18-Des-hydroxy Cytochalasin: an antiparasitic compound of Diaporthe phaseolorum-92C, an endophytic fungus isolated from Combretum lanceolatum Pohl ex Eichler
18-Des-hydroxy Cytochalasin: an antiparasitic compound of Diaporthe phaseolorum-92C, an endophytic fungus isolated from Combretum lanceolatum Pohl ex Eichler
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DOI：
10.1007/s00436-017-5451-9
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发表时间：
2017-07-01
影响因子：
2
通讯作者：
Soares, Marcos Antonio
中科院分区：
文献类型：
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作者：
Brissow, Elson Rudimar;da Silva, Igor Pereira;Soares, Marcos Antonio
对从杉木根中分离的内生真菌Diaporthe phaseolorum-92C （92C）的乙酸乙酯提取物进行化学研究，分离出18-去羟基Cytochalasin H（化合物1）。对92C提取物的杀锥虫和血吸虫活性及细胞毒性进行了评价。检测了化合物1的杀血吸虫、杀利什曼尼、抗菌、抗氧化作用，以及对乳腺癌细胞MDA-MB-231和MCF-7的抗肿瘤活性，以及对正常人肺成纤维细胞GM07492A的细胞毒性。92C提取物（20 μ g/mL）具有较强的杀锥虫活性，可使克氏锥虫的无尾线虫和锥虫数量减少82%。化合物1在50 μ g/mL时，对曼氏血吸虫成虫的杀伤率为50%。化合物1可降低亚马逊利什曼原虫（Leishmania amazonenses promastigotes）和癌细胞MDA-MB-231和MCF-7 （IC50分别为17.5和8.88 μ g/mL）的活力，具有中等的抗氧化活性，对正常细胞GM07492A的细胞毒性IC50为2049.7 +/- 39.9 μ g/mL。这一知识与寻找新的有希望的治疗目的的化合物高度相关。
Chemical investigation of the ethyl acetate extract from the endophytic fungus Diaporthe phaseolorum-92C (92C) isolated from the roots of Combretum lanceolatum led to the isolation of 18-des-hydroxy Cytochalasin H (compound 1). The trypanocidal and schistosomicidal activity and cytotoxicity of the extract from 92C were evaluated. The schistosomicidal, leishmanicidal, antimicrobial, and antioxidant actions, as well as the antitumor activity against the breast cancer cells MDA-MB-231 and MCF-7, and the cytotoxicity towards normal human lung fibroblasts GM07492A of compound 1 was tested. The extract from 92C (20 mu g/mL) exerted potent trypanocidal activity, reducing 82% of the number of amastigotes and trypomastigotes of Trypanosoma cruzi. Compound 1 at 50 mu g/mL killed 50% of Schistosoma mansoni adult worms. Compound 1 reduced the viability of Leishmania amazonenses promastigotes (IC50 = 9.2 mu g/mL) and of the cancer cells MDA-MB-231 and MCF-7 (IC50 = 17.5 and 8.88 mu g/mL, respectively), presented moderate antioxidant activity, and gave IC50 of 2049.7 +/- 39.9 mu g/mL for the cytotoxicity towards normal cells GM07492A. This knowledge is highly relevant to the search for new promising compounds for therapeutic purposes.