Accessible Method for the Development of Novel Sterol Analogues with Dipeptide-like Side Chains That Act as Neuroinflammation Inhibitors

doi:10.1021/acschemneuro.5b00256

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	Accessible Method for the Development of Novel Sterol Analogues with Dipeptide-like Side Chains That Act as Neuroinflammation Inhibitors
	Chen, Hongli1 ; Han, Chaojun 2,3; Wu, Jing 2,3; Liu, Xiaoyu1 ; Zhan, Yuexiong1 ; Chen, Jiakang1 ; Chen, Yanke 2,3; Gu, Ruinan 2,3; Zhang, Li 2,3; Chen, Shuangshuang 2,3; Jia, Jia 2,3; Zhen, Xuechu 2,3; Zheng, Long Tai 2,3; Jiang, Biao1
	2016-03
发表期刊	ACS CHEMICAL NEUROSCIENCE (IF:4.1[JCR-2023],4.3[5-Year])
ISSN	1948-7193
卷号	7 期号:3 页码:305-315
发表状态	已发表
DOI	10.1021/acschemneuro.5b00256
摘要	A number of novel sterol derivatives with dipeptide-like side chains were synthesized using an Ugi four component condensation method and assayed to test their anti-inflammatory effects in activated microglial cells. Compound 18b ((3S,10R,13S)-N-((R)-1-(tert-butylamino)-1-oxo-3-phenylpropan-2-y1)-3-hydroxy-N,10,13-trimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthrene-17-carboxamide) was identified as the most potent anti-inflammatory agent in the series of compounds analyzed. Compound 18b markedly inhibited the expression of proinflammatory factors, including inducible nitric oxide synthase, interleukin (IL)-6, IL-1 beta, tumor necrosis factor-alpha, and cyclooxygenase-2 in lipopolysaccharide-stimulated microglial cells. Further studies showed that compound 18b significantly suppressed the transcriptional activity of AP-1 and NF-kappa B in activated microglial cells, which was likely mediated by the inhibition of the p38 MAPK and JNK signal transduction pathways. In addition, compound 18b displayed neuroprotective effects in a microglial-conditioned medium/neuron coculture and an experimental focal ischemic mouse model.
关键词	Ugi four-component condensation microglia neuroinflammation neuroprotection focal ischemic mouse model
收录类别	SCI
语种	英语
资助项目	Jiangsu Science and Technology Commission[BY2011131]
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Neurosciences & Neurology
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Neurosciences
WOS记录号	WOS:000372479600006
出版者	AMER CHEMICAL SOC
WOS关键词	ISCHEMIC BRAIN-INJURY ; NITRIC-OXIDE SYNTHASE ; NF-KAPPA-B ; MULTICOMPONENT REACTIONS ; BV-2 MICROGLIA ; DERIVATIVES ; ACTIVATION ; INFLAMMATION ; MECHANISMS ; RESPONSES
原始文献类型	Article
引用统计	正在获取...
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/1906
专题	免疫化学研究所生命科学与技术学院免疫化学研究所_特聘教授组_抗体化学实验室免疫化学研究所_公共科研平台_分析化学平台生命科学与技术学院_硕士生
通讯作者	Chen, Hongli; Zheng, Long Tai; Jiang, Biao
作者单位	1.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China 2.Soochow Univ, Jiangsu Key Lab Translat Res & Therapy Neuropsych, Suzhou 215021, Jiangsu, Peoples R China 3.Soochow Univ, Coll Pharmaceut Sci, Suzhou 215021, Jiangsu, Peoples R China
第一作者单位	免疫化学研究所
通讯作者单位	免疫化学研究所
第一作者的第一单位	免疫化学研究所
推荐引用方式 GB/T 7714	Chen, Hongli,Han, Chaojun,Wu, Jing,et al. Accessible Method for the Development of Novel Sterol Analogues with Dipeptide-like Side Chains That Act as Neuroinflammation Inhibitors[J]. ACS CHEMICAL NEUROSCIENCE,2016,7(3):305-315.
APA	Chen, Hongli.,Han, Chaojun.,Wu, Jing.,Liu, Xiaoyu.,Zhan, Yuexiong.,...&Jiang, Biao.(2016).Accessible Method for the Development of Novel Sterol Analogues with Dipeptide-like Side Chains That Act as Neuroinflammation Inhibitors.ACS CHEMICAL NEUROSCIENCE,7(3),305-315.
MLA	Chen, Hongli,et al."Accessible Method for the Development of Novel Sterol Analogues with Dipeptide-like Side Chains That Act as Neuroinflammation Inhibitors".ACS CHEMICAL NEUROSCIENCE 7.3(2016):305-315.