Lu Fushen, Haque Sk Anwarul, Yang Sheng-Tao, Luo Pengju G, Gu Lingrong, Kitaygorodskiy Alex, Li Huaping, Lacher Sebastian, Sun Ya-Ping
Department of Chemistry and Laboratory for Emerging Materials and Technology, Clemson University, Clemson, South Carolina 29634-0973.
J Phys Chem C Nanomater Interfaces. 2009 Oct 15;113(41):17768. doi: 10.1021/jp906750z.
Covalent conjugates of fullerene C(60) and the highly effective anticancer drug doxorubicin (DOX) were prepared and studied. The conjugation was through the amide linkage to preserve the intrinsic properties of DOX and fullerene cage. As designed, the conjugates with hydrophilic ethylene glycol spacers exhibited much improved aqueous compatibility, with significant solubility in water-DMSO mixtures. The anti-neoplastic activities of DOX were apparently unaffected in the conjugates according to evaluations in vitro with a human breast cancer cell line.
制备并研究了富勒烯C(60)与高效抗癌药物阿霉素（DOX）的共价缀合物。通过酰胺键进行缀合以保留DOX和富勒烯笼的固有性质。如设计的那样，带有亲水性乙二醇间隔基的缀合物表现出大大改善的水相相容性，在水 - 二甲基亚砜混合物中有显著的溶解度。根据用人乳腺癌细胞系进行的体外评估，DOX的抗肿瘤活性在缀合物中显然未受影响。
