CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability

Autor: Ki Bum Hong, Darong Kim, Bo-Kyung Kim, Seo Yeon Woo, Ji Hoon Lee, Seung-Hee Han, Gyu-Un Bae, Soosung Kang
Jazyk: angličtina
Rok vydání: 2018
Předmět:
Zdroj: Molecules, Vol 23, Iss 8, p 2030 (2018)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules23082030
Popis: 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.
Databáze: Directory of Open Access Journals
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