Agbe A, Yielding K L
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston 77555-1031, USA.
J Parasitol. 1995 Dec;81(6):968-73.
Trypanosoma brucei E164 and a dyskinetoplastic derivative, Dysk164, were injected into mice that were treated subsequently with methylglyoxal-bis-guanylhydrazone, berenil, ethidium bromide, and acriflavine. Additionally, parasites were photoaffinity labeled with ethidium monoazide to effect covalent drug attachment prior to injection into animals. In all cases, killing of animals with E164 was blocked by the drug treatment, whereas killing due to Dysk164 was not. These findings are consistent with the view that the intact kinetoplast plays an essential role in the action of these drugs.
将布氏锥虫E164及其动质体发育不全的衍生物Dysk164注射到小鼠体内,随后用甲基乙二醛双脒腙、贝尼尔、溴化乙锭和吖啶黄对小鼠进行治疗。此外,在将寄生虫注射到动物体内之前,先用单叠氮乙锭对其进行光亲和标记,以实现药物的共价附着。在所有情况下,药物治疗均能阻止E164对动物的致死作用,而Dysk164导致的致死作用则不受影响。这些发现与完整动质体在这些药物作用中起重要作用的观点一致。