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In Vitro Anticancer...
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Burgos-Moron, EstefaniaUniv Seville, Fac Pharm, Dept Pharmacol, Seville 41012, Spain.
(author)
In Vitro Anticancer Activity and Mechanism of Action of an Aziridinyl Galactopyranoside
- Article/chapterEnglish2022
Publisher, publication year, extent ...
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2021-12-25
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MDPI AG,2022
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electronicrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:uu-469184
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https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-469184URI
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https://doi.org/10.3390/biomedicines10010041DOI
Supplementary language notes
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Language:English
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Summary in:English
Part of subdatabase
Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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We recently screened a series of new aziridines beta-D-galactopyranoside derivatives for selective anticancer activity and identified 2-methyl-2,3-[N-(4-methylbenzenesulfonyl)imino]propyl 2,3-di-O-benzyl-4,6-O-(S)-benzylidene-beta-D-galactopyranoside (AzGalp) as the most promising compound. In this article, we explore the possible mechanisms involved in the cytotoxicity of this aziridine and evaluate its selective anticancer activity using cancer cells and normal cells from a variety of tissues. Our data show that AzGalp induces DNA damage (comet assay). Cells deficient in the nucleotide excision repair (NER) pathway were hypersensitive to the cytotoxicity of this compound. These results suggest that AzGalp induces bulky DNA adducts, and that cancer cells lacking a functional NER pathway may be particularly vulnerable to the anticancer effects of this aziridine. Several experiments revealed that neither the generation of oxidative stress nor the inhibition of glycolysis played a significant role in the cytotoxicity of AzGalp. Combinations of AzGalp with oxaliplatin or 5-fluorouracil slightly improved the ability of both anticancer drugs to selectively kill cancer cells. AzGalp also showed selective cytotoxicity against a panel of malignant cells versus normal cells; the highest selectivity was observed for two acute promyelocytic leukemia cell lines. Additional preclinical studies are necessary to evaluate the anticancer potential of AzGalp.
Subject headings and genre
Added entries (persons, corporate bodies, meetings, titles ...)
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Pastor, NuriaUniv Seville, Fac Biol, Dept Cell Biol, Seville 41012, Spain.
(author)
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Orta, Manuel LuisUniv Seville, Fac Biol, Dept Cell Biol, Seville 41012, Spain.
(author)
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Jimenez-Alonso, Julio JoseUniv Seville, Fac Pharm, Dept Pharmacol, Seville 41012, Spain.
(author)
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Palo-Nieto, CarlosUppsala universitet,Nanoteknologi och funktionella material,Institutionen för läkemedelskemi,Univ Seville, Fac Pharm, Dept Organ & Med Chem, Seville 41012, Spain.(Swepub:uu)carpa373
(author)
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Vega-Holm, MargaritaUniv Seville, Fac Pharm, Dept Organ & Med Chem, Seville 41012, Spain.
(author)
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Vega-Perez, Jose ManuelUniv Seville, Fac Pharm, Dept Organ & Med Chem, Seville 41012, Spain.
(author)
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Iglesias-Guerra, FernandoUniv Seville, Fac Pharm, Dept Organ & Med Chem, Seville 41012, Spain.
(author)
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Mateos, SantiagoUniv Seville, Fac Biol, Dept Cell Biol, Seville 41012, Spain.
(author)
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Lopez-Lazaro, MiguelUniv Seville, Fac Pharm, Dept Pharmacol, Seville 41012, Spain.
(author)
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Calderon-Montano, Jose ManuelUniv Seville, Fac Pharm, Dept Pharmacol, Seville 41012, Spain.
(author)
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Univ Seville, Fac Pharm, Dept Pharmacol, Seville 41012, Spain.Univ Seville, Fac Biol, Dept Cell Biol, Seville 41012, Spain.
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In:Biomedicines: MDPI AG10:12227-9059
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