Albendazole is an anthelmintic drug widely used in the treatment of neurocysticercosis (NCC), an infection of the brain with Taenia N eurocysticercosis (NCC) is a major cause of adult-onset seizures and epilepsy in many areas of the developing world. It is an infection with the larval cyst form of the cestode tapeworm Taenia solium acquired through the accidental ingestion of ova shed in the feces of human tapeworm carriers. The released oncospheres find their way to the bloodstream and are carried throughout the body but develop mostly in the muscles, subcutaneous tissues, and brain. Almost all the symptoms are due to brain involvement (1).Two drugs, the benzimidazole albendazole (ABZ) and the pyrazinoisoquinoline praziquantel (PZQ), are commonly used to treat neurocysticercosis, usually with accompanying immunosuppressive/anti-inflammatory medication (2-4). Albendazole is frequently preferred to praziquantel because it is more widely available, has a lower cost, and normally requires shorter courses of treatment (and hence represents lower hospitalization-associated expenses) for higher efficacy (2, 5-7).In susceptible parasites, the main effect of ABZ is the inhibition of tubulin polymerization into microtubules, but the drug also causes biochemical changes such as inhibition of mitochondrial fumarate reductase, reduced glucose transport, and uncoupling of oxidative phosphorylation, impairing ATP generation (8, 9). Although ABZ has been used since the 1970s (10, 11), it is not completely effective in killing cysts; 12% and 45% of total cysts remain after the usual dosing regimens used with albendazole and praziquantel, respectively (12). Cure rates are unacceptably low for both drugs at about 40% to 50%, so retreatments are often required.After oral administration, the nonchiral ABZ is oxidized in the liver to its active metabolite, albendazole sulfoxide (ABZSO), with one chiral center in the sulfoxide group. The two possible enan- (13), show different pharmacokinetics and affinities for cytosolic proteins from different parasites (28). Kinetic parameters of (ϩ)-(R)-and (Ϫ)-(S)-ABZSO enantiomers in NCC patients treated with ABZ differ in renal excretion (14), accumulation in plasma (15), and, most importantly, distribution in the cerebrospinal fluid (12). Even though the levels of effectiveness of the two enantiomers against a number of other helminths differ, the effect of the isolated enantiomers against T. solium metacestodes (cysts) has not been reported. tiomers, (ϩ)-(R)-and (Ϫ)-(S)-ABZSOA sensitive in vitro system to quantify drug effects on cysts of T. solium has been recently reported (16). In this system, drug sensitivity to both ABZSO and PZQ correlates with the degree of inhibition of alkaline phosphatase (AP) release from cysts, obtained from naturally infected pigs and cultured in vitro (16). Using this system, we compared the anthelmintic effect of the (ϩ)-(R)-and (Ϫ)-(S)-ABZSO enantiomers to effects of the ABZSO racemic mixture and of PZQ. Here we show that the antiparasitic effect of the drug ...
Polysaccharide-based chiral stationary phases (CSP) demonstrate great versatility and higher chiral selectivity for a variety of chiral compounds in multimodal elution modes (normal, reverse and polar organic). The main role of CSP phenyl carbamate based derivatives as chiral selectors is the formation of diastereoisomeric complexes by means of π-π interaction, dipole-dipole, hydrogen bonding and/or inclusion complex mechanisms. Nevertheless, the mechanism behind their enantioselectivity requires clarification. High resolution magic angle spinning nuclear magnetic resonance spectroscopy ((1)H HR/MAS NMR) has provided key information on the recognition process at the binding sites of the CSP surface. Herein we report the results obtained using omeprazole as a probe for these investigations.
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