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J Ethnopharmacol. 2018 Oct 28;225:342-358. doi: 10.1016/j.jep.2018.05.019. Epub 2018 May 22.

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

Author information

1
Department of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Republic of Korea.
2
School of Systems Biomedical Science, Soongsil University, Seoul 06978, Republic of Korea. Electronic address: kimmy@ssu.ac.kr.
3
Department of Genetic Engineering, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address: jaecho@skku.edu.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE:

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.

AIM OF THE REVIEW:

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.

MATERIALS AND METHODS:

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.

RESULTS:

Luteolin is a flavonoid commonly found in medicinal plants and has strong anti-inflammatory activity in vitro and in vivo. 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 (STAT3) pathway are its major target transcription factors. A clinical trial with a formulation containing luteolin showed excellent therapeutic effect against inflammation-associated diseases.

CONCLUSION:

In silico, in vitro, in vivo, 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.

KEYWORDS:

Flavonoid; Inflammatory diseases; Inflammatory signaling; Luteolin; Luteolin (PubChem CID: 5280445); Luteolin-5-O-glucoside (PubChem CID: 44258061); Luteolin-6-C-glucoside (PubChem CID: 49852298); Luteolin-7-O-glucoside (PubChem CID: 5280637); Luteolin-8-C-glucoside (PubChem CID: 5281675)

PMID:
29801717
DOI:
10.1016/j.jep.2018.05.019
[Indexed for MEDLINE]

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