Journal
JOURNAL OF NATURAL PRODUCTS
Volume 86, Issue 10, Pages 2379-2390Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.3c00580
Keywords
-
Ask authors/readers for more resources
In this study, diterpenoids from Euphorbia fischeriana were found to possess inhibitory effects on the Kv1.3 ion channel. Macrocyclic jatrophanes and lathyranes exhibited selective blocking activity on the Kv1.3 channel, indicating their potential as therapeutic agents for autoimmune diseases.
Euphorbia diterpenoids possess inhibitory effects of Kv1.3 ion channel, but most of this research has focused on diterpenoids with jatrophane-related or ingenane-related skeletons. In the present study, nine undescribed (1-9) and 16 known (10-25) diterpenoids, based on jatrophane, lathyrane, ingenane, abietane, and atisane skeletons, were identified from the methanol extract of the aerial parts of Euphorbia fischeriana. The structures were established by analysis of the spectroscopic data as well as by single-crystal X-ray diffraction analysis. Among the isolated diterpenoids, macrocyclic jatrophanes and lathyranes exerted Kv1.3 blocking activity. Compound 8 exhibited good selectivity on the inhibition of the Kv 1.3 channel rather than hERG channel, with a selectivity index over 7.0. The selective activity of lathyrane diterpenoids indicates that macrocyclic diterpenoids have the potential to be further investigated as therapeutic agents for the treatment of autoimmune diseases.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available