Abstract

Background: Scutellaria barbata (S. barbata) is promising for cancer therapy. However, its anti-cancer material basis is unclear, and a sensitive detection method for the trace level of highly active ingredients in S. barbata is lacking.

Objective: The present study aims to develop an efficient procedure for screening and quantifying the active ingredient groups of phenolic acid and flavonoids in S. barbata and to preliminarily evaluate S. barbata material on multi-ingredient and multi-target bases.

Methods: Hollow fibre cell fishing with high performance liquid chromatography (HFCF–HPLC) based on human renal adenocarcinoma ACHN cell and hollow fibre liquid phase microextraction with HPLC (HF-LPME–HPLC) were developed and employed to study the active groups of phenolic acid and flavonoids in S. barbata.

Results: The active ingredients were screened, and some of their structures were confirmed, including protocatechuic acid, scutellarin, baicalein, luteolin, apigenin and wogonin; these S. barbata active ingredients are used to treat renal cancer. The contents of these confirmed active ingredients were quantified. The cell apoptosis rates of ACHN cells and cell fishing factors of the active ingredients screened by HFCF–HPLC were determined. The binding sites of the active groups on ACHN cells were preliminarily studied.

Conclusion: With simultaneous functions of active screening, confirming and quantifying, the procedures of HFCF–HPLC coupled with HF-LPME–HPLC, can not only improve the efficiency of drug research and narrow the gap from blind to clear for defining active ingredients but also confirms the multi-ingredient and multi-target characteristics of TCMs.

Keywords: Hollow fibre, liquid phase microextraction, activity screening, renal cancer, Scutellaria barbata, bioactive.

Graphical Abstract