title: Application of an efficient strategy for discovery and purification of bioactive compounds from Chinese herbal medicines, a case study on the Puerariae thomsonii Flos.
abstract: 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.
authors: Department of Resources Science of Traditional Chinese Medicines, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
authors: Qi
authors: Q
authors: Wang
authors: Xiao-Lan
authors: XL
authors: Cheng
authors: Huan
authors: H
authors: Li
authors: Xiao-Ying
authors: XY
authors: Qin
authors: Chi-Yu
authors: CY
authors: Ge
authors: Rui
authors: R
authors: Liu
authors: Lian-Wen
authors: LW
authors: Qi
authors: Min-Jian
authors: MJ
authors: Qin
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D003377:Countercurrent Distribution; D055808:Drug Discovery / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D020834:Ethnopharmacology; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000502:physiology; D020128:Inhibitory Concentration 50; D007529:Isoflavones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology / Q000502:physiology; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D029908:Pueraria; D021241:Spectrometry, Mass, Electrospray Ionization; D053719:Tandem Mass Spectrometry
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004365:Drugs, Chinese Herbal; D006027:Glycosides; D007529:Isoflavones; C442841:Puerariae Flos extract; C581943:tectorigenin 7-O-(apiofuranosyl-beta-D-xylopyranosyl-(1-6)-beta-D-glucopyranoside); C120039:tectorigenin; C120040:tectoridin