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抗肿瘤药物,325。从海笔属物种中分离出具有人癌细胞生长抑制作用的环状八肽海笔抑素10和11及其结构

Antineoplastic agents, 325. Isolation and structure of the human cancer cell growth inhibitory cyclic octapeptides phakellistatin 10 and 11 from Phakellia sp.

作者信息

Pettit G R, Tan R, Ichihara Y, Williams M D, Doubek D L, Tackett L P, Schmidt J M, Cerny R L, Boyd M R, Hooper J N

机构信息

Cancer Research Institute, Arizona State University, Tempe 85287-1604, USA.

出版信息

J Nat Prod. 1995 Jun;58(6):961-5. doi: 10.1021/np50120a025.

Abstract

The two new marine sponge (Phakellia sp., western Pacific Ocean) constituents, phakellistatin 10 [1] and 11 [2], were found to be cyclic octapeptides that significantly inhibited growth of the murine P-388 lymphocytic leukemia (ED50 values of 2.1 and 0.20 micrograms/ml, respectively) and human cancer cell lines. The structures were established based on results of extensive tandem ms/ms and high-field (500-MHz) 2D 1H- and 13C-nmr analyses. All of the amino acid units (except Trp, not determined) were found to correspond to the (S)-configuration.

摘要

发现来自两种新的海洋海绵(Phakellia sp.,西太平洋)的成分,即海兔毒素10[1]和11[2],是环八肽,它们能显著抑制小鼠P-388淋巴细胞白血病的生长(ED50值分别为2.1和0.20微克/毫升)以及人类癌细胞系的生长。基于广泛的串联质谱/质谱和高场(500兆赫)二维氢谱和碳谱分析结果确定了其结构。发现所有氨基酸单元(除未确定的色氨酸外)均对应于(S)-构型。

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