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Open AccessArticle

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

New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu 41061, Korea
Central Research Laboratory, KOREA PHARMA Co. Ltd., jeyakgongdan 3-gil, Hyangnam-eup, Hwaseong-si, Gyeonggi-do 18622, Korea
Research Center for Cell Fate Control, College of Pharmacy, Sookmyung Women’s University, Seoul 03760, Korea
College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Korea
Author to whom correspondence should be addressed.
Molecules 2018, 23(8), 2030;
Received: 26 July 2018 / Revised: 8 August 2018 / Accepted: 13 August 2018 / Published: 14 August 2018
(This article belongs to the Section Medicinal Chemistry)
PDF [1033 KB, uploaded 14 August 2018]


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. View Full-Text
Keywords: mollugin; inflammatory bowel disease; ADME; solubility mollugin; inflammatory bowel disease; ADME; solubility

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Hong, K.B.; Kim, D.; Kim, B.-K.; Woo, S.Y.; Lee, J.H.; Han, S.-H.; Bae, G.-U.; Kang, S. CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability. Molecules 2018, 23, 2030.

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