Purpose: Chalcones are precursors of flavonoids with a wide range of pharmacological activities. This study evaluates the anti-inflammatory effect of indole based chalcone derivative (2E)-3-(4-bromophenyl)-1-(1H-indol-3-yl) prop-2-en-1-one (IC9) on lipopolysaccharide (LPS) activated murine macrophages RAW264.7 cells and carrageenan-induced acute model in rats.Materials and methods: LPS-treated RAW264.7 cell lines and carrageenan-induced animal model were employed to evaluate the anti-inflammatory activity of IC9. The cell cytotoxicity studies were carried out by MTT assay. Reactive oxygen species (ROS) production and other inflammatory markers such as prostaglandin E2 (PGE2), nitric oxide (NO) as well as cyclooxygenase-2 (COX-2) activity were determined using ELISA. The RT-PCR was performed to determine mRNA expressions in the case of inducible nitric oxide synthase (iNOS), COX-2, Toll-like receptor-4 (TLR-4) and also nuclear translocation of NF-κB activity.Results: LPS-activated RAW264.7 cells showed an increased level of ROS generation and other inflammatory markers such as PGE2, NO level and COX-2 activity. Expression of iNOS, COX- 2 and TLR-4 mRNA expression were also up-regulated along with nuclear translocation of NF-κB. On IC9 supplementation, all the above parameters of LPS-activated cells were found to be reversed, resembling the control group. Moreover, IC9 significantly inhibited paw swelling and exhibited maximum inhibition of 78.45% at low dose of 7.5 mg/kg.bwt.Conclusions: The targeting anti-inflammatory efficacy and profound NF-κB sensitive transcriptional regulatory mechanism of IC9 accounts for its effective anti-inflammatory action.

中文翻译：

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合成的吲哚基查尔酮（2E）-3-（4-溴苯基）-1-（1H-吲哚-3-基）丙-2-烯-1-酮的抗炎作用：体内和体外研究。

目的：查耳酮是类黄酮的前体，具有广泛的药理活性。这项研究评估了吲哚基查尔酮衍生物（2E）-3-（4-溴苯基）-1-（1H-吲哚-3-基）丙-2-烯-1-酮（IC9）对脂多糖的抗炎作用（LPS）激活鼠巨噬细胞RAW264.7细胞和角叉菜胶诱导的急性大鼠模型。材料和方法：用LPS处理的RAW264.7细胞系和角叉菜胶诱导的动物模型评估IC9的抗炎活性。通过MTT测定法进行细胞毒性研究。使用ELISA测定了活性氧（ROS）的产生和其他炎症标记物，例如前列腺素E2（PGE2），一氧化氮（NO）以及环氧合酶2（COX-2）的活性。进行RT-PCR来测定诱导型一氧化氮合酶（iNOS），COX-2，Toll样受体4（TLR-4）以及NF-κB活性的核易位的mRNA表达。激活的RAW264.7细胞显示出更高水平的ROS生成水平和其他炎症标记，例如PGE2，NO水平和COX-2活性。iNOS，COX-2和TLR-4 mRNA的表达也随着NF-κB的核转位而上调。在补充IC9时，发现上述所有LPS激活细胞的参数均被逆转，类似于对照组。此外，IC9在7.5 mg / kg.bwt的低剂量下可显着抑制爪肿胀并最大抑制78.45％。