4.6 Article

Novel molecular drug carrier: encapsulation of oxaliplatin in cucurbit[7]uril and its effects on stability and reactivity of the drug

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ORGANIC & BIOMOLECULAR CHEMISTRY
卷 3, 期 11, 页码 2122-2125

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ROYAL SOC CHEMISTRY
DOI: 10.1039/b504487a

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Oxaliplatin forms a stable 1 : 1 inclusion complex with cucurbit[7] uril as indicated by NMR, mass spectrometry, isothermal titration calorimetry and X-ray crystallography. The encapsulation of the drug results in a large enhancement in stability, a moderate decrease in reactivity toward guanosine but a much larger decrease in reactivity toward L-methionine, which suggests the encapsulation not only increases the stability of the drug but also may reduce unwanted side effects caused by protein binding of the platinum drug. A preliminary in vitro assay using various tumor cell lines reveals that the encapsulation results in a decrease in the antitumor activity of oxaliplatin.

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