Cohen M
Life Sci. 1985 Nov 25;37(21):1949-61. doi: 10.1016/0024-3205(85)90026-8.
The available preclinical literature on the antihyperlipidemic properties of beta-pyridylcarbinol is reviewed. Similarities between the pharmacological profiles for beta-pyridylcarbinol and nicotinic acid, and evidence for the metabolic conversion of beta-pyridylcarbinol to nicotinic acid are discussed. Several reviews discussing the antihyperlipidemic effects of beta-pyridylcarbinol (beta-PC, nicotinyl alcohol, Roniacol) and nicotinic acid (NA) have appeared during the last 15 years (1-6). However, continuing clinical interest in the ability of nicotinic acid analogs to reduce plasma lipids indicated that an update and critical evaluation of the preclinical literature on this subject would be of value in order to permit a more complete assessment of the relevance of several animal models to effects in human subjects. The literature reviewed included (a) preclinical studies of beta-PC where it was the sole compound examined; (b) comparative studies of beta-PC and NA; and (c) studies relating to the metabolism of beta-PC. The literature chosen included experiments involving fasted animals, satiated animals, and effects of Triton-induced hyperlipidemia. Data on other pharmacological properties of beta-PC and/or NA that might contribute to antihyperlipidemic efficacy (e.g., fibrinolysis, inhibition of platelet aggregation, erythrocyte membrane changes) were also included where available.
本文综述了关于β-吡啶甲醇抗高血脂特性的现有临床前文献。讨论了β-吡啶甲醇与烟酸药理学特征的相似性,以及β-吡啶甲醇代谢转化为烟酸的证据。在过去15年中出现了几篇讨论β-吡啶甲醇(β-PC、烟醇、Roniacol)和烟酸(NA)抗高血脂作用的综述(1-6)。然而,临床对烟酸类似物降低血脂能力的持续关注表明,对该主题的临床前文献进行更新和批判性评估将具有价值,以便更全面地评估几种动物模型与对人类受试者影响的相关性。所综述的文献包括:(a)β-PC作为唯一研究化合物的临床前研究;(b)β-PC与NA的比较研究;以及(c)与β-PC代谢相关的研究。所选用的文献包括涉及禁食动物、饱腹动物的实验,以及Triton诱导的高脂血症的影响。如有可用数据,还包括关于β-PC和/或NA可能有助于抗高血脂疗效的其他药理学特性(例如纤维蛋白溶解、抑制血小板聚集、红细胞膜变化)的数据。