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.

Succinimido–Ferrocidiphenol Complexed with Cyclodextrins Inhibits Glioblastoma Tumor Growth In Vitro and In Vivo without Noticeable Adverse Toxicity

“…Finally, cyclodextrins should not be considered as simple solubility enhancers, since the formation of the inclusion complex might also affect the bioavailability of the tissue distribution of drugs, and thereby therapeutic response [ 23 , 24 ].…”

Interaction of Arsenous Acid with the Dithiol-Type Chelator British Anti-Lewisite (BAL): Structure and Stability of Species Formed in an Unexpectedly Complex System

“…Nevertheless, the lipophilic character of BAL probably goes together with its high ability to remove arsenicals from both the extracellular space and cells across the membrane barriers. Applying BAL can still be advantageous for the treatments of organoarsenical poisoning or in cases when the intervention time is critical. , Recently, the anticancer effects of some organoarsenic dithiol complexes were described, including the BAL-containing classical antimicrobial chemotherapeutic agent melarsoprol and arsthinol. , In addition, the dithiol complexes of arylarsenicals containing 72 As or 77 As isotopes proved to be potential positron emission tomographic imaging and radiotherapeutic agent candidates, respectively . These could perhaps start a new chapter in the therapeutic applications of BAL in the future.…”

Phthalimido–ferrocidiphenol cyclodextrin complexes: Characterization and anticancer activity

“…Currently, CD complexes represent one of the most promising and most investigated delivery systems for various lipophilic drugs (Madan et al, 2014;Rodgers et al, 2011), including cancer therapy (Becherirat et al, 2013;Xiong et al, 2014). They are bucket-shaped, cyclic oligosaccharides, comprising 6, 7, or 8 glucopyranose units, linked by α, 1-4-glycosidic bonds (El-Maradny et al, 2008).…”