CF3-substituted mollugin 2-(4-morpholinyl)-ethyl ester as a potential anti-inflammatory agent with improved aqueous solubility and metabolic stability

Ki Bum Hong, Darong Kim, Bo Kyung Kim, Seo Yeon Woo, Ji Hoon Lee, Seung Hee Han, Gyu Un Bae, Soosung Kang

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

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.

Original languageEnglish
Article number2030
JournalMolecules
Volume23
Issue number8
DOIs
StatePublished - 14 Aug 2018

Bibliographical note

Funding 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).

Publisher Copyright:
© 2018 by the authors.

Keywords

  • ADME
  • Inflammatory bowel disease
  • Mollugin
  • Solubility

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