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

我们主要关注阿育吠陀传统医学，通过过氧化物酶体增殖激活受体（PPAR）的表达，研究了治疗生活方式相关疾病的有效成分。结果发现，产自印度和东南亚的山柰（Kaempferia parviflora）、莲花（Nelumbo nucifera）的therhi茎提取物和成分，以及沙巴胡椒（Piper chaba）果实的酰胺成分对3T3-L1脂肪细胞具有类似PPARγ激动剂的作用。活性成分3,5,7,3 ',4 ' -五-甲氧基黄酮醇，n -去甲花籽碱，胡椒明及其衍生物均能增强PPARγ2， C/EBPα和β mRNA，但对PPARγ水平的拮抗作用较弱。此外，在给药哌隆明和逆转录酶甲酰胺A后测定小鼠血浆浓度，并合成逆转录酶甲酰胺A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.