Cornell R C, Milstein H G, Fox R M, Stoughton R B
Arch Dermatol. 1976 Dec;112(12):1717-23.
Azaribine is an effective agent in the treatment of psoriasis. In this investigation the extent of clinical dermatologic remission appeared to correlate with the degree of metabolic block induced by 6-azauridylic acid, as quantitated by the urinary excretion of orotic acid and orotidine, and the development of anemia. Following azaribine therapy there was a coordinate rise of the specific activities of erythrocyte orotate phosphoribosyltransferase and orotidine-5'-monophosphate decarboxylase. There was no correlation between the pretreatment activity of these enzymes and the clinical response to azaribine. The anemia of azaribine therapy was mile and of a megaloblastic type. Uridine effectively corrected the azaribine-induced anemia, but led to exacerbation of the patients' psoriasis. Following uridine therapy there was a reduction in the urinary excretion of orotic acid and orotidine, presumable reflecting end-product inhibition or repression of the first steps of a repeated pyrimidine biosynthesis.
阿扎立宾是治疗银屑病的一种有效药物。在本次研究中,临床皮肤症状缓解的程度似乎与由6-氮杂乳清酸诱导的代谢阻滞程度相关,这种代谢阻滞程度通过乳清酸和乳清苷的尿排泄量以及贫血的发生情况来定量。阿扎立宾治疗后,红细胞乳清酸磷酸核糖基转移酶和乳清苷-5'-单磷酸脱羧酶的比活性协同升高。这些酶的治疗前活性与对阿扎立宾的临床反应之间没有相关性。阿扎立宾治疗引起的贫血症状较轻,属于巨幼细胞贫血类型。尿苷可有效纠正阿扎立宾诱导的贫血,但会导致患者银屑病病情加重。尿苷治疗后,乳清酸和乳清苷的尿排泄量减少,推测这反映了重复嘧啶生物合成第一步的终产物抑制或阻遏。