Abstract：
:In a two-microelectrode voltage clamp assay with Xenopus laevis oocytes, a petroleum ether extract (100 μg/mL) of the resin of Boswellia thurifera (Burseraceae) potentiated GABA-induced chloride currents (IGABA) through receptors of the subtype α₁β₂γ₂s by 319.8% ± 79.8%. With the aid of HPLC-based activity profiling, three known terpenoids, dehydroabietic acid (1), incensole (2), and AKBA (3), were identified in the active fractions of the extract. Structure elucidation was achieved by means of HR-MS and microprobe 1D/2D NMR spectroscopy. Compound 1 induced significant receptor modulation in the oocyte assay, with a maximal potentiation of IGABA of 397.5% ± 34.0%, and EC₅₀ of 8.7 μM ± 1.3 μM. This is the first report of dehydroabietic acid as a positive GABAA receptor modulator.
journal_name
Fitoterapiajournal_title
Fitoterapiaauthors
Rueda DC,Raith M,De Mieri M,Schöffmann A,Hering S,Hamburger Mdoi
10.1016/j.fitote.2014.09.002subject
Has Abstractpub_date
2014-12-01 00:00:00pages
28-34eissn
0367-326Xissn
1873-6971pii
S0367-326X(14)00238-Xjournal_volume
99pub_type
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