Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo.
Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo.
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DOI：
10.1080/14756366.2022.2124983
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发表时间：
2022-12
影响因子：
5.6
通讯作者：
Liu, Xinhua
中科院分区：
文献类型：
--
作者：
Xiao, Yun;Yan, Yaoyao;Du, Juncheng;Feng, Xiaoxiao;Zhang, Famin;Han, Xu;Hu, Yong;Liu, Xinhua
设计、合成和优化具有较好抗炎活性的类黄酮衍生物具有重要意义。本研究旨在设计和合成一系列具有抗炎作用的新型2-苯基- 4h -铬-4-酮化合物；其中，化合物8被发现为最佳化合物。然后，在体内进行了化合物8对TLR4/MAPK信号通路的影响，结果表明化合物8可以下调NO、IL-6、TNF-α的表达，并通过抑制TLR4/MAPK通路抑制lps诱导的炎症。此外，化合物8通过lps诱导的炎症性疾病小鼠模型在体内减少炎症。结果表明，化合物8通过调控TLR4/MAPK通路具有抗炎症的潜力，可进一步用于药物开发。
It is significant to design, synthesise and optimise flavonoid derivatives with better anti-inflammatory activity. This study aims to design and synthesise a series of novel 2-phenyl-4H-chromen-4-one compounds with anti-inflammatory; among them, compound 8 was discovered as the best one. And then, the effects of compound 8 on the TLR4/MAPK signalling pathway was carried out in vivo, the results indicated that compound 8 could downregulate NO, IL-6, and TNF-α expression, and suppress LPS-induced inflammation by inhibiting the TLR4/MAPK pathways. Furthermore, compound 8 reduced inflammation by a mouse model of LPS-induced inflammatory disease in vivo. The results suggest that compound 8 has the potential against inflammation through regulating TLR4/MAPK pathway and can be assessed further for drug development.
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影响因子：
7.3
作者：
Chen, Liu Zeng;Zhang, Xing Xing;Liu, Xin Hua
通讯作者：
Liu, Xin Hua
DOI：
10.1016/j.bbrc.2018.09.173
发表时间：
2018-11-02
影响因子：
3.1
作者：
Saiki, Papawee;Nakajima, Yoshihiro;Miyazaki, Koyomi
通讯作者：
Miyazaki, Koyomi
影响因子：
7
作者：
Serafini, Mauro;Peluso, Ilaria;Raguzzini, Anna
通讯作者：
Raguzzini, Anna
DOI：
10.1007/s00018-020-03656-y
发表时间：
2021-03
期刊：
Cellular and molecular life sciences : CMLS
影响因子：
--
作者：
Ciesielska A;Matyjek M;Kwiatkowska K
通讯作者：
Kwiatkowska K
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DOI：
10.1016/j.niox.2016.11.004
发表时间：
2017-02-28
期刊：
Nitric oxide : biology and chemistry
影响因子：
--
作者：
Poulos TL;Li H
通讯作者：
Li H