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Taxifolin suppresses rat and human testicular androgen biosynthetic enzymes

Fei Ge1, Erpo Tian2, Li Wang2

  • 1Department of Anesthesiology, the Second Affiliated Hospital and Yuying Children's Hospital, Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.

Fitoterapia
|February 7, 2018
PubMed

Insights

Taxifolin, a flavonoid supplement, may help treat prostate cancer by suppressing androgen production in Leydig cells. This study shows taxifolin inhibits key enzymes in testosterone biosynthesis.

Area of Science:

  • Biochemistry
  • Endocrinology
  • Pharmacology

Background:

  • Taxifolin is a flavonoid with chemopreventive properties.
  • It is investigated for potential benefits in prostate cancer treatment.
  • Prostate cancer progression is often linked to androgen production.

Purpose of the Study:

  • To investigate the effects of taxifolin on androgen production in rat Leydig cells.
  • To examine taxifolin's impact on testosterone biosynthetic enzyme activities in rats and humans.
  • To determine the inhibitory potential of taxifolin on key enzymes in steroidogenesis.

Main Methods:

  • Isolated rat Leydig cells were incubated with taxifolin under various stimulation conditions (basal, LH, 8BR) and with steroid substrates.
  • Androgen concentrations (DIOL and testosterone) in the medium were measured.
  • Enzyme kinetics and inhibition constants (IC50) were determined for rat and human 3β-hydroxysteroid dehydrogenase and 17α-hydroxylase/17, 20-lyase.

Main Results:

  • Taxifolin significantly suppressed basal and stimulated androgen production by Leydig cells.
  • It inhibited rat 3β-hydroxysteroid dehydrogenase and 17α-hydroxylase/17, 20-lyase with low IC50 values (14.55±0.013μM and 16.75±0.011μM, respectively).
  • Taxifolin also inhibited these enzymes in human testis (IC50 ≈ 100μM) and acted as a competitive inhibitor.

Conclusions:

  • Taxifolin effectively suppresses androgen production in Leydig cells.
  • It inhibits crucial enzymes in the testosterone biosynthesis pathway in both rats and humans.
  • These findings suggest taxifolin's potential as a therapeutic agent for androgen-dependent conditions like prostate cancer.
Keywords:
17α-hydroxylase/17,20-lyase3β-hydroxysteroid dehydrogenaseLeydig cellsSteroidogenesisTaxifolin

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