| Description: |
Kuwanon E inhibited cholinesterase enzyme in a dose-dependent manner with K_i values ranging between 3.1 and 37.5 μM and between 1.7 and 19.1 μM against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes, respectively. Kuwanon E also inhibited the production of MUC5AC mucin induced by PMA from NCI-H292 cells,. |
| Targets: |
BChE | AChE |
| In vitro: |
| Journal of Agricultural & Food Chemistry, 2011, 59(9):4589-4596. | | Isolation of Cholinesterase-lnhibiting Flavonoids from Moras Ihou.[Reference: WebLink] | Cholinesterases are key enzymes that play important roles in cholinergic transmission.
METHODS AND RESULTS:
Nine flavonoids displaying cholinesterase inhibitory activity were isolated from the root bark oiMorus Ihou L., a cultivated edible plant.
The isolated compounds were identified as a new flavone (1), 5'-geranyl-5,7,2',4'-tetrahydroxyflavone (2), kuwanon U (3), kuwanon E (4), morusin (5), morusinol (6), cyclomorusin (7), neocyclomorusin (8), and kuwanon C (9). All compounds apart from compound 6 inhibited cholinesterase enzyme in a dose-dependent manner with K_i values ranging between 3.1 and 37.5 μM and between 1.7 and 19.1 μM against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes, respectively. The new compound was char-actierized as S'-geranyl-4'-methoxv-5,7,2'-trihydroxyflavone (1). It showed the most potent inhibitory activity (K_i = 3.1 μM for AChE, K_i= 1.74 μM for BChE). Lineweaver-Burk and Dixon plots and their secondary replots indicated that flavones (5-9) with prenyl substitution on C-3 were noncompetitive inhibitors, whereas those unsubstituted (1 -4) at C-3 were mixed inhibitors of both AChE and BChE.
CONCLUSIONS:
In conclusion, this is the first study to demonstrate that alkylated flavonoids of M. lhou have potent inhibitory activities against AChE and BChE. |
|
| In vivo: |
| Tuberculosis and Respiratory Diseases, 2014, 77(2):65-72. | | Effects of Morus alba L. and Natural Products Including Morusin on In Vivo Secretion and In Vitro Production of Airway MUC5AC Mucin.[Pubmed: 25237377 ] | It is valuable to find the potential activity of regulating the excessive mucin secretion by the compounds derived from various medicinal plants. We investigated whether aqueous extract of the root bark of Morus alba L. (AMA), kuwanon E, kuwanon G, mulberrofuran G, and morusin significantly affect the secretion and production of airway mucin using in vivo and in vitro experimental models.
METHODS AND RESULTS:
Effect of AMA was examined on hypersecretion of airway mucin in sulfur dioxide-induced acute bronchitis in rats. Confluent NCI-H292 cells were pretreated with ethanolic extract, kuwanon E, kuwanon G, mulberrofuran G, or morusin for 30 minutes and then stimulated with phorbol 12-myristate 13-acetate (PMA) for 24 hours. The MUC5AC mucin secretion and production were measured by enzyme-linked immunosorbent assay. AMA stimulated the secretion of airway mucin in sulfur dioxide-induced bronchitis rat model; aqueous extract, ethanolic extract, kuwanon E, kuwanon G, mulberrofuran G and morusin inhibited the production of MUC5AC mucin induced by PMA from NCI-H292 cells, respectively.
CONCLUSIONS:
These results suggest that extract of the root bark and the natural products derived from Morus alba L. can regulate the secretion and production of airway mucin and, at least in part, explains the folk use of extract of Morus alba L. as mucoregulators in diverse inflammatory pulmonary diseases. |
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