Kamebakaurin |
Catalog No.GC39093 |
Kamebakaurin es un compuesto natural aislado de Isodon japonicus.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 73981-34-7
Sample solution is provided at 25 µL, 10mM.
Kamebakaurin, a compound of kaurane diterpenes was isolated from traditional Chinese medicinal plant Isodon excia. It is a potent inhibitor of NF-kappaB activation by directly targeting DNA-binding activity of p50[6].
Treated with different concentrations of kamebakaurin (0-30µM;24 h), The activity of HCT116 cells did not decrease significantly, but Kamebakaurin inhibits HIF-1α protein expression in cells [1]. Kamebakaurin (0.1, 1.0, 5 µM) significantly inhibited the LPS-induced production of nitric oxide (NO) in a concentration-dependent fashion in activated microglial cells[2]. Kamebakaurin (0-500ng/ml;4h)dose-dependently attenuated iNOS gene expression in LPS-activated dendritic cells (DCs). Kamebakaurin significantly inhibited the gene expression and protein production of the inflammatory cytokines TNF-α, IL-12, and IL-1β[4].
Kamebakaurin (50 mg/kg;40 days;p.o.) produced significant growth inhibition of HCT116 cells in tumor xenograft model[1]. 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[3]. Pretreatment with Kamebakaurin reduced the magnitude of Acetaminophen (N-acetyl-p-aminophenol, APAP)-induced increases in plasma levels of hepatic injury markers, lipid peroxidation, and inflammatory response[5].
References:
[1]. Wang KS, Ma J, et,al. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. Oncol Rep. 2016 Apr;35(4):2045-52. doi: 10.3892/or.2016.4576. Epub 2016 Jan 19. PMID: 26781327.
[2]. Kim BW, Koppula S, et,al.Anti-neuroinflammatory activity of Kamebakaurin from Isodon japonicus via inhibition of c-Jun NH?-terminal kinase and p38 mitogen-activated protein kinase pathway in activated microglial cells. J Pharmacol Sci. 2011;116(3):296-308. doi: 10.1254/jphs.10324fp. Epub 2011 Jun 25. PMID: 21705843.
[3]. Lee JH, Choi JK, et,al. Anti-inflammatory effect of kamebakaurin in in vivo animal models. Planta Med. 2004 Jun;70(6):526-30. doi: 10.1055/s-2004-827152. PMID: 15241890.
[4]. Kim JY, Kim HS, et,al. Inhibition of TAK1 by kamebakaurin in dendritic cells. Int Immunopharmacol. 2013 Jan;15(1):138-43. doi: 10.1016/j.intimp.2012.11.004. Epub 2012 Nov 15. PMID: 23159603.
[5]. Yoshioka H, Aoyagi Y, et,al. Suppressive effect of kamebakaurin on acetaminophen-induced hepatotoxicity by inhibiting lipid peroxidation and inflammatory response in mice. Pharmacol Rep. 2017 Oct;69(5):903-907. doi: 10.1016/j.pharep.2017.04.004. Epub 2017 Apr 12. PMID: 28624597.
[6]. Lee JH, et,al.Kaurane diterpene, kamebakaurin, inhibits NF-kappa B by directly targeting the DNA-binding activity of p50 and blocks the expression of antiapoptotic NF-kappa B target genes. J Biol Chem. 2002 May 24;277(21):18411-20. doi: 10.1074/jbc.M201368200. Epub 2002 Mar 4. PMID: 11877450.
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