Probucol normalizes cholesteryl ester transfer in IDDM

Diabetes Care. 1995 Oct;18(10):1341-6. doi: 10.2337/diacare.18.10.1341.

Abstract

Objective: Cholesteryl ester transfer (CET) is pathologically increased in insulin-dependent diabetes mellitus (IDDM), and the resulting enrichment of the apolipoprotein B-containing lipoproteins with cholesteryl ester (CE) is believed to increase their atherogenicity. Because we have shown previously that treatment with the lipid-modifying antioxidant probucol normalizes CET in nondiabetic patients with hypercholesterolemia, we sought to determine whether the same beneficial effects could be achieved in IDDM.

Research design and methods: CET was measured by both mass and isotopic assay in eight normolipidemic (triglyceride, 102; cholesterol, 192; high-density lipoprotein [HDL] cholesterol, 45 mg/dl) IDDM patients (fructosamine 495 +/- 146 mumol/l; normal 174-286) before and after 2 months of treatment with probucol (1.0 g/day).

Results: Before treatment, CET was accelerated abnormally (P < 0.001). As expected, probucol decreased plasma (-13%; P < 0.025) and HDL2 cholesterol levels (-52%; P < 0.025) and the concentration of lipoprotein A-I particles (P < 0.025). In conjunction with these changes, CET fell dramatically in all subjects (mass assay: -94%; isotopic assay: -22%, P < 0.001) with no change in the mass of cholesteryl ester transfer protein (CETP) (pretreatment 2.91 +/- 0.97 vs. posttreatment 3.21 +/- 1.03 micrograms/ml). Glycemic control, however, improved significantly (fructosamine 409 +/- 85 mumol/l, P < 0.025).

Conclusions: Because it is believed that accelerated CET promotes the formation of apolipoprotein B-containing lipoproteins enriched with atherogenic CE, the capacity of probucol to reverse this functional abnormality without adversely affecting glycemic control suggests that it has a place in the therapy of IDDM.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Anticholesteremic Agents / pharmacology
  • Anticholesteremic Agents / therapeutic use*
  • Apolipoproteins / blood
  • Carrier Proteins / blood*
  • Carrier Proteins / drug effects
  • Cholesterol / blood
  • Cholesterol Ester Transfer Proteins
  • Cholesterol Esters / blood*
  • Cholesterol, HDL / blood
  • Cholesterol, LDL / blood
  • Diabetes Mellitus, Type 1 / blood*
  • Diabetes Mellitus, Type 1 / drug therapy
  • Female
  • Fructosamine
  • Glycoproteins*
  • Hexosamines / blood
  • Humans
  • Kinetics
  • Lipoproteins / blood
  • Male
  • Probucol / pharmacology
  • Probucol / therapeutic use*
  • Reference Values
  • Time Factors
  • Triglycerides / blood

Substances

  • Anticholesteremic Agents
  • Apolipoproteins
  • CETP protein, human
  • Carrier Proteins
  • Cholesterol Ester Transfer Proteins
  • Cholesterol Esters
  • Cholesterol, HDL
  • Cholesterol, LDL
  • Glycoproteins
  • Hexosamines
  • Lipoproteins
  • Triglycerides
  • Fructosamine
  • Cholesterol
  • Probucol