Design, synthesis, and anti-inflammatory activity both in vitro and in vivo of new betulinic acid analogues having an enone functionality in ring A

Fifteen new betulinic acid analogues were designed, synthesized, and tested for anti-inflammatory activity. Many of these analogues effectively suppress nitric oxide (NO) production in RAW cells stimulated with interferon-γ. Analogue 10 is highly and orally active in vivo for induction of the anti-inflammatory and cytoprotective enzyme, heme oxygenase-1.

Graphical abstractThe new betulinic acid analogue 10, at oral dosing of 2 μM, causes significant induction of the anti-inflammatory, cytoprotective enzyme, heme oxygenase-1, in the liver.Figure optionsDownload full-size imageDownload as PowerPoint slide