Division of Pharmaceutical Biology, University of Basel, Basel, Switzerland.
Planta Med. 2012 Feb;78(3):207-10. doi: 10.1055/s-0031-1298171. Epub 2012 Jan 23.
In a two-microelectrode voltage clamp assay using Xenopus laevis oocytes, a petroleum ether extract prepared from a commercial sample of the traditional Chinese herbal drug labelled as " Chaihu" (Bupleurum chinense DC. roots) enhanced the I(GABA) by 156 % ± 22 % when tested at 100 µg/mL. By means of HPLC-based activity profiling combined with high-resolution LC-MS and microprobe NMR, the germacranolide aristolactone was identified as one of the main active compounds (EC₅₀ 56.02 µM ± 5.09 µM). However, aristolactone has been previously reported only from the genus Aristolochia (Aristolochiaceae), suggesting a possible adulteration. With the aid of a validated HPTLC protocol for detection of aristolochic acids and with reference samples, the commercial sample was confirmed to be a mixture of Aristolochia manshuriensis root and Bupleurum chinense root. This finding was corroborated by macroscopic inspection of the drug. This case of adulteration with a highly nephrotoxic drug raises concerns about adequate quality control of TCM drugs commercialized in Europe.
在使用非洲爪蟾卵母细胞的双微电极电压钳测定中，用 100μg/ml 浓度处理时，从一种标称为“柴胡”（柴胡根）的市售中药提取物中提取的石油醚提取物使 I（GABA）增强了 156%±22%。通过基于 HPLC 的活性分析与高分辨率 LC-MS 和微探针 NMR 相结合的方法，鉴定出大根香叶烯内酯是主要的活性化合物之一（EC₅₀ 为 56.02 µM±5.09 µM）。然而，此前仅从马兜铃属（马兜铃科）中报道过该内酯，这表明可能存在掺假。借助经验证的用于检测马兜铃酸的 HPTLC 方案和对照样品，证实该商业样品是东北细辛根和柴胡根的混合物。药物的宏观检查证实了这一发现。这种掺假的高肾毒性药物引起了对在欧洲商业化的中药药物进行充分质量控制的关注。
