| In vivo: |
| Pharm Biol. 2014 Jun;52(6):729-34. | | Protective effects and mechanisms of mogroside V on LPS-induced acute lung injury in mice.[Pubmed: 24621273] | Mogroside V, a compound isolated from Momordica grosvenori Swingle, which belongs to the Cucurbitaceae, is a traditional Chinese medicine reported to have anti-inflammatory potential in murine macrophages and a murine ear edema model. OBJECTIVE: To investigate the effects and mechanisms of action of this compound in a model of acute lung injury (ALI) induced by lipopolysaccharides (LPS).
METHODS AND RESULTS:
Female BALB/c mice were treated with commercial Mogroside V (2.5, 5 and 10 mg/kg) for 1 h prior to intranasal injection of LPS (10 μg in 50 μl). After 12 h, airway inflammation in the ALI model was determined by the wet/dry weight (W/D) ratio, myeloperoxidase (MPO) activity of lung tissue, leukocyte recruitment and cytokine levels in the bronchoalveolar lavage fluid (BALF). Additionally, lung tissue was examined by histology and western blotting to investigate the changes in pathology and the signalling in the presence and absence of Mogroside V. Mogroside V at 5 and 10 mg/kg inhibited airway inflammation induced by LPS as measured by the decrease in the histological changes (44 and 67.3% reduction in lung injury score, respectively), a 28.9 and 55.3% reduction in lung MPO activity, and inflammatory cell counts, interleukin-1β (IL-1β, 382 and 280 pg/ml, respectively), IL-6 (378 and 232 pg/ml, respectively) and tumor necrosis factor-α (TNF-α, 12.5 and 7.8 ng/ml, respectively) levels in the BALF. Additionally, Mogroside V treatment reduced the activation of cyclooxygenase 2 (COX-2), inducible NO synthase (iNOS), and the nuclear factor (NF)-κB.
CONCLUSIONS:
Together, these data suggest that Mogroside V has the potential to protect against LPS-induced airway inflammation in a model of ALI. | | Rsc Adv., 2016, 6(9):7034-41. | | In vitro AMPK activating effect and in vivo pharmacokinetics of mogroside V, a cucurbitane-type triterpenoid from Siraitia grosvenorii fruits[Reference: WebLink] | The aim of this study was to explore the anti-diabetic effects of cucurbitane-type triterpenoids, Mogroside V (MV) and its aglycone mogrol (MO), both isolated from the fruits of Siraitia grosvenorii Swingle, and to investigate the pharmacokinetic behaviors of MV and its metabolite MO in rats.
METHODS AND RESULTS:
The anti-diabetic effects by activating AMPK of MV and MO were evaluated in this study. Furthermore, a sensitive and specific liquid chromatography electrospray ionization-tandem mass spectrometry method for the simultaneous quantification of MV and its metabolite MO in rat plasma has been developed and validated. The assay has been successfully used for pharmacokinetic evaluation of MV and its metabolite MO after intravenous and oral administration of a single dose of MV in rats at 2.0 mg kg−1 and 5.0 mg kg−1, respectively. In vitro activities indicated that MV and its aglycone MO were both potent AMPK activators. MV and MO could activate the AMPK heterotrimer α2β1γ1 by 2.4 and 2.3 fold with an EC50 of 20.4 and 4.2 μM, respectively. This result suggested AMPK activation by MV and MO was proved to contribute at least partially to the anti-diabetic properties of S. grosvenorii. The pharmacokinetic results showed that MV was rapidly deglycosylated and metabolized into MO, and both of these were determined after intravenous administration of 2.0 mg kg−1 of MV in rats. MV was not detected in rat plasma after oral administration, whereas a trace amount of MO was found. The oral absolute bioavailability (F) of MV was estimated to be 8.73 ± 1.46% and the elimination half-life (t1/2) of metabolite MO in rats was 2.46 ± 0.19 h.
CONCLUSIONS:
It was indicated that MV showed poor absorption and/or strong metabolism in vivo. Its metabolite MO may be the main pharmacological activity form after oral administration of MV in rats. |
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