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Planta Med 2015; 81(03): 228-234
DOI: 10.1055/s-0034-1396242
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Oleanane-Type Triterpenoids of Aceriphyllum rossii and Their Diacylglycerol Acyltransferase-Inhibitory Activity

Jee-Hee Seo   *
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
,
Mun-Ock Kim   *
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
,
Ah-Reum Han
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
,
Eun-Bin Kwon
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
,
Myung Ji Kang
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
,
Sungchan Cho
2   Incurable Diseases Therapeutics Research Center, KRIBB, Cheongju, Korea
,
Dong-Oh Moon
3   Department of Biology Education, Daegu University, Gyungsan, Gyeongbuk, Korea
,
Jung-Ran Noh
4   Laboratory Animal Center, KRIBB, Yuseong-gu, Daejeon, Korea
,
Chul-Ho Lee
4   Laboratory Animal Center, KRIBB, Yuseong-gu, Daejeon, Korea
,
Young-Soo Kim
5   Department of Pharmacology, Chungbuk National University, Cheongju, Korea
,
Hyun-Sun Lee
1   Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea
› Author Affiliations
Further Information

Publication History

received 24 July 2014
revised 12 December 2014

accepted 19 December 2014

Publication Date:
11 February 2015 (online)

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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.

Key words

Aceriphyllum rossii - Saxifragaceae - diacylglycerol acyltransferase - triacylglycerol - triterpenoid

* These authors contributed equally to this work.


Supporting Information

 

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