期刊
PHYSIOLOGICAL RESEARCH
卷 66, 期 4, 页码 687-693出版社
ACAD SCIENCES CZECH REPUBLIC, INST PHYSIOLOGY
DOI: 10.33549/physiolres.933516
关键词
Setipiprant; Asthma; Aldose reductase inhibition; Inflammation; Androgenic alopecia
类别
资金
- Slovak Research and Development Agency [APVV-15-0455]
- SAS TUBITAK Joint Project [JRP 2015/7]
- [VEGA 2/0041/15]
- [VEGA 2/0033/14]
The aim of this study was to investigate aldose reductase inhibitory action of setipiprant as a potential additional mechanism contributing to its anti-inflammatory action. Aldose reductase activity was determined by spectrophotometric measuring of NADPH consumption. Setipiprant was found to inhibit aldose reductase/NADPH-mediated reduction of 4-hydroxynonenal, 4-hydroxynonenal glutathione and prostaglandin H2 substrates, all relevant to the process of inflammation. Molecular modeling simulations into the aldose reductase inhibitor binding site revealed an interaction pattern of setipiprant. Considering multifactorial etiology of inflammatory pathologies, it is suggested that, in addition to the antagonizing prostaglandin D2 receptor, inhibition of aldose reductase may contribute to the reported anti-inflammatory action of setipiprant.
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