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CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability
- Title
- CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability
- Authors
- Hong, Ki Bum; Kim, Darong; Kim, Bo-Kyung; Woo, Seo Yeon; Lee, Ji Hoon; Han, Seung-Hee; Bae, Gyu-Un; Kang, Soosung
- Ewha Authors
- 강수성
- SCOPUS Author ID
- 강수성
- Issue Date
- 2018
- Journal Title
- MOLECULES
- ISSN
- 1420-3049
- Citation
- MOLECULES vol. 23, no. 8
- Keywords
- mollugin; inflammatory bowel disease; ADME; solubility
- Publisher
- MDPI
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- 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-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.
- DOI
- 10.3390/molecules23082030
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
- Files in This Item:
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CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester.pdf(1.03 MB)
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