Rueda Diana C, Raith Melanie, De Mieri Maria, Schöffmann Angela, Hering Steffen, Hamburger Matthias
Division of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.
Institute of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria.
Fitoterapia. 2014 Dec;99:28-34. doi: 10.1016/j.fitote.2014.09.002. Epub 2014 Sep 6.
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.
在使用非洲爪蟾卵母细胞的双微电极电压钳测定中，乳香科植物索马里乳香树脂的石油醚提取物（100μg/mL）通过α₁β₂γ₂s亚型受体使γ-氨基丁酸（GABA）诱导的氯离子电流（IGABA）增强了319.8%±79.8%。借助基于高效液相色谱的活性分析，在提取物的活性部分鉴定出三种已知的萜类化合物，脱氢枞酸（1）、榄香烯（2）和乙酰基-11-酮基-β-乳香酸（3）。通过高分辨质谱和微探针一维/二维核磁共振光谱进行结构解析。化合物1在卵母细胞测定中诱导了显著的受体调节，IGABA的最大增强幅度为397.5%±34.0%，半数有效浓度（EC₅₀）为8.7μM±1.3μM。这是关于脱氢枞酸作为一种GABAA受体阳性调节剂的首次报道。
