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自1963年首次由链丝菌Streptomycespeucetius的培养基中提取到柔红霉素,特别是1968年从其变种S.p.var caesium中分离到阿霉素后,蒽环类抗肿瘤药物受到广泛重视。但很快发现这类药物具有骨髓抑制和心脏毒性。随后,很多学者希望通过改变其结构,从而降低毒性、提高疗效或扩大有效抗瘤谱,目前比较突出的是表阿霉素(Epirubicin,Pharmorubicin,EPI)。表阿霉素与阿霉素的区别是在氨基糖部分4’位的OH基由顺式变成了反式。这种立体结构上的细微变化,使骨髓和心脏的毒性有相当的差异。
Since 1963, daunorubicin was first extracted from the Streptomyces peucetius culture medium, and in particular after isolation of doxorubicin from its variant S. p. var caesium in 1968, anthracycline antitumor drugs have received extensive attention. However, these drugs were soon found to have myelosuppression and cardiotoxicity. Subsequently, many scholars hope to reduce the toxicity, increase the efficacy, or expand the effective anti-tumor spectrum by changing its structure. Currently prominent epirubicin (Epirubicin, Pharmorubicin, EPI). The difference between epirubicin and doxorubicin is that the OH group at the 4’ position of the amino sugar moiety changes from cis to trans. This slight change in the three-dimensional structure makes the bone marrow and heart toxicity quite different.