In vitro: |
Arch. Pharm. Res.,2003, 26(9):735-8. | Inhibitory effect of trans-N-p-coumaroyl tryamine from the twigs of Celtis chinensis on the acetylcholinesterase.[Pubmed: 14560923] | METHODS AND RESULTS: The methanolic extract of the twigs of Celtis chinensis was found to show inhibitory activity on acetylcholinesterase (AChE), an enzyme that plays a role in the metabolic hydrolysis of ACh. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of N-p-trans-Coumaroyltyramine, as an inhibitor on AChE. CONCLUSIONS: This compound inhibited AChE activity in a dose-dependent manner, and the IC50 value of N-p-trans-Coumaroyltyramine was 34.5 microg/mL (122 microM). | Nat Prod Commun. 2012 Jun;7(6):753-5. | Cinnamoylphenethyl amides from Polygonum hyrcanicum possess anti-trypanosomal activity.[Pubmed: 22816300] | METHODS AND RESULTS: A methanolic extract from aerial parts of Polygonum hyrcanicum (Polygonaceae) showed high activity against Trypanosoma brucei rhodesiense (IC50 = 3.7 microg/mL). Bioassay-guided fractionation of the extract resulted in isolation of cinnamoylphenethyl amides, including N-trans-caffeoyltyramine (1), N-p-trans-Coumaroyltyramine (7), and N-trans-feruloyltyramine (8) as the main active constituents (IC50s ranging from 2.2 to 13.3 microM). Some structurally related, but less active compounds, such as cannabisin B (2), tyrosol (3), p-coumaric acid (4), ferulic acid (5), and N-cis-feruloyltyramine (6) were also identified, along with N-trans-3,4-dimethoxycinnamoyldopamine (9). CONCLUSIONS: Cytotoxicity of the active compounds in L6 cells was determined, and selectivity indices (SI) of 7.9 to 33.4 were calculated. |
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