title: A novel compound NSC745885 exerts an anti-tumor effect on tongue cancer SAS cells in vitro and in vivo.
abstract: OBJECTIVE
  Oral squamous cell carcinoma (OSCC) is a prevalent cancer, especially in developing countries. Anthracyclines and their anthraquinone derivatives, such as doxorubicin, exhibit a cell growth inhibitory effect and have been used as anti-cancer drugs for many years. However, the cardiotoxicity of anthracycline antibiotics is a major concern in their clinical application. NSC745885 is a novel compound synthesized from 1,2-diaminoanthraquinone, which subsequently reacts with thionyl chloride and triethylamine. The present study aimed to investigate the anti-oral cancer potential and the safety of NSC745885.
  
  
  METHODS
  We investigated the anti-cancer potential of NSC745885 in oral squamous carcinoma cell lines and in an in vivo oral cancer xenograft mouse model. The expression of apoptotic related genes were evaluated by real-time RT-PCR and western bloting, and the in vivo assessment of apoptotic marker were measured by immunohistochemical staining. The anti-tumor efficiency and safety between doxorubicin and NSC745885 were also compared.
  
  
  RESULTS
  Our results demonstrated that NSC745885 exhibits anti-oral cancer activity through the induction of apoptosis in cancer cells and in tumor-bearing mice, and this treatment did not induce marked toxicity in experimental mice. This compound also exhibits a comparable anti-tumor efficiency and a higher safety in experimental mice when compared to doxorubicin.
  
  
  CONCLUSIONS
  The data of this study provide evidence for NSC745885 as a potential novel therapeutic drug for the treatment of human OSCC.
authors.affiliation: School of Dentistry, National Defense Medical Center, Taipei, Taiwan, Republic of China; Department of Oral and Maxillofacial Surgery, Tri-Service General Hospital, Taipei, Taiwan, Republic of China.
authors.forename: Yuan-Wu
authors.initials: YW
authors.lastname: Chen
authors.affiliation: School of Pharmacy, National Defense Medical Center, Taipei, Taiwan, Republic of China; Graduate Institute of Cancer Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, Taiwan, Republic of China.
authors.forename: Hsu-Shan
authors.initials: HS
authors.lastname: Huang
authors.affiliation: School of Dentistry, National Defense Medical Center, Taipei, Taiwan, Republic of China.
authors.forename: Yi-Shing
authors.initials: YS
authors.lastname: Shieh
authors.affiliation: Department of Biology and Anatomy, National Defense Medical Center, Taipei, Taiwan, Republic of China.
authors.forename: Kuo-Hsing
authors.initials: KH
authors.lastname: Ma
authors.affiliation: Department of Biology and Anatomy, National Defense Medical Center, Taipei, Taiwan, Republic of China; Department of General Surgery, Tri-Service General Hospital, Taipei, Taiwan, Republic of China.
authors.forename: Shing-Hwa
authors.initials: SH
authors.lastname: Huang
authors.affiliation: Department of Neurological Surgery, Tri-Service General Hospital, Taipei, Taiwan, Republic of China.
authors.forename: Dueng-Yuan
authors.initials: DY
authors.lastname: Hueng
authors.affiliation: Department of Microbiology and Immunology, National Defense Medical Center, Taipei, Taiwan, Republic of China.
authors.forename: Huey-Kang
authors.initials: HK
authors.lastname: Sytwu
authors.affiliation: Department of Biology and Anatomy, National Defense Medical Center, Taipei, Taiwan, Republic of China.
authors.forename: Gu-Jiun
authors.initials: GJ
authors.lastname: Lin
mesh_terms: D000818:Animals; D000880:Anthraquinones / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects*; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy*; D053148:Caspase 3 / Q000096:biosynthesis / Q000235:genetics / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004317:Doxorubicin / Q000009:adverse effects / Q000627:therapeutic use; D006801:Humans; D051379:Mice; D016688:Mice, Inbred NOD; D016513:Mice, SCID; D009062:Mouth Neoplasms / Q000188:drug therapy*; D009364:Neoplasm Recurrence, Local / Q000188:drug therapy; D012333:RNA, Messenger / Q000096:biosynthesis; D013830:Thiadiazoles / Q000009:adverse effects / Q000627:therapeutic use*; D014059:Tongue / Q000473:pathology; D014062:Tongue Neoplasms / Q000188:drug therapy*; D051636:X-Linked Inhibitor of Apoptosis Protein / Q000096:biosynthesis / Q000235:genetics; D023041:Xenograft Model Antitumor Assays
chemical_list: D000880:Anthraquinones; D000970:Antineoplastic Agents; D012333:RNA, Messenger; D013830:Thiadiazoles; D051636:X-Linked Inhibitor of Apoptosis Protein; C496866:XIAP protein, human; C000604512:anthra(2,1-c)(1,2,5)thiadiazole-6,11-dione; D004317:Doxorubicin; D053148:Caspase 3; C118201:1,2-diaminoanthraquinone