| Literature DB >> 27704815 |
Fabrizio Dal Piaz1, Mariela Beatriz Vera Saltos2, Silvia Franceschelli1, Giovanni Forte1, Stefania Marzocco1, Tiziano Tuccinardi3, Giulio Poli3, Samad Nejad Ebrahimi4, Matthias Hamburger5, Nunziatina De Tommasi1, Alessandra Braca3.
Abstract
Five new diterpenes (1-5) and a megastigmane derivative (6) were isolated from the aerial parts of Euphorbia laurifolia, along with several known compounds. Their structures were elucidated by NMR, MS, and ECD and by chemical methods. A chemical proteomics drug affinity responsive target stability (DARTS) approach to investigate the lathyrane diterpene 1, laurifolioside, on its putative cellular target(s) was performed. Clathrin heavy chain 1, a protein mainly involved in selective uptake of proteins, viruses, and other macromolecules at the plasma membrane of cells, was identified as the major interaction partner of compound 1. The modulation of clathrin activity by 1 was studied through microscopy, molecular docking, and molecular dynamics studies, suggesting a new activity of lathyrane diterpenes in the modulation of trafficking pathways.Entities:
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Year: 2016 PMID： 27704815 DOI： 10.1021/acs.jnatprod.6b00627
Source DB: PubMed Journal: J Nat Prod ISSN： 0163-3864 Impact factor: 4.050