In vivoandin vitroanti-inflammatory effects of a novel derivative of icariin

Abstract

Icariin is the major active constituent of Epimedii Herba. Our recent study showed that icariin displayed anti-inflammatory potential. One novel derivate of icariin is 3,5,7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)-flavone (ICT). Little is known about ICT's pharmacological activities. In our study, the anti-inflammatory properties of ICT were evaluated. Murine RAW264.7 cells and C57BL/6J mice stimulated by lipopolysaccharide (LPS) was used as in vitro and in vivo inflammatory model, respectively. Our data showed that ICT (1-100 μg/mL) significantly inhibited LPS-induced tumor necrosis factor-α (TNF-α), nitric oxide (NO), prostaglandin E2 (PGE2) production in vitro. These effects did not depend on cytotoxicity. The in vivo assay displayed that pretreatment of C57BL/6J mice with ICT (25-100 mg/kg, by gavage) for 3 days decreased LPS-induced serum levels of TNF-α, PGE2, and neutrophils CD11b expression dose-dependently. Furthermore, our data suggested that ICT reduced NO and PGE2 levels by inhibiting inducible NO synthase and cyclooxygenase-2 protein expression. To our knowledge, it is the first time that the anti-inflammatory effects of ICT have been evaluated.

Attenuation of LPS-induced inflammation by ICT, a derivate of icariin, via inhibition of the CD14/TLR4 signaling pathway in human monocytes

“…Similarly, a dose-dependent impairment of TNF-α production was observed in PBMC and human primary monocytes. Our previous MTT assay has verified that the anti-inflammatory effects of ICT did not depend on the cytotoxity [22]. In this study, no significant cell death was observed after the cells were treated with ICT at various concentrations (Fig.…”

“…Recent studies demonstrated that icariin could be used to treat septic arthritis and brain dysfunction induced by LPS [27,28]. In our previous study, we demonstrated that ICT, a novel flavonoid derivative of icariin, had similar effects to icariin in murine macrophages [22]. In the current study, we demonstrate that ICT blocks the ability of THP-1 monocytic cell line to produce TNF-α in response to LPS stimulation.…”

“…Furthermore, our group has demonstrated that ICT, the icariin derivative, can have similar effects in murine macrophages [22]. It is unknown whether this same effect occurs in human cells.…”

“…Several of its components have been studied, with icariin being identified as the main active ingredient [14,21]. Recently, we described a novel derivative of icariin named, 3, 5, 7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)-flavone (ICT) which displayed antiinflammatory potential in murine macrophage cell lines as well as in a mouse model of inflammation [22]. In the present study, we evaluated the anti-inflammatory potential of ICT in human innate immune cells and investigated its effects on the CD14/TLR4 signaling pathway.…”

Targeting Tumor Microenvironment: Effects of Chinese Herbal Formulae on Macrophage‐Mediated Lung Cancer in Mice

“…The above formula is frequently used in treatment of chronic inflammatory diseases in the respiratory system and immunocompromised diseases in TCM. Increasing evidence revealed that QRHX and its components, extracts, and derivative have the ability of anticancer and anti-inflammation [12–14]. Nevertheless, there are no reports which concerned the alleviated effects of QRHX on macrophage-mediated lung cancer.…”