CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability
- 주제(키워드) mollugin , inflammatory bowel disease , ADME , solubility
- 주제(기타) Biochemistry & Molecular Biology; Chemistry, Multidisciplinary
- 설명문(일반) [Hong, Ki Bum; Kim, Darong; Kim, Bo-Kyung; Woo, Seo Yeon; Lee, Ji Hoon; Kang, Soosung] Daegu Gyeongbuk Med Innovat Fdn DGMIF, New Drug Dev Ctr, Daegu 41061, South Korea; [Han, Seung-Hee] KOREA PHARMA Co Ltd, Cent Res Lab, Jeyakgongdan 3 Gil, Hwaseong Si 18622, Gyeonggi Do, South Korea; [Bae, Gyu-Un] Sookmyung Womens Univ, Coll Pharm, Res Ctr Cell Fate Control, Seoul 03760, South Korea; [Kang, Soosung] Ewha Womans Univ, Coll Pharm, Seoul 03760, South Korea; [Kang, Soosung] Ewha Womans Univ, Grad Sch Pharmaceut Sci, Seoul 03760, South Korea
- 등재 SCIE, SCOPUS
- 발행기관 MDPI
- 발행년도 2018
- URI http://www.dcollection.net/handler/ewha/000000156766
- 본문언어 영어
- Published As http://dx.doi.org/10.3390/molecules23082030
초록/요약
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.
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