Diacylglycerol acyltransferase 1 (DGAT1) inhibition by furofuran lignans from stems of Acanthopanax senticosus
- 192 Downloads
Two new furofuran lignans were isolated from the stems of Acanthopanax senticosus, along with seven known compounds. Their structures were all determined by spectroscopic analyses and chemical methods. All the isolates were evaluated for in vitro inhibitory activity against DGAT1 and DGAT2. Compounds 1 and 2 were found to exhibit selective inhibitory activity on DGAT1 with IC50 values 89.5 ± 1.5 and 57.5 ± 1.3 µM, respectively.
KeywordsAcanthopanax senticosus Araliaceae DGAT Furofuran lignans
This research was supported by a Grant from KRIBB Research Initiative Program and Technological Developing Scheme of Jilin Province of People’s Republic of China (20150101225JC).
- Cases S, Smith SJ, Zheng YW, Myers HM, Lear SR, Sande E, Novak S, Collins C, Welch CB, Lusis AJ, Erickson SK, Farese RV (1998) Identification of a gene encoding an acyl CoA: diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis. J Natl Acad Sci 95:13018–13023CrossRefGoogle Scholar
- Deyama T, Nishibe S, Nakazawa Y (2012) Constituents and pharmacological effects of Eucommia and Siberian ginseng. Acta Pharmacol Sin 22:1057–1070Google Scholar
- Jin XQ, Xu DM, Xu YJ (1993) Structure determination of zhebeiresinol. Yao Xue Xue Bao 3:212–215Google Scholar
- Lardizabal KD, Mai JT, Wagner NW, Wyrick A, Voelker T, Hawkins DJ (2001) DGAT2 is a new diacylglycerol acyltransferase gene family: purification, cloning, and expression in insect cells of two polypeptides from Mortierella ramanniana with diacylglycerol acyltransferase activity. J Biol Chem 276:38862–38869CrossRefPubMedGoogle Scholar
- Li YC, Kuo YH (2001) Four new compounds, ficusal, ficusesquilignan A, B, and ficusolide diacetate from the heartwood of Ficus microcarpa. ChemInform 32:1862–1865Google Scholar
- Xie LH, Akao T, Hamasaki K (2003) Biotransformation of pinoresinol diglucoside to mammalian lignans by human intestinal microflora, and isolation of Enterococcus faecalis strain PDG-1 responsible for the transformation of (+)-pinoresinol to (+)-pLariciresinol. Chem Pharm Bull 51:508–515CrossRefPubMedGoogle Scholar