Abstract |
We have synthesized a series of novel phenylester compounds and present our assessment of such a derivative of aspirin, 3-((diethoxyphosphoryloxy)methyl)phenyl 2-acetoxybenzoate, provisionally named phosphoaspirin. We determined its anticancer activity both in vitro and in vivo. Phosphoaspirin inhibited the growth of HT-29 human colon adenocarcinoma cells (IC(50) = 276.6+/-12.3 microM (mean +/- SEM)] through a combined antiproliferative and mainly proapoptotic effect. Phosphoaspirin (100 mg/kg body weight intraperitoneally daily for 21 days) also inhibited the growth of HT-29 tumors grown as xenografts in nude mice. The size of the tumors decreased progressively in the phosphoaspirin treated group, compared to controls, being reduced by 57% (p<0.001) on day 21. Phosphoaspirin achieved this effect by modulating cell kinetics; the proliferation index of cancer cells was reduced by 18.13% compared to controls (p<0.001) and the apoptosis index was increased by 94.6% (p<0.003). There was no apparent toxicity from phosphoaspirin. We conclude that phosphoaspirin is a promising agent for the control of cancer that deserves further evaluation.
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Authors | Basil Rigas, Vasiliki Kozoni |
Journal | International journal of oncology
(Int J Oncol)
Vol. 32
Issue 1
Pg. 97-100
(Jan 2008)
ISSN: 1019-6439 [Print] Greece |
PMID | 18097547
(Publication Type: Journal Article)
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Chemical References |
- Antineoplastic Agents
- Organophosphates
- phosphoaspirin
- Nitric Oxide
- Aspirin
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Topics |
- Animals
- Antineoplastic Agents
(pharmacology)
- Aspirin
(analogs & derivatives, pharmacology)
- HT29 Cells
- Humans
- Mice
- Neoplasm Transplantation
- Nitric Oxide
(physiology)
- Organophosphates
(pharmacology)
- Transplantation, Heterologous
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