CAJ | 학술논문

研究了七元瓜环(Q[7])与抗癌药物阿糖胞苷(Ara-C)的不同质子化存在形式之间的超分子相互作用，探讨了超分子包合作用对药物电离平衡常数及药物稳定性的影响.结果表明， Q[7]使得 Ara-C 的 pKa降低了约0.3个单位， Q[7]与 Ara-C 的2种存在形式(Ara-C+及 Ara-C)均可形成1：1的主客体包结配合物， Ara-C 以其嘧啶环进入 Q[7]空腔，而核糖环位于瓜环端口发生相互作用； Q[7]与 Ara-C 作用后对药物起到保护性载体的作用，从而提高了药物的稳定性.
연구료칠원과배(Q[7])여항암약물아당포감(Ara-C)적불동질자화존재형식지간적초분자상호작용，탐토료초분자포합작용대약물전리평형상수급약물은정성적영향.결과표명， Q[7]사득 Ara-C 적 pKa강저료약0.3개단위， Q[7]여 Ara-C 적2충존재형식(Ara-C+급 Ara-C)균가형성1：1적주객체포결배합물， Ara-C 이기밀정배진입 Q[7]공강，이핵당배위우과배단구발생상호작용； Q[7]여 Ara-C 작용후대약물기도보호성재체적작용，종이제고료약물적은정성.
The interaction of cucurbit[7]uril(Q[7]) with cytarabine(Ara-C) in different proton forms were studied by ultraviolet absorption spectroscopy and 1 H NMR technique in details. Complexation by Q[7] has also been investigated to cause pKa shifts and stability of drug. The results showed that Q[7] encapsulated the Ara-C and shifted its pKa value by down to 0. 3 units. Ara-C in different proton forms with Q[7] informed 1 : 1 inclusion complexes, and the formation constants were (9. 48±0. 29)×103 L/ mol and (6. 30±0. 04)×103 L/ mol for the Q[7]-Ara-C+ system and Q[7]-Ara-C system, respectively. Moreover, The formation of inclu-sion complexes between Q[7] with Ara-C was confirmed by 1 H NMR, the pyrimidine moiety of Ara-C were entrapped in the cavity of the host and the D-ribose ring was likely located at the outside cucurbituril cavity. In addition, stability studies were investigated by initial uniform rate experiment. The results revealed that complexation of Ara-C with Q[7] offers a major improvement in drug stability.