Search for effective constituents for life-style related diseases through expression of PPAR

我们主要集中在阿育吠陀传统医学和研究的活性成分，通过表达过氧化物酶体增殖物激活受体（过氧化物酶体增殖物激活受体）的生活方式相关疾病的治疗。结果发现，在3 T3-L1脂肪细胞中，来自印度和东南亚栽培的山柰、荷花的根茎的提取物和成分以及来自胡椒果实的酰胺成分显示出PPARγ激动剂样作用。活性成分3，5，7，3 '，4'-五甲氧基黄酮醇、N-去甲荷叶碱、piperlonguminine及其衍生物对C/EBPα和β mRNA的表达有增强作用，但对PPARγ的激动作用较弱。此外，本研究还测定了小鼠灌胃给予piperlonguminine和retrofactorA后的血药浓度，并合成了retrofactorA及其衍生物，以寻找更有效的成分。

We mainly focused on Ayurvedic traditional medicine and have researched the active constituents for therapeutics of life-style related diseases through expression of peroxisome proliferator-activated receptor (PPAR). As the results, the extracts and the constituents from therhizomes of Kaempferia parviflora, flower of Nelumbo nucifera, and amide constituents from the fruit of Piper chaba, which are cultivated in India as well as southeast Asia, were found to show PPARγ agonist-like effects in 3T3-L1 adipocytes. The active constituents, 3,5,7,3’,4’-penta- mehoxyflavonol, N-nornuciferine, piperlonguminine, and their derivatives showed enhancement of PPARγ2, C/EBPα and β mRNA, although they had less agonistic activity at PPARγ levels. Furhermore,plasma concentrations were determined after administration of piperlonguminine and retrofractamide A in mice, together with synthesis of retrofactamide A and its derivatives to find more effectiveconstituents.