Fujii Y, Kojima E, Ohtani I, Mukai R, Murakami K, Yoshikawa Y
National Institute of Infectious Disease, Haciman-tai, Japan.
Nucleic Acids Symp Ser. 1997(37):173-4.
By using tissue and blood from mice and mice themselves, biological behavior of 6-chloro-2',3'-dideoxyguanosine (6-Cl-ddG) and 6-chloro-2',3'-dideoxyinosine (6-Cl-ddI) was examined in vitro and in vivo. Both compounds resemble each other in chemical structure. They are converted to ddG and ddI, respectively, by adenosine deaminase in the cells, and express their anti-HIV activity in vitro. According to our recent data about their biological behaviour in vivo; however, it was revealed that they are fairly different especially as the agent working in the brain. After injection of each drug into the body of mice, ddG, or metabolite of 6-Cl-ddG, was observed in the brain, while ddI was not found there.
利用小鼠的组织和血液以及小鼠本身,在体外和体内研究了6-氯-2',3'-二脱氧鸟苷(6-Cl-ddG)和6-氯-2',3'-二脱氧肌苷(6-Cl-ddI)的生物学行为。这两种化合物在化学结构上彼此相似。它们在细胞中分别被腺苷脱氨酶转化为ddG和ddI,并在体外表现出抗HIV活性。然而,根据我们最近关于它们在体内生物学行为的数据,发现它们有相当大的差异,特别是作为在大脑中起作用的药物。将每种药物注射到小鼠体内后,在大脑中观察到了ddG或6-Cl-ddG的代谢产物,而在那里没有发现ddI。