Chemopreventive effects of resveratrol and resveratrol derivatives

Resveratrol is considered to have a number of beneficial effects. Recently, our group modified the molecule and synthesized a number of compounds with different biochemical effects. Polymethoxy and polyhydroxy derivatives of resveratrol were shown to inhibit tumor cell growth in various cell lines a...

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Bibliographic Details
Published in:Annals of the New York Academy of Sciences 2011-01, Vol.1215 (1), p.89-95
Main Authors: Szekeres, Thomas, Saiko, Philipp, Fritzer-Szekeres, Monika, Djavan, Bob, Jäger, Walter
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - metabolism
Antineoplastic Agents, Phytogenic - therapeutic use
antitumor effects
Cell growth
Chemoprevention - methods
free radicals
Humans
Lymphatic system
Melanoma
Metastasis
Neoplasms - drug therapy
Neoplasms - metabolism
polyhydroxyphenols
resveratrol
resveratrol metabolism
ribonucleotide reductase
Rodents
Stilbenes - chemistry
Stilbenes - metabolism
Stilbenes - therapeutic use
Structure-Activity Relationship
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Summary:Resveratrol is considered to have a number of beneficial effects. Recently, our group modified the molecule and synthesized a number of compounds with different biochemical effects. Polymethoxy and polyhydroxy derivatives of resveratrol were shown to inhibit tumor cell growth in various cell lines and inflammation pathways (cyclooxygenases activity), in part more effectively than resveratrol itself. One lead compound (hexahydroxystilbene, M8) turned out to be the most effective inhibitor of tumor cell growth and of cyclooxygenase 2 activity. M8 was then studied in two different human melanoma mouse models. This novel resveratrol analog was able to inhibit melanoma tumors in a primary tumor model alone and in combination with dacarbacine, an anticancer compound that is used for melanoma treatment. We also tested the development of lymph node metastasis in a second melanoma model and again M8 successfully inhibited the tumor as well as the size and weight of lymph node metastasis. Hydroxylated resveratrol analogs therefore represent a novel class of anticancer compounds and promising candidates for in vivo studies.
ISSN:0077-8923
1749-6632
DOI:10.1111/j.1749-6632.2010.05864.x