Anti-inflammatory effects of luteolin: A review of in vitro, in vivo, and in silico studies

다국어 초록 (Multilingual Abstract)

<P><B>Abstract</B></P> <P><B>Ethnopharmacological relevance</B></P> <P>Luteolin (3′, 4′, 5,7-tetrahydroxyflavone) has been identified as commonly present in plants. Plants with a high luteolin content have been used ethnopharmacologically to treat inflammation-related symptoms. Both isolated luteolin and extracts from luteolin-rich plants have been studied using various models and exhibited anti-inflammatory activity.</P> <P><B>Aim of the review</B></P> <P>This paper uses recent research findings with a broad range of study models to describe the anti-inflammatory activity of luteolin, particularly its mechanisms at the molecular level; provide guidance for future research; and evaluate the feasibility of developing luteolin into an anti-inflammatory drug.</P> <P><B>Materials and methods</B></P> <P>We summarize reports about the anti-inflammatory activity of luteolin published since 2009, which we found in MEDLINE/PubMed, Scopus, Web of Knowledge, and Google Scholar. To acquire broad information, we extended our search to online FDA documents.</P> <P><B>Results</B></P> <P>Luteolin is a flavonoid commonly found in medicinal plants and has strong anti-inflammatory activity <I>in vitro</I> and <I>in vivo</I>. Some of its derivatives, such as luteolin-7-O-glucoside, have also shown anti-inflammatory activity. The action mechanism of luteolin varies, but Src in the nuclear factor (NF)-κB pathway, MAPK in the activator protein (AP)− 1 pathway, and SOCS3 in the signal transducer and activator of transcription 3 <B>(</B>STAT3) pathway are its major target transcription factors. A clinical trial with a formulation containing luteolin showed excellent therapeutic effect against inflammation-associated diseases.</P> <P><B>Conclusion</B></P> <P> <I>In silico</I>, <I>in vitro</I>, <I>in vivo</I>, and clinical studies strongly suggest that the major pharmacological mechanism of luteolin is its anti-inflammatory activity, which derives from its regulation of transcription factors such as STAT3, NF-κB, and AP-1. Much work remains to ensure the safety, quality, and efficacy of luteolin before it can be used to treat inflammation-related diseases in humans.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>