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他莫昔芬及相关化合物可降低脂质体的膜流动性。他莫昔芬抗氧化作用的机制及其与抗癌和心脏保护作用的相关性?

Tamoxifen and related compounds decrease membrane fluidity in liposomes. Mechanism for the antioxidant action of tamoxifen and relevance to its anticancer and cardioprotective actions?

作者信息

Wiseman H, Quinn P, Halliwell B

机构信息

Biomedical Sciences Division, King's College, University of London, UK.

出版信息

FEBS Lett. 1993 Sep 6;330(1):53-6. doi: 10.1016/0014-5793(93)80918-k.

Abstract

Tamoxifen and related compounds decrease membrane fluidity in ox-brain phospholipid liposomes: their order of effectiveness is, 4-hydroxytamoxifen > 17 beta-oestradiol > tamoxifen > cis-tamoxifen > N-desmethyltamoxifen > cholesterol. A good positive correlation was demonstrated between the decrease in membrane fluidity by these compounds and their antioxidant ability as inhibitors of liposomal and microsomal lipid peroxidation (correlation coefficient, r = 0.99, P < 0.001, in both cases). The ability of tamoxifen to decrease membrane fluidity is suggested to be the mechanism of its antioxidant action and is discussed in relation to its anticancer and cardioprotective actions.

摘要

他莫昔芬及相关化合物可降低牛脑磷脂脂质体的膜流动性

其有效性顺序为,4-羟基他莫昔芬>17β-雌二醇>他莫昔芬>顺式他莫昔芬>N-去甲基他莫昔芬>胆固醇。这些化合物引起的膜流动性降低与其作为脂质体和微粒体脂质过氧化抑制剂的抗氧化能力之间呈现出良好的正相关(两种情况下相关系数r = 0.99,P < 0.001)。他莫昔芬降低膜流动性的能力被认为是其抗氧化作用的机制,并结合其抗癌和心脏保护作用进行了讨论。

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