中文摘要
前期研究从杜鹃花科植物美丽马醉木枝叶的镇痛活性部位中获取了15个木藜芦烷型二萜类成分,8个为结构新颖的化合物。活性筛选发现,8个化合物表现出显著的镇痛活性(P < 0.01),其中3个化合物镇痛活性更加显著,在0.08 mg/kg剂量下抑制率分别能达到37.6%、49.8%和56.8%。而对照品吗啡在十倍的剂量下才能达到相同的镇痛效果。.本项目拟在此基础上,将化学筛选和活性筛选集成应用,从美丽马醉木(Pieris formosa)的根和茎、马醉木(P. japonica)的根和枝叶的镇痛活性部位中快速识别、锁定二萜类成分,进而针对性地获取可能是新颖结构的活性二萜类化合物,并测定它们的化学结构。对获得的化合物进行体内外镇痛活性的测定,根据活性测定结果和化合物的结构特征,分析初步的构效关系和初步作用机制研究,优选出1-2个结构新颖、活性显著的创新药物先导化合物,为创制新型镇痛药物奠定基础。
英文摘要
The leaves and branches of Pieris formosa are used to treat tinea and scabies as a traditional Chinese medicine. Previously several diterpenoids with analgesic activity were isolated from the active ethyl acetate extract of the twigs of P. formosa. Therefore, on the chemical screen and the activity screen, we plan to carry out the investigation of two species in the genus Pieris (roots and stems of P. formosa, roots and twigs of P. japonica) to find 1-2 active diterpenoids with novel structures and significant analgesic activity to treat pain.
