Department of Resources Science of Traditional Chinese Medicines, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
J Pharm Biomed Anal. 2013 Mar 5;75:25-32. doi: 10.1016/j.jpba.2012.11.009. Epub 2012 Nov 16.
In this study, an efficient strategy based on bioassay-guided fractionation, high-performance liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry (HPLC-ESI-Q/TOF-MS) and high-speed counter-current chromatography (HSCCC) was established to screen and purify bioactive compounds from Chinese herbal medicines (CHMs). This screening system was efficient and successfully applied to reveal anti-prostate cancer candidates from Puerariae thomsonii Flos. As a result, an active fraction with strong in vitro anti-prostate cancer activity was obtained, and the main compounds in the fraction were purified by HSCCC, giving 82 mg of tectoridin, 36 mg of tectorigenin-7-O-[β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside and 64 mg of tectorigenin. Among them, tectorigenin, possessing the highest anti-prostate cancer activity with IC₅₀ value of 0.08 μM, has priority to be lead compound. The results of this work demonstrated that the developed method was efficient and could be employed for the rapid screening, identification and purification of active components from CHMs.
在这项研究中，建立了一种基于生物测定指导分离、高效液相色谱/电喷雾电离四极杆飞行时间质谱（HPLC-ESI-Q/TOF-MS）和高速逆流色谱（HSCCC）的有效策略，用于筛选和纯化中草药（CHM）中的生物活性化合物。该筛选系统高效，成功应用于从葛根花中揭示抗前列腺癌候选物。结果，获得了具有体外强抗前列腺癌活性的活性部位，并通过 HSCCC 对该部位的主要化合物进行了纯化，得到了 82mg 的葛根素、36mg 的大豆苷元和 64mg 的大豆苷元。其中，大豆苷元具有最高的抗前列腺癌活性，IC₅₀值为 0.08μM，优先作为先导化合物。这项工作的结果表明，所开发的方法高效，可用于从 CHM 中快速筛选、鉴定和纯化活性成分。
