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Epoxyquinophomopsins A and B from endophytic fungus Phomopsis sp. and their activity against tyrosine kinase
Journal of Natural Medicines ( IF 3.3 ) Pub Date : 2020-10-08 , DOI: 10.1007/s11418-020-01454-1
Elvira Hermawati , Suzany D. Ellita , Lia D. Juliawaty , Euis H. Hakim , Yana M. Syah , Hayato Ishikawa

Two new quinone derivatives, epoxyquinophomopsins A (1) and B (2), were purified from the EtOAc extract of endophytic fungus Phomopsis sp isolated from Morus cathayana. The structures of both compounds were determined based on 1D and 2D NMR and mass spectral data, as well as by x-ray diffraction analysis for 1. Compounds 1 and 2 were screened against eight receptor- (RTKs) and eight non-receptor tyrosine kinases (nRTKs). Both compounds showed strong inhibitory properties against Bruton’s Tyrosine Kinase (nRTK) with their kinase activity were 19% and 20%, respectively. Only compound 1 that showed strong inhibitory properties against RTKs EGFR and HER-4 with its kinase activity were 16 and 15%, respectively. Thus, both compounds have potential as tyrosine kinase inhibitors.



中文翻译:

内生真菌Phomopsis sp。的环氧喹啉菌素A和B。及其对酪氨酸激酶的活性

桑树(Morus cathayana)分离的内生真菌Phomopsis sp的EtOAc提取液中纯化了两种新的醌衍生物,环氧喹啉菌素A(1)和B(2)。物的基础上确定一维和二维NMR和质谱数据,以及通过x射线衍射分析的两种化合物的结构为1。化合物12针对八种受体(RTK)和八种非受体酪氨酸激酶(nRTK)进行筛选。两种化合物均显示出对布鲁顿酪氨酸激酶(nRTK)的强抑制特性,其激酶活性分别为19%和20%。仅显示出对RTKs EGFR和HER-4具有强激酶活性的强抑制特性的化合物1分别为16%和15%。因此,两种化合物都具有作为酪氨酸激酶抑制剂的潜力。

更新日期:2020-10-08
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