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Epoxyquinophomopsins A and B from endophytic fungus Phomopsis sp. and their activity against tyrosine kinase

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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 .… Click to show full abstract

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.

Keywords: endophytic fungus; kinase; fungus phomopsis; activity; tyrosine kinase

Journal Title: Journal of Natural Medicines
Year Published: 2020

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