[Effect of neferine on the chemotherapic sensitivity of STI 571 to K562/A02 cells].
OBJECTIVE
To explore the effect of neferine on the chemotherapic sensitivity of STI 571 to K562/A02 cells and to reveal its mechanism.


METHODS
MTT method was used to observe the alteration of the proliferation of K562/A02 cell line treated with STI571 alone or combined with neferine. The transcription of mdrl gene was detected by semi-quantitative RT-PCR and the P-gp expression was determined by Western blot after STI 571 alone or combined with neferine treatment.


RESULTS
The cytotoxic effect of STI 571 (1 micromol/L) combined with neferine (IC50 = 3.02 micromol/L) on K562/A02 cell line was significantly higher than that of STI 571 alone (IC50 = 0.689 micromol/L). After treating with STI571 combined with neferine, the synergistic interaction on K562/A02 cells increased 4.38 folds (P < 0.05); the mdrl mRNA expression by semi-quantitative RT-PCR was significantly reduced by (45.4 +/- 2.5) % (P < 0.01); and the P-gp expression by Western blot was deregulated by 40.58% (P < 0.05).


CONCLUSIONS
Neferine significantly enhances the antineoplastic effect of STI 571 on K562/A02 cells by reducing mdrl mRNA transcription and blocking P-gp expression.
Xiao
Xi-Bin
XB
Department of Hematology, Xiangya Hospital, Central South University, Changsha, China. xzxchangsha@163.com
Xie
Zhao-Xia
ZX
Chen
Jie
J
Qin
Qun
Q
Zhu
Yan
Y
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000096:biosynthesis* / Q000235:genetics; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D001549:Benzamides; D044182:Benzylisoquinolines / Q000494:pharmacology*; D049109:Cell Proliferation; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004357:Drug Synergism; D006801:Humans; D000068877:Imatinib Mesylate; D020014:K562 Cells; D010879:Piperazines / Q000494:pharmacology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D011743:Pyrimidines / Q000494:pharmacology*
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000972:Antineoplastic Agents, Phytogenic; D001549:Benzamides; D044182:Benzylisoquinolines; D010879:Piperazines; D011743:Pyrimidines; C057222:neferine; D000068877:Imatinib Mesylate; D011505:Protein-Tyrosine Kinases