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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 BumKim, DarongKim, Bo-KyungWoo, Seo YeonLee, Ji HoonHan, Seung-HeeBae, Gyu-UnKang, Soosung
Ewha Authors
강수성
SCOPUS Author ID
강수성scopus
Issue Date
2018
Journal Title
MOLECULES
ISSN
1420-3049JCR Link
Citation
MOLECULES vol. 23, no. 8
Keywords
mollugininflammatory bowel diseaseADMEsolubility
Publisher
MDPI
Indexed
SCIE; SCOPUS WOS 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
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