4.4 Article

Synthesis and Anti-Inflammatory Evaluation of Novel C66 Analogs for the Treatment of LPS-Induced Acute Lung Injury

期刊

CHEMICAL BIOLOGY & DRUG DESIGN
卷 86, 期 4, 页码 753-763

出版社

WILEY-BLACKWELL
DOI: 10.1111/cbdd.12548

关键词

acute lung injury; C66; chemical stability; drug design; synthesis

资金

  1. National Natural Science Funding of China [21202124, 21472142, 81402783]
  2. Zhejiang Medical & Health Science and Technology Project [2013KYB168]
  3. SRF for ROCS, SEM
  4. Zhejiang Key Group Project in Scientific Innovation [2010R50042]

向作者/读者索取更多资源

We previously reported a symmetric monocarbonyl analog of curcumin (MACs), C66, which demonstrated potential anti-inflammatory activity and low toxicity. In continuation of our ongoing research, we designed and synthesized 34 asymmetric MACs based on C66 as a lead molecule. A majority of the C66 analogs effectively inhibited LPS induction of TNF- and IL-6 expression. Additionally, a preliminary SAR was conducted. Furthermore, active compounds 4a11 and 4a16 were found to effectively reduce theW/D ratio in the lungs and the protein concentration in the bronchoalveolar lavage fluid (BALF). Meanwhile, a histopathological examination indicated that these two analogs significantly attenuate tissue injury in the lungs with LPS-induced ALI rats. 4a11 and 4a16 also inhibited mRNA expression of several inflammatory cytokines, including TNF-, IL-6, IL-1, COX-2, ICAM-1 and VCAM-1, in the Beas-2B cellsafter LPS challenge. Altogether, the data exhibit a series of new C66 analogs as promising anti-inflammatory agents for the treatment of LPS-induced ALI.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.4
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据