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Liposomal formulation of alpha-tocopheryl maleamide: In vitro and in vivo toxicological profile and anticancer effect against spontaneous breast carcinomas in mice
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SYSNO ASEP 0340455 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Liposomal formulation of alpha-tocopheryl maleamide: In vitro and in vivo toxicological profile and anticancer effect against spontaneous breast carcinomas in mice Author(s) Turánek, J. (CZ)
Wang, X. F. (AU)
Knötigová, P. (CZ)
Koudelka, Š. (CZ)
Dong, L. F. (AU)
Vrublová, E. (CZ)
Mahdavian, E. (US)
Procházka, L. (CZ)
Sangsura, S. (US)
Vacek, A. (CZ)
Salvatore, B. A. (US)
Neužil, Jiří (BTO-N) RIDSource Title Toxicology and Applied Pharmacology. - : Elsevier - ISSN 0041-008X
Roč. 237, č. 3 (2009), s. 249-257Number of pages 9 s. Language eng - English Country US - United States Keywords Liposome ; apoptosis ; vitamin E analogues Subject RIV FR - Pharmacology ; Medidal Chemistry R&D Projects KAN200520703 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) IAA500520602 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR) CEZ AV0Z50520701 - BTO-N (2007-2013) UT WOS 000266689800001 DOI 10.1016/j.taap.2009.01.027 Annotation The vitamin E analogue α-tocopheryl succinate (α-TOS) is an efficient anti-cancer drug. Improved efficacy was achieved through the synthesis of an esterase-resistant α-tocopheryl maleamide (α-TAM). In vitro tests demonstrated higher cytotoxicity of α-TAM towards cancer cells (MCF-7, B16F10) compared to α-TOS prone to esterase-catalyzed hydrolysis. We developed lyophilized liposomal formulations of both α-TOS and α-TAM to solve the problem with cytotoxicity of free α-TAM, as well as the low solubility of both drugs. Neither acute toxicity nor immunotoxicity implicated by in vitro tests was detected in vivo after application of liposomal α-TAM, which significantly reduced the growth of cancer cells in hollow fiber implants. Moreover, liposomal formulation of α-TAM and α-TOS each prevented the growth of tumours in transgenic FVB/N c-neu mice bearing spontaneous breast carcinomas. Liposomal formulation of α-TAM demonstrated anti-cancer activity at levels 10-fold lower than those of α-TOS. Workplace Institute of Biotechnology Contact Monika Kopřivová, Monika.Koprivova@ibt.cas.cz, Tel.: 325 873 700 Year of Publishing 2010
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