Lignans and flavonoids inhibit aromatase enzyme in human preadipocytes

Chuanfeng Wang, Taru Mäkelä, Tapio Hase, Herman Adlercreutz, Mindy S. Kurzer

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Lignans and flavonoids are naturally-occurring diphenolic compounds found in high concentrations in whole grains, legumes, fruits and vegetables. Seven lignans and six flavonoids were evaluated for their abilities to inhibit aromatase enzyme activity in a human preadipose cell culture system. The lignan, enterolactone (Enl) and its theoretical precursors, 3′-demethoxy-3O-demethylmatairesinol (DMDM) and didemethoxymatairesinol (DDMM) decreased aromatase enzyme activity, with Ki values of 14.4, 5.0 and 7.3 μM, respectively. The flavonoids, coumestrol, luteolin and kaempferol also decreased aromatase enzyme activity, with Ki values of 1.3, 4.8 and 27.2 μM, respectively. Amino-glutethimide, a pharmaceutical aromatase inhibitor, showed a Ki value of 0.5 μM. Kinetic studies showed the inhibition by all compounds to be competitive. Smaller decreases in aromatase activity were observed with the lignan, enterodiol (End) and its theoretical precursors, O-demethylsecoisolariciresinol (ODSI), demethoxysecoisolariciresinol (DMSI) and didemethylsecoisolariciresinol (DDSI). The flavonoids, O-demethylangolensin (O-Dma), fisetin and morin showed no inhibitory effects. The inhibition of human preadipocyte aromatase activity by lignans and flavonoids suggests a mechanism by which consumption of lignan- and flavonoid-rich plant foods may contribute to reduction of estrogen-dependent disease, such as breast cancer.

Original languageEnglish (US)
Pages (from-to)205-212
Number of pages8
JournalJournal of Steroid Biochemistry and Molecular Biology
Issue number3-4
StatePublished - Aug 1994

Bibliographical note

Funding Information:
Acknowledgements--This work was supported by Minnesota Agricultural Experiment Station project 18-34 and an International Life Science Institute-Nutrition Foundation Future Leader Award (MSK). Synthesis of the lignan intermediates and O-Dma was supported by NIH grant CA56289-01 to H.A. The authors are grateful to Dr Bruce Cunningham (Department of Surgery, University of Minnesota) and the staff of the St Paul Surgical Center, St Paul Ramsey Medical Center (St Paul, MN) for assistance in obtaining adipose tissue and to Dr K. W~ih~il~i (Department of Chemistry, University of Helsinki, Finland) for the synthesis of O-Dma.


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