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Article
November 1961

Mode of Action of Cholesterol-Lowering AgentsA Critique of Facts and Theories

Arch Intern Med. 1961;108(5):717-732. doi:10.1001/archinte.1961.03620110057009
Abstract

The implication of hypercholesteremia in atherogenesis has stimulated a continued search for cholesterol-lowering agents within the last decades. In addition to various dietary regimens ranging from a glass of orange juice to special formula diets, a great number of drugs ranging from household remedy aspirin (acetylsalicylic acid) to new sophisticated compounds have been reported to possess hypocholesteremic activity. Their efficacy, side-effects, and clinical usefulness will be discussed elsewhere.1

The present review is confined to the mode of action of unsaturated fats, sitosterol, nicotinic acid, thyroid hormones and analogues, and triparanol. They are selected for discussion because they have been extensively studied clinically and with respect to their mode of action. Since, as will be delineated, these agents act at different sites of the metabolic pathways of cholesterol, several avenues are thus opened for further investigation of cholesterol metabolism and atherogenesis.

Unsaturated Fats  It has long been known that the

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