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Phytochemicals for breast cancer prevention by targeting aromatase
1Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E. Duarte Rd. Duarte, CA, USA.
Abstract:
Aromatase is a cytochrome P450 enzyme (CYP19) and is the rate limiting enzyme in the conversion of androgens to estrogens. Suppression of in situ estrogen production through aromatase inhibition is the current treatment strategy for hormone-responsive breast cancers. Drugs that inhibit aromatase have been developed and are currently utilized as adjuvant therapy for breast cancer in post-menopausal women with hormone dependent breast cancer. Natural compounds have been studied extensively for important biologic effects such as antioxidant, anti-tumor and anti-viral effects. A significant number of studies have also investigated the aromatase inhibitory properties of a variety of plant extracts and phytochemicals. The identification of natural compounds that inhibit aromatase could be useful both from a chemopreventive standpoint and in the development of new aromatase inhibitory drugs. This review will discuss whole food extracts and the common classes of phytochemicals which have been investigated for potential aromatase inhibitory activity. We will review reported aromatase inhibition, kinetic data and possible structural variations that may inhibit or enhance the interaction of phytochemicals with the aromatase enzyme.
Insights
Natural compounds show promise for inhibiting aromatase, the enzyme crucial for estrogen production in hormone-responsive breast cancers. This review explores plant extracts and phytochemicals for potential chemopreventive and therapeutic applications.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Aromatase (cytochrome P450 19, CYP19) is the key enzyme in estrogen biosynthesis.
- Aromatase inhibition is a primary treatment for hormone-dependent breast cancer in postmenopausal women.
- Natural compounds are extensively studied for diverse biological activities, including anti-tumor effects.
Purpose of the Study:
- To review natural compounds, including whole food extracts and phytochemicals, with aromatase inhibitory activity.
- To discuss the potential of these natural compounds for cancer chemoprevention and drug development.
- To analyze reported aromatase inhibition, kinetic data, and structure-activity relationships.
Main Methods:
- Literature review of studies investigating aromatase inhibition by natural compounds.
- Analysis of phytochemical classes and whole food extracts with reported activity.
- Examination of kinetic data and structural features influencing enzyme-inhibitor interactions.
Main Results:
- Numerous plant extracts and phytochemicals exhibit aromatase inhibitory properties.
- Specific classes of phytochemicals demonstrate significant potential for aromatase inhibition.
- Structure-activity relationships are being elucidated to optimize inhibitory potential.
Conclusions:
- Natural compounds offer a promising avenue for developing novel aromatase inhibitors.
- Further research into phytochemicals could lead to new strategies for breast cancer prevention and treatment.
- Understanding structure-activity relationships is crucial for designing effective natural aromatase inhibitors.
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