title: Cantharidin reverses multidrug resistance of human hepatoma HepG2/ADM cells via down-regulation of P-glycoprotein expression.
abstract: Multidrug resistance (MDR) is a serious obstacle encountered in cancer treatment. In this study, we established an in vitro multiple drug resistant HepG2 cell line (HepG2/ADM), and characterized its MDR. This model was used to screen potential candidate chemosensitisers from over 200 purified naturally occurring compounds extracted from plants and animals. Cantharidin was found to have a significant reversal on MDR in our model. Further, our results showed that Cantharidin could significantly inhibit P-gp (P-glycoprotein) expression, mRNA transcription, as well as MDR1 promoter activity. These results suggest that Cantharidin is a novel and potent MDR reversal agent and may be a potential adjunctive agent for tumor chemotherapy.
authors.affiliation: Institute of Genetics and Cytology, Northeast Normal University, 130024 ChangChun, China. zhenglihua_108@yahoo.com.cn
authors.forename: Li Hua
authors.initials: LH
authors.lastname: Zheng
authors.forename: Yong Li
authors.initials: YL
authors.lastname: Bao
authors.forename: Yin
authors.initials: Y
authors.lastname: Wu
authors.forename: Chun Lei
authors.initials: CL
authors.lastname: Yu
authors.forename: Xiangying
authors.initials: X
authors.lastname: Meng
authors.forename: Yu Xin
authors.initials: YX
authors.lastname: Li
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000187:drug effects / Q000235:genetics*; D002193:Cantharidin / Q000494:pharmacology* / Q000627:therapeutic use; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000235:genetics*; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015536:Down-Regulation; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D022781:Hepatocytes / Q000166:cytology / Q000187:drug effects; D006801:Humans; D007668:Kidney; D008113:Liver Neoplasms / Q000188:drug therapy / Q000235:genetics*; D012333:RNA, Messenger / Q000235:genetics; D012334:RNA, Neoplasm / Q000235:genetics
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D004791:Enzyme Inhibitors; D012333:RNA, Messenger; D012334:RNA, Neoplasm; D002193:Cantharidin