Jin Zhen, Yang Yao-Zhi, Chen Jian-Xin, Tang You-Zhi
Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.
J Pharm Pharmacol. 2017 Jul;69(7):865-874. doi: 10.1111/jphp.12714. Epub 2017 Mar 10.
Flavonoids are a class of compounds that having the benzo-γ-pyrone skeleton, which possess anti-inflammatory properties in vitro and in vivo. The aim of this study was to investigate the inhibition of two flavonoids 7-hydroxyflavone (HF) and 7,8-dihydroxyflavone (DHF) on the production of pro-inflammatory mediators in RAW264.7 cells activated by lipopolysaccharides (LPS).
For this purpose, we selected four pro-inflammatory mediators including nitric oxide (NO), prostaglandin E (PGE ), tumour necrosis factor-α (TNF-α) and interleukin-6 (IL-6) as markers to evaluate the anti-inflammatory activity of HF and DHF.
In this regard, we showed that HF and DHF dose-dependently reduced the production of NO, PGE , TNF-α and IL-6 through downregulating mRNA expression of inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX2), TNF-α and IL-6, respectively. Moreover, DHF generally possesses more efficient than HF in reducing these markers secretion in this study.
Consider together, these findings suggest that DHF and HF can inhibit LPS-induced inflammation via attenuating the production of NO, PGE , TNF-α and IL-6, indicating that they may be lead compounds for developing anti-inflammatory agent.
黄酮类化合物是一类具有苯并-γ-吡喃酮骨架的化合物,在体外和体内均具有抗炎特性。本研究的目的是研究两种黄酮类化合物7-羟基黄酮(HF)和7,8-二羟基黄酮(DHF)对脂多糖(LPS)激活的RAW264.7细胞中促炎介质产生的抑制作用。
为此,我们选择了四种促炎介质,包括一氧化氮(NO)、前列腺素E(PGE)、肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)作为标志物,以评估HF和DHF的抗炎活性。
在这方面,我们表明HF和DHF通过分别下调诱导型一氧化氮合酶(iNOS)、环氧化酶2(COX2)、TNF-α和IL-6的mRNA表达,剂量依赖性地降低了NO、PGE、TNF-α和IL-6的产生。此外,在本研究中,DHF在减少这些标志物分泌方面通常比HF更有效。
综合考虑,这些发现表明DHF和HF可以通过减弱NO、PGE、TNF-α和IL-6的产生来抑制LPS诱导的炎症,表明它们可能是开发抗炎药物的先导化合物。