Johnson W D, Morrissey R L, Kapetanovic I, Crowell J A, McCormick D L
Life Sciences Group, IIT Research Institute, Chicago, IL 60616, USA.
Food Chem Toxicol. 2008 Mar;46(3):1068-78. doi: 10.1016/j.fct.2007.11.001. Epub 2007 Nov 12.
Se-methylselenocysteine (MSC) is an organoselenium compound being developed for breast cancer chemoprevention. To characterize MSC toxicity, CD rats received daily gavage doses of 0, 0.5, 1.0, or 2.0 mg/kg/day (0, 3, 6, or 12 mg/m(2)/day), and beagle dogs received daily gavage doses of 0, 0.15, 0.3, or 0.6 mg/kg/day (0, 3, 6, or 12 mg/m(2)/day) for 28 days. In rats, MSC induced dose-related hepatomegaly in both sexes; mild anemia, thrombocytopenia, and elevated liver enzymes were observed in high dose females only. Microscopic pathology included hepatocellular degeneration (high dose males, all doses in females); arrested spermatogenesis (high dose males); and atrophy of corpora lutea (middle and high dose females). In dogs, MSC induced mild anemia in middle and high dose males, and in high dose females. Toxicologically significant microscopic lesions in dogs were seen only in the liver (peliosis and vacuolar degeneration in high dose males, midzonal necrosis in males in all dose groups). Based on liver pathology seen in female rats in all dose groups, the no observed adverse effect level (NOAEL) for MSC in rats is <0.5mg/kg/day. Based on alterations in hematology parameters and liver morphology in male dogs in all dose groups, the NOAEL for MSC in dogs is <0.15 mg/kg/day.
硒甲基硒代半胱氨酸(MSC)是一种正在开发用于乳腺癌化学预防的有机硒化合物。为了表征MSC的毒性,CD大鼠每天经口灌胃给予0、0.5、1.0或2.0mg/kg/天(0、3、6或12mg/m²/天)的剂量,比格犬每天经口灌胃给予0、0.15、0.3或0.6mg/kg/天(0、3、6或12mg/m²/天)的剂量,持续28天。在大鼠中,MSC在两性中均诱导了剂量相关的肝肿大;仅在高剂量雌性大鼠中观察到轻度贫血、血小板减少和肝酶升高。微观病理学包括肝细胞变性(高剂量雄性大鼠,所有剂量雌性大鼠);精子发生停滞(高剂量雄性大鼠);以及黄体萎缩(中、高剂量雌性大鼠)。在犬中,MSC在中、高剂量雄性犬以及高剂量雌性犬中诱导了轻度贫血。在犬中,仅在肝脏中观察到具有毒理学意义的微观病变(高剂量雄性犬的血囊肿和空泡变性,所有剂量组雄性犬的中区坏死)。基于所有剂量组雌性大鼠的肝脏病理学,大鼠中MSC的未观察到不良反应水平(NOAEL)<0.5mg/kg/天。基于所有剂量组雄性犬血液学参数和肝脏形态的改变,犬中MSC的NOAEL<0.15mg/kg/天。