| Description: |
Moschamine is a very potent compound that is able to inhibit COX-I by 58% and COX-II by 54%, at the concentration of 0.1 μmol L⁻1, it may suppress cAMP formation via binding to 5-HT1 receptors in the cells. Moschamine exerts antitumour effects on HeLa, MCF7 and A431 cells. |
| Targets: |
COX | cAMP | 5-HT Receptor |
| In vitro: |
| Phytother Res. 2010 Nov;24(11):1664-9. | | Bioactivity-guided isolation of antiproliferative compounds from Centaurea arenaria.[Pubmed: 21031625 ] |
METHODS AND RESULTS:
Flavonoids (eupatilin, eupatorin, 3'-methyleupatorin, apigenin and isokaempferid), lignans (arctigenin, arctiin and matairesinol), the sesquiterpene cnicin, serotonin conjugates (Moschamine and cis-Moschamine), β-amyrin and β-sitosterin-β-D-glycopyranoside, identified by means of UV, MS and NMR spectroscopy, were obtained for the first time from this species.
CONCLUSIONS:
The isolated compounds were also evaluated for their tumour cell growth inhibitory activities on HeLa, MCF7 and A431 cells, and different types of secondary metabolites were found to be responsible for the antitumour effects of the extracts; in addition to moderately active compounds (isokaempferid and Moschamine), especially apigenin, eupatorin, arctigenin, arctiin, matairesinol and cnicin exert marked antitumour effects against these cell lines. |
|
| In vivo: |
| Nat Prod Res. 2012;26(16):1465-72. | | Synthesis, biological activities and bioavailability of moschamine, a safflomide-type phenylpropenoic acid amide found in Centaurea cyanus.[Pubmed: 21978225] | Moschamine is a phenylpropenoic acid amide found in plants. In this article, the synthesis and two biological activities (serotoninergic and cyclooxygenase (COX) inhibitory activities) and bioavailability of Moschamine were described.
METHODS AND RESULTS:
Moschamine was synthesised and confirmed using NMR spectroscopic methods. Using the Moschamine synthesised, serotoninergic and COX inhibitory activities were investigated. At the concentration of 10 µmol L⁻¹, Moschamine was able to inhibit forskolin-stimulated cAMP formation by 25% (p < 0.015), via inhibiting serotonin receptors in the OK cells.
CONCLUSIONS:
The inhibition was repressed by two 5-HT1 antagonists (Nan-190 and spiperone), suggesting that Moschamine may suppress cAMP formation via binding to 5-HT1 receptors in the cells. Also, Moschamine was a very potent compound that is able to inhibit COX-I by 58% (p < 0.012) and COX-II by 54% (p < 0.014), at the concentration of 0.1 µmol L⁻¹. The oral bioavailability of Moschamine was also determined in mice. |
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