4 research outputs found
Pilot in Vivo Structure–Activity Relationship of Dihydromethysticin in Blocking 4‑(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced <i>O</i><sup>6</sup>‑Methylguanine and Lung Tumor in A/J Mice
(+)-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-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced short-term <i>O</i><sup>6</sup>-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