RRC ID 51908
著者 Hayashi N, Kataoka H, Yano S, Kikuchi JI, Tanaka M, Nishie H, Kinoshita Y, Hatano M, Nomoto A, Ogawa A, Inoue M, Mizoshita T, Shimura T, Mori Y, Kubota E, Tanida S, Joh T.
タイトル Anticancer Effects of a New Aminosugar-conjugated Platinum Complex Agent Against Cisplatin-resistant Gastric Cancer.
ジャーナル Anticancer Res
Abstract BACKGROUND/AIM:Resistance against cisplatin is a problem for the success of gastric cancer chemotherapy. Herein, we evaluated the antitumor effect of a new aminosugar-conjugated, mono-functional platinum complex (Pt-Oqn), which forms a single covalent bond with DNA.
MATERIALS AND METHODS:We compared the cytotoxicity of Pt-Oqn to that of cisplatin (CDDP), oxaliplatin (L-OHP) and carboplatin (CBDCA). We also compared Pt-Oqn and cisplatin for DNA double-strand breaks based on phosphorylated histone H2AX levels in cancer cells and antitumor effects in xenograft models.
RESULTS:The resistance factor (RF) for Pt-Oqn was low among the four drugs, indicating the potential of Pt-Oqn for overcoming CDDP-induced resistance. In MKN45-R cells, γ-H2AX protein increased following treatment with Pt-Oqn, but not with cisplatin. Finally, Pt-Oqn, but not cisplatin, showed significant antitumor effects in MKN45-R xenografts.
CONCLUSION:This new aminosugar-conjugated platinum complex is a promising candidate agent for overcoming the drug resistance of cisplatin-resistant stomach cancer.
巻・号 36(11)
ページ 6005-6009
公開日 2016-11-1
DOI 10.21873/anticanres.11189
PII 36/11/6005
PMID 27793927
MeSH Cisplatin / pharmacology* Drug Resistance, Neoplasm / drug effects* Humans Platinum Compounds / chemistry Platinum Compounds / therapeutic use* Stomach Neoplasms / drug therapy*
IF 1.994
引用数 6
リソース情報
ヒト・動物細胞 MKN45(RCB1001)