title: The antitumor effects of an arsthinol-cyclodextrin complex in a heterotopic mouse model of glioma.
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. (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-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.
authors.affiliation: EA 3452, CITHEFOR, Université de Lorraine, Nancy, France.
authors.forename: Selma
authors.initials: S
authors.lastname: Becherirat
authors.forename: Marie-Claire
authors.initials: MC
authors.lastname: Lanhers
authors.forename: Marie
authors.initials: M
authors.lastname: Socha
authors.forename: Mehdi
authors.initials: M
authors.lastname: Yemloul
authors.forename: Alain
authors.initials: A
authors.lastname: Astier
authors.forename: Caroline
authors.initials: C
authors.lastname: Loboda
authors.forename: Natália
authors.initials: N
authors.lastname: Aniceto
authors.forename: Stéphane
authors.initials: S
authors.lastname: Gibaud
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D000077237:Arsenic Trioxide; D001152:Arsenicals / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D005079:Excipients / Q000737:chemistry; D005260:Female; D005910:Glioma / Q000188:drug therapy* / Q000473:pathology; D006801:Humans; D007274:Injections, Intraperitoneal; D009682:Magnetic Resonance Spectroscopy; D008549:Melarsoprol / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008819:Mice, Nude; D010087:Oxides / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D001152:Arsenicals; D005079:Excipients; D010087:Oxides; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C031215:betadex; C546471:arsthinol; D000077237:Arsenic Trioxide; D008549:Melarsoprol
keywords: Arsenic; Brain tumors; Cancer; Cyclodextrin; Glioblastoma; Glioma