Azorellane diterpenoids from Laretia acaulis inhibit nuclear factor-kappa B activity

作者：Borquez Jorge^*; Loyola Luis A; Morales Glauco; San Martin Aurelio; Roldan Raquel; Marquez Nieves; Munoz Eduardo

来源：Phytotherapy Research, 2007, 21(11): 1082-1086.

DOI：10.1002/ptr.2218

• NF-kappa B
• Laretia acaulis
• azorellane diterpenoids
• inflammation
• apiaceae

Transcription factor NF-kappa B plays a key role in the inducible expression of genes mediating proinflammatory effects, and is thus an important target for the development of antiinflammatory drugs. Laretia acaulis (Cav.) Gill et Hook (Apiaceae) is a medicinal plant used in the high Andes mountains for different ailments such as diabetes, inflammation and for general pain. In addition to the known azorellanol (2) and 7-deacetylazorellanol (4), 13-epiazorellanol (1) was also isolated from the aerial part of this plant. Its structure was based on spectroscopic comparison with azorellanol (2) and by chemical characterization. While compounds 2 and 4 showed potent anti-NF-kappa B activity by targeting the activity of the I kappa B alpha kinase, compound 1 was completely inactive highlighting the importance of position 13 in the biological activities of this class of tetracyclic diterpenoids.

• 出版日期2007-11