| Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages. | |
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MedLine Citation:
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PMID: 20934787 Owner: NLM Status: In-Process |
Abstract/OtherAbstract:
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Curcumin is a multifunctional natural product with regulatory effects on inflammation. However, a major limitation for the application of curcumin is its poor bioavailability. We previously demonstrated that the mono-carbonyl analogues of curcumin possessed improved pharmacokinetic profiles. In this study, 33 novel mono-carbonyl analogues of curcumin were synthesized and their inhibition against TNF-α and IL-6 release was evaluated in LPS-stimulated RAW 264.7 macrophages. Based on the screening data, quantitative structure-activity relationship was conducted, indicating that electron-withdrawing groups in benzene ring are favourable to anti-inflammatory activities of B-class compounds. Furthermore, compounds AN1 and B82 demonstrated anti-inflammatory abilities in a dose-dependent manner. These raise the possibility that these compounds might serve as potential agents for the treatment of inflammatory diseases. |
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Authors:
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Chengguang Zhao; Yuepiao Cai; Xuzhi He; Jianling Li; Li Zhang; Jianzhang Wu; Yunjie Zhao; Shulin Yang; Xiaokun Li; Wulan Li; Guang Liang |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-10-08 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: 45 ISSN: 1768-3254 ISO Abbreviation: Eur J Med Chem Publication Date: 2010 Dec |
Date Detail:
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Created Date: 2010-11-24 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: France |
Other Details:
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Languages: eng Pagination: 5773-80 Citation Subset: IM |
Copyright Information:
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Copyright © 2010 Elsevier Masson SAS. All rights reserved. |
Affiliation:
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School of Pharmacy, Wenzhou Medical College, 1210 College Town, Wenzhou, Zhejiang 325035, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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