新型混合脂质体的制备及其与药物的分子识别研究

设计、合成了含核酸碱基的双亲化合物N6-十四酰基-9-辛基腺嘌呤三甲基溴化铵;用目标化合物和卵磷脂制备混合脂质体受体。分别研究了受体与巴比妥酸、核黄素药物在混合脂质体亲脂区通过互补氢键进行的分子识别。紫外可见光谱研究表明,底物巴比妥酸在258nm的吸收峰,核黄素在222nm,264nm的吸收峰随时间的延长而逐渐降低,这种减色作用归因于脂质体内的巴比妥酸和核黄素在亲脂区分别与双亲化合物上的腺嘌呤形成了氢键。

Preparation of Novel Phosphatidylcholine/Cationic Amphiphilic Coliposomes and Molecular Recognition between the Amphiphile and Drug Substrates in Coliposomes

A novel amphiphile, N6 myristoyl9octanyl adenine trimethylammonium bromide (4), was synthesized as receptor for molecular recognition. The coliposomes were prepared from phosphatidylcholine (PC) and N6 myristoyl9octanyl adenine trimethylammonium bromide by sonication of CHCl3 cast films of amphiphile mixtures (molar ratio: PC:4 =10:1) in doubly distilled water with a bathtype sonicator at 80 W for 3 h. As barbituric acid and riboflavin was respectively added into PC/4 coliposomal solution, the absorbivity of barbituric acid at 258 nm, and riboflavin at 222 nm and 264 nm decreased slowly with time. The onset of a hypochromic effect can be ascribed to adeninebarbituric acid or riboflavin interaction. The absorption band levels off at about 63.8% for barbituric acid and 91% for riboflavin of its initial value and stabilizes after several weeks.