PubMed · 2012 · 57 citations · 15 references
MedicineOncologyPharmacologyApoptosisBiochemical PharmacologyCancer PharmacologyApoptosis PharmacologyCytotoxic ChemotherapyLipid MetabolismOncology PharmacologyAnnexin V AssaysAnnexin V ImagingAnticancer ActivityAnticancer ChemotherapyAnticancer Natural ProductsCell Cycle InhibitionCell Death AssaysMitochondrial Membrane Potential Collapse
BACKGROUND: Antineoplastic phospholipids (ALPs) represent a promising class of drugs with a novel mode of action undergoes rapid turnover in the cell membrane of tumors, interfering with lipid signal transduction, inducing cell death. The aim of this study was to investigate the synthetic phosphoethanolamine (Pho-s) as a new anticancer agent. MATERIALS AND METHODS: Cell viability and morphology were assessed by (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), Hoechst and rhodamine staining. Apoptosis was assessed by Annexin V and propidium iodide (PI) staining, caspase-3 activity, mitochondrial membrane potential (ΔmΨ) and cell cycle analysis, combined with evaluation of tumor growth in Ehrlich Ascites Tumor (EAT) bearing mice. RESULTS: We found that Pho-s 2.30 mg/ml induced cytotoxicity in all tumor cell lines studied without affecting normal cells. In vitro studies with EAT cells indicated that Pho-s induced apoptosis, demonstrated by an increase in Annexin-V positive cells, loss of mitochondrial potential (ΔmΨ) and increased caspase-3 activity. It was also shown to increase the sub-G(1) apoptotic fraction and inhibit progression to the S phase of the cell cycle. Additionally, antitumor effects on the EAT-bearing mice showed that Pho-s, at a concentration of 35 and 70 mg/kg, inhibited tumor growth and increased the lifespan of animals without causing liver toxicity. CONCLUSION: These findings suggest that Pho-s is a potential anticancer candidate drug.
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Faustino Mollinedo, José L. Fernández-Luna, Consuelo Gajate et al. · PubMed · 1997 · 223 citations
Faustino Mollinedo, Janis de la Iglesia-Vicente, Consuelo Gajate et al. · Clinical Cancer Research · 2010 · 91 citations · Full text
Medicine, Oncology, Pharmacology +17
Mojtaba Panjehpour, Fatemeh Karami‐Tehrani, Siamak Salami · Journal of Cancer Research and Clinical Oncology · 2011 · 66 citations · Full text