Application of an efficient strategy for discovery and purification of bioactive compounds from Chinese herbal medicines, a case study on the Puerariae thomsonii Flos

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.

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► An efficient strategy based on bioassay-guided fractionation, HPLC-ESI-Q/TOF-MS and HSCCC was established to screen and purify bioactive compounds from CHMs.
► The screening system succeeded in discovering anti-prostate cancer candidates from Puerariae thomsonii Flos.
► Tectoridin, tectorigenin-7-O-[β-d-xylopyranosyl-(1 → 6)-β-d-glucopyranoside and tectorigenin were prepared from Puerariae thomsonii Flos by HSCCC for the first time.
► Tectorigenin possessed potent inhibition effect on growth of RM-1 prostate cancer cells with IC50 value of 0.08 μM.