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Oleanane-Type Triterpenoids of Aceriphyllum rossii and Their Diacylglycerol Acyltransferase-Inhibitory Activity.
- Source :
-
Planta Medica . 2015, Vol. 81 Issue 3, p228-234. 7p. - Publication Year :
- 2015
-
Abstract
- Six known triterpenoid compounds, 3-oxoolean-12-en-27-oic acid (1), gypsogenic acid (2), 3α-hydroxyolean-12-en-27-oic acid (3), 3β-hydroxyolean- 12-en-27-oic acid (4), aceriphyllic acid A (5), and oleanolic acid (6), were isolated from the roots of Aceriphyllum rossii. Their chemical structures were determined by comparison with available ¹H-NMR and 13C-NMR data on known compounds. All the isolated compounds were evaluated for inhibitory activity against human diacylglycerol acyltransferases 1 and 2. Most of the isolates exhibited a better inhibitory activity against diacylglycerol acyltransferase 2 (IC50: 11.6-44.2 μM) than against diacylglycerol acyltransferase 1 (IC50: 22.7-119.5 μM). In particular, compounds 1 and 5 showed strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and appeared to act competitively against oleoyl-CoA in vitro. The results also indicated that both compounds reduced newly synthesized triacylglycerol in HuTu80 and HepG2 cells. Oral administration of compound 1 significantly reduced postprandial triacylglycerol in mice following an oral lipid challenge. In conclusion, the current study indicates that compound 1 suppresses both de novo triacylglycerol biosynthesis and resynthesis through the inhibition of diacylglycerol acyltransferase activity, and therefore may be a useful agent for treating diseases associated with a high triacylglycerol level. [ABSTRACT FROM AUTHOR]
- Subjects :
- *CHROMATOGRAPHIC analysis
*ACYLTRANSFERASES
*ANALYSIS of variance
*ANIMAL experimentation
*BIOLOGICAL assay
*BIOPHYSICS
*CELL culture
*MASS spectrometry
*RESEARCH methodology
*MICE
*MOLECULAR structure
*NUCLEAR magnetic resonance spectroscopy
*OBESITY
*REGRESSION analysis
*RESEARCH funding
*PLANT roots
*STATISTICS
*TERPENES
*DATA analysis
*DATA analysis software
*DESCRIPTIVE statistics
*IN vitro studies
*CHEMICAL inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 00320943
- Volume :
- 81
- Issue :
- 3
- Database :
- Academic Search Index
- Journal :
- Planta Medica
- Publication Type :
- Periodical
- Accession number :
- 101125219
- Full Text :
- https://doi.org/10.1055/s-0034-1396242