A monastrol-derived compound, LaSOM 63, inhibits ecto-5'nucleotidase/CD73 activity and induces apoptotic cell death of glioma cell lines
BACKGROUND/AIM: 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.
MATERIALS AND 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.
RESULTS AND DISCUSSION: 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.
CONCLUSION: LaSOM 63 may be useful for in vivo experiments on the treatment of GBM.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2014 |
|---|---|
| Erschienen: |
2014 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:34 |
|---|---|
| Enthalten in: |
Anticancer research - 34(2014), 4 vom: 01. Apr., Seite 1837-42 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Figueiró, Fabrício [VerfasserIn] |
|---|
| Anmerkungen: |
Date Completed 15.06.2014 Date Revised 16.11.2017 published: Print Citation Status MEDLINE |
|---|
| Förderinstitution / Projekttitel: |
|
|---|
| PPN (Katalog-ID): |
NLM236986252 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM236986252 | ||
| 003 | DE-627 | ||
| 005 | 20231224110717.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231224s2014 xx |||||o 00| ||eng c | ||
| 028 | 5 | 2 | |a pubmed24n0790.xml |
| 035 | |a (DE-627)NLM236986252 | ||
| 035 | |a (NLM)24692717 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Figueiró, Fabrício |e verfasserin |4 aut | |
| 245 | 1 | 2 | |a A monastrol-derived compound, LaSOM 63, inhibits ecto-5'nucleotidase/CD73 activity and induces apoptotic cell death of glioma cell lines |
| 264 | 1 | |c 2014 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 15.06.2014 | ||
| 500 | |a Date Revised 16.11.2017 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a BACKGROUND/AIM: 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 | ||
| 520 | |a MATERIALS AND 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 | ||
| 520 | |a RESULTS AND DISCUSSION: 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 | ||
| 520 | |a CONCLUSION: LaSOM 63 may be useful for in vivo experiments on the treatment of GBM | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Glioma | |
| 650 | 4 | |a LaSOM 63 | |
| 650 | 4 | |a ecto-5’nucleotidase | |
| 650 | 4 | |a monastrol | |
| 650 | 7 | |a 5-ethoxycarbonyl-6-methyl-4-(4-N,N-dimethylaminophenyl)-3,4-dihydropyrimidin-2-(1H)-thione |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Pyrimidines |2 NLM | |
| 650 | 7 | |a Thiones |2 NLM | |
| 650 | 7 | |a monastrol |2 NLM | |
| 650 | 7 | |a 6BSM97YZ8G |2 NLM | |
| 650 | 7 | |a 5'-Nucleotidase |2 NLM | |
| 650 | 7 | |a EC 3.1.3.5 |2 NLM | |
| 700 | 1 | |a Mendes, Franciane Brackmann |e verfasserin |4 aut | |
| 700 | 1 | |a Corbelini, Patricia Frasson |e verfasserin |4 aut | |
| 700 | 1 | |a Janarelli, Fernanda |e verfasserin |4 aut | |
| 700 | 1 | |a Jandrey, Elisa Helena Farias |e verfasserin |4 aut | |
| 700 | 1 | |a Russowsky, Dennis |e verfasserin |4 aut | |
| 700 | 1 | |a Eifler-Lima, Vera Lucia |e verfasserin |4 aut | |
| 700 | 1 | |a Battastini, Ana Maria Oliveira |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Anticancer research |d 1987 |g 34(2014), 4 vom: 01. Apr., Seite 1837-42 |w (DE-627)NLM012601454 |x 1791-7530 |7 nnns |
| 773 | 1 | 8 | |g volume:34 |g year:2014 |g number:4 |g day:01 |g month:04 |g pages:1837-42 |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 34 |j 2014 |e 4 |b 01 |c 04 |h 1837-42 | ||