Summary
The relationship between the content of probucol in plasma and lipid lowering was studied after administration of probucol. The study group consisted of 44 patients with Type II hyperlipidaemia (mean age 56 y).
Total cholesterol level was decreased from 293 to 232 mg · dl−1 by the administration of probucol. The plasma probucol concentration was 2.03 mg · dl−1 after 4 weeks of administration of 500 mg b. d. Although there was no relationship between the change in total cholesterol and the plasma probucol, a linerar relation was observed between the decrease in LDL-cholesterol concentration and the probucol concentration in LDL. Neither the VLDL nor the HDL-probucol content were related to the magnitude of the decrease in lipoprotein cholesterol.
The present study has demonstrated that an increase in the probucol content in LDL was associated with a decrease in plasma LDL-cholesterol.
Similar content being viewed by others
References
Barnhart JW, Rytter JD, Molello JA (1977) An overview of the biochemical pharmacology of probucol. Lipids 12: 29–33
Buckley MMT, Goa KL, Price AH, Brogden RN (1989) Probucol. A reappraisal of its pharmacological properties and therapeutic use in hypercholesterolaemia. Drugs 37: 761–800
Kesänniemi YA, Grundy SM (1984) Influence of probucol on cholesterol and lipoprotein metabolism in man. J Lipid Res 25: 780–790
Goldberg RB, Mendez A (1988) Probucol enhances cholesterol efflux from cultured human skin fibroblasts. Am J Cardiol 62: 488–518
Li JR, Holets RJ, Kottke BA (1980) Effect of probucol on cholesterol metabolism in the rat. Atherosclerosis 36: 559–565
Marshall FN (1982) Pharmacology and toxicology of probucol. Artery 10: 7–21
Richmond W (1973) Preparation and properties of cholesterol oxidase from Nocardia sp. and its application to the enzymatic assay of total cholesterol in serum. Clin Chem 19: 1350–1356
Smith L, Lucas D, Lehmus G (1979) Automated measurement of total cholesterol and triglycerides. In: “Tandem”, on the discrete sample analyzer, Gilford System 3500. Clin Chem 25: 439–442
Goto Y, Akanuma Y, Harano Y, Hata Y, Itakura H, Kajiyama G, Kawade M, Koga S, Kuzuya F, Maruhama Y, Matsuzawa Y, Murai A, Murase T, Naito C, Nakai T, Noma A, Saito Y, Sasaki J, Takeuchi N, Tamachi H, Uzawa H, Yamamoto A, Yamazaki S, Yasugi T, Yukawa S (1986) Determination by the SRID method of normal values of serum apo-lipoproteins (A-I, A-II, B, C-III and E) in normolipidemic healthy Japanese subjects. J Clin Biochem Nutr 1: 73–88
Havel RJ, Eder HA, Bragdon JH (1955) The distribution and chemical composition of ultracentrifugally separated lipoproteins in human serum. J Clin Invest 34: 1345–1353
Yagi K (1976) A simple fluorometric assay for lipoperoxide in blood plasma. Biochem Med 15: 212–216
Dachet C, Jacotot B, Buxtorf JC (1985) The hypolipidemic action of probucol. Atherosclerosis 58: 261–268
Sudo K, Midorikawa K, Tachizawa H, Hata Y, Saito Y (1983) Studies on the distribution of probucol in human serum lipoprotein fractions. Jpn J Atheroscler 11: 591–595
Urien S, Riant P, Albeugres E, Brioude R, Tillement JP (1984) In vitro studies on the probucol distribution of probucol among human plasma lipoproteins. Mol Pharmacol 26: 322–327
Felin R, Gasparotto A, Valerio G, Baiocchi MR, Pardrini R, Lamon S, Vitale E, Baggio G, Crepaldi G (1986) Effect of probucol treatment on lipoprotein cholesterol and drug levels in blood and lipoproteins in familial hypercholesterolemia. Atherosclerosis 59: 47–56
Parthasarathy S, Young SG, Witztum JL, Pittman RC, Steinberg D (1986) Probucol inhibits oxidative modification of low density lipoprotein. J Clin Invest 77: 641–644
Reaven PD, Parthasarathy S, Beltz WF, Witztum JL (1992) Effect of probucol dosage on plasma lipid and lipoprotein levels and on protection of low density lipoprotein against in vitro oxidation in humans. Arterioscler Thromb 12: 318–324
Franceschini G, Sirtori M, Vaccarino V, Gianfranceschi G, Rezzonico L, Chiesa G, Sirtori CR (1989) Mechanism of HDL reduction after probucol. Changes in HDL subfractions and increased reverse cholesteryl ester transfer. Arterioscler Throm 9: 462–469
Chiesa G, Franceschini G, Sirtori CR (1990) In vivo activity of probucol on cholesteryl ester transport. Biophys Biochim Acta 1045: 302–304
Naruszewicz M, Carew TE, Pittman RC, Witztum JL, Steinberg D (1984) A novel mechanism by which probucol lowers low density lipoprotein levels demonstrated in the LDL receptor-deficient rabbit. J Lipid Res 25: 1206–1213
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Shinomiya, M., Shirai, K., Saito, Y. et al. Positive correlation between probucol in low density lipoprotein and LDL-lowering. Eur J Clin Pharmacol 45, 343–346 (1993). https://doi.org/10.1007/BF00265952
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00265952