title: [Reversal effect of cinobufacini on multidrug resistance of Raji/ADR cells and its mechanisms].
abstract: The aim of this study was to explore the reversing effect of cinobufacini on multidrug resistance of Raji/ADR cells and its mechanisms. The growth inhibitory rate, half inhibitory concentration (IC50), reversing multiples to adriamycin- resistance were detected by MTT, and the curve of growth inhibitory rate was drawn; the MDR-1 and MRP-1 gene transcription was determined by RT-PCR; the expressions of P-gp and MRP-1 proteins were assayed by Western blot and flow cytometry. The results showed that the inhibitory rates of cinobufacini on Raji and Raji/ADR cells at 72 h were 75.6% and 69.3% respectively, the IC50 were 3.9 mmol/L and 4.6 mmol/L without significant difference (P > 0.05). The reversing multiples to adriamycin-resistance were 255.7 multiples, the transcription of mdr-1 and mrp-1 genes and the expression of P-gp and MRP-1 proteins significantly decreased (P < 0.05) in Raji/ADR cells after the treatment with cinobufotalin. It is concluded that cinobufotalin can reverse the adriamycin-resistance in Raji/ADR cells and the expression of P-gp and MRP-1 proteins were down-regulated through the transcriptional pathway. The cinobufotalin is an effective reversal agent for the multidrug resistance of tumors.
authors.affiliation: Department of Hematology, The First Affiliated Hospital of Nanyang Medical College, Nanyang 473000, Henan Province, China. E-mail: physicianzc@163.com.
authors.forename: Cheng
authors.initials: C
authors.lastname: Zhang
authors.affiliation: Department of Hematology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, Henan Province, China.
authors.forename: Ding-Ming
authors.initials: DM
authors.lastname: Wan
authors.affiliation: Department of Hematology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, Henan Province, China.
authors.forename: Wei-Jie
authors.initials: WJ
authors.lastname: Cao
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000664:Amphibian Venoms; D002018:Bufanolides / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004317:Doxorubicin; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D006801:Humans; D020133:Reverse Transcriptase Polymerase Chain Reaction
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000664:Amphibian Venoms; D002018:Bufanolides; C545813:huachansu; D004317:Doxorubicin; C063451:cinobufotalin