Highly purified fractions from human urine exhibiting antineoplastic activity and processes for their preparation are described. The fractions comprise biologically active, small sized, low molecular weight peptides which exert cytostatic and cytotoxic activity toward neoplastic cell cultures and human neoplastic diseases. The fractions have been termed antineoplaston fractions. An antineoplastic active peptide common to each of the various antineoplaston fractions has been isolated and identified as 3-[N-phenylacetylaminopiperidinel-2, 6 dion. A synthetic mechanism for the preparation of 3-[N-phenylacetyl- aminopiperidine]-2, 6-dion is also disclosed, involving a combination reaction between L-glutamine and phenylacetyl chloride. Also disclosed are the hydrolysis degradation products of 3-[N-phenylacetylaminopiperidine)-2, 6-dion which also exhibit antineoplastic activity when administered according to the general teachings presented in this disclosure.
本文介绍了从人尿中提取的具有抗肿瘤活性的高纯度馏分及其制备方法。这些馏分由
生物活性小分子量肽组成,对肿瘤
细胞培养物和人类肿瘤疾病具有细胞抑制和细胞毒性活性。这些馏分被称为抗肿瘤馏分。目前已分离出一种抗肿瘤活性肽,这种肽在各种抗肿瘤馏分中都有,并被鉴定为 3-[N-苯乙酰
氨基
哌啶-2,6-二酮]。还公开了制备 3-[N-
苯乙酰基-
氨基
哌啶]-2,6-二酮的合成机制,涉及 L-谷
氨酰胺和
苯乙酰氯的结合反应。还公开了 3-[N-苯乙酰
氨基
哌啶]-2,6-二酮的
水解降解产物,根据本公开的一般教导给药时,这些产物也显示出抗肿瘤活性。