Dipartimento di Scienze Chimiche, Università degli Studi di Napoli Federico II, Complesso Universitario di Monte S. Angelo, via Cintia, 80126 Naples, Italy.
Biomaterials. 2012 May;33(14):3770-82. doi: 10.1016/j.biomaterials.2012.01.057. Epub 2012 Feb 21.
A new organometallic ruthenium complex, named AziRu, along with three amphiphilic nucleoside-based ruthenium complexes, ToThyRu, HoThyRu and DoHuRu, incorporating AziRu in their skeleton, have been synthesized, stabilized in POPC phospholipid formulations and studied for their antineoplastic activity. Self-aggregation behavior of these complexes was investigated, showing that the three synthesized AziRu derivatives able to form liposomes and, under specific conditions, elongated micelles. The formulations prepared in POPC proved to be stable for months and showed high in vitro antiproliferative activity. The here described results open new scenarios in the design of innovative transition metal-based supramolecular systems for anticancer drugs vectorization.
一种新的有机金属钌配合物,命名为 AziRu,以及三种两亲性核苷基钌配合物,ToThyRu、HoThyRu 和 DoHuRu,它们的骨架中都含有 AziRu,已被合成、稳定在 POPC 磷脂制剂中,并研究了它们的抗肿瘤活性。这些配合物的自聚集行为已被研究,表明三种合成的 AziRu 衍生物能够形成脂质体,并在特定条件下形成伸长的胶束。在 POPC 中制备的制剂能够稳定数月,并显示出高的体外抗增殖活性。这里描述的结果为设计用于癌症药物载体化的创新过渡金属基超分子系统开辟了新的前景。