title: Antitumor activity of lobaplatin alone or in combination with antitubulin agents in non-small-cell lung cancer.
abstract: OBJECTIVE
  Lobaplatin is used to treat patients with breast cancer, small-cell lung cancer, and chronic myelogenous leukemia in China. In this study, we assessed the in-vitro and in-vivo activities of lobaplatin alone or in combination with antitubulin agents against human non-small-cell lung cancer (NSCLC).
  
  
  METHODS
  The cytotoxicities of lobaplatin against NSCLC cells were determined by the sulforhodamine B (SRB) assay. Cell cycle analysis and apoptosis were assessed using flow cytometry, and the in-vivo antitumor activities were evaluated in human NSCLC xenografts in nude mice.
  
  
  RESULTS
  The cytotoxicity of lobaplatin was similar to or higher than that of cisplatin and carboplatin, with a mean IC(50) of 2.5 μmol/l in a variety of NSCLC cells. In addition, lobaplatin arrested cells in the S phase and triggered apoptosis. The combination of lobaplatin with antitubulin agents yielded synergistic cytotoxic activity in vitro. In NSCLC xenografts, lobaplatin alone showed significant antitumor activity. The combination of lobaplatin with antitubulin agents, especially with paclitaxel, led to significantly enhanced activity, which was superior to that of cisplatin combined with antitubulin agents.
  
  
  CONCLUSIONS
  These data demonstrate that the use of lobaplatin alone or in combination with antitubulin agents might be a rational and novel therapeutic strategy for human NSCLC and warrants further clinical investigation.
authors.affiliation: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
authors.forename: Cheng-Ying
authors.initials: CY
authors.lastname: Xie
authors.forename: Yong-Ping
authors.initials: YP
authors.lastname: Xu
authors.forename: Wei
authors.initials: W
authors.lastname: Jin
authors.forename: Li-Guang
authors.initials: LG
authors.lastname: Lou
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects*; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy* / Q000473:pathology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003503:Cyclobutanes / Q000008:administration & dosage / Q000494:pharmacology; D000077143:Docetaxel; D004357:Drug Synergism; D005260:Female; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D009944:Organoplatinum Compounds / Q000008:administration & dosage / Q000494:pharmacology; D017239:Paclitaxel / Q000008:administration & dosage; D043823:Taxoids / Q000008:administration & dosage; D050257:Tubulin Modulators / Q000008:administration & dosage; D047368:Tumor Burden / Q000187:drug effects; D014747:Vinblastine / Q000008:administration & dosage / Q000031:analogs & derivatives; D000077235:Vinorelbine; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D003503:Cyclobutanes; D009944:Organoplatinum Compounds; D043823:Taxoids; D050257:Tubulin Modulators; D000077143:Docetaxel; D014747:Vinblastine; C066228:lobaplatin; D017239:Paclitaxel; D000077235:Vinorelbine