs caused by MRP1 in HL60/ADR and HL60/MRP cell lines and this was in a dose-dependent manner. The reversal effect is related to the increase of intracellular accumulation of chemotherapeutic drugs.
作者 李玲 樊青霞
出处 《中华实用诊断与治疗杂志》 2009年第9期857-859,共3页 Journal of Chinese Practical Diagnosis and Therapy
关键词 五味子甲素 多药耐药 MRP1 逆转剂 Schisandrin A muhidrug resistance muhidrug resistance-associated protein 1 modulator
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  • 1Huang M, Jin J, Sun H, et al. Reversal of P glycoprotein- mediated multidrug resistance of cancer cells by five schizandrins isolated from the Chinese herb Fructus Schizandrae[J]. Cancer Chemother Pharmacol,2008,62(6) :1015-1026.
  • 2Pan Q, Lu Q, Hu X, et al. Dibenzocyclooctadienc a class of novel inhibitors of P-glycoproteins [J]. Cancer Chemother Pharmacol, 2006,58 ( 1 ) : 99-106.
  • 3SharomFJ. ABCmultidrugtransporters: structure, function and role in chemoresistance[J]. Pharmacogenomics, 2008,9 ( 1 ) : 105- 127.
  • 4Shukla S, Wu C P, Ambudkar S V. Development of inhibitors of ATP binding cassette drug transporters: present status and challenges[J]. Expert Opin Drug Metab Toxicol, 2008,4(2): 205-223.
  • 5Triller N, Korosec P, Kern I, et al. Muhidrug resistance in small cell lung cancer: expression of P glycoprotein, multidrug resistance protein 1 and lung resistance protein in chemo-naive patients and in relapsed disease[J]. Lung Cancer, 2006, 54(2): 235- 240.
  • 6Coburger C, Large H, Moinar J, et al. Impact of novel MDR modulators on human cancer cells: reversal activities and induction studies[J]. Pharm Res,2009,26(1):182 -188.
  • 7Gandhi L, Harding M W, Neubauer M, et al. A phase Ⅱ study of the safety and efficacy of the multidrug resistance inhibitor VX 710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer[J]. Cancer, 2007,109 (5):924-932.
  • 8Chen Z S, Furukawa T, Sumizawa T, et al. ATP dependent efflux of CPT-11 and SN 38 by the multidrug resistance protein (MRP) and its inhibition by PAK 104P[J]. Mol Pharmacol,1999,55(5): 921 -928.
  • 9Wang R, Kong J, Wang D, et al. A survey of Chinese herbal ingredients with live protection activities[J]. Chin Med, 2007,10 (2):5- 10.
  • 10Dogan A L, Legrand O, Faussat A M, et al. Evaluation and comparison of MRP1 activity with three fluorescent dyes and three modulators in leukemic cell lines[J]. Leuk Res, 2004, 28(6):619-622.

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