A new pancreatic lipase inhibitor isolated from the roots of Actinidia arguta
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A new coumaroyl triterpene, 3-O-trans-p-coumaroyl actinidic acid (1), as well as five known triterpenes, ursolic acid (2), 23-hydroxyursolic acid (3), corosolic acid (4), asiatic acid (5) and betulinic acid (6) were isolated from an EtOAc-soluble extract of the roots of Actinidia arguta. The structure of compound 1 was elucidated from interpretation of the spectroscopic data, particularly by extensive 1D and 2D NMR studies. All the isolates (1–6) were evaluated in vitro for their inhibitory activities on pancreatic lipase (PL). Of the isolates, the new compound 1 possessed the highest inhibitory activity on PL, with an IC50 of 14.95 μM, followed by ursolic acid (2, IC50 = 15.83 μM). The other four triterpenes (3–6) also showed significant PL inhibitory activity, with IC50 values ranging from 20.42 to 76.45 μM.
Key wordsActinidia arguta Actinidiaceae 3-O-trans-p-Coumaroyl actinidic acid Triterpene Pancreatic lipase Obesity
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- Aguirre, M. C., Delporte, C., Backhouse, N., Erazo, S., Letelier, M. E., Cassels, B. K., Silva, X., Alegría, S., and Negrete, R., Topical anti-inflammatory activity of 2α-hydroxy pentacyclic triteroene acids from the leaves of Ugni molinae. Bioorg. Med. Chem., 14, 5673–5677 (2006).PubMedCrossRefGoogle Scholar
- Borgstrom, B., Exocrine Pancreas, Pathology and Diseases. Raven Press, New York, pp. 361–401, (1981).Google Scholar
- Drent, M. L. and van der Veen, E. A., Lipase inhibition: a novel concept in the treatment of obesity. Int. J. Obes., 17, 241–244 (1993).Google Scholar
- Ferguson, R., Actinidia arguta — the hardy kiwifruit. New Zealand Kiwifruit, 81, 23–24 (1991).Google Scholar
- Jang, D. S., Kim, J. M., Lee, G. Y., Kim, J.-H., and Kim, J. S., Ursane-type triterpenoids from the aerial parts of Potentilla discolor. Agric. Chem. Biotechnol., 49, 48–50 (2006).Google Scholar
- Kim, J.-G. and Xiao, P.-G., Traditional Drugs of the East Color Edition. Young-Rim Publishing Co., Seoul, p. 207, (1995).Google Scholar
- Lim, H.-W., Kang, S.-J., Park, M., Yoon, J. H., Han, B.-H., Choi, S.-E., and Lee, M.-W., Anti-oxidative and nitric oxide production inhibitory activities of Phenolic compounds from the fruits of Actinidia arguta. Nat. Prod. Sci., 12, 221–225 (2006).Google Scholar
- Whang, J. I., Moon, H. I., and Zee, O. P., Phytochemical constituents of Actinidia arguta. Kor. J. Pharmacogn., 31, 357–363 (2000).Google Scholar