| Literature DB >> 27240273 |
Heping Zhu1, Tingting Xu2, Chenyu Qiu1, Beibei Wu2, Yali Zhang1, Lingfeng Chen1, Qinqin Xia1, Chenglong Li1, Bin Zhou3, Zhiguo Liu4, Guang Liang1.
Abstract
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 molecule 8f. The most active compound 7a was effective in reducing the Wet/Dry ratio in the lungs and protein concentration in bronchoalveolar lavage fluid. Meanwhile, 7a also 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 that 7a could be therapeutically beneficial for use as an anti-inflammatory agent in the clinical treatment of acute lung injury (ALI).Entities:
Keywords: Acute lung injury; Chemical stability; Drug design; Mono-carbonyl analogs of curcumin; Water solubility
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Year: 2016 PMID： 27240273 DOI： 10.1016/j.ejmech.2016.05.041
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514