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从红海海绵红斑迪卡海绵中提取的抗疟疾、抗病毒和抗弓形虫的降三萜过氧化物酸。

Antimalarial, antiviral, and antitoxoplasmosis norsesterterpene peroxide acids from the Red Sea sponge Diacarnus erythraeanus.

作者信息

El Sayed K A, Hamann M T, Hashish N E, Shier W T, Kelly M, Khan A A

机构信息

The Department of Pharmacognosy, and National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, USA.

出版信息

J Nat Prod. 2001 Apr;64(4):522-4. doi: 10.1021/np000529+.

DOI:10.1021/np000529+
PMID:11325240
Abstract

A new norsesterterpene acid, named muqubilone (1), along with the known sigmosceptrellin-B and muqubilin were isolated from the Red Sea sponge Diacarnus erythraeanus. The structure determination of 1 was based primarily on 1D and 2D NMR analyses. Sigmosceptrellin-B exhibits significant in vitro antimalarial activity against Plasmodium falciparum (D6 and W2 clones) with IC(50) values of 1200 and 3400 ng/mL, respectively. Muqubilin and 1 show in vitro antiviral activity against herpes simplex type 1 (HSV-1) with ED(50) values of 7.5 and 30 microg/mL, respectively. Muqubilin and sigmosceptrellin-B display potent in vitro activity against Toxoplasma gondii at a concentration of 0.1 microM without significant toxicity.

摘要

从红海海绵红斑肉芝软珊瑚(Diacarnus erythraeanus)中分离出一种新的降倍半萜烯酸,命名为穆库比隆(1),以及已知的西格莫西普特雷林 - B和穆库比林。化合物1的结构确定主要基于一维和二维核磁共振分析。西格莫西普特雷林 - B对恶性疟原虫(D6和W2克隆)表现出显著的体外抗疟活性,IC(50)值分别为1200和3400 ng/mL。穆库比林和1对1型单纯疱疹病毒(HSV - 1)表现出体外抗病毒活性,ED(50)值分别为7.5和30 μg/mL。穆库比林和西格莫西普特雷林 - B在浓度为0.1 μM时对刚地弓形虫显示出强大的体外活性,且无明显毒性。

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