Sex steroids mediate discrete effects on HDL cholesterol efflux capacity and particle concentration in healthy men

J Clin Lipidol. 2018 Jul-Aug;12(4):1072-1082. doi: 10.1016/j.jacl.2018.04.013. Epub 2018 Apr 30.

Abstract

Background: Exogenous testosterone decreases serum concentrations of high-density lipoprotein cholesterol (HDL-C) in men, but whether this alters cardiovascular risk is uncertain.

Objective: To investigate the effects of testosterone and estradiol on HDL particle concentration (HDL-Pima) and metrics of HDL function.

Methods: We enrolled 53 healthy men, 19 to 55 years of age, in a double-blinded, placebo-controlled, randomized trial. Subjects were rendered medically castrate using the GnRH receptor antagonist acyline and administered either (1) placebo gel, (2) low-dose transdermal testosterone gel (1.62%, 1.25 g), (3) full replacement dose testosterone gel (1.62%, 5 g) or (4) full replacement dose testosterone gel together with an aromatase inhibitor for 4 weeks. At baseline and end of treatment, serum HDL total macrophage and ABCA1-specific cholesterol efflux capacity (CEC), HDL-Pima and size, and HDL protein composition were determined.

Results: Significant differences in serum HDL-C were observed with treatment across groups (P = .01 in overall repeated measures ANOVA), with increases in HDL-C seen after both complete and partial testosterone deprivation. Medical castration increased total HDL-Pima (median [interquartile range] 19.1 [1.8] nmol/L at baseline vs 21.3 [3.1] nmol/L at week 4, P = .006). However, corresponding changes in total macrophage CEC and ABCA1-specific CEC were not observed. Change in serum 17β-estradiol concentration correlated with change in total macrophage CEC (β = 0.33 per 10 pg/mL change in serum 17β-estradiol, P = .03).

Conclusions: Testosterone deprivation in healthy men leads to a dissociation between changes in serum HDL-C and HDL CEC. Changes in serum HDL-C specifically due to testosterone exposure may not reflect changes in HDL function.

Trial registration: ClinicalTrials.gov NCT01686828.

Keywords: Cardiovascular disease; Cholesterol efflux; HDL; Lipoproteins; Sex steroids.

Publication types

  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter 1 / metabolism
  • Adult
  • Aromatase Inhibitors / administration & dosage
  • Cardiovascular Diseases / diagnosis
  • Cell Line
  • Cholesterol, HDL / blood*
  • Cholesterol, HDL / chemistry
  • Double-Blind Method
  • Estradiol / blood
  • Humans
  • Injections, Subcutaneous
  • Macrophages / cytology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Male
  • Middle Aged
  • Oligopeptides / administration & dosage*
  • Particle Size
  • Placebo Effect
  • Testosterone / administration & dosage*
  • Testosterone / blood
  • Testosterone / pharmacology
  • Young Adult

Substances

  • ABCA1 protein, human
  • ATP Binding Cassette Transporter 1
  • Aromatase Inhibitors
  • Cholesterol, HDL
  • Oligopeptides
  • Testosterone
  • Estradiol
  • acyline

Associated data

  • ClinicalTrials.gov/NCT01686828