抗肿瘤药物。535. 从印度洋-太平洋海绵黑扁海绵中分离出普拉考他汀1和2并确定其结构。

Antineoplastic agents. 535. Isolation and structure of plakorstatins 1 and 2 from the Indo-Pacific sponge Plakortis nigra.

作者信息

Pettit George R, Nogawa Toshihiko, Knight John C, Doubek Dennis L, Hooper J N A

机构信息

Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, Tempe, Arizona 85287-2404, USA.

出版信息

J Nat Prod. 2004 Sep;67(9):1611-3. doi: 10.1021/np040043j.

DOI:10.1021/np040043j

PMID:15387674

Abstract

Two new cancer cell growth inhibiting cyclic peroxides, plakorstatins 1 (1) and 2 (2), were isolated from the Indonesian marine sponge Plakortis nigra. The structures of plakorstatins 1 and 2 including relative configuration were elucidated on the basis of mass and 2D NMR spectroscopic interpretations. These are the first plakortides with an epoxy group in the side chain. Plakorstatin 2 was found to differ from plakorstatin 1 only in the configuration of the epoxide group. Both exhibited moderate cancer cell growth inhibition against the murine P388 lymphocytic leukemia cell line with ED(50) values of 1.1 and 0.91 microg/mL, respectively, for peroxides 1 and 2.

摘要

从印度尼西亚海洋海绵黑扁海绵（Plakortis nigra）中分离出两种新型抑制癌细胞生长的环状过氧化物——普拉考他汀1（1）和2（2）。基于质谱和二维核磁共振波谱分析，阐明了普拉考他汀1和2的结构，包括相对构型。它们是侧链带有环氧基的首批普拉考他汀类化合物。发现普拉考他汀2与普拉考他汀1的区别仅在于环氧基的构型。两种化合物对小鼠P388淋巴细胞白血病细胞系均表现出中等程度的癌细胞生长抑制作用，过氧化物1和2的半数有效剂量（ED50）值分别为1.1和0.91微克/毫升。