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深礁加勒比海绵 Plakortis angulospiculatus 和 Plakortis halichondrioides 的化学成分及其抗炎活性。

Chemical constituents of the deep reef caribbean sponges Plakortis angulospiculatus and Plakortis halichondrioides and their anti-inflammatory activities.

机构信息

Department of Pharmacognosy, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, USA.

出版信息

J Nat Prod. 2010 Sep 24;73(9):1494-8. doi: 10.1021/np100233d.

DOI:10.1021/np100233d
PMID:20738102
Abstract

Chemical investigations of two collections of the deep reef Caribbean sponge Plakortis angulospiculatus resulted in the isolation of a new compound (1) along with the known compound spiculoic acid B (2) belonging to the spiculoic acid class and four other new compounds (3-6) belonging to the zyggomphic acid class. Three new aromatic compounds (7-9) were isolated from the Caribbean sponge Plakortis halichondrioides. The structural determination of the compounds was based on extensive NMR and mass spectroscopic analysis. The isolated compounds 1-7 were tested for their anti-inflammatory activity using in vitro assays for inhibition of inducible nitric oxide synthase and nuclear factor kappa B (NFκB) activity, as well as inhibition of intracellular reactive oxygen species generation as a result of oxidative stress. The cytotoxicity of these compounds was also evaluated to determine the selectivity index of their bioactivity with respect to cytotoxicity. Compounds 1 and 4 were more potent than the positive control in inhibiting NFκB activity and had IC(50) values of 0.47 and 2.28 μM, respectively.

摘要

对两批加勒比深海珊瑚海绵 Plakortis angulospiculatus 的化学成分研究,分离得到一个新化合物(1),以及属于 Spiculoic acid 类的已知化合物 Spiculoic acid B(2)和四个属于 Zyggomphic acid 类的新化合物(3-6)。从加勒比海绵 Plakortis halichondrioides 中分离出三个新的芳香族化合物(7-9)。根据广泛的 NMR 和质谱分析确定了化合物的结构。对分离得到的化合物 1-7 进行了体外抑制诱导型一氧化氮合酶和核因子 kappa B(NFκB)活性以及抑制氧化应激导致的细胞内活性氧生成的抗炎活性测试。还评估了这些化合物的细胞毒性,以确定其生物活性相对于细胞毒性的选择性指数。化合物 1 和 4 在抑制 NFκB 活性方面比阳性对照更有效,其 IC50 值分别为 0.47 和 2.28 μM。

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