Denigrins A-C: new antitubercular 3,4-diarylpyrrole alkaloids from Dendrilla nigra
Denigrins A-C: new antitubercular 3,4-diarylpyrrole alkaloids from Dendrilla nigra
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DOI：
10.1080/14786419.2014.891112
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发表时间：
2014-06-18
影响因子：
2.2
通讯作者：
Rao, Desaraju Venkata
中科院分区：
文献类型：
--
作者：
Kumar, Muthyala Murali Krishna;Naik, Jarpula Devilal;Rao, Desaraju Venkata
化学多样性对于抗结核药物的发现至关重要，因为它确保了新的生物活性特征。迄今为止，海洋海绵已经提供了1000多种新的生物活性分子。从海绵Dendrilla nigra的乙酸乙酯提取物中分离得到3个具有抗结核活性的新化合物denigrins A-C。光谱和化学分析证实，这三个化合物属于3，4-二芳基吡咯生物碱类。苯环上的单羟基取代在从海洋无脊椎动物中分离的片螺素和相关的3，4-二芳基吡咯生物碱中并不常见。其中，denigrin C对结核分枝杆菌H37 Rv的最低抑菌浓度为4g/mL。
Chemical diversity is vital to antitubercular drug discovery as it ensures a novel bioactivity profile. Marine sponges have so far provided more than 1000 new bioactive molecules. Ethyl acetate extract of the marine sponge Dendrilla nigra on bioactivity-guided screening yielded three new compounds denigrins A-C, with potent antitubercular activity. Spectral and chemical analyses confirmed that these three compounds belong to the 3,4-diaryl pyrrole alkaloid category. The presence of monohydroxy substitution on benzene rings is not very common in lamellarin and related 3,4-diaryl pyrrole alkaloids isolated from marine invertebrates. Among these, denigrin C showed highest potency (minimum inhibitory concentration 4g/mL) against Mycobacterium tuberculosis H37Rv.