Jatrophane Diterpenoids with Kv1.3 Ion Channel Inhibitory Effects from <i>Euphorbia helioscopia</i>.
Basic Information
ID: ALA5120778
Journal: J Nat Prod
Title: Jatrophane Diterpenoids with Kv1.3 Ion Channel Inhibitory Effects from Euphorbia helioscopia.
Authors: Zhou CG, Xiang ZN, Zhao N, Sun X, Hu ZF, Wu JL, Xia RF, Chen C, Su JC, Chen JC, Wan LS.
Abstract: Chemical investigation of bioactive components from the whole plant of Euphorbia helioscopia resulted in the isolation and identification of 17 new jatrophane diterpenoids, namely, heliojatrone D (1) and helioscopids A-P (2-17), along with 11 known analogues (18-28). The structural elucidation of the new diterpenoids was achieved by the comprehensive analysis of HRESIMS, NMR, and X-ray crystallographic data, as well as using electronic circular dichroism. Structurally, heliojatone D (1) is the fourth natural diterpenoid with a rare bicyclo[8.3.0]tridecane skeleton. The inhibitory effect of the isolated diterpenoids against Kv1.3 ion channels was evaluated in a human embryonic kidney 293 cell model transfected with plasmid encoding Kv1.3, resulting in the identification of a series of potent Kv1.3 ion channel inhibitors, with the most active ones (2 and 15) showing IC50 values of 0.9 μM.
CiteXplore: 35245067
DOI: 10.1021/acs.jnatprod.1c00879
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