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Review
. 2021 Aug 20:2021:6851798.
doi: 10.1155/2021/6851798. eCollection 2021.

Biological Activity, Hepatotoxicity, and Structure-Activity Relationship of Kavalactones and Flavokavins, the Two Main Bioactive Components in Kava (Piper methysticum)

Yingli Wang  1 , Chao Su  1 , Bo Zhang  1 , Yang Niu  1 , Ruru Ren  1 , Xiaojun Zhao  1 , Lingling Yang  1 , Wannian Zhang  1 , Xueqin Ma  1
Affiliations
Review

Biological Activity, Hepatotoxicity, and Structure-Activity Relationship of Kavalactones and Flavokavins, the Two Main Bioactive Components in Kava (Piper methysticum)

Yingli Wang et al. Evid Based Complement Alternat Med. .

Abstract

Kava (Piper methysticum Forst) is a popular and favorable edible medicinal herb which was traditionally used to prepare a nonfermented beverage with relaxant beneficial for both social and recreational purposes. Numerous studies conducted on kava have confirmed the presence of kavalactones and flavokawains, two major groups of bioactive ingredients, in this miraculous natural plant. Expectedly, both kavalactone and flavokawain components exhibited potent antianxiety and anticancer activities, and their structure-activity relationships were also revealed. However, dozens of clinical data revealed the hepatotoxicity effect which is indirectly or directly associated with kava consumption, and most of the evidence currently seems to point the compounds of flavokawains in kava were responsible. Therefore, our aim is to conduct a systematic review of kavalactones and flavokawains in kava including their biological activities, structure-activity relationships, and toxicities, and as a result of our systematic investigations, suggestions on kava and its compounds are supplied for future research.

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Conflict of interest statement

The authors have no conflicts of interest.

Figures

Figure 1
Figure 1
Chemical structures of compounds 1–29.
Figure 2
Figure 2
Content of seven major kavalactones in kava with different extracting solvents (mg/g extract).
Figure 3
Figure 3
Chemical structures of compounds 30–37.
Figure 4
Figure 4
The pharmacological activities of kava.
Figure 5
Figure 5
The proposed model of the FKA-mediated anti-inflammation via nuclear factor-κB (NF-κB) blockade and AP-1 activation in RAW 264.7 macrophages.
Figure 6
Figure 6
Proposed diagrams of DHM-induced G0/G1 phase arrest and apoptosis through phosphoinositide 3-kinase (PI3K)/nucleotide-oligomerization domain-like receptor subfamily C3 (NLRC3) signaling pathway inhibition in colorectal cancer cells.
Figure 7
Figure 7
The structure modification of kavalactone.
Figure 8
Figure 8
The structure-activity relationships of flavokawain.
See this image and copyright information in PMC

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