Abstract
Novel proanthocyanidin fractions from grape stem extracts were purified using Amberlite XAD-1180N, Sephadex-LH-20, Toyopearl HW40F and reverse phase high-performance liquid chromatography. Two key compounds were estimated as epigallocatechin-(epicatechin)7 gallate using electron-spray ionization time-of-flight mass spectrometry. Epigallocatechin-(epicatechin)7 gallate (compound 1) showed significant anti-cancer activity in PC-3 prostate cancer cells. In particular, compound 1 suppressed the gene expression of fatty acid-binding protein 5 (FABP5), which is involved in promoting cell proliferation and metastasis in prostate cancer cells.
Highlights
Novel proanthocyanidin fractions from grape stem extracts were purified using Amberlite XAD-1180N, Sephadex-LH-20, Toyopearl HW40F and reverse phase high-performance liquid chromatography
The high-performance liquid chromatography (HPLC) chromatogram of crude grape stem extracts is shown in Supplementary Fig. 1
Compound 1 showed much higher inhibition of cell growth of PC-3 cells compared with epigallocatechin 3-gallate (EGCG)
Summary
Novel proanthocyanidin fractions from grape stem extracts were purified using Amberlite XAD-1180N, Sephadex-LH-20, Toyopearl HW40F and reverse phase high-performance liquid chromatography. Epigallocatechin-(epicatechin)[7] gallate (compound 1) showed significant anti-cancer activity in PC-3 prostate cancer cells. Proanthocyanidins reportedly show various biological activities such as the suppression of endotherin-1 gene expression[3], anti-inflammatory effects[4] and inhibition of cancer cell proliferation[5,6,7,8,9,10]. Gel filtration chromatography and HPLC was successfully applied in the present study to isolate a novel proanthocyanidin. This compound was octameric epicatechins with an epigallocatechin unit and a gallate unit, respectively. Www.nature.com/scientificreports the compound suppressed the expression of the cancer-promoting gene FABP512,13 and exhibited superior activity compared with that of epigallocatechin 3-gallate (EGCG)
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