title: A novel synthetic mono-carbonyl analogue of curcumin, A13, exhibits anti-inflammatory effects in vivo by inhibition of inflammatory mediators.
abstract: Curcumin is a pleiotropic molecule against inflammatory related diseases. However, poor bioavailability greatly limits its application in clinic. Our previous study synthesized and evaluated a hydrosoluble mono-carbonyl analogue of curcumin, (2E,5E)-2,5-bis(4-(3-(dimethylamino)-propoxy)benzylidene)cyclopentanone (A13). In the present study, we further evaluated the anti-inflammatory effect of A13 in vivo. In lipopolysaccharide-challenged mice, pretreatment of A13 (15 mg/kg, i.v.) attenuated the increase of plasma level of NO, TNF-α, and IL-6, significantly inhibited the increase of hepatic inflammatory gene transcription, and improved pulmonary damages. In addition, A13 (10 or 30 mg/kg, i.p.) reduced vascular permeability in Institute of Cancer Research mice and inhibited pain reaction in chemically induced inflammatory models. Together, A13 exhibits anti-inflammatory activities both in vitro and in vivo by the inhibition of various inflammatory mediators.
authors: Bioorganic and Medicinal Chemistry Research Center, School of Pharmaceutical Science, Wenzhou Medical College, Wenzhou, 325035, China.
authors: Yi
authors: Y
authors: Wang
authors: Congcong
authors: C
authors: Yu
authors: Yong
authors: Y
authors: Pan
authors: Xuyi
authors: X
authors: Yang
authors: Yi
authors: Y
authors: Huang
authors: Zhiguo
authors: Z
authors: Feng
authors: Xiaokun
authors: X
authors: Li
authors: Shulin
authors: S
authors: Yang
authors: Guang
authors: G
authors: Liang
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