Synthesis and Anti-Inflammatory Activity of 1-Methylhydantoin Cinnamoyl Imides

被引:6
作者
Wang, Shihan [1 ]
Ji, Li [1 ]
Zhang, Dongxue [1 ]
Guo, Hongye [2 ]
Wang, Yongsheng [2 ]
Li, Wei [1 ]
机构
[1] Jilin Agr Univ, Coll Chinese Med Mat, Changchun 130118, Peoples R China
[2] Jilin Univ, Sch Pharmaceut Sci, Changchun 130021, Peoples R China
关键词
Oviductus Ranae; natural product; inflammatory; 1-Methylhydantoin; trans-cinnamic acid; ACID; DERIVATIVES; INFLAMMATION; ANTAGONISTS; INHIBITION; DISCOVERY; MOLECULES; ESTERS;
D O I
10.3390/molecules27238481
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In this study, 1-methylhydantoin cinnamic imides were synthesized from 1-methylhydantoin and trans-cinnamic acid, and their anti-inflammatory activity was investigated. The anti-inflammatory activity in vitro was evaluated by measuring the contents of NO, TNF-alpha and IL-1 beta in the supernatant of RAW264.7 cells stimulated by LPS. The cytotoxicity of 1-methylhydantoin cinnamoyl imides on RAW264.7 cells was detected using the CCK-8 method. The results showed that compounds 2 and 4 can significantly inhibit the release of NO and reduce the secretion of TNF-alpha and IL-1 beta. Compound 3 inhibited the production of TNF-alpha. The inhibition rate of COX was evaluated in vitro. The in vivo anti-inflammatory activities of the five compounds were evaluated by establishing an animal model of xylene ear swelling. The results showed that 1-methylhydantoin cinnamic imides could alleviate xylene-induced ear edema in mice in a dose-dependent manner. Among them, the effect of compound 5 was the most significant. Under the action of high dosage, its ear swelling inhibition rate was as high as 52.08%.
引用
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页数:12
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