Article ID Journal Published Year Pages File Type
2083721 European Journal of Pharmaceutics and Biopharmaceutics 2013 9 Pages PDF
Abstract

In this paper, we examined arsthinol–cyclodextrin complexes, which display an anticancer activity. The association constants were 17,502 ± 522 M−1 for hydroxypropyl-β-cyclodextrin and 12,038 ± 10,168 M−1 for randomized methylated β-cyclodextrin. 1H NMR experiments in solution also confirmed the formation of these complexes and demonstrated an insertion of the arsthinol (STB) with its dithiarsolane extremity into the wide rim of the hydroxypropyl-β-cyclodextrin cavity. Complexed arsthinol was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, we observed significant antitumor activity against heterotopic xenografts after i.p. administration and did not see any signs of toxicity. This remains to be verified using an orthotopic model.

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