Department of Chemistry, Dartmouth College, Hanover, NH 03755, USA.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2275-8. doi: 10.1016/j.bmcl.2010.02.007. Epub 2010 Feb 6.
2-Cyano-3,10-dioxooleana-1,9(11)-dien-28-oic acid anhydride (CDDO anhydride) has been synthesized, which is the first example of an oleanane triterpenoid anhydride. CDDO anhydride shows potency similar to or higher than the corresponding acid (CDDO) in various in vitro and in vivo assays related to inflammation and carcinogenesis. Notably, preliminary phamacokinetics studies show that CDDO anhydride levels are higher than CDDO levels in mouse tissues and blood. Further evaluation of CDDO anhydride is in progress.
2-氰基-3,10-二氧代齐墩果-1,9(11)-二烯-28-酸酐(CDDO 酸酐)已被合成,这是齐墩果烷三萜酸酐的首例。在与炎症和致癌有关的各种体外和体内测定中,CDDO 酸酐的活性与相应酸(CDDO)相似或更高。值得注意的是,初步的药代动力学研究表明,CDDO 酸酐在小鼠组织和血液中的水平高于 CDDO 水平。CDDO 酸酐的进一步评估正在进行中。