Diterpenoids from Euphorbia fischeriana with Kv1.3 Inhibitory Activity.
J Nat Prod
; 86(10): 2379-2390, 2023 10 27.
Article
em En
| MEDLINE
| ID: mdl-37796721
ABSTRACT
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Euphorbia
/
Diterpenos
Idioma:
En
Revista:
J Nat Prod
Ano de publicação:
2023
Tipo de documento:
Article