Inhibition of [3H]-LSD Binding to 5-HT7 Receptors by Flavonoids from Scutellaria lateriflora

The hot water and 70% ethanol extracts of dried mad-dog skullcap (Scutellaria lateriflora) both bound to the 5-HT(7) receptor, with 87.2 +/- 6.2% and 56.7 +/- 1.3% inhibition of [(3)H]-LSD binding to the receptor at 100 microg/mL, respectively. The on-line analysis of a 70% ethanol extract by HPLC-U...

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Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2003-04, Vol.66 (4), p.535-537
Main Authors: GAFNER, Stefan, BERGERON, Chantal, BATCHA, Laura L., REICH, Jesse, ARNASON, John T., BURDETTE, Joanna E., PEZZUTO, John M., ANGERHOFER, Cindy K.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cells, Cultured - drug effects
Flavones
Flavonoids - chemistry
Flavonoids - isolation & purification
Flavonoids - pharmacology
General pharmacology
Humans
Inhibitory Concentration 50
Medical sciences
Molecular Structure
Nuclear Magnetic Resonance, Biomolecular
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Plants, Medicinal - chemistry
Receptors, Serotonin - drug effects
Scutellaria - chemistry
Serotonin Antagonists - chemistry
Serotonin Antagonists - isolation & purification
Serotonin Antagonists - pharmacology
Vermont
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Summary:The hot water and 70% ethanol extracts of dried mad-dog skullcap (Scutellaria lateriflora) both bound to the 5-HT(7) receptor, with 87.2 +/- 6.2% and 56.7 +/- 1.3% inhibition of [(3)H]-LSD binding to the receptor at 100 microg/mL, respectively. The on-line analysis of a 70% ethanol extract by HPLC-UV/MS resulted in the identification of five flavones (1-5). Fractionation of the ethanol extract resulted in the isolation of three flavone-glucuronides (6-8) and a flavanone-glucuronide (9), including one new compound, lateriflorin (5,6,-dihydroxy-7-glucuronyloxy-2'-methoxyflavone) (8). The structure of 8 was determined by NMR ((1)H NMR, (13)C NMR, and NOESY experiments) and MS analysis. From the results obtained in the testing of the pure compounds, it is evident that the activity on the 5-HT(7) receptor is at least partly due to the presence of flavonoids. Scutellarin and ikonnikoside I showed the highest inhibition of [(3)H]-LSD binding with IC(50) values of 63.4 and 135.1 microM, respectively.
ISSN:0163-3864
1520-6025
DOI:10.1021/np0205102