A ginsenoside with diverse biological activities
Ginsenoside Rg5 is a ginsenoside originally isolated from P. ginseng that has diverse biological activities, including anticancer, anti-inflammatory, neuroprotective, and antioxidant properties.1,2,3 It inhibits the growth of HeLa and MS751 cervical cancer cells (IC50s = ~2.5-10 μM) and induces apoptosis in a concentration-dependent manner.1 Ginsenoside Rg5 (5 and 10 μM) inhibits LPS-induced increases in IL-1β, TNF-α, COX-2, and inducible nitric oxide synthase (iNOS) protein levels in murine alveolar macrophages.2 It also inhibits LPS-induced increases in the number of neutrophils and protein levels of IL-1β, TNF-α, COX-2, and iNOS in lung in a mouse model of acute lung inflammation when administered at a dose of 10 mg/kg. In a rat model of Alzheimer's disease induced by streptozotocin , ginsenoside Rg5 blocks STZ-induced increases in amyloid-β accumulation in the hippocampus and cerebral cortex and prevents STZ-induced decreases in step through latency time in a passive avoidance foot-shock test in a dose-dependent manner.3
1.Liang, L.-D., He, T., Du, T.-W., et al.Ginsenoside?Rg5 induces apoptosis and DNA damage in human cervical cancer cellsMol. Med. Rep.11(2)940-946(2015) 2.Kim, T.-W., Joh, E.-H., Kim, B., et al.Ginsenoside Rg5 ameliorates lung inflammation in mice by inhibiting the binding of LPS to toll-like receptor-4 on macrophagesInt. Immunopharmacol.12(1)110-116(2012) 3.Chu, S., Gu, J., Feng, L., et al.Ginsenoside Rg5 improves cognitive dysfunction and beta-amyloid deposition in STZ-induced memory impaired rats via attenuating neuroinflammatory responsesInt. Immunopharmacol.19(2)317-326(2014)
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Kinase experiment: |
HUVECs are cultured in 24-well plates overnight. The cells are changed to serum-free M199 and incubated for 1 h. The medium is removed, and cells are incubated with fresh serum-free medium containing 0.1 μM-50 mM Ginsenoside Rg5 at 37°C for 20 min followed by the addition of 50 μL (1 μCi) of [125I]IGF-1 and then further incubated for 10 min. The medium is decanted, and cell plates are washed twice with serum-free medium. Cells are lysed in 300 μL of 0.1 N NaOH solution containing 0.1% SDS, transferred to scintillation vials, and mixed with 1 mL of Ultima Gold mixture solution. Cell-associated [125I]IGF-1 is analyzed in a scintillation counter. The nonspecific binding is determined by coincubation with unlabeled IGF-1 (50 nM)[1]. |
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Cell experiment: |
MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) human breast cancer cell lines are maintained using RPMI 1640 medium supplemented with 10% (vol/vol) FBS plus 100 units/mL Penicillin and Streptomycin in a 5% carbon dioxide air incubator at 37°C. Cell cytotoxicity is measured by MTT assay. Cells are seeded in 96-well tissue culture plates at the density of 0.2×104 cells per well with 100 μL medium, and are allowed to become attached for 24 h. One hundred microliters of the medium with different concentrations of Ginsenoside Rg5 (e.g., 0 μM, 25 μM, 50 μM, and 100 μM) are added to each well. At indicated times, 30 μL MTT stock solution (3 mg/mL) are added to each well. After culturing the cells at 37°C for 2 h, DMSO is added to dissolve the formazan crystals. The absorbance is read at the wavelength of 540 nm with a microplate reader[3]. |
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Animal experiment: |
Mice[2]Male ICR mice (6 to 8 weeks old), weighing 25-27 g, are used. After acclimation for one week, mice are randomly assigned into 4 experimental groups with 8 mice in each group: normal control, Cisplatin control, and Cisplatin+Ginsenoside Rg5 groups (10 and 20 mg/kg, respectively). Ginsenoside Rg5 is administered intragastrically at the dose of 10 and 20 mg/kg for 10 days. On the 7th day, animals in Cisplatin control and Ginsenoside Rg5-treated groups receive a single intraperitoneal injection of Cisplatin (25 mg/kg) to induce nephrotoxicity in mice. Mice are anaesthetized with pentobarbital, subsequently sacrificed at 72 h after Cisplatin injection (Day 10). Blood samples are collected and then centrifuged at 3000 rpm to separate the serum and stored at -20 °C for determining blood urea nitrogen (BUN) and creatinine (CRE) levels. |
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参考文献: [1]. Cho YL, et al. Specific activation of insulin-like growth factor-1 receptor by ginsenoside Rg5 promotes angiogenesis and vasorelaxation. J Biol Chem. 2015 Jan 2;290(1):467-77. |
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