[EN] NOVEL CATIONIC AMPHIPHILES WITH MANNOSE-MIMICKING HEAD-GROUPS AND A PROCESS FOR THE PREPARATION THEREOF<br/>[FR] NOUVEAUX AMPHIPHILES CATIONIQUES À TÊTES POLAIRES IMITANT LA MANNOSE, ET LEURS MÉTHODES DE PRÉPARATION
申请人:COUNCIL SCIENT IND RES
公开号:WO2012035557A1
公开(公告)日:2012-03-22
The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization.
本发明公开了包含类似于甘露糖的樟脑酸和奎尼酸头基的新型阳离子两性分子,以及一种制备具有类似于甘露糖极性头基的阳离子两性分子(如樟脑酸和奎尼酸)的方法。本文描述的研究结果还表明,本发明的化合物可以通过APC(抗原呈递细胞)如巨噬细胞和树突状细胞表面上表达的甘露糖受体,将模型DNA疫苗定位到目标细胞。与其甘露基对照相比,本文披露的阳离子两性分子在小鼠基因免疫中表现出更强的细胞和体液免疫应答。本发明中描述的具有类似于甘露糖的奎尼酸和樟脑酸头基的阳离子两性分子可能在基因免疫领域找到未来的应用。