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抗瘤酮是机体自身产生的一类天然抗癌物质,是癌的生化防御系统的成分,一些中、小肽类和氨基酸衍生物,通过对癌细胞的诱导分化作用形成了对癌的防御。本文系统介绍了抗瘤酮的分离、提纯、鉴定和化学合成。根据不同的分离条件和药理筛选从人尿中得到五个抗癌组分:抗瘤酮A_1、A_2、A_3、A_4、A_5及抗瘤酮A_(10)是通过提纯并经化学合成确证了结构的第一个化合物,其活性降解产物为A_S2—5和A_S2—1.并介绍了抗瘤酮的国内外药理毒理学研究、化学防护和诱导分化作用,以及抗瘤酮各个亚组分和A_(10)合成衍生物的I期临床研究。
Anti-tumor ketones are a kind of natural anti-cancer substances produced by the body itself and are components of cancer’s biochemical defense system. Some medium and small peptides and amino acid derivatives form a defense against cancer through the induction and differentiation of cancer cells. This article systematically introduced the isolation, purification, identification and chemical synthesis of anti-tumor ketones. According to different separation conditions and pharmacological screening, five anticancer components were obtained from human urine: anti-tumor ketones A_1, A_2, A_3, A_4, A_5 and anti-tumor ketones A_10 were confirmed by chemical synthesis and purification Of the first compound, the active degradation products A_S2-5 and A_S2-1. And introduced the anti-tumor ketones at home and abroad pharmacology and toxicology studies, chemical protection and induction of differentiation, as well as anti-tumor ketones sub-components and A_ (10) Phase I clinical studies of synthetic derivatives.