Disease relevance of Arprinocide

• Efficacy of arprinocid against coccidiosis of broilers in battery and floor-pen trials [1].
• Arprinocid prevented mortality, increased weight gains, and reduced or eliminated intestinal lesions and oocyst production [2].
• Chemotherapeutic effect of arprinocid in experimental cryptosporidiosis [3].

High impact information on Arprinocide

• Thirty p.p.m. arprinocid reduced sporulation of the oocysts of E. brunetti and caused enlargement of the perinuclear space in the late merozoites and swelling of the endoplasmic reticulum around wall-forming bodies II [4].
• When arprinocid was tested against Eimeria tenella in cultures of chick kidney epithelial cells, which do not metabolize the drug appreciably, it was found to block the development of the parasite with an ID50 of 20 ppm [5].
• Arprinocid was active in chick liver cell systems but totally inactive in chick kidney cell systems, although its N-oxide was active in both cell types [6].
• The anticoccidial drug arprinocid and arprinocid-N-oxide, a metabolite produced in vivo, blocked the growth of Toxoplasma gondii in human fibroblasts [7].
• Genetic recombination of markers for precocious development, arprinocid resistance, and isoenzymes of glucose phosphate isomerase in Eimeria acervulina [8].

Biological context of Arprinocide

• These results suggest that halofuginone is active over a broader part of the life cycle than arprinocid, but both drugs had a predominantly coccidiocidal action [9].
• A mating was made between two populations of Eimeria tenella possessing the complementary traits of normal development (virulence) + resistance to the anticoccidial drug arprinocid or precocious development (attenuation) + drug-sensitivity [10].

Anatomical context of Arprinocide

• Neither arprinocid nor its liver microsomal metabolite arprinocid-1-N-oxide binds to calf thymus DNA [11].

Associations of Arprinocide with other chemical compounds

• Medication of broilers with arprinocid [MK-302, 9-(2-chloro-6-fluorbenzyl adenine)] had 3 distinct effects on oocysts; (1) the number of oocysts produced was decreased, (2) fewer of the oocysts sporulated, and (3) those oocysts which did sporulate were less infective than those from unmedicated birds [12].
• Effects of the anthelmintics clorsulon, rafoxanide, mebendazole and arprinocid on Echinostoma caproni in ICR mice [13].
• The stability of experimentally induced resistance to halofuginone, decoquinate or arprinocid in lines of Eimeria tenella, was examined after 10 passages in unmedicated chickens [14].

Analytical, diagnostic and therapeutic context of Arprinocide

• Drug-ranging experiments indicated that arprinocid was effective at 50 and 25 mg/kg/d, but not at 12.5 mg/kg/d. These results suggest that further testing of arprinocid in different animal models, or in phase-I clinical trials, is warranted [15].
• An HPLC method for determining arprinocid [9-(2-chloro-6-fluorophenyl)methyl-9H-purin-6-amine] in feed was evaluated in an interlaboratory collaborative study [16].
• Resistance to arprinocid was developed in Eimeria tenella after seven serial passages in chickens given progressively greater concentrations of drug [17].

References