Antimetastatic activity and low systemic toxicity of tetradecyl gallate in a preclinical melanoma mouse model

作者：Locatelli Claudriana; Carvalho Deborah Regina; Mascarello Alessandra; Silva de Cordova Clarissa Amorin; Yunes Rosendo Augusto; Nunes Ricardo Jose; Pilati Celso; Creczynski Pasa Tania Beatriz^*

来源：Investigational New Drugs, 2012, 30(3): 870-879.

DOI：10.1007/s10637-010-9628-7

• Melanoma
• Antimetastatic
• Cell adhesion
• Gallic acid derivative

Gallates with eight or more carbon atoms in the lateral chain show potent anticancer activity against various cell lines. However, studies regarding the in vivo antimelanoma activity of tetradecyl gallate (C-14) have not yet been reported. In this study an evaluation of the ability of C-14 to inhibit metastasis, using lung metastases as a model, was carried out. The experimental mouse melanoma model was established by intravenous injection of metastatic B16F10 melanoma cells. The systemic toxicity of C-14 was evaluated in vivo by monitoring the weight, survival, biochemical and hematological parameters, and through histological analysis. It was observed that C-14 decreased lung metastasis in vivo by 80% and increased the survival rate of the animals without toxic effects. Additionally, C-14 induced cytotoxic effects on B16F10 cells, inhibited the inter-cellular adhesion molecule 1 (ICAM-1) and vascular cell adhesion molecule 1 (VCAM-1) expression, and significantly decreased cell adhesion. These results reveal that C-14 has potent antimetastatic ability and is a good candidate for further study as a potential therapeutic agent for tumor metastases.

• 出版日期2012-6