Ostos Francisco J, Lebrón José A, Moyá Maria L, López-López Manuel, Sánchez Antonio, Clavero Amparo, García-Calderón Clara B, Rosado Iván V, López-Cornejo Pilar
Departamento de Química Física, Facultad de Química, Universidad de Sevilla, c/ Prof. García González n° 1, Seville, 41012, Spain.
Departamento de Ingeniería Química, Química FísicayCiencias de los Materiales, Facultad de Ciencias Experimentales, Universidad de Huelva, Campus 'El Carmen", E-21071, Huelva, Spain.
Chem Asian J. 2017 Mar 16;12(6):679-689. doi: 10.1002/asia.201601713. Epub 2017 Feb 28.
Given the high toxicity of the anthracycline antibiotic doxorubicin (DOX), it is relevant to search for nanocarriers that decrease the side effects of the drug and are able to transport it towards a therapeutic target Here, the encapsulation of DOX by p-sulfocalix[6]arene (calix) has been studied. The interaction of DOX with the macrocycle, as well as with DNA, has been investigated and the equilibrium constant for each binding process estimated. The results showed that the binding constant of DOX to DNA, K , is three orders of magnitude higher than that to calix, K . The ability of calixarenes to encapsulate DOX molecules, as well as the capability of the DOX molecules included into the inner cavity of the macrocycle to bind with DNA have been examined. Cytotoxicity measurements were done in different cancer and normal cell lines to probe the decrease in the toxicity of the encapsulated DOX. The low toxicity of calixarenes has also been demonstrated for different cell lines.
鉴于蒽环类抗生素阿霉素（DOX）具有高毒性，寻找能降低该药物副作用并能将其转运至治疗靶点的纳米载体具有重要意义。在此，研究了对磺基杯[6]芳烃（杯芳烃）对DOX的包封作用。研究了DOX与大环以及与DNA的相互作用，并估算了每个结合过程的平衡常数。结果表明，DOX与DNA的结合常数K比与杯芳烃的结合常数K高三个数量级。研究了杯芳烃包封DOX分子的能力，以及包含在大环内腔中的DOX分子与DNA结合的能力。在不同的癌细胞系和正常细胞系中进行了细胞毒性测量，以探究包封DOX后毒性的降低情况。杯芳烃对不同细胞系也显示出低毒性。
