A partial peroxisome proliferator-activated receptor gamma agonist isolated from the roots of Euphorbia sikkimensis

Chemical constituents of the Euphorbia sikkimensis roots was investigated and twelve known compounds were isolated, including three ent-atisane diterpenes: ent-(13S)-hydroxyatis-16-ene-3,14-dione (1), ent-(5 beta,8 alpha,9 beta,10 alpha,11 alpha,12 alpha)-11-hydroxyatis-16-ene-3,14-dione (2), ent-atisane-3-oxo-16 alpha,17-diol (3); two kaurene diterpenes: ent-kaurane-3-oxo-16 alpha,17-diol (4), ent-kaurane-3-oxo-16 beta,17-diol (5); one lathyane diterpene of latilagascene B (6); two flavonoids: quercetin (7), luteolin (8); one lignin d-pinoresinol (9); one coumarin scopoletin (10); together with ethyl gallate (11), p-hydroxybenzaldehyde (12). Their structures were identified based on the extensive spectroscopic analysis in comparison with the literature data. Compounds 1, 2, 4, 6 and 9 were isolated from Euphorbia sikkimensis for the first time. The agonistic activity of peroxisome proliferator-activated receptor gamma (PPAR gamma) for compounds 1, 7, 8, 9 and 11 was evaluated. Compound 1 exhibited moderate agonistic activity for PPAR gamma receptor with relative fluorescence intensity of 10.19 at 30.0 mu M, in comparison with that of the positive control of rosiglitazone (28.50 at 2.0 mu M).

Automated summary

The chemical constituents of Euphorbia sikkimensis roots were investigated, resulting in the isolation of twelve known compounds. Five of these compounds were isolated from Euphorbia sikkimensis for the first time. The agonistic activity of peroxisome proliferator-activated receptor gamma (PPARγ) was evaluated for several compounds, and compound 1 showed moderate agonistic activity.