Trilobatin

Trilobatin attenuates the LPS-mediated inflammatory response by suppressing the NF-κB signaling pathway.[Pubmed: 25053100 ]

Food Chem. 2015 Jan 1;166:609-15.

We investigated the anti-inflammatory effect of Trilobatin, the flavonoid isolated from the leaves of Lithocarpus polystachyus Rehd, as well as the underlying molecular mechanisms.
METHODS AND RESULTS:
Treatment with Trilobatin (0.005-5 μM) dose-dependently inhibited the lipopolysaccharide (LPS)-induced mRNA expression and secretion of pro-inflammatory cytokines, including tumor necrosis factor α (TNFα), interleukin-1β (IL-1β) and interleukin-6 (IL-6), in RAW 264.7 macrophages. However, no further inhibition was detected when the concentration of Trilobatin was increased to 50 μM. Western blot analysis confirmed that the mechanism of the anti-inflammatory effect was correlated with the inhibition of LPS-induced inhibitor of nuclear factor-kappa B α (IκBα) degradation and nuclear factor-kappa B (NF-κB) p65 phosphorylation. In addition, Trilobatin also showed a significant inhibition of LPS-induced TNFα and IL-6 at both the mRNA and protein levels in a mouse model.
CONCLUSIONS:
Our results suggest that Trilobatin potentially inhibits the LPS-induced inflammatory response by suppressing the NF-κB signaling pathway.

Antioxidant activities of three dihydrochalcone glucosides from leaves of Lithocarpus pachyphyllus.[Pubmed: 15813365]

Z Naturforsch C. 2004 Jul-Aug;59(7-8):481-4.

In vitro antioxidant activities of three sweet dihydrochalcone glucosides from the leaves of Lithocarpus pachyphyllus (Kurz) Rehd. (Fagaceae), Trilobatin 2"-acetate (1), phloridzin (2) and Trilobatin (3), were investigated.
METHODS AND RESULTS:
The IC50 (50% inhibitory concentration) values for compounds 1-3 of lipid peroxidation in rat liver homogenate were 261, 28, 88 microM, respectively. Compounds 1-3 increased superoxide dismutase (SOD) activity with EC50 (50% effective concentration) values of 575, 167, 128 microM, and glutathione peroxidase (GSH-Px) activity with EC50 values of 717, 347, 129 microM, respectively, and showed only weak DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging activity.

Inhibitory potential of trilobatin from Lithocarpus polystachyus Rehd against α-glucosidase and α-amylase linked to type 2 diabetes.[Reference: WebLink]

Food Chemistry, 2012, 130(2):261-266.

The chemical structure of the sweet compound from Lithocarpus polystachyus Rehd was identified as Trilobatin on the basis of HPLC, EIS-MS and NMR analyses.
METHODS AND RESULTS:
The inhibitory activities of Trilobatin against α-glucosidase and α-amylase were evaluated, and the inhibition mechanism was analysed with Lineweaver–Burk plots. Also the antioxidant activity evaluation of Trilobatin was conducted by DPPH radical scavenging assay. Comparing with acarbose, Trilobatin showed a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase. The Lineweaver–Burk plots analysis elucidated that Trilobatin inhibited the enzyme non-competitively. DPPH scavenging activity of Trilobatin (IC 50 02=020.5702mg/ml) was higher than rutin (IC 50 02=020.7202mg/ml), which indicated that Trilobatin had a moderate antioxidant potential.
CONCLUSIONS:
These results suggest that Trilobatin is a potential effective α-glucosidase inhibitor for management of postprandial hyperglycemia with less side effect, and provide strong rationale for further animal and clinical studies.