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植物甾醇的药理学特性:体内和体外观察

Pharmacological properties of plant sterols in vivo and in vitro observations.

作者信息

Moghadasian M H

机构信息

Healthy Heart Program and Department of Pathology and Laboratory Medicine, St. Paul's Hospital and the University of British Columbia, 180-1081 Burrard St., Vancouver, British Columbia V6Z 1Y6 Canada.

出版信息

Life Sci. 2000 Jun 30;67(6):605-15. doi: 10.1016/s0024-3205(00)00665-2.

DOI:10.1016/s0024-3205(00)00665-2
PMID:12659166
Abstract

Plant sterols have been investigated as one of the safe potential alternative methods in lowering plasma cholesterol levels. Several human studies have shown that plant sterols/stanols significantly reduce plasma total and LDL cholesterol. In this article, pharmacological characteristics of plant sterols/stanols have been summarized and discussed. In particular, experimental data that demonstrate the effects of dietary phytosterols on lipid metabolism and development of atherosclerotic lesions have been critically reviewed. Despite their similar chemical structures, phytosterols and cholesterol differ markedly from each other in regard to their pharmacological characteristics including intestinal absorption and metabolic fate. Compared to cholesterol, plant sterols have poor intestinal absorption. The most and best studied effects of plant sterols are their inhibition of intestinal cholesterol absorption. Other biological activities of phytosterols such as effects on lecithin:cholesterol acyltransferase activity, bile acid synthesis, oxidation and uptake of lipoproteins, hepatic and lipoprotein lipase activities and coagulation system have been linked to their anti-atherogenic properties. Moreover, evidence for beneficial effects of plant sterols on disorders such as cutaneous xanthomatosis, colon cancer and prostate hyperplasia has been discussed. Finally, the potential adverse effects of plant sterols as well as pathophysiology of hereditary sitosterolemia are also reviewed. In conclusion, more pharmacokinetic data are needed to better understand metabolic fate of plant sterols/stanols and their fatty acid esters as well as their interactions with other nutraceutical/pharmaceutical agents.

摘要

植物甾醇已被作为降低血浆胆固醇水平的一种安全的潜在替代方法进行研究。多项人体研究表明,植物甾醇/甾烷醇可显著降低血浆总胆固醇和低密度脂蛋白胆固醇水平。本文总结并讨论了植物甾醇/甾烷醇的药理学特性。特别是,对证明膳食植物甾醇对脂质代谢和动脉粥样硬化病变发展影响的实验数据进行了严格审查。尽管植物甾醇和胆固醇化学结构相似,但在包括肠道吸收和代谢命运等药理学特性方面却有显著差异。与胆固醇相比,植物甾醇肠道吸收较差。植物甾醇研究最多且最显著的作用是其对肠道胆固醇吸收的抑制作用。植物甾醇的其他生物活性,如对卵磷脂胆固醇酰基转移酶活性、胆汁酸合成、脂蛋白氧化和摄取、肝脂酶和脂蛋白脂酶活性以及凝血系统的影响,都与其抗动脉粥样硬化特性有关。此外,还讨论了植物甾醇对诸如皮肤黄瘤病、结肠癌和前列腺增生等疾病有益作用的证据。最后,还综述了植物甾醇的潜在不良反应以及遗传性谷甾醇血症的病理生理学。总之,需要更多的药代动力学数据来更好地了解植物甾醇/甾烷醇及其脂肪酸酯的代谢命运,以及它们与其他营养保健品/药物的相互作用。

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