Synthesis of PEGylated fullerene-5-fluorouracil conjugates to enhance the antitumor effect of 5-fluorouracil.
Many drugs have been delivered by different types of nanoscale vehicles to enhance their therapeutic efficacy. 5-Fluorouracil (5FU) is a widely used antitumor drug, however its bioavailability still needs to be improved. Herein we synthesized a polyethylene glycol monomethylether-C(60)-5FU conjugate (mPEG-C(60)-5FU) and evaluated its antitumor efficacy in vitro. The results show that the inhibition abilities of mPEG-C(60)-5FU to the human breast cancer cell line MCF-7 and the human gastric carcinoma cell line BGC-823 are significantly higher than that of 5FU. The conjugate has good stability in murine serum for at least 24 h. Moreover, the PEGylated fullerene (mPEG-C(60)) vehicle is non-toxic to MCF-7 cells. These results demonstrate that mPEG-C(60) is an efficient vehicle for the delivery of 5FU.
Beijing National Laboratory for Molecular Science, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing, China.
Zengpei
Z
Dou
Yingying
Y
Xu
Hongfang
H
Sun
Yuanfang
Y
Liu
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D005472:Fluorouracil / Q000737:chemistry*; D037741:Fullerenes / Q000737:chemistry*; D006801:Humans; D049329:Nanostructures / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry*
D000970:Antineoplastic Agents; D004337:Drug Carriers; D037741:Fullerenes; D011092:Polyethylene Glycols; D005472:Fluorouracil