College of Science and Technology, Nihon University, 1-5-1 Kandasurugadai, Chiyoda, Tokyo 101-0062, Japan.
Department of Biomedical Information Engineering, Graduate School of Medical Science, Yamagata University, 2-2-2 Iidanishi, Yamagata 990-9585, Japan.
Molecules. 2017 Nov 22;22(11):2030. doi: 10.3390/molecules22112030.
The increased number of patients with type 2 diabetes (T2D) has become a worldwide problem, and insulin sensitizers such as thiazolidinediones (TZDs) are used as therapeutic agents. We found that extracts of L. (), a medicinal plant from Myanmar, induced adipogenesis similar to rosiglitazone (ROS), which is a TZD, in 3T3-L1 preadipocytes. In the present study, we attempted to isolate from those compounds that showed ROS-like effects. Among the extracts of hexane, ethyl acetate, and methanol obtained from , the ethyl acetate extract with the strongest ROS-like effects was purified by various chromatographic methods to obtain three known compounds: vitexilactone (), vitexicarpin () and oleanolic acid (). Among the isolated compounds, the ROS-like action of was the strongest. The effects of on 3T3-L1 cells during adipogenesis were compared with those of ROS. Both and ROS increased lipid accumulation, the expression of adiponectin and GLUT4 in the cell membrane and decreased both the size of adipocytes and the phosphorylation of IRS-1, ERK1/2 and JNK in 3T3-L1 cells. In contrast, unlike ROS, the induction of proteins involved in lipogenesis was partial. ROS-like effects of in 3T3-L1 cells were suppressed by the addition of bisphenol A diglycidyl ether (BADGE), one of a peroxisome proliferator-activated receptor γ (PPARγ) antagonists, suggesting that the action of on adipocytes is mediated by PPARγ. From the results of the present study, it can be concluded that is a novel insulin sensitizer candidate.
2 型糖尿病（T2D）患者数量的增加已成为全球性问题，噻唑烷二酮类（TZDs）等胰岛素增敏剂被用作治疗药物。我们发现，来自缅甸药用植物的提取物（）在 3T3-L1 前脂肪细胞中诱导脂肪生成的作用类似于罗格列酮（ROS），即 TZD。在本研究中，我们试图从 中分离出具有类似 ROS 作用的化合物。从 中得到的正己烷、乙酸乙酯和甲醇提取物中，具有最强 ROS 样作用的乙酸乙酯提取物通过各种色谱方法进行纯化，得到三种已知化合物：牡荆素内酯（）、牡荆素（）和齐墩果酸（）。在所分离的化合物中，的 ROS 样作用最强。与 ROS 相比，对 3T3-L1 细胞在脂肪生成过程中的作用。和 ROS 均增加了脂质积累、细胞内膜上脂联素和 GLUT4 的表达，降低了脂肪细胞的大小和 IRS-1、ERK1/2 和 JNK 的磷酸化。相比之下，与 ROS 不同，脂生成相关蛋白的诱导是部分的。在 3T3-L1 细胞中，的 ROS 样作用被一种过氧化物酶体增殖物激活受体 γ（PPARγ）拮抗剂双酚 A 二缩水甘油醚（BADGE）的添加所抑制，表明在脂肪细胞中起作用的是 PPARγ。从本研究的结果可以得出结论，是一种新型的胰岛素增敏剂候选物。
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