苦瓜提取物苦瓜素对人过氧化物酶体增殖物激活受体 δ 启动子的激活作用。
Activating effect of momordin, extract of bitter melon (Momordica Charantia L.), on the promoter of human PPARdelta.
机构信息
Department of Diabetes and Endocrinology, Saitama Medical University, Japan.
出版信息
J Atheroscler Thromb. 2009;16(6):888-92. doi: 10.5551/jat.2790. Epub 2009 Dec 22.
AIM
Bitter melon (Momordica charantia L.) is a common vegetable grown in Okinawa that has also been used recently in medicine for the treatment of diseases such as diabetes, hypertension, and dyslipidemia. Among Bitter melon extracts compounds, we focused on an extract known as momordin in the present study, to examine its effect on peroxisome-proliferator activated-receptor (PPAR) delta (also called PPARdelta in rodents) expression and promoter activity of the human PPARdelta gene.
METHODS
A human PPARdelta promoter-reporter plasmid was made as a template from a BAC CLONE (RPCI-11C) containing a -3076 bp (BglI site) +74 bp (EcoRI site) sequence. Luciferase assay of PPARdelta promoter activity was performed using HepG2 cells.
RESULTS
10 and 25 nM Momordin significantly increased the expression of PPARdelta mRNA 1.5-fold (relative to the control). Moreover, 10 and 25 nM Momordin significantly increased PPARdelta promoter activity in a dose-dependent manner, reaching more than 1.5-fold relative to the control.
CONCLUSION
Our present data obtained through successful cloning of the PPARdelta promoter demonstrate that PPARdelta production and activation are upregulated through PPARdelta promoter activity following momordin treatment.
目的
苦瓜（Momordica charantia L.）是冲绳常见的一种蔬菜，最近也被用于治疗糖尿病、高血压和血脂异常等疾病。在苦瓜提取物的化合物中，本研究集中研究了一种称为 momordin 的提取物，以检查其对过氧化物酶体增殖物激活受体（PPAR）delta（在啮齿动物中也称为 PPARdelta）表达和人 PPARdelta 基因启动子活性的影响。
方法
使用包含-3076 bp（BglI 位点）+74 bp（EcoRI 位点）序列的 BAC CLONE（RPCI-11C）作为模板，制备人 PPARdelta 启动子报告质粒。使用 HepG2 细胞进行 PPARdelta 启动子活性的荧光素酶测定。
结果
10 和 25 nM Momordin 使 PPARdelta mRNA 的表达显著增加了 1.5 倍（相对于对照）。此外，10 和 25 nM Momordin 以剂量依赖性方式显著增加 PPARdelta 启动子活性，相对于对照增加了 1.5 倍以上。
结论
我们通过成功克隆 PPARdelta 启动子获得的现有数据表明，Momordin 处理后，通过 PPARdelta 启动子活性上调 PPARdelta 的产生和激活。
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