Selective in vitro and in silico cholinesterase inhibitory activity of isoflavones and stilbenes from Belamcandae chinensis rhizoma
| Autor: | Ilkay Erdogan Orhan, Horacio Pérez-Sánchez, Adam Matkowski, Anna Stochmal, Łukasz Pecio, F. Sezer Senol Deniz, Sylwester Ślusarczyk, Dorota Woźniak, José P. Cerón-Carrasco, Helena den-Haan Alonso |
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| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Tectorigenin
Piceatannol biology Traditional medicine 010405 organic chemistry Plant Science Iris domestica Tectoridin Isoflavones biology.organism_classification 01 natural sciences Biochemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Xanthone Mangiferin Agronomy and Crop Science Butyrylcholinesterase Biotechnology |
| Popis: | Isoflavonoids and stilbenes were suggested as potential lead structures for inhibition of cholinesterases and in management of dementia. The Traditional Chinese (TCM) herb Belamcandae chinensis rhizoma (the rhizome of Iris domestica (L.) Goldblatt & Mabb) contains both classes of natural products. Here, we isolated eight isoflavonoids: irisflorentin (1), tectorigenin(2), iristectorigenin B(3), irigenin (4), irilin D (5), iridin (6), tectoridin (7), iristectorin B (8), two stilbenes; piceatannol (9) and resveratrol (10) as well as the xanthone glucoside – mangiferin (11). The compounds weretested against acetyl- (AChE) and butyrylcholinesterase (BChE) using ELISA microtiter assay. Molecular docking studies were also performed on the active compounds. Among the tested polyphenols, piceatannol inhibited both cholinesterases (up to 67% and 91% of AChE and BChE, respectively) whereas irilin D and resveratrol were only active against BChE. Irisflorentin was selective but weak inhibitor against AChE (36% inhibition at 100 μg/mL). The remaining isoflavones were moderately active against BChE (below 40% inhibition). In conclusion, the TCM and pharmacopoeial drug – Belamcandae chinensis rhizoma is rich in potential cholinesterase inhibitors that can provide lead structures for further development of selective drugs. Moreover, the in vitro results would suggest a novel indication of this traditional anti-inflammatory, phytoestrogenic and antiallergic herb. |
| Databáze: | OpenAIRE |
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