Vasudevachari M B, Antony A
Antiviral Res. 1982 Oct;2(5):291-300. doi: 10.1016/0166-3542(82)90052-3.
The cupric and ferric complexes of isonicotinic acid hydrazide (INH) inhibit the DNA synthesis catalysed by avian myeloblastosis virus (AMV) reverse transcriptase. The inhibition was to the extent of 95% by 50 microM of cupric-INH complex and 55% by 100 microM of ferric-INH complex. These complexes have been found to bind preferentially to the enzyme than to the template-primer. Kinetic analysis showed that the cupric-INH complex is a non-competitive inhibitor with respect to dTTP. The time course of inhibition has revealed that the complexes are inhibitory even after the initiation of polynucleotide synthesis. In vivo toxicity studies in 1-day-old chicks have shown that the complexes are not toxic up to a concentration of 500 microgram per chick. Infection of the 1-day-old chicks with AMV pretreated with 150 microgram of either of the complexes prevented symptoms of leukemia due to virus inactivation.
异烟肼（INH）的铜络合物和铁络合物可抑制禽成髓细胞瘤病毒（AMV）逆转录酶催化的DNA合成。50微摩尔的铜-INH络合物可产生95%的抑制率，100微摩尔的铁-INH络合物可产生55%的抑制率。已发现这些络合物与酶的结合优先于与模板引物的结合。动力学分析表明，铜-INH络合物对dTTP而言是一种非竞争性抑制剂。抑制的时间进程表明，即使在多核苷酸合成开始后，这些络合物仍具有抑制作用。对1日龄雏鸡进行的体内毒性研究表明，浓度高达每只雏鸡500微克时，这些络合物无毒。用150微克任何一种络合物预处理AMV后感染1日龄雏鸡，可因病毒失活而预防白血病症状。
