| In vitro: |
| J Chromatogr A. 2015 May 1;1392:20-7. | | Fabrication of enzyme-immobilized halloysite nanotubes for affinity enrichment of lipase inhibitors from complex mixtures.[Pubmed: 25798866 ] | Lipase is the key enzyme for catalyzing triglyceride hydrolysis in vivo, and lipase inhibitors have been used in the management of obesity.
METHODS AND RESULTS:
We present the first report on the use of lipase-adsorbed halloysite nanotubes as an efficient medium for the selective enrichment of lipase inhibitors from natural products. A simple and rapid approach was proposed to fabricate lipase-adsorbed nanotubes through electrostatic interaction. Results showed that more than 85% lipase was adsorbed into nanotubes in 90 min, and approximately 80% of the catalytic activity was maintained compared with free lipase. The specificity and reproducibility of the proposed approach were validated by screening a known lipase inhibitor (i.e., orlistat) from a mixture that contains active and inactive compounds. Moreover, we applied this approach with high performance liquid chromatography-mass spectrometry technique to screen lipase inhibitors from the Magnoliae cortex extract, a medicinal plant used for treating obesity. Two novel biphenyl-type natural lipase inhibitors magnotriol A and magnaldehyde B were identified, and their IC50 values were determined as 213.03 and 96.96 μM, respectively.
CONCLUSIONS:
The ligand-enzyme interactions of magnaldehyde B were further investigated by molecular docking. Our findings proved that enzyme-adsorbed nanotube could be used as a feasible and selective affinity medium for the rapid screening of enzyme inhibitors from complex mixtures. | | Phytother Res. 2013 Sep;27(9):1419-22. | | Apoptosis-inducing and antitumor activity of neolignans isolated from Magnolia officinalis in HeLa cancer cells.[Pubmed: 23192855 ] | Two neolignans, 4'-methoxymagndialdehyde (1) and magnaldehyde B (2), were isolated from the stem bark of Magnolia officinalis (Magnoliaceae), evaluated for apoptosis-inducing effects in human cervical epitheloid carcinoma HeLa cells.
METHODS AND RESULTS:
The apoptosis-inducing activity of compounds 1 and 2 were assessed by DNA content using flow cytometric analysis. In the immunoblotting analysis, the treatment with 1 and 2 resulted in the cleavage of procaspase-8 and -3 and poly(ADP-ribose)polymerase into active forms. In addition, in vivo, the administration of 2 to Lewis lung carcinoma-inoculated mice evidenced a significant inhibition of tumor growth (volume) with reduction of 28.7% at concentration of 20 mg/kg, as compared with the control mice.
CONCLUSIONS:
These findings suggest that 2 can inhibit the proliferation of tumor cells, and might be an anti-tumoric agent. |
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