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Resveratrol and resveratrol analogues--structure-activity relationship
Thomas Szekeres1, Monika Fritzer-Szekeres, Philipp Saiko
1Department of Medical and Chemical Laboratory Diagnostics, General Hospital of Vienna, Medical University of Vienna, Waehringer Guertel 18-20, 1090 Vienna, Austria. Thomas.szekeres@meduniwien.ac.at
Pharmaceutical Research
|March 17, 2010
Summary
Resveratrol, a compound in red wine, shows anti-inflammatory and anti-aging properties. A synthetic analogue, hexahydroxystilbene (M8), effectively inhibits human melanoma tumor and metastasis growth in animal models.
Area of Science:
- Natural Product Chemistry
- Pharmacology
- Oncology
Background:
- Resveratrol, a stilbenoid found in red wine, is associated with various health benefits, including cardiovascular protection, anti-inflammatory effects, and potential roles in tumor inhibition and aging.
- Understanding the structure-activity relationship of resveratrol is crucial for developing more potent analogues with enhanced therapeutic effects.
Purpose of the Study:
- To investigate the structure-activity relationship of resveratrol and its analogues concerning free radical scavenging and antitumor activities.
- To synthesize novel resveratrol analogues aimed at improving its beneficial effects, particularly in cancer treatment.
- To evaluate the efficacy of a potent synthetic analogue, hexahydroxystilbene (M8), against human melanoma growth and metastasis.
Main Methods:
- Analysis of structural properties of resveratrol and its synthesized analogues to correlate with observed biological effects.
- Synthesis of novel resveratrol analogues, including hexahydroxystilbene (M8).
- In vivo evaluation of M8's efficacy in inhibiting human melanoma tumor and metastasis growth in two distinct animal models, both as a single agent and in combination with dacarbazine.
Main Results:
- Identification of key structural features responsible for the biological activities of resveratrol.
- Hexahydroxystilbene (M8) emerged as the most effective synthetic analogue, demonstrating significant in vivo activity.
- M8 demonstrated inhibition of both tumor and metastasis growth in human melanoma xenografts in animal models, with and without combination therapy using dacarbazine.
Conclusions:
- Hexahydroxystilbene (M8) represents a promising synthetic analogue of resveratrol with potent antitumor and antimetastasis activity against human melanoma.
- The structure-activity relationship studies provide a basis for the rational design of improved resveratrol-based therapeutic agents.
- M8 holds potential for further development as a therapeutic agent in melanoma treatment, possibly in combination regimens.
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