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New sorbicillinoid derivatives with GLP-1R and eEF2K affinities from a sponge-derived fungus Penicillium chrysogenum 581F1

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posted on 2019-04-16, 11:52 authored by Min-Jia Cao, Tao Zhu, Jing-Tang Liu, Liang Ouyang, Fan Yang, Hou-Wen Lin

Two new sorbicillinoids, 13-hydroxy-dihydrotrichodermolide (1) and 10,11,27,28-tetrahydrotrisorbicillinone C (2), were isolated from the sponge-derived fungus Penicillium chrysogenum 581F1. Their structures were determined on the basis of spectroscopic analysis. Compounds 1 and 2 displayed high affinities to target proteins GLP-1R (diabetes) and eEF2K (cancer) with Kd values of 0.0285 μM, 0.0162 μM for GLP-1R and 0.118 μM, 0.0746 μM for eEF2K, respectively.

Funding

This work was financially supported by National Key Research and Development Program of China [grant number 2018YFC0310900]; National Natural Science Fund of China [grant number U1605221]; Shanghai Municipal Health Commission excellent young talent program [grant number 2018YQ28]; Sichuan Science and Technology Program [grant number 2018JZ0017].

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