Goijman S G, Stoppani A O
Biochem Pharmacol. 1985 Apr 15;34(8):1331-6. doi: 10.1016/0006-2952(85)90514-3.
Nifurtimox and benznidazole, two nitroheterocyclic drugs, inhibited DNA, RNA and protein synthesis, stimulated macromolecular degradation, and stimulated unscheduled DNA synthesis in Trypanosoma cruzi (Tulahuen strain). Significant differences in the mode of action of these drugs could be established and, in every case, nifurtimox was more active than benznidazole. The inhibition of macromolecular synthesis varied with drug concentration, precursor and incubation time. Nifurtimox effect was time dependent and irreversible. When assayed on macromolecular degradation, nifurtimox was more effective on DNA and protein than on RNA, while benznidazole displayed almost the same activity on DNA, RNA and protein. Labeling of RNA with [3H]uridine in the presence of nifurtimox followed atypical kinetics since, depending on incubation time and concentration, RNA degradation prevailed over RNA synthesis.
硝呋替莫和苯硝唑这两种硝基杂环药物，抑制了克氏锥虫（图拉亨株）的DNA、RNA和蛋白质合成，刺激了大分子降解，并刺激了其非预定DNA合成。可以确定这两种药物作用方式存在显著差异，而且在每种情况下，硝呋替莫都比苯硝唑更具活性。大分子合成的抑制作用随药物浓度、前体和孵育时间而变化。硝呋替莫的作用具有时间依赖性且不可逆。在检测大分子降解时，硝呋替莫对DNA和蛋白质的作用比对RNA更有效，而苯硝唑对DNA、RNA和蛋白质的活性几乎相同。在硝呋替莫存在的情况下用[3H]尿苷标记RNA呈现非典型动力学，因为根据孵育时间和浓度的不同，RNA降解超过了RNA合成。
