Design, synthesis and biological activity of novel asymmetric C66 analogs as anti-inflammatory agents for the treatment of acute lung injury
Design, synthesis and biological activity of novel asymmetric C66 analogs as anti-inflammatory agents for the treatment of acute lung injury
复制标题
新型不对称 C66 类似物作为抗炎剂治疗急性肺损伤的设计、合成和生物活性
DOI:
10.1016/j.ejmech.2014.11.054
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发表时间:
2015
影响因子:
6.7
通讯作者:
Liang Guang
中科院分区:
文献类型:
--
作者:
Yu Pengtian;Dong Lili;Zhang Yali;Chen Wenbo;Xu Shanmei;Wang Zhe;Shan Xiaoou;Zhou Jianmin;Liu Zhiguo;Liang Guang
Acute lung injury (ALI) is a leading cause of morbidity and mortality in critically-ill patients. Previously, we reported that a symmetric mono-carbonyl analog of curcumin, (C66), exhibits enhanced stability and was found to have efficacy and be involved in potential cytokines inhibition. In the present study, a series of novel asymmetric C66 analogs were designed and synthesized. A majority of them effectively inhibited the LPS-induced expression of TNF-α and IL-6. Significantly, compound4b2was found to effectively reduce LPS-induced pulmonary inflammation, as reflected by reductions in concentration of total protein, inflammatory cell count as well as the lungW/Dratio in bronchoalveolar lavage (BAL) fluid. Furthermore,in vivoadministration of4b2resulted in remarkable improvement in histopathological changes of lung in rats.