Pilot in Vivo Structur-Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O-6-Methylguanine and Lung Tumor in A/J Mice

摘要

(+)-Dihydromethysticin was recently identified as a promising, lung cancer chemopreventive agent, while (+)-dihydrokavain was completely ineffective. A pilot in vivo structure activity relationship (SAR) was explored, evaluating the efficacy of its analogs in blocking 4-(methylnitrosamin6)-1(3-pyridyl)-1-butanone-induced short-term O-6-methylguanine and long-term adenoma formation in the lung tissues in A/J mice. Both results revealed cohesive SARs, demonstrating that the methylenedioxy functional group in DHM is essential while the lactone functional group tolerates modifications.