Inhibition of aromatase activity by flavonoids

  • Hyeh -Jean Jeong
  • Young Geun Shin
  • Il -Hyuk Kim
  • John M. Pezzuto
Research Articles Natural Products

Abstract

In searching for potent cancer chemopreventive agents from synthetic or natural products, 28 randomly selected flavonoids were screened for inhibitory effects against partially purified aromatase prepared from human placenta. Over 50% of the flavonoids significantly inhibited aromatase activity, with greatest activity being demonstrated with apigenin (IC50: 0.9 μg/mL), chrysin (IC50: 1.1 μg/mL), and hesperetin (IC50: 1.0 μg/mL).

Key words

Aromatase inhibition Flavonoids Breast cancer 

References Cited

  1. Brodie, A. M. H. and Njar, V. C. O.: Aromatase inhibitors and breast cancer.Semin. Oncol., 23, 10–20 (1996).PubMedGoogle Scholar
  2. Conn, P. M. and Crowley, W. F., Gonadotrophin-releasing hormone and its analogues.N. Engl. J. Med., 324, 93–103 (1991).PubMedGoogle Scholar
  3. Harvey, H. A.: Aromatase inhibitors in clinical practice: Current status and a look to the future.Semin. Oncol., 23, Suppl., 9, 33–38 (1996).PubMedGoogle Scholar
  4. Hoffman, P. G., Jones, L. A., Kuhn, R. W. and Sitteri, P. K.: Progesterone receptors: saturation analysis by a solid phase hydroxyapatite adsorption technique.Cancer, 46, 2801–2804 (1980).PubMedCrossRefGoogle Scholar
  5. Kellis, J. T. Jr. and Vickery, L. E.: Purification and characterization of human placental aromatase cytochrome P-450,J. Biol. Chem., 262, 4413–4420 (1987).PubMedGoogle Scholar
  6. Rabe, T., Rabe, D. and Punnebaum, B.: New aromatase assay and its application for inhibitory studies of aminogluthetimide on microsomes of human term placenta.J. Steroid Biochem., 7, 305–309 (1982).Google Scholar
  7. Santen, R. J., Manni, A. and Harvey, H. A.: Endocrine treatment of breast cancer in women.Endocr. Rev., 11, 221–265 (1990).PubMedCrossRefGoogle Scholar
  8. Santen, R. J., Martel, J. and Hoagland, M.: Stromal spindle cells contain aromatase in human breast tumors.J. Clin. Endocrinol. Metab., 79, 627–632 (1994).PubMedCrossRefGoogle Scholar
  9. Siiteri, P. K.: Review of studies on estrogen biosynthesis in the human.Cancer Res., 42, 3269s-3273s (1982).PubMedGoogle Scholar
  10. Thompson, E. A. and Siiteri, P. K.: The involvement of human placental microsomal cytochrome P-450 in aromatization.J. Biol. Chem., 249, 5373–5378 (1974a).PubMedGoogle Scholar
  11. Thompson, E. A. and Siiteri, P. K.: Utilization of oxygen and reduced nicotinamide adenine dinucleotide phosphate by human placental microsomes during aromatization of androstenedione.J. Biol. Chem., 249, 5364–5372 (1974b).PubMedGoogle Scholar

Copyright information

© The Pharmaceutical Society of Korea 1999

Authors and Affiliations

  • Hyeh -Jean Jeong
    • 1
  • Young Geun Shin
    • 1
  • Il -Hyuk Kim
    • 2
  • John M. Pezzuto
    • 1
  1. 1.Program for Collaborative Research in the Pharmaceutical Sciences and Department of Medicinal Chemistry and Pharmacognosy, College of PharmacyUniversity of Illinois at ChicagoChicagoUSA
  2. 2.College of PharmacyChungAng UniversitySeoulKorea
  3. 3.National Institute of HealthBethesdaUSA

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