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Synthesis of methotrexate-poly (ethylene glycol) conjugate and their anti-tumor activity in vitro / 药学学报
Acta Pharmaceutica Sinica ; (12): 607-610, 2007.
Artigo em Chinês | WPRIM | ID: wpr-268631
ABSTRACT
To improve the physical property and bioactivity of methotrexate, this paper investigated the new formation of conjugate methotrexate-poly (ethylene glycol) and in vitro anti-tumor activity of the synthesized conjugate. The conjugate of methotrexate-poly (ethylene glycol), which was verified by the spectroscopy analysis of UV, IR and 13C NMR, was synthesized by chemical catalysis and micro-wave irritation. The determination for the conjugate of solubility in water and distribution coefficient in octanol-water system of the conjugate was done to examine its deliquescence property. The solubility in water and the distribution coefficient of the conjugate was greatly improved, which was increased by 128 folds and 5 folds, respectively. The in vitro anti-tumor activity of the conjugate was tested by mouse L(1210) leukaemia cells, and the synthesized conjugate showed the same anti-tumor activity as the original methotrexate. Compared to the reported literature, the modification of methotrexate by poly (ethylene glycol) is more rapid and convenient.
Assuntos
Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Polietilenoglicóis / Solubilidade / Leucemia L1210 / Química / Metotrexato / Tratamento Farmacológico / Antineoplásicos Limite: Animais Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2007 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Polietilenoglicóis / Solubilidade / Leucemia L1210 / Química / Metotrexato / Tratamento Farmacológico / Antineoplásicos Limite: Animais Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2007 Tipo de documento: Artigo