The antitumor effects of an arsthinol–cyclodextrin complex in a heterotopic mouse model of gliomaReport as inadecuate




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1 CITHEFOR - Cibles thérapeutiques, formulation et expertise pré-clinique du médicament 2 SIGRETO - Signalisation, Génomique et Recherche Translationnelle en Oncologie 3 CRM2 - Cristallographie, Résonance Magnétique et Modélisations 4 Pôle Pharmacie 5 Centre Hospitalier de Neufchâteau 6 Pharmacie Clinique - Nancy

Abstract : In this paper, we examined arsthinol–cyclodextrin complexes, which display an anticancer activity. The association constants were 17,502 ± 522 M À1 for hydroxypropyl-b-cyclodextrin and 12,038 ± 10,168 M À1 for randomized methylated b-cyclodextrin. 1 H 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-b-cyclodextrin cavity. Complexed arsthinol was more effective than arsenic trioxide As 2 O 3 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.

Keywords : Glioma Cyclodextrin Glioblastoma Arsenic Brain tumors Cancer





Author: Selma Becherirat - Marie-Claire Lanhers - Marie Socha - Mehdi Yemloul - Alain Astier - Caroline Loboda - Nathalia Aniceto - Stép

Source: https://hal.archives-ouvertes.fr/



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