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Effect of synthetic and naturally occurring chalcones on ovarian cancer cell growth: structure-activity relationships
R De Vincenzo1, G Scambia, P Benedetti Panici
1Department of Gynecology, Centro Chimica dei Recettori C.N.R., Rome, Italy.
Abstract:
This study was carried out to determine the effect of 15 different natural and synthetic chalcones on the proliferation of both established and primary ovarian cancer cells expressing type II oestrogen binding sites (type II EBS). The binding affinity of chalcones for type II EBS was also tested. At concentrations from 0.1 to 10 microM, chalcones inhibited ovarian cancer cell proliferation and [3H]oestradiol ([3H]E2) binding to type II EBS. Considering the structure-related variation in IC50 (concentration resulting in a 50% inhibition of cell growth) and Di50 (concentration resulting in a 50% displacement of [3H]E2 bound to type II EBS), it appeared that the presence of an alpha-beta double bond, the hydroxylation in 3 or 2 of ring B and the absence of a prenyl group were important to both the antiproliferative and binding activity. Structure-related variations in IC50 and Di50 were significantly concordant (Fisher's exact test: P = 0.0291), suggesting that there may be a type II EBS-mediated mechanism for chalcone antiproliferative activity. Our data indicate that chalcones could be considered as potential new anticancer drugs.
Insights
This study investigated chalcones as potential ovarian cancer drugs. Certain chalcones effectively inhibited cancer cell growth and binding to estrogen receptors, suggesting a new therapeutic avenue.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Ovarian cancer remains a significant health challenge.
- Estrogen binding sites (EBS) play a role in cancer progression.
- Chalcones are natural compounds with potential therapeutic properties.
Purpose of the Study:
- To evaluate the antiproliferative effects of 15 chalcones on ovarian cancer cells.
- To assess the binding affinity of chalcones to type II estrogen binding sites (type II EBS).
- To explore the structure-activity relationship of chalcones in inhibiting cancer cell proliferation and EBS binding.
Main Methods:
- Testing 15 natural and synthetic chalcones against established and primary ovarian cancer cells.
- Measuring inhibition of cell proliferation (IC50) and [3H]estradiol binding to type II EBS (Di50).
- Analyzing structure-activity relationships using statistical methods (Fisher's exact test).
Main Results:
- Chalcones inhibited ovarian cancer cell proliferation and [3H]estradiol binding to type II EBS at concentrations of 0.1–10 microM.
- Specific structural features of chalcones, including an alpha-beta double bond and hydroxylation, were crucial for activity.
- A significant concordance between antiproliferative activity (IC50) and binding affinity (Di50) was observed (P = 0.0291).
Conclusions:
- Chalcones demonstrate significant antiproliferative effects on ovarian cancer cells.
- A type II EBS-mediated mechanism may underlie the observed anticancer activity of chalcones.
- Chalcones represent promising candidates for the development of novel anticancer drugs.