Abstract:

The purpose of the present work was to obtain anti-breast cancer compounds from Cudrania tricuspidata fruits. The
methanol extract of Cudrania tricuspidata fruits was sequentially extracted with petroleum ether (PE), ethyl acetate (AE) and n-butyl
alcohol (n-BuOH) to obtain PE, AE and n-BuOH fractions. MTT assay was used to evaluate the anti-breast cancer activity
of the methanol extract and its three fractions against breast cancer cell lines MDA-MB-231 and MCF-7. The results showed
that the AE fraction had significant inhibitory activity on MDA-MB-231 and MCF-7 cells with half maximal inhibitory
concentrations (IC50) of 75.4 and 66.8 μg/mL, respectively. Then, the AE fraction was further separated by silica gel
column chromatography and Sephadex LH-20 column chromatography assay. The structures of crystals obtained from this
separation process were identified using single-crystal X diffraction. Two major crystal components were identif??ied including
4’-O-methylalpinumisoflavone and alpinumisoflavone. As evaluated by MTT assay, the inhibitory rate of alpinumisoflavone
against MCF-7 cell growth was 56.7%. Therefore, the AE fraction from Cudrania tricuspidata fruits containing isoflavones
and alpinumisoflavones has potent anti-breast cancer activity depending on the presence of alpinumisoflavone.

Key words: Cudrania tricuspidata (Carr.) Bur. fruits, separation and extraction, anti-breast cancer, structural identification