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-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.
Highlights
Rubia cordifolia is a flowering plant in the coffee family (Rubiaceae), widely distributed fromAfrica to Asia and Australia [1]
RPMI 1640 medium and fetal bovine serum (FBS) were from HyClone-Pierce Co. (Logan, UT, USA), and penicillin-streptomycin and trypsin/EDTA were from WelGENE (Gyeongsan, Korea)
HT-29 human colonic epithelial cells and U937 human pre-monocytic cells were grown in RPMI
Summary
Rubia cordifolia is a flowering plant in the coffee family (Rubiaceae), widely distributed fromAfrica to Asia and Australia [1]. Rubia cordifolia is a flowering plant in the coffee family (Rubiaceae), widely distributed from. Its roots have been used as a traditional medicine in India [2] and. China [3] for their anti-inflammatory, astringent, tonic, antiseptic, deobstruent, and antidysenteric effects [4,5]. Mollugin (1), a methyl ester derivative of naphthoquinone (Figure 1), has been identified as a major active component of the roots of Rubia cordifolia [6]. Recent pharmacological data show that mollugin (1) manifests a wide range of biologically interesting properties, such as antibacterial, anti-inflammatory, antileukemia, and anti-allergic activities [7]. Mollugin (1) displays efficacy against inflammatory bowel disease (IBD) in both a TNF-α-induced colon inflammation cell culture model and a DSS/TNBS-induced IBD animal model [8].
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