title: A monastrol-derived compound, LaSOM 63, inhibits ecto-5'nucleotidase/CD73 activity and induces apoptotic cell death of glioma cell lines.
abstract: OBJECTIVE
  Glioblastoma multiforme is the most malignant type of glioma. Ecto-5'-nucleotidase (ecto-5'NT), a glioma-overexpressed enzyme can induce a protective effect on tumor cells. Monastrol, a kinesin spindle protein-specific inhibitor, is reported to be an interesting prototype for cancer therapy. We describe the effect of LaSOM 63, a monastrol derivative, on ecto-5'NT activity and on glioma cell survival.
  
  
  METHODS
  Glioma cells were treated with LaSOM 63 and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), trypan blue assay (viability), flow cytometry (cell cycle/cell death) and malachite green method for ecto-5'NT activity were carried out.
  
  
  CONCLUSIONS
  Treatment with LaSOM 63 reduces glioma cell viability and cell growth. In contrast to monastrol, LaSOM 63 did not cause glioma cell-cycle arrest, but inhibited ecto-5'NT enzyme activity. Furthermore, this compound induces apoptotic death of C6 and U138 glioma cells.
  
  
  CONCLUSIONS
  LaSOM 63 may be useful for in vivo experiments on the treatment of GBM.
authors.affiliation: Ramiro Barcelos Street, 2600 Lab 22, Zip code: 90035-003, Porto Alegre/RS. abattastini@gmail.com.
authors.forename: Fabrício
authors.initials: F
authors.lastname: Figueiró
authors.forename: Franciane Brackmann
authors.initials: FB
authors.lastname: Mendes
authors.forename: Patricia Frasson
authors.initials: PF
authors.lastname: Corbelini
authors.forename: Fernanda
authors.initials: F
authors.lastname: Janarelli
authors.forename: Elisa Helena Farias
authors.initials: EH
authors.lastname: Jandrey
authors.forename: Dennis
authors.initials: D
authors.lastname: Russowsky
authors.forename: Vera Lucia
authors.initials: VL
authors.lastname: Eifler-Lima
authors.forename: Ana Maria Oliveira
authors.initials: AM
authors.lastname: Battastini
mesh_terms: D015720:5'-Nucleotidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D005910:Glioma / Q000378:metabolism*; D006801:Humans; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013871:Thiones / Q000737:chemistry / Q000494:pharmacology
chemical_list: C000588860:5-ethoxycarbonyl-6-methyl-4-(4-N,N-dimethylaminophenyl)-3,4-dihydropyrimidin-2-(1H)-thione; D000970:Antineoplastic Agents; D011743:Pyrimidines; D013871:Thiones; C400223:monastrol; D015720:5'-Nucleotidase
keywords: Glioma; LaSOM 63; ecto-5’nucleotidase; monastrol