Synthesis and optimization of novel allylated mono-carbonyl analogs of curcumin (MACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI) in rats
Synthesis and optimization of novel allylated mono-carbonyl analogs of curcumin (MACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI) in rats
复制标题
新型烯丙基化单羰基姜黄素类似物 (MAC) 的合成和优化可作为有效的抗炎剂，对抗 LPS 诱导的大鼠急性肺损伤 (ALI)
DOI：
10.1016/j.ejmech.2016.05.041
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发表时间：
2016
影响因子：
6.7
通讯作者：
Liang Guang
中科院分区：
文献类型：
--
作者：
Zhu Heping;Xu Tingting;Qiu Chenyu;Wu Beibei;Zhang Yali;Chen Lingfeng;Xia Qinqin;Li Chenglong;Zhou Bin;Liu Zhiguo;Liang Guang
采用适当的合成路线合成了一系列新型的姜黄素的对称和不对称烯丙基化单羰基类似物（MACs），并通过LPS诱导TNF-α和IL-6的表达进行了实验评价。与铅分子8 f相比，大多数所得化合物作为盐酸盐表现出改善的水溶性。最具活性的化合物7a有效降低肺中的湿/干比和支气管肺泡灌洗液中的蛋白质浓度。同时，7a还能抑制脂多糖（LPS）刺激的Beas-2B细胞TNF-α、IL-6、IL-1β和VCAM-1 mRNA的表达。这些结果表明，在急性肺损伤（ALI）的临床治疗中，7作为抗炎剂可能是有益的。
A series of novel symmetric and asymmetric allylated mono-carbonyl analogs of curcumin (MACs) were synthesized using an appropriate synthetic route and evaluated experimentally thru the LPS-induced expression of TNF-α and IL-6. Most of the obtained compounds exhibited improved water solubility as a hydrochloride salt compared to lead molecule8f. The most active compound7awas effective in reducing the Wet/Dry ratio in the lungs and protein concentration in bronchoalveolar lavage fluid. Meanwhile,7aalso inhibited mRNA expression of several inflammatory cytokines, including TNF-α, IL-6, IL-1β, and VCAM-1, in Beas-2B cells after Lipopolysaccharide (LPS) challenge. These results suggest that7acould be therapeutically beneficial for use as an anti-inflammatory agent in the clinical treatment of acute lung injury (ALI).