Next Article in Journal
The Splicing Factor SF2 Is Critical for Hyperproliferation and Survival in a TORC1-Dependent Model of Early Tumorigenesis in Drosophila
Next Article in Special Issue
Nutraceuticals in the Treatment of Pulmonary Arterial Hypertension
Previous Article in Journal
Life in the Current: Anatomy and Morphology of Utricularia neottioides
Previous Article in Special Issue
Purified Tea (Camellia sinensis (L.) Kuntze) Flower Saponins Induce the p53-Dependent Intrinsic Apoptosis of Cisplatin-Resistant Ovarian Cancer Cells
Article

Norditerpenoids with Selective Anti-Cholinesterase Activity from the Roots of Perovskia atriplicifolia Benth.

1
Department of Pharmaceutical Biology and Botany, Wroclaw Medical University, 50556 Wroclaw, Poland
2
Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Ankara, Turkey
3
Structural Bioinformatics Group, Institute for Physiology & ECRC, Charité University Medicine, 10115 Berlin, Germany
4
Department of Biochemistry and Crop Quality, IUNG-Institute of Soil Science and Plant Cultivation, 24100 Puławy, Poland
5
Structural Bioinformatics and High Performance Computing Research Group, Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain
6
Reconocimiento y Encapsulación Molecular (REM), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain
7
Department of Inorganic Chemistry, Wroclaw Medical University, 50556 Wroclaw, Poland
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(12), 4475; https://doi.org/10.3390/ijms21124475
Received: 8 May 2020 / Revised: 16 June 2020 / Accepted: 19 June 2020 / Published: 23 June 2020
Inhibition of cholinesterases remains one of a few available treatment strategies for neurodegenerative dementias such as Alzheimer’s disease and related conditions. The current study was inspired by previous data on anticholinesterase properties of diterpenoids from Perovskia atriplicifolia and other Lamiaceae species. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition by the three new natural compounds—(1R,15R)-1-acetoxycryptotanshinone (1), (1R)-1-acetoxytanshinone IIA (2), and (15R)-1-oxoaegyptinone A (3)—as well as, new for this genus, isograndifoliol (4) were assessed. Three of these compounds exhibited profound inhibition of butyrylcholinesterase (BChE) and much weaker inhibition of acetylcholinesterase (AChE). All compounds (14) selectively inhibited BChE (IC50 = 2.4, 7.9, 50.8, and 0.9 µM, respectively), whereas only compounds 3 and 4 moderately inhibited AChE (IC50 329.8 µM and 342.9 µM). Molecular docking and in silico toxicology prediction studies were also performed on the active compounds. Natural oxygenated norditerpenoids from the traditional Central Asian medicinal plant P. atriplicifolia are selective BChE inhibitors. Their high potential makes them useful candidate molecules for further investigation as lead compounds in the development of a natural drug against dementia caused by neurodegenerative diseases. View Full-Text
Keywords: tanshinones; cholinesterases; molecular docking; structure elucidation tanshinones; cholinesterases; molecular docking; structure elucidation
Show Figures

Graphical abstract

MDPI and ACS Style

Ślusarczyk, S.; Senol Deniz, F.S.; Abel, R.; Pecio, Ł.; Pérez-Sánchez, H.; Cerón-Carrasco, J.P.; den-Haan, H.; Banerjee, P.; Preissner, R.; Krzyżak, E.; Oleszek, W.; E. Orhan, I.; Matkowski, A. Norditerpenoids with Selective Anti-Cholinesterase Activity from the Roots of Perovskia atriplicifolia Benth. Int. J. Mol. Sci. 2020, 21, 4475. https://doi.org/10.3390/ijms21124475

AMA Style

Ślusarczyk S, Senol Deniz FS, Abel R, Pecio Ł, Pérez-Sánchez H, Cerón-Carrasco JP, den-Haan H, Banerjee P, Preissner R, Krzyżak E, Oleszek W, E. Orhan I, Matkowski A. Norditerpenoids with Selective Anti-Cholinesterase Activity from the Roots of Perovskia atriplicifolia Benth. International Journal of Molecular Sciences. 2020; 21(12):4475. https://doi.org/10.3390/ijms21124475

Chicago/Turabian Style

Ślusarczyk, Sylwester, F. S. Senol Deniz, Renata Abel, Łukasz Pecio, Horacio Pérez-Sánchez, José P. Cerón-Carrasco, Helena den-Haan, Priyanka Banerjee, Robert Preissner, Edward Krzyżak, Wiesław Oleszek, Ilkay E. Orhan, and Adam Matkowski. 2020. "Norditerpenoids with Selective Anti-Cholinesterase Activity from the Roots of Perovskia atriplicifolia Benth." International Journal of Molecular Sciences 21, no. 12: 4475. https://doi.org/10.3390/ijms21124475

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop