Anti-inflammatory effect of kamebakaurin in in vivo animal models

Planta medica
Jeong Hyung LeeJune Joon Lee

Abstract

We have identified kamebakaurin as an inhibitor of NF-KB and elucidated its molecular mechanism as a specific inhibitor in the DNA-binding activity of the p50 subunit of NF-KB. Here, we describe its anti-inflammatory activity in in vitro and in vivo models. Kamebakaurin dose-dependently inhibited not only the expression of inflammatory NF-KB target genes such as iNOS,COX-2, and TNF-x, but also the production of PGE2 and TNF-a in LPS-stimulated RAW264.7 cells. Moreover, in an air pouch model of inflammation, it suppressed the recruitment of neutrophils,production of TNF-a as well as PGE2 in the pouch exudates induced by carrageenan. In addition, kamebakaurin dose-dependently suppressed the inflammation in an adjuvant arthritis model. Oral administration of 20 mg/kg kamebakaurin resulted in the 75% decrease of paw volume. Taken together, kamebakaurin, a specific inhibitor of DNA-binding activity of the p50 subunit, is a valuable candidate for the intervention in NF-KB-dependent pathological conditions such as inflammation.

Citations

Aug 4, 2007·Science·Guokai ChenAdam Kuspa
Nov 20, 2012·International Immunopharmacology·Jee Youn KimSang-Bae Han
Jun 15, 2019·Mini Reviews in Medicinal Chemistry·Yuanzhen XuJinming Gao

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