Transglycosylation of neolignans by enzymatic synthesis and evaluation of their antitumor activity / 南方医科大学学报
Journal of Southern Medical University
;
(12): 1570-1574, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-232569
ABSTRACT
<p><b>OBJECTIVE</b>To improve the water solubility and biological activity of neoligans (magnolol and honokiol) and test the antitumor activity of the modified compounds.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>The glycoslated products show enhanced water solubility and drug sensitivity against SMMC7721 cells, suggesting their value as potential therapeutic drugs.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Mass Spectrometry
/
Biphenyl Compounds
/
Glycosylation
/
Magnetic Resonance Spectroscopy
/
Chemistry
/
Chromatography, High Pressure Liquid
/
Lignans
/
Cell Line, Tumor
/
Glucosides
/
Antineoplastic Agents, Phytogenic
Limits:
Humans
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2015
Type:
Article
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