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SHR Neuro Cancer Cardio Lipid Metab Microb
Crockett, SL; Wenzig, EM; Kunert, O; Bauer, R.
Anti-inflammatory phloroglucinol derivatives from Hypericum empetrifolium.
Phytochem Lett. 2008; 1(1):37-43
Doi: 10.1016/j.phytol.2007.12.003
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- Crockett Sara
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- Abstract:
- Phytochemical investigation of Hypericum empetrifolium Willd. (Clusiaceae), a species native to Greece and Turkey has led to the bioassay-guided identification of two acylphloroglucinol derivatives with potent in vitro anti-inflammatory activity. Using NMR spectroscopy and mass spectrometry, the acylphloroglucinol derivatives were characterized as 3-geranyl-1-(2'-methylpropanoyl)phloroglucinol (1) and 3-geranyl-1-(2'-methylbutanoyl)phloroglucinol (2). Hypotheses are proposed regarding the biosynthetic origin of these and similar acylphloroglucinols from related Hypericum species. Compounds 1 and 2 were evaluated for in vitro inhibitory activity against COX-1, COX-2 and 5-LOX catalyzed LTB(4) formation. Compound 1 displayed good activity (IC(50) values: 6.0, 29.9, and 2.2 μM, respectively) in all three assays. Compound 2 showed good activity (IC(50) value: 5.8 μM) against LTB(4) formation and moderate activity (IC(50) value: 26.2 μM) against COX-1.
- Find related publications in this database (Keywords)
- Hypericum empetrifolium
- Clusiaceae
- Guttiferae
- Section Coridium
- Anti-inflammatory
- Acylphloroglucinol derivative