8-氯腺苷在大鼠体内代谢途径及其代谢产物的鉴定

Identification of the metabolites and passway of metabolism of 8 chloro adenosine in rats

对单次ｉｖ８－氯腺苷１００ｍｇ·ｋｇ－１后大鼠体内出现的两种８－氯腺苷代谢产物进行了定性鉴定．合成了８－氯肌苷及８－氯腺嘌呤的标准品．应用高效液相色谱法，光电二极管阵列检测法及高效液相色谱－质谱联用３种方法分析大鼠体内８－氯腺苷代谢物的保留时间，紫外吸收图谱，单离子流图和质谱图．结果表明８－氯腺苷在大鼠体内通过水解和脱氨两种代谢途径生成８－氯腺嘌呤和８－氯肌苷两种主要代谢产物．

The metabolites of 8 chloro adenosine, a new drug with promising anticancer action were studied in rats. According to the chemical structure of 8 chloro adenosine and the metabolism passway of similar chemical substance of adenosine in vivo, we postulated that the two metabolites, which produced after a single iv dose in rats, might be 8 chloro adenine and 8 chloro inosine. The standard samples of 8 chloro adenine and 8 chloro inosine were synthesized. The retention time and UV spectrogram of standard samples of 8 chloro adenine and 8 chloro inosine and metabolites in rats serum were compared by HPLC method. The SIR spectrogram and mass spectrograms of 8 chloro adenine and 8 chloro inosine in rat′s serum and in standard sample were compared by HPLC MS study. The results show that the two main metabolites of 8 chloro adenosine are 8 chloro adenine and 8 chloro inosine.