Mayer R D, Lee K E, Cockett A T
Department of Urology, University of Rochester School of Medicine, New York 14642.
Cancer Chemother Pharmacol. 1987;20(3):207-10. doi: 10.1007/BF00570486.
DL-Buthionine-(S,R)-sulfoximine (BSO), a glutathione-depleting agent, was found to diminish the nephrotoxic effect of cisplatin (cis-diamminedichloroplatinum). Pretreatment of rats with BSO (4 mmol/kg s.c.) 2 h prior to cisplatin, either as a single dose of 5 mg/kg or at a daily dose of 2.5 mg/kg for 3 consecutive days, resulted in diminished elevations of plasma BUN concentration and decreased cisplatin-induced inhibition of renal gamma-glutamylcysteine synthetase and gamma-glutamyl transpeptidase activity measured 6 days following treatment. Administration of BSO prior to cisplatin at 7.5 mg/kg did not significantly alter the effect of cisplatin on either BUN concentration or enzyme activity. The influence of BSO pretreatment on the antitumor activity of cisplatin was studied using implantation of a murine bladder cancer (MBT-2) in C3H mice. Pretreatment of mice with BSO (5 mmol/kg) did not influence cisplatin antitumor efficacy.
DL-丁硫氨酸-(S,R)-亚砜亚胺（BSO）是一种可消耗谷胱甘肽的药物，已发现它能减轻顺铂（顺二氨二氯铂）的肾毒性作用。在给大鼠注射顺铂前2小时，以4 mmol/kg的剂量皮下注射BSO，顺铂剂量为单次5 mg/kg或连续3天每日剂量为2.5 mg/kg，结果显示血浆尿素氮（BUN）浓度升高幅度减小，且在治疗6天后，顺铂诱导的肾γ-谷氨酰半胱氨酸合成酶和γ-谷氨酰转肽酶活性抑制作用减弱。在顺铂前以7.5 mg/kg的剂量给予BSO，对顺铂对BUN浓度或酶活性的影响没有显著改变。使用C3H小鼠植入鼠膀胱癌（MBT-2）模型研究了BSO预处理对顺铂抗肿瘤活性的影响。用BSO（5 mmol/kg）预处理小鼠不影响顺铂的抗肿瘤疗效。
