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Prednimustine(泼尼氮芥,PM)是一新型的抗肿瘤药,1969年首次合成。实验证实PM具有较强的抗肿瘤活性,毒性作用并不严重。近年已应用于乳腺癌治疗,本文作简单综述。PM体内外抗肿瘤活性M是苯丁酸氮芥(Chlorambucil)的强的松龙酯(表1)。其分子量为647。由于肿瘤组织内含有大量的糖皮质激素受体,故PM较苯丁酸氮芥更易与肿瘤组织结合而发挥其抗肿瘤作用。在口服PM后,动物或人体血浆中并无完整的PM可检出,表明其被机体吸收后即快速分解。研究表明,PM的苯丁酸氮芥部分在体内的排泄要较强的松龙部分更慢更少。1984年,Gunnarsson等实验结果发现,PM经酰基转移酶的转酞基
Prednimustine (PM) is a novel antitumor drug that was first synthesized in 1969. The experiment confirmed that PM has strong anti-tumor activity and the toxic effect is not serious. In recent years, it has been applied to the treatment of breast cancer. This article gives a brief review. The anti-tumor activity M of PM in vitro and in vivo was prednisolone of Chlorambucil (Table 1). Its molecular weight is 647. Because the tumor tissue contains a large number of glucocorticoid receptors, PM is more easily combined with tumor tissue than the chlorambucil to exert its anti-tumor effect. After oral administration of PM, no intact PM is detectable in animal or human plasma, indicating that it is rapidly degraded after being absorbed by the body. Studies have shown that the excretion of the chlorambuciline part of the PM in the body is slower and less intense than the strong pineal fraction. In 1984, Gunnarsson et al. found that PM was transferred to the sulfhydryl group of acyltransferase.