Albendazole Oxide

Albendazole Oxide

Effect of aminoguanidine and albendazole on inducible nitric oxide synthase (iNOS) activity in T. spiralis-infected mice muscles.[Pubmed:16201316]

Folia Histochem Cytobiol. 2005;43(3):157-9.

The aim of this study was to provide evidence for the expression of iNOS in the cells of inflammatory infiltrates around larvae in skeletal muscles of T. spiralis infected mice. The BALB/c mice (n = 8) divided into subgroups, received either aminoguanidine (AMG)--a specific iNOS inhibitor or albendazole (ALB)--an antiparasitic drug of choice in trichinellosis treatment. Control animals (n = 2 in each subgroup) were either uninfected and treated or uninfected and untreated. Frozen sections of hind leg muscles from mice sacrificed at various time intervals after infection were cut and subjected to immunohistochemistry, using monoclonal anti-iNOS antibody. The ALB-treated mice revealed stronger iNOS staining in the infiltrating cells around larvae than the infected and untreated animals. On the contrary, in the AMG-treated animals, the infiltrating cells did not show any specific iNOS reaction. These data confirm the specificity of iNOS staining in the cellular infiltrates around T. spiralis larvae and shed some light on the role of nitric oxide during ALB treatment in experimental trichinellosis.

Examination of commercially available copper oxide wire particles in combination with albendazole for control of gastrointestinal nematodes in lambs.[Pubmed:26790729]

Vet Parasitol. 2016 Jan 15;215:1-4.

Control of gastrointestinal nematodes (GIN) remains a critical issue due to the prevalence of anthelmintic resistance. The objective of the experiment was to determine the efficacy of copper oxide wire particles (COWP) from three commercial sources and a combination of COWP and albendazole to control GIN and/or Haemonchus contortus in lambs. Naturally infected Katahdin lambs in early June 2014 and 2015 were randomly assigned to receive no COWP (CON; n=9 and 12) or 2g COWP in a gel capsule as Copasure((R)) (COP; n=4 and 17; Animax Ltd.), copper oxide-wire form (AUS; n=7 in 2014 only; Pharmplex), Ultracruz (ULT; n=8 and 15; Santa Cruz Animal Health), no COWP and albendazole (CON+alb; n=10 in 2015 only; 15mg/kg BW; Valbazen((R)); Zoetis Animal Health), or COWP+alb (n=7 and 11; in 2014, lambs were administered alb on day 3). Lambs grazed grass pastures as a group and were supplemented with 227g/lamb daily of a commercial grain mix (15% crude protein) and the same amount of alfalfa pellets. Feces were collected on days 0 (day of COWP treatment), 7, and 14 for determination of fecal egg counts (FEC). Pooled (2014) or pooled treatment group feces were cultured on days 0, 7, and 14 (2015 only) to determine GIN genera. Data were analyzed using repeated measures in a mixed model, and FEC were log transformed. The predominant GIN on day 0 was H. contortus (87%) in 2014, and there was a mixed population in 2015. The mean FEC was reduced by day 7 in AUS and ULT lambs (treatmentxday, P=0.001), and all of the COWP products were similar. By day 14, the AUS FEC were lower than the CON and COP groups. When examining the combination of COWP and synthetic anthelmintic, the FEC of COWP+alb were reduced to nearly 0eggs/g (back-transformed) and lower than the other groups (treatmentxday, P=0.001). The percentage of H. contortus in cultured feces was reduced to a greater extent in the COWP than CON or CON+alb groups of lambs. In a mixed GIN population, the COWP products appeared to be similar in efficacy and using a combination of COWP+alb increased the efficacy not only against H. contortus, but all GIN genera present, offering options in the face of resistance to benzimidazoles.

Copper(II) oxide nanoparticles augment antifilarial activity of Albendazole: In vitro synergistic apoptotic impact against filarial parasite Setaria cervi.[Pubmed:26827921]

Int J Pharm. 2016 Mar 30;501(1-2):49-64.

Mass treatment of lymphatic filariasis with Albendazole (ABZ), a therapeutic benzimidazole, is fraught with serious limitations such as possible drug resistance and poor macrofilaricidal activity. Therefore, we need to develop new ABZ-based formulations to improve its antifilarial effectiveness. CuO nanoparticles were used as an adjuvant with ABZ to form ABZ-CuO nanocomposite, which was characterized by UV-vis spectroscopy, FT-IR, AFM and SEM. Antifilarial activity of nanocomposite was evaluated using relative motility assay and dye exclusion test in dark and under UV light. ROS generation, antioxidant levels, lipid peroxidation and DNA fragmentation in nanocomposite treated parasites were estimated. Biophysical techniques were employed to ascertain the mode of binding of nanocomposite to parasitic DNA. Nanocomposite increases parasite mortality as compared to ABZ in dark, and its antifilarial effect was increased further under UV light. Elevated ROS production and decline of parasitic-GST and GSH levels were observed in nanocomposite treated worms in dark, and these effects were pronounced further under UV light. Nanocomposite leads to higher DNA fragmentation as compared to ABZ alone. Further, we found that nanocomposite binds parasitic DNA in an intercalative manner where it generates ROS to induce DNA damage. Thus, oxidative stress production due to ROS generation and consequent DNA fragmentation leads to apoptosis in worms. This is the first report supporting CuO nanoparticles as a potential adjuvant with ABZ against filariasis along with enhanced antifilarial activity of nanocomposite under UV light. These findings, thus, indicate that development of ABZ-loaded nanoparticle compounds may serve as promising leads for filariasis treatment.

Albendazole is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.

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