Aly Amal H, Edrada-Ebel RuAngelie, Indriani Ine Dewi, Wray Victor, Müller Werner E G, Totzke Frank, Zirrgiebel Ute, Schächtele Christoph, Kubbutat Michael H G, Lin W H, Proksch Peter, Ebel Rainer
Institut für Pharmazeutische Biologie and Biotechnologie, Heinrich-Heine-Universität, Universitätsstrasse 1, Geb. 26.23, D-40225 Düsseldorf, Germany.
J Nat Prod. 2008 Jun;71(6):972-80. doi: 10.1021/np070447m. Epub 2008 May 22.
From the Egyptian medicinal plant Polygonum senegalense the fungal endophyte Alternaria sp. was isolated. Extracts of the fungus grown either in liquid culture or on solid rice media exhibited cytotoxic activity when tested in vitro against L5178Y cells. Chromatographic separation of the extracts yielded 15 natural products, out of which seven were new compounds, with both fungal extracts differing considerably with regard to their secondary metabolites. Compounds 1, 2, 3, 6, and 7 showed cytotoxic activity with EC 50 values ranging from 1.7 to 7.8 microg/mL. When analyzed in vitro for their inhibitory potential against 24 different protein kinases, compounds 1- 3, 5- 8, and 15 inhibited several of these enzymes (IC 50 values 0.22-9.8 microg/mL). Interestingly, compounds 1, 3, and 6 were also identified as constituents of an extract derived from healthy leaves of the host plant P. senegalense, thereby indicating that the production of natural products by the endophyte proceeds also under in situ conditions within the plant host.
从埃及药用植物塞内加尔蓼中分离出真菌内生菌链格孢属(Alternaria sp.)。在液体培养或固体大米培养基上生长的真菌提取物,在体外对L5178Y细胞进行测试时表现出细胞毒性活性。提取物的色谱分离得到了15种天然产物,其中7种是新化合物,两种真菌提取物的次生代谢产物有很大差异。化合物1、2、3、6和7表现出细胞毒性活性,EC50值范围为1.7至7.8微克/毫升。在体外分析它们对24种不同蛋白激酶的抑制潜力时,化合物1-3、5-8和15抑制了其中几种酶(IC50值为0.22-9.8微克/毫升)。有趣的是,化合物1、3和6也被鉴定为宿主植物塞内加尔蓼健康叶片提取物的成分,从而表明内生菌在植物宿主内的原位条件下也能产生天然产物。