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Direct Interaction of Garcinol and Related Polyisoprenylated Benzophenones of Garcinia cambogiaFruits with the Transcription Factor STAT-1 as a Likely Mechanism of Their Inhibitory Effect on Cytokine Signaling Pathways
| العنوان: | Direct Interaction of Garcinol and Related Polyisoprenylated Benzophenones of Garcinia cambogiaFruits with the Transcription Factor STAT-1 as a Likely Mechanism of Their Inhibitory Effect on Cytokine Signaling Pathways |
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| المؤلفون: | Masullo, Milena, Menegazzi, Marta, Di Micco, Simone, Beffy, Pascale, Bifulco, Giuseppe, Dal Bosco, Martina, Novelli, Michela, Pizza, Cosimo, Masiello, Pellegrino, Piacente, Sonia |
| المصدر: | Journal of Natural Products; March 2014, Vol. 77 Issue: 3 p543-549, 7p |
| مستخلص: | Garcinol (1), a polyisoprenylated benzophenone occurring in Garciniaspecies, has been reported to exert anti-inflammatory activity in LPS-stimulated macrophages, through inhibition of NF-κB and/or JAK/STAT-1 activation. In order to provide deeper insight into its effects on the cytokine signaling pathway and to clarify the underlying molecular mechanisms, 1was isolated from the fruits of Garcinia cambogiaalong with two other polyisoprenylated benzophenones, guttiferones K (2) and guttiferone M (3), differing from each other in their isoprenyl moieties and their positions on the benzophenone core. The affinities of 1–3for the STAT-1 protein have been evaluated by surface plasmon resonance and molecular docking studies and resulted in KDvalues in the micromolar range. Consistent with the observed high affinity toward the STAT-1 protein, garcinol and guttiferones K and M were able to modulate cytokine signaling in different cultured cell lines, mainly by inhibiting STAT-1 nuclear transfer and DNA binding, as assessed by an electrophorectic mobility shift assay. |
| قاعدة البيانات: | Supplemental Index |
| تدمد: | 01633864 15206025 |
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| DOI: | 10.1021/np400804y |