Effect of Leptin Replacement on PCSK9 in ob/ob Mice and Female Lipodystrophic Patients

Endocrinology. 2016 Apr;157(4):1421-9. doi: 10.1210/en.2015-1624. Epub 2016 Jan 29.

Abstract

Leptin treatment has beneficial effects on plasma lipids in patients with lipodystrophy, but the underlying mechanism is unknown. Proprotein convertase subtilisin/kexin type 9 (PCSK9) decreases low-density lipoprotein (LDL) clearance, promotes hypercholesterolemia, and has recently emerged as a novel therapeutic target. To determine the effect of leptin on PCSK9, we treated male and female ob/ob mice with leptin for 4 days via sc osmotic pumps (∼24 μg/d). Leptin reduced body weight and food intake in all mice, but the effects of leptin on plasma PCSK9 and lipids differed markedly between the sexes. In male mice, leptin suppressed PCSK9 but had no effect on plasma triglycerides or cholesterol. In female mice, leptin suppressed plasma triglycerides and cholesterol but had no effect on plasma PCSK9. In parallel, we treated female lipodystrophic patients (8 females, ages 5-23 y) with sc metreleptin injections (∼4.4 mg/d) for 4-6 months. In this case, leptin reduced plasma PCSK9 by 26% (298 ± 109 vs 221 ± 102 ng/mL; n = 8; P = .008), and the change in PCSK9 was correlated with a decrease in LDL cholesterol (r(2) = 0.564, P = .03). In summary, in leptin-deficient ob/ob mice, the effects of leptin on PCSK9 and plasma lipids appeared to be independent of one another and strongly modified by sex. On the other hand, in lipodystrophic females, leptin treatment reduced plasma PCSK9 in parallel with LDL cholesterol.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adolescent
  • Animals
  • Blotting, Western
  • Child
  • Child, Preschool
  • Cholesterol / blood
  • Cholesterol, LDL / blood
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Gene Expression / drug effects
  • Humans
  • Leptin / pharmacology*
  • Lipodystrophy / blood*
  • Lipodystrophy / physiopathology
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Mice, Obese
  • Obesity / blood*
  • Obesity / physiopathology
  • Proprotein Convertase 9
  • Proprotein Convertases / blood*
  • Proprotein Convertases / genetics
  • Proprotein Convertases / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Serine Endopeptidases / blood*
  • Serine Endopeptidases / genetics
  • Serine Endopeptidases / metabolism
  • Sex Factors
  • Triglycerides / blood
  • Young Adult

Substances

  • Cholesterol, LDL
  • Leptin
  • Triglycerides
  • Cholesterol
  • Pcsk9 protein, mouse
  • Proprotein Convertase 9
  • Proprotein Convertases
  • Serine Endopeptidases