In vitro analysis of albendazole sulfoxide enantiomers shows that (+)-®-albendazole sulfoxide is the active enantiomer against Taenia solium
Antimicrobial agents and chemotherapy | 12 Dec 2012
A Paredes, T de Campos Lourenço, M Marzal, A Rivera, P Dorny, S Mahanty, C Guerra-Giraldez, HH García, TE Nash and QB Cass
Albendazole is an anthelmintic drug widely used in the treatment of neurocysticercosis (NCC), an infection of the brain with Taenia solium cysts. However, drug levels of its active metabolite, albendazole sulfoxide (ABZSO), are erratic, likely resulting in decreased efficacy and suboptimal cure rates in NCC. Racemic albendazole sulfoxide is composed of (ABZSO (+)-®- and (-)-(S)- enantiomers that have been shown to differ in pharmacokinetics and activity against other helminths. The antiparasitic activities of racemic ABZSO and its (+)-®- and (-)-(S)- enantiomers were evaluated in vitro against T. solium cysts. Parasites were collected from naturally infected pigs, cultured and exposed to the racemic mixture or to each enantiomer (range 10 to 500 ng/ml) or to praziquantel as a reference drug. The activity of each compound on cysts was assayed by measuring ability to evaginate and inhibition of alkaline phosphatase (AP) and parasite antigen release. (+)-®-ABZSO was significantly more active than (-)-(S)-ABZSO in suppressing the release of AP and antigen into the supernatant in a dose- and time- dependent manner, indicating that most of the activity of ABZSO resides in the (+)-®-enantiomer. Use of this enantiomer alone may lead increased efficacy and/or less toxicity compared to albendazole.
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