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AL721,一种新型的膜流化剂。

AL721, a novel membrane fluidizer.

作者信息

Antonian L, Shinitzky M, Samuel D, Lippa A S

机构信息

Matrix Research Laboratories, Inc., Fort Lee, NJ 07024.

出版信息

Neurosci Biobehav Rev. 1987 Winter;11(4):399-413. doi: 10.1016/s0149-7634(87)80010-6.

Abstract

AL721, which is a novel lipid mixture extracted from egg yolks, is believed to be a therapeutic pharmacologic agent. AL721 interacts with membranes of various types of cells with a common mode of action. AL721 modifies cellular membrane composition and fluidity through passive extraction and/or exchange of cholesterol. Physiologically diminished cell function due to rigidification of its membrane is reversible both in vitro and in vivo by AL721. Fluidization of aged membranes with AL721 has been shown to restore brain serotonin receptor function both in vitro and in vivo. AL721 can also successfully restore deficient immune responsiveness of lymphocytes to mitogen stimulation in aged subjects. Drug tolerance to morphine and ethanol develops upon elevation of the viscosity of neuronal cell membranes in order to counteract the fluidization effect of the drug. Treatment of rigidified cellular membranes with AL721 in vivo can markedly reduce withdrawal symptoms. The virucidal effect of AL721 on the human immunodeficiency virus is believed to operate by lowering of viral membrane cholesterol thus interfering with the binding of the viral antigen to the host cell. Non-toxicity of AL721 is clearly demonstrated in animal and human safety studies.

摘要

AL721是一种从蛋黄中提取的新型脂质混合物,被认为是一种治疗性药物制剂。AL721以一种共同的作用方式与各种类型细胞的膜相互作用。AL721通过被动提取和/或交换胆固醇来改变细胞膜的组成和流动性。由于细胞膜僵化导致的生理性功能减退,在体外和体内均可被AL721逆转。已证明,在体外和体内,用AL721使老化的细胞膜流化可恢复脑血清素受体功能。AL721还能成功恢复老年受试者淋巴细胞对有丝分裂原刺激的免疫反应缺陷。为了抵消药物的流化作用,当神经元细胞膜粘度升高时会产生对吗啡和乙醇的药物耐受性。在体内用AL721处理僵化的细胞膜可显著减轻戒断症状。据信,AL721对人类免疫缺陷病毒的杀病毒作用是通过降低病毒膜胆固醇从而干扰病毒抗原与宿主细胞的结合来实现的。动物和人体安全性研究清楚地证明了AL721的无毒性。

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