Although mollugin, the main ingredient of the oriental medicinal herb Rubia cordifolia, has considerable anti-inflammatory effects, it has poor aqueous solubility as well as poor metabolic and plasma stability. To overcome these shortfalls, various mollugin derivatives have been synthesized and evaluated for their ability to inhibit U937 monocyte cell adhesion to HT-29 colonic epithelial cells in TNF-α- or IL-6-induced models of colon inflammation. The 2-(4-morpholinyl)-ethyl ester of CF3-substituted mollugin (compound 15c) showed good water solubility, improved metabolic and plasma stability, and greater inhibitory activity than mesalazine in both the TNF-α- and IL-6-induced colonic epithelial cell adhesion assays, suggesting that 15c is a potential anti-inflammatory agent.
Bibliographical noteFunding Information:
This research was funded by the R&D support program of the New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF) and by a National Research Foundation of Korea (NRF) grants funded by the Korean government (MSIT) (No. 2018R1A5A202528 and 2018M3A9A7057263).
© 2018 by the authors.
- Inflammatory bowel disease