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Bioactive natural products from marine sponges and fungal endophytes

机译:来自海洋海绵的生物活性天然产品和真菌内心生物

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This review highlights recent findings of our group on bioactive marine natural products isolated from marine sponges and marine derived fungi. The activated chemical defence of the Mediterranean sponge Aplysina aerophoba is introduced as an example of a dynamic response of marine sponges to wounding. Following tissue disrupture preformed brominated isoxazoline alkaloids are enzymatically cleaved and thereby give rise to aeroplysinin-1 which is believed to protect sponges from invasion of pathogenic bacteria. A preliminary characterization of the membrane bound enzyme(s) involved in the cleavage reaction is presented. Bromotyrosine derived, oxime group bearing peptides, the so called bastadins, obtained from the sponge Ianthella basta and some of their synthetic derivatives were shown to exhibit pronounced anti-fouling activity against larvae of the barnacle Bala-nus improvisus. The antifouling activity could be traced to the oxime group as an important pharmacophore that was also found to be present in other sponge derived natural products exhibiting antifouling activity. Marine derived fungi that reside within invertebrates such as sponges or inside Mangrove plants are emerging as a new source of bioactive metabolites as demonstrated for Aspergillus ustus and Alternaria sp. that were isolated from the sponge Suberites domuncula or from the Mangrove plant Sonneratia alba, respectively. The former fungus yielded new moderately cytotoxic sesquiterpenoids of the drifnane type whereas the latter was found to produce polyketides such as alternariol that exhibited strong and selective inhibitory activity against several protein kinases, for instance Aurora A and B which are targets for anticancer chemotherapy.
机译:本综述介绍了我们对从海洋海绵和海洋衍生的真菌隔离的生物活性海洋天然产品的集团的最新调查结果。引入了地中海海绵的激活的化学防御Aplyoina Aerophoba作为海绵到伤害的动态响应的示例。在组织破坏后,预先形成的溴化异恶唑啉生物碱进行酶促切割,从而产生Aeroplysinin-1,其被认为可以保护海绵免受致病细菌的侵袭。介绍了参与切割反应中涉及的膜结合酶的初步表征。溴旋转胺衍生,肟基携带肽,所谓的牌蛋白,由海绵氏菌Basta获得,其一些合成衍生物显示出对Bala-Nus IngeLisus的幼虫的明显防污活动。可以将防污活性追溯到肟基团中,作为一个重要的药镜,其也发现存在于表现出呈现防污活性的其他海绵衍生的天然产物中。海洋衍生的真菌,这些真菌在诸如海绵或美洲红树植物之类的无脊椎动物中,是作为生物活性代谢物的新来源,如曲霉Ustus和alertaria sp所示。从海绵芬泰杜鹃隔离,分别从海绵植物Sonneratia Alba分离。前真菌产生了新的中间细胞毒性倍二萜腺苷萜烯酮,而后者被发现制备聚酮化合物,例如对几种蛋白激酶具有强烈的选择性抑制活性,例如Aurora A和B,其是抗癌化疗的靶标。

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