INFLUENCE OF LOCAL AND NEUTRAL ANESTHETICS ON THE POLYMORPHIC PHASE PREFERENCES OF EGG-YOLK PHOSPHATIDYLETHANOLAMINE
INFLUENCE OF LOCAL AND NEUTRAL ANESTHETICS ON THE POLYMORPHIC PHASE PREFERENCES OF EGG-YOLK PHOSPHATIDYLETHANOLAMINE
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DOI：
10.1016/0005-2736(81)90256-x
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发表时间：
1981-01-01
期刊：
影响因子：
--
通讯作者：
CULLIS, PR
中科院分区：
文献类型：
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作者：
HORNBY, AP;CULLIS, PR
在正常醇和不同链长的烷烃以及带电胺麻醉剂的存在下，研究了卵磷脂酰乙醇胺的多态相偏好。带电荷的麻醉剂、乙醇和丁醇可以稳定鸡蛋磷脂酰乙醇胺的双层结构。相比之下，较长的链(C . gtoq。6)正常醇和烷烃诱导六方（HII）相。局部麻醉剂（氯丙嗪、二布卡因、丁卡因和普鲁卡因）在体外的相对效力反映在它们稳定水合鸡蛋磷脂酰乙醇胺双层结构的相对能力上。影响磷脂多态性所需的麻醉水浓度对脂质组成敏感。例如，在卵磷脂酰乙醇胺分散体中加入20摩尔%的卵磷脂酰丝氨酸，可以将诱导明显的双分子层稳定效应所需的二布卡因水溶液浓度从5.0-0.5 mM降低。显然，两亲性分子（如麻醉剂）影响卵磷脂酰乙醇胺多态性的能力源于它们的分子形状。麻醉分子利用这种形状特性发挥作用的可能性提高了。
The polymorphic phase preferences of egg phosphatidylethanolamine were examined in the presence of normal alcohols and alkanes of varying chain length, as well as charged amine anesthetics. The charged anesthetics, ethanol and butanol can stabilize a bilayer arrangement for egg phosphatidylethanolamine. In contrast, longer chain (C .gtoreq. 6) normal alcohols and alkanes induce the hexagonal (HII) phase. The relative potency of local anesthetics in vitro (chlorpromazine, dibucaine, tetracaine and procaine) is mirrored by their relative ability to stabilize bilayer structure for hydrated egg phosphatidylethanolamine. The aqueous concentrations of anesthetic required to affect phospholipid polymorphism is sensitive to the lipid composition. For example, the inclusion of 20 mol% egg phosphatidylserine in egg phosphatidylethanolamine dispersions can reduce the aqueous concentrations of dibucaine required to induce appreciable bilayer stabilization effects from 5.0-0.5 mM. Apparently, the ability of amphipathic molecules such as anesthetics to influence phosphatidylethanolamine polymorphism arises from their molecular shape. The possibility that anesthetic molecules may exert their effects by virtue of this shape property is raised.