Abstract: Objective To improve the water solubility and biological activity of neoligans (magnolol and honokiol) and test the
antitumor activity of the modified compounds. Methods The glycosylated products of magnolol and honokiol were obtained
by enzymatic synthesis using a UDP-glycosyltransferase (YjiC) from Bacillus. The products were characterized by
high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometry (LC-MS), and nuclear magnetic
resonance (NMR) analysis. MTT assay was used to detect the growth inhibition of 4 human cancer cell lines induced by the
compounds. Results We obtained two glucosides of neolignans (magnolol and honokiol) for the first time by enzymatic
synthesis using a UDP-glycosyltransferase. Based on the spectroscopic data, the glucosides were identified as magnolol-2-
O-β-D-glucopyranoside (1) and honokiol-4’-O-β-D-glucopyranoside (2). Compounds 1-4 exhibited moderate anti-proliferative
activities against the 4 human cancer cell lines, with IC50 values ranging from 9.41 to 111.21 μmol/L. Conclusion The
glycoslated products show enhanced water solubility and drug sensitivity against SMMC7721 cells, suggesting their value as
potential therapeutic drugs.