Anti-inflammatory Effects of Flavokavain C from Kava (Piper methysticum) Root in the LPS-induced Macrophages

Abstract

Kava (Piper methysticum, P. methysticum) is used as traditional herbal medicine for urogenital diseases, rheumatisms, gastrointestinal problems, respiratory irritations, and pulmonary pains. We identified a flavokavain C (FKC) from P. methysticum, which showed anti-inflammatory activity on nuclear factor κB (NF-κB)-dependent nitric oxide (NO) production and expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. FKC inhibited accumulation of reactive oxygen species (ROS), such as hydrogen peroxide, and was able to dose-dependently reduce the LPS-induced NO production and the expression of various inflammation-associated genes (iNOS, IL-1β, IL-6) through inhibition of NF-κB and MAPKs (ERK and JNK). In conclusion, these results indicate that FKC may have the potential to prevent inflammation process including NF-κB and MAPKs pathways, and it could be applicable to functional cosmetics for anti-inflammation and antioxidant properties.

Kavalactones and Flavokavins Profiles Contribute to Quality Assessment of Kava (Piper methysticum G. Forst.), the Traditional Beverage of the Pacific

“…Some studies suggest that FKA and FKB are cytotoxic to cancer cells [9][10][11] and that FKB is a major hepatotoxin in organic kava extracts [12], although others have questioned whether the levels in these extracts are high enough to produce hepatotoxicity [13,14]. FKC has been shown to have the potential to prevent the inflammation process with antioxidant properties [15]. However, when cytotoxicity against human lung adenocarcinoma A549 cancer cells was tested with kava extracts, FKA and FKB were found to be the major but not sole compounds responsible for the extract toxicity while KLs were less likely to be involved [16].…”