Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava's chemopreventive activity.
Nuclear factor-kappaB (NF-kappaB) is a transcription factor that plays an essential role in cancer development. The results of our recent chemopreventive study demonstrate that kava, a beverage in the South Pacific Islands, suppresses NF-kappaB activation in lung adenoma tissues, potentially a mechanism responsible for kava's chemopreventive activity. Methysticin is identified as a potent NF-kappaB inhibitor in kava with minimum toxicity. Other kava constituents, including four kavalactones of similar structures to methysticin, demonstrate minimum activities in inhibiting NF-kappaB.
Shaik
Ahmad Ali
AA
Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard St SE, Minneapolis, MN 55455, United States.
Hermanson
David Lee
DL
Xing
Chengguo
C
D016588:Anticarcinogenic Agents / Q000737:chemistry; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D020901:Kava / Q000737:chemistry*; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011714:Pyrans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
D016588:Anticarcinogenic Agents; D000972:Antineoplastic Agents, Phytogenic; D016328:NF-kappa B; D011714:Pyrans; C076881:methysticin