| Description: |
Puerarin 6''-O-xyloside possesses significant anti-osteoporotic activity on ovariectomy mice, it has significant antitumour activities, the mechanisms are related to increased levels of caspase-3, caspase-7, caspase-9 and Bax, and reduced levels Bcl-2.
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| Targets: |
Bcl-2/Bax | Caspase |
| In vitro: |
| Pharm Biol. 2016 Sep;54(9):1793-9. | | In vitro and in vivo antitumour activities of puerarin 6″-O-xyloside on human lung carcinoma A549 cell line via the induction of the mitochondria-mediated apoptosis pathway.[Pubmed: 26730946] | Pueraria lobata (Leguminoseae) shows cytotoxic effects against cancer cells; however, its active components remain unclear. This study investigated the antitumour activity of puerarin 6″-O-xyloside (POS) on the human lung carcinoma A549 cell line.
METHODS AND RESULTS:
The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to determine the cytotoxicity of POS (at 10, 20 and 40 μM) in vitro, and xenograft nude mice were established to evaluate the antitumour effect of POS (at 40 mg/kg/d) in vivo by 15 days intraperitoneal injection (ip). To explore its mechanism of action, flow cytometry was performed to determine the pro-apoptotic effect of POS (at 10, 20 and 40 μM). Subsequently, the expression of caspase-3, caspase-7, caspase-9, Bcl-2 and Bax in A549 cells were determined. POS showed significant cytotoxicity toward A549 cells (p < 0.05) by inducing apoptosis. Treatment with POS significantly upregulated the levels of caspase-3 (p < 0.01), caspase-7 (p < 0.01), caspase-9 (p < 0.01) and Bax (p < 0.01) in A549 cells, and Bcl-2 was downregulated (p < 0.01). Additionally, the in vivo animal study showed that POS significantly inhibited tumour growth in A549 cells (p < 0.01).
CONCLUSIONS:
Our study demonstrated the POS has significant antitumour activities. The mechanisms are related to increased levels of caspase-3, caspase-7, caspase-9 and Bax, and reduced levels Bcl-2.
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| In vivo: |
| Pharm Biol. 2015 Apr 10:1-7. | | Anti-osteoporotic activity of puerarin 6″-O-xyloside on ovariectomized mice and its potential mechanism.[Pubmed: 25857587] | Osteoporosis is one of the most common bone diseases, and radix of Pueraria lobata (Willd.) Ohwi possesses an obvious therapeutical effect on postmenopausal osteoporosis.
This study investigates the anti-osteoporotic activity of the puerarin 6"-O-xyloside (PXY) on ovariectomized mice and its related mechanism.
METHODS AND RESULTS:
Osteoporotic mice model was established by ovariectomy (OVX). A total of 50 mice were divided into five groups (n = 10): sham, OVX group, PXY treatment groups (20, 40, and 60 mg/kg/d, i.p.). After 12 weeks' treatment, body weights were recorded. Then, mice were sacrificed, and serum samples were collected to determine the blood calcium, blood phosphorus, alkaline phosphatase (ALP), and osteoprotegerin (OPG) concentrations and uterine index was assayed. The thigh-bones of mice were collected to evaluate histopathological changes. In the in vitro experiment, the effect of PXY on osteoblasts' proliferation was evaluated and western blotting was performed to determine expressions of OPG and the receptor activators of NF-κB ligand (RANKL), as well as the ratio of OPG/RANKL.
PXY (40 and 60 mg/kg/d, i.p.) obviously decreased body weights and increased uterine index of OVX (p < 0.05), and improved osteoporotic syndromes of OVX mice; PXY also significantly increased the concentrations of blood calcium, blood phosphorus, ALP, and OPG of OVX mice (p < 0.05); moreover, PXY obviously up-regulated the ratio of OPG/RANKL (p < 0.05).
CONCLUSIONS:
Our results demonstrated that the puerarin 6"-O-xyloside possesses significant anti-osteoporotic activity on ovariectomy mice.
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