| Kinase Assay: |
| Mol Med Rep. 2018 Feb;17(2):3267-3273. | | Protective effect of gigantol against hydrogen peroxide‑induced apoptosis in rat bone marrow mesenchymal stem cells through the PI3K/Akt pathway.[Pubmed: 29257286] | Bone marrow mesenchymal stem cell (BMSC) transplants are promising for the treatment of certain central nervous system diseases. However, oxidative stress is one of the major factors that may limit the survival of the transplanted BMSCs.
METHODS AND RESULTS:
The present study investigated the effect of pretreatment with Gigantol on hydrogen peroxide (H2O2)‑induced apoptosis in rat BMSCs (rBMSCs) and the potential underlying mechanisms. The results demonstrated that Gigantol pretreatment significantly inhibited H2O2‑induced apoptosis of rBMSCs. rBMSCs were incubated with 600 μM H2O2 in the absence or presence of different doses of Gigantol (1‑100 μM). Cell viability and apoptosis ratios were assessed by MTT assays and flow cytometry, respectively. Morphological alterations and reactive oxygen species were measured by the fluorescent‑based methods of Hoechst staining and dichlorodihydrofluorescein diacetate, respectively. Furthermore, the protein levels of phosphorylated‑protein kinase B (Akt), B‑cell lymphoma‑2 (Bcl‑2), Bcl‑2‑associated X (Bax), caspase‑3 and caspase‑9 were investigated by western blotting. Following incubation with H2O2 for 2 h, Gigantol significantly inhibited the H2O2‑induced reductions in the cell viability of rBMSCs in a dose‑dependent manner. Furthermore, Gigantol upregulated Akt phosphorylation and Bcl‑2 expression, downregulated Bax expression, and reduced the expression of caspase‑3 and caspase‑9 in H2O2‑treated rBMSCs, whereas an opposite effect was detected when LY294002, an inhibitor of phosphatidylinositol 3‑kinase, was administered in combination with Gigantol.
CONCLUSIONS:
These results indicate that Gigantol may be developed as a promising neuroprotective agent for successful MSC transplantation in ischemic diseases. | | Oncol Rep. 2017 Feb;37(2):865-870. | | Gigantol attenuates the proliferation of human liver cancer HepG2 cells through the PI3K/Akt/NF-κB signaling pathway.[Pubmed: 27959444] | Gigantol is a phenolic substance extracted from plants in the genus Dendrobium and used in traditional Chinese medicine. In the present study, we aimed to investigate the growth inhibition and apoptotic effects of Gigantol on human liver cancer cells through the PI3K/Akt/NF-κB signaling pathway.
METHODS AND RESULTS:
HepG2 cells were treated with different concentrations of Gigantol (0-150 μM) for 12, 24 and 48 h. It was found that Gigantol significantly inhibited the proliferation and induced apoptosis of the HepG2 cells. The results of fluorescence micrographs showed that a 48-h treatment with Gigantol induced typical apoptotic morphological features, which were consistent with the flow cytometric analysis where 20% of apoptotic cells were detected in response to Gigantol treatment. In addition, western blot analysis indicated that Gigantol enhanced the activities of caspase-3, PARP and p53 and downregulated the expression of p-Akt/Akt.
CONCLUSIONS:
Collectively, the present data suggest that Gigantol induces growth inhibition and apoptosis of HepG2 cells via the PI3K/Akt/NF-κB signaling pathway. | | Nat Prod Res. 2014;28(21):1900-5. | | Isolation of α-glucosidase inhibitors including a new flavonol glycoside from Dendrobium devonianum.[Pubmed: 25189122] |
METHODS AND RESULTS:
From the whole plant of Dendrobium devonianum, a new flavonol glycoside, 5-hydroxy-3-methoxy-flavone-7-O-[β-D-apiosyl-(1 → 6)]-β-D-glucoside, as well as 13 known compounds, was isolated. Their structures were identified based on extensive spectroscopic studies including HR-EI-MS, (1)H, (13)C NMR, DEPT, H-H COSY, HSQC, HMBC and NOESY spectra.
CONCLUSIONS:
The new compound and Gigantol were evaluated for their α-glucosidase inhibitory activity, and both displayed more potent α-glucosidase inhibitory activity than acarbose, one of the most potent α-glucosidase inhibitor drugs, with the inhibition rate of 43.4% and 36.7%, respectively, in the concentration of 437.5 μmol/L. |
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