CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability
  • Hong, Ki Bum
  • Kim, Darong
  • Kim, Bo-Kyung
  • Woo, Seo Yeon
  • Lee, Ji Hoon
  • ... Bae, Gyu-Un
  • 외 2명
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초록

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-alpha- 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-alpha- and IL-6-induced colonic epithelial cell adhesion assays, suggesting that 15c is a potential anti-inflammatory agent.

키워드

mollugininflammatory bowel diseaseADMEsolubilityRUBIA-CORDIFOLIAINHIBITORDRUGS
제목
CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability
저자
Hong, Ki BumKim, DarongKim, Bo-KyungWoo, Seo YeonLee, Ji HoonHan, Seung-HeeBae, Gyu-UnKang, Soosung
DOI
10.3390/molecules23082030
발행일
2018-08
유형
Article
저널명
Molecules
23
8