title: Icaritin reverses multidrug resistance of HepG2/ADR human hepatoma cells via downregulation of MDR1 and P‑glycoprotein expression.
abstract: Multidrug resistance (MDR) of tumor cells is a serious obstacle encountered in cancer treatment. In the current study a multiple drug‑resistant HepG2/adriamycin (HepG2/ADR) cell line was established and its MDR was characterized. Icaritin, an active ingredient isolated from the medical plant Herba Epimedium, was observed to reverse MDR in the present model. Icaritin significantly increased the intracellular accumulation of ADR and decreased the expression of the MDR1 gene in HepG2/ADR cells compared with drug‑sensitive HepG2 cells. In addition, the present results showed that icaritin may significantly downregulate the expression of P‑glycoprotein. These results indicate that icaritin is a novel and potent MDR reversal agent and may be a promising drug for tumor chemotherapy.
authors.affiliation: Department of Laboratory Medicine, The Second Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu 210011, P.R. China.
authors.forename: Li
authors.initials: L
authors.lastname: Sun
authors.forename: Weigang
authors.initials: W
authors.lastname: Chen
authors.forename: Lili
authors.initials: L
authors.lastname: Qu
authors.forename: Jie
authors.initials: J
authors.lastname: Wu
authors.forename: Jin
authors.initials: J
authors.lastname: Si
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics* / Q000378:metabolism; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000235:genetics* / Q000473:pathology; D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002999:Clone Cells; D015536:Down-Regulation / Q000187:drug effects / Q000235:genetics*; D004317:Doxorubicin / Q000494:pharmacology*; D018432:Drug Resistance, Multiple / Q000187:drug effects* / Q000235:genetics; D019008:Drug Resistance, Neoplasm / Q000187:drug effects / Q000235:genetics*; D005419:Flavonoids / Q000494:pharmacology*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D042541:Intracellular Space / Q000187:drug effects / Q000378:metabolism; D008113:Liver Neoplasms / Q000188:drug therapy / Q000235:genetics / Q000473:pathology; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism
chemical_list: C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D005419:Flavonoids; D012333:RNA, Messenger; D004317:Doxorubicin; C499403:icaritin