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高等植物中的环肽。二十八。紫菀中环五肽阿斯汀的抗肿瘤活性及肝微粒体生物转化

Cyclic peptides from higher plants. XXVIII. Antitumor activity and hepatic microsomal biotransformation of cyclic pentapeptides, astins, from Aster tataricus.

作者信息

Morita H, Nagashima S, Uchiumi Y, Kuroki O, Takeya K, Itokawa H

机构信息

Department of Pharmacognosy, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1996 May;44(5):1026-32. doi: 10.1248/cpb.44.1026.

Abstract

Antitumor activities on Sarcoma 180A of a series of cyclic pentapeptides, astins, isolated from the roots of Aster tataricus, were examined. The activities on various congeners of the dichlorinated proline residues prepared by chemical conversion and a hepatic microsomal biotransformation in rats suggested that 1,2-cis dichlorinated proline residues of astins A, B and C play an important role in the antitumor activity of astins.

摘要

研究了从紫菀根部分离得到的一系列环五肽阿斯汀对肉瘤180A的抗肿瘤活性。通过化学转化和大鼠肝微粒体生物转化制备的二氯脯氨酸残基各种同系物的活性表明,阿斯汀A、B和C的1,2-顺式二氯脯氨酸残基在阿斯汀的抗肿瘤活性中起重要作用。

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