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Phytochemical profiling of Curcuma kwangsiensis rhizome extract, and identification of labdane diterpenoids as positive GABAA receptor modulators.
Journal article

Phytochemical profiling of Curcuma kwangsiensis rhizome extract, and identification of labdane diterpenoids as positive GABAA receptor modulators.

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  • 2013-09-10
Published in:
  • Phytochemistry. - 2013
CE
CPCM
Cotton effect
Curcuma kwangsiensis
ECD
Electronic circular dichroism (ECD)
GABA
GABA(A) receptor modulation
GABA-induced chloride current
HPLC-based activity profiling
I(GABA)
Labdane diterpenoids
OPLS
SCRF
TCM
TDDFT
Xenopus oocyte assay
Zingiberaceae
conductor-like polarizable continuum model
electronic circular dichroism
gamma-aminobutyric acid
optimized potential for liquid simulations
self-consistent reaction field
time-dependent density function theory
traditional Chinese medicine
Animals
Chromatography, High Pressure Liquid
Curcuma
Diterpenes
Drugs, Chinese Herbal
Nuclear Magnetic Resonance, Biomolecular
Oocytes
Receptors, GABA-A
Rhizome
Xenopus
English An ethyl acetate extract of Curcuma kwangsiensis S.G. Lee & C.F. Liang (Zingiberaceae) rhizomes (100 μg/ml) enhanced the GABA-induced chloride current (IGABA) through GABAA receptors of the α1β2γ2S subtype by 79.0±7.0%. Potentiation of IGABA was measured using the two-microelectrode voltage-clamp technique and Xenopus laevis oocytes. HPLC-based activity profiling of the crude extract led to the identification of 11 structurally related labdane diterpenoids, including four new compounds. Structure elucidation was achieved by comprehensive analysis of on-line (LC-PDA-ESI-TOF-MS) and off-line (microprobe 1D and 2D NMR) spectroscopic data. The absolute configuration of the compounds was established by comparison of experimental and calculated ECD spectra. Labdane diterpenes represent a new class of plant secondary metabolites eliciting positive GABAA receptor modulation. The highest efficiency was observed for zerumin A (maximum potentiation of IGABA by 309.4±35.6%, and EC50 of 24.9±8.8 μM).
Language
  • English
Open access status
closed
Identifiers
Persistent URL
https://sonar.ch/global/documents/53464
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