Terminalia 属植物的成分可增加 PPARα 和 PPARγ 的水平，并刺激葡萄糖摄取，而不增强脂肪细胞分化。
Constituents from Terminalia species increase PPARα and PPARγ levels and stimulate glucose uptake without enhancing adipocyte differentiation.
机构信息
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, School of Pharmacy, University of Mississippi, MS 38677, USA.
出版信息
J Ethnopharmacol. 2013 Sep 16;149(2):490-8. doi: 10.1016/j.jep.2013.07.003. Epub 2013 Jul 10.
ETHNOPHARMACOLOGICAL RELEVANCE
The fruits of Terminalia bellerica Roxb. (Combretaceae) and T. chebula Retz. (Combretaceae) are important components of triphala, a popular Ayurvedic formulation, for treating diabetes in Indian traditional medicine.
AIM OF THE STUDY
The aim of this study was to evaluate the effects of the constituents of T. bellerica and T. chebula fruit extracts on PPARα and PPARγ signaling/expression, cellular glucose uptake and adipogenesis.
MATERIALS AND METHODS
PPARα and PPARγ signaling and expression (luciferase assay and western blot) and the insulin-stimulated uptake of 2-NBDG were determined in HepG2 cells. The effects on adipogenesis were determined in 3T3-L1 cells by Oil red O staining and measurement of lipid content by AdipoRed reagent.
RESULTS
Out of the 20 compounds, two ellagitannins, chebulagic acid (1) and corilagin (2), and three gallotannins, 2,3,6-tri-O-galloyl-β-D-glucose (3), 1,2,3,6-tetra-O-galloyl-β-D-glucose (4), and 1,2,3,4,6-penta-O-galloyl-β-D-glucose (5), showed the enhancement of PPARα and/or PPARγ signaling. Two of the gallotannins (4 and 5) also increased PPARα and PPARγ protein expression, while all three (3-5) enhanced insulin-stimulated glucose uptake into HepG2 cells. Compound 1,2,3,6-tetra-O-galloyl-β-D-glucose (4) was the most potent in increasing cellular glucose uptake (9.92-fold increase at 50 μM). In the test for adipogenesis, 3-5 did not enhance the differentiation of 3T3-L1 preadipocytes but inhibited the adipogenic effect of rosiglitazone.
CONCLUSION
Three gallotannins (3-5) from Terminalia fruits acting as enhancers of both PPARα and PPARγ signaling increased insulin-stimulated glucose uptake without inducing the adipogenesis, with 1,2,3,6-tetra-O-galloyl-β-D-glucose (4) being the most effective in stimulating glucose uptake and 1,2,3,4,6-penta-O-galloyl-β-D-glucose (5) being most effective in increasing PPAR protein expression.
民族药理学相关性
诃子（使君子科）和诃子（使君子科）的果实是 Triphala 的重要成分，Triphala 是一种在印度传统医学中用于治疗糖尿病的流行阿育吠陀配方。
研究目的
本研究旨在评估诃子和诃子果实提取物成分对 PPARα 和 PPARγ信号/表达、细胞葡萄糖摄取和脂肪生成的影响。
材料和方法
在 HepG2 细胞中测定 PPARα 和 PPARγ信号和表达（荧光素酶测定和 Western blot）以及胰岛素刺激的 2-NBDG 摄取。通过油红 O 染色和 AdipoRed 试剂测量脂质含量来确定脂肪生成的影响在 3T3-L1 细胞中。
结果
在 20 种化合物中，两种鞣花酸，诃子酸（1）和诃子酸（2）和三种没食子鞣质，2,3,6-三-O-没食子酰基-β-D-葡萄糖（3），1,2,3,6-四-O-没食子酰基-β-D-葡萄糖（4）和 1,2,3,4,6-五-O-没食子酰基-β-D-葡萄糖（5），表现出增强 PPARα 和/或 PPARγ 信号的作用。两种没食子鞣质（4 和 5）还增加了 PPARα 和 PPARγ 蛋白表达，而所有三种（3-5）都增强了胰岛素刺激的 HepG2 细胞内葡萄糖摄取。化合物 1,2,3,6-四-O-没食子酰基-β-D-葡萄糖（4）在增加细胞内葡萄糖摄取方面最有效（在 50 μM 时增加 9.92 倍）。在脂肪生成测试中，3-5 并未增强 3T3-L1 前脂肪细胞的分化，但抑制了罗格列酮的脂肪生成作用。
结论
三种来自诃子果实的没食子鞣质（3-5）作为 PPARα 和 PPARγ 信号的增强剂，增加了胰岛素刺激的葡萄糖摄取而不诱导脂肪生成，其中 1,2,3,6-四-O-没食子酰基-β-D-葡萄糖（4）在刺激葡萄糖摄取方面最有效，1,2,3,4,6-五-O-没食子酰基-β-D-葡萄糖（5）在增加 PPAR 蛋白表达方面最有效。
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