Robustanic acid as a glutaminase and Na+, K+-ATPase inhibitor from leaves of Eucalyptus globulus

Author:

Shimada Atsumi1,Ueno Hiroshi2,Kawabata Kohei3,Inagaki Masanori3

Affiliation:

1. Division of Food and Nutrition , 73489 Nakamura Gakuen University Junior College , Fukuoka 814-0198 , Japan

2. Department of Medical Technology , Kawasaki University of Medical Welfare , Kurashiki , Okayama 701-0193 , Japan

3. Faculty of Pharmacy, Department of Pharmaceutical Chemistry , Yasuda Women’s University , Hiroshima 731-0153 , Japan

Abstract

Abstract This study was to compare glutaminase and Na+, K+-ATPase inhibitory activities of 20 herbal extracts and investigate the isolation, structural elucidation and those inhibitory activities of three triterpenes from the selected extract of Eucalyptus globulus Labill. Three triterpenes, ursolic acid (1), robustanic acid (2) and ursolic acid lactone (3), were identified by analyzing their NMR and MS spectral data and comparison of these with reported data. The IC50 values of 13 and the control compound against glutaminase, 6-diazo-5-oxo-l-norleucine (DON), were 443 μM, 334 μM, 963 μM and 134 μM, respectively. The IC50 values of 1, 2 and the control compound against Na+, K+-ATPase and ouabain, were 180 μM, 56 μM and 0.5 μM, respectively. Compounds 1 and 2 may serve as potential lead compounds for the prevention and treatment of neurodegenerative and lifestyle-related diseases by targeting glutaminase and Na+, K+-ATPase. This is the first report on glutaminase and Na+, K+-ATPase inhibitory activities of 2.

Publisher

Walter de Gruyter GmbH

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