2. Academic Validation
  3. Pentacyclic triterpene acids, rotungenic acid and barbinervic acid, from fresh leaves of Diospyros kaki Thunberg and their glutaminase inhibitory activities

Pentacyclic triterpene acids, rotungenic acid and barbinervic acid, from fresh leaves of Diospyros kaki Thunberg and their glutaminase inhibitory activities

  • Nat Prod Res. 2022 Nov 26:1-5. doi: 10.1080/14786419.2022.2150765.
Atsumi Shimada 1,  Hiroshi Ueno 2,  Kenta Yamamoto 3,  Kohei Kawabata 4,  Masanori Inagaki 4
Affiliations

Affiliations

  • 1 Division of Food and Nutrition, Nakamura Gakuen University Junior College, Fukuoka, Japan.
  • 2 Department of Medical Technology, Kawasaki University of Medical Welfare, Okayama, Japan.
  • 3 Department of Food Management, Faculty of Nutritional Sciences, Nakamura Gakuen University, Fukuoka, Japan.
  • 4 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yasuda Women's University, Hiroshima, Japan.
PMID: 36434778 DOI: 10.1080/14786419.2022.2150765
Abstract

Glutaminase is an important target that is often over-expressed in neurodegenerative and lifestyle-related diseases but few effective inhibitors of this Enzyme have yet reached clinical trials. Three compounds isolated from fresh leaves of Diospyros kaki Thunberg, ursolic acid (1), rotungenic acid (2) and barbinervic acid (3), were identified by analyzing their NMR and MS spectral data and comparison of these with reported data. The IC50 values of 1-3 and 6-diazo-5-oxo-L-norleucine (DON) as control were 775, 13, 14, and 434 μM, respectively. Compounds 2 and 3 showed higher Glutaminase inhibitory activities than DON. Compounds 2 and 3 may serve as potential lead compounds for the prevention and treatment of neurodegenerative and lifestyle-related diseases by targeting Glutaminase. This is the first report on Glutaminase inhibitory activities of 2 and 3.

Keywords

Diospyros kaki Thunberg; Ebenaceae; barbinervic acid; glutaminase inhibitor; rotungenic acid; ursolic acid.

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