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Anti-cancer activity of di- and tri-organotin(IV) compounds with D-(+)-Galacturonic acid on human tumor cells.
- Source :
-
Journal of inorganic biochemistry [J Inorg Biochem] 2018 Nov; Vol. 188, pp. 102-112. Date of Electronic Publication: 2018 Apr 09. - Publication Year :
- 2018
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Abstract
- We have compared the anti-proliferative activity in vitro, of R <subscript>2</subscript> SnGala (1-3) [R = Me, n-Bu, Ph] and novel R <subscript>3</subscript> SnGala (4, 5) [R = Me, n-Bu] with D-(+)-Galacturonic acid [HGala; Gala <superscript>q-</superscript> , q = (2) and (1) for R <subscript>2</subscript> SnGala and R <subscript>3</subscript> SnGala, respectively] compounds, towards human tumor cell lines of intestinal carcinoma (HCT-116) and breast adenocarcinoma (MCF-7). The new synthesized 4 and 5 compounds were characterized, in solution, by <superscript>1</superscript> H, <superscript>13</superscript> C and <superscript>119</superscript> Sn NMR, that showed that HGala acts as monoanionic moiety and evidenced the dynamic behavior of the compounds, due to inter-conversions involving the anomeric carbon atom of the ligand. Cell viability, apoptosis induction and cell cycle distribution were analyzed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay and flow cytometry, respectively. The cytotoxicity of the compounds, in the micro-submicromolar range, changed in the order of the organotin(IV) moieties, according to 5 > 3 > 2, while 1 and 4, containing Me <subscript>n</subscript> Sn(IV) (n = 2,3) moieties, were ineffective. Compound 5 showed peculiar cytotoxic effects. It did not cause time dependent inhibition of cell growth nor accumulated into the cells. Cell death induced by the active 2, 3, and 5, was shown to be apoptotic by measuring the exposure of phosphatidylserine to the outer membrane and the loss of mitochondrial potential. All the cytotoxic compounds induced an accumulation of cells in the subG0/G1phase, while only 2 and 3 perturbed the cell cycle confining viable cells in G0/G1phase. Finally, none of the compounds investigated affected the viability of normal intestinal or liver cells, indicating selectivity towards tumor cells.<br /> (Copyright © 2018. Published by Elsevier Inc.)
- Subjects :
- Caco-2 Cells
Cell Survival drug effects
HCT116 Cells
Humans
MCF-7 Cells
Adenocarcinoma drug therapy
Adenocarcinoma metabolism
Adenocarcinoma pathology
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Apoptosis drug effects
Breast Neoplasms drug therapy
Breast Neoplasms metabolism
Breast Neoplasms pathology
Hexuronic Acids chemistry
Hexuronic Acids pharmacology
Intestinal Neoplasms drug therapy
Intestinal Neoplasms metabolism
Intestinal Neoplasms pathology
Organotin Compounds chemical synthesis
Organotin Compounds chemistry
Organotin Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3344
- Volume :
- 188
- Database :
- MEDLINE
- Journal :
- Journal of inorganic biochemistry
- Publication Type :
- Academic Journal
- Accession number :
- 29807841
- Full Text :
- https://doi.org/10.1016/j.jinorgbio.2018.04.006