Ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry analysis of icariside II metabolites in rats

Sun, E; Xu, Fei; Qian, Qian; Cui, Li; Tan, Xuecai; Jia, Xiao‐Bin

doi:10.1080/14786419.2014.921684

Cited by 12 publications

(5 citation statements)

References 9 publications

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“…We also found that IS down-regulated cFLIP partially through inhibition of NF-κB nuclear translocation (summarized in Figure 6E). The anti-inflammatory, anticancer activities and the pharmacokinetic of IS have been studied [21, 32, 33]. IS might be a promising agent in reversing TRAIL resistance.…”

Section: Discussionmentioning

confidence: 99%

Icariside II overcomes TRAIL resistance of melanoma cells through ROS-mediated downregulation of STAT3/cFLIP signaling

et al. 2016

Oncotarget

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Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a promising antitumor agent. However, many melanoma cells show weak responses to TRAIL. Here, we investigated whether Icariside II (IS), an active component of Herba Epimedii, could potentiate antitumor effects of TRAIL in melanoma cells. Melanoma cells were treated with IS and/or TRAIL and cell death, apoptosis and signal transduction were analyzed. We showed that IS promoted TRAIL-induced cell death and apoptosis in A375 melanoma cells. Mechanistically, IS reduced the expression levels of cFLIP in a phospho-STAT3 (pSTAT3)-dependent manner. Ectopic expression of STAT3 abolished IS-induced cFLIP down-regulation and the associated potentiation of TRAIL-mediated cell death. Moreover, IS-induced reactive oxygen species (ROS) production preceded down-regulation of pSTAT3/cFLIP via activating AKT, and the consequent sensitization of cells to TRAIL. We also found that IS treatment down-regulated cFLIP via ROS-mediated NF-κB pathway. In addition, IS converted TRAIL-resistant melanoma MeWo and SK-MEL-28 cells into TRAIL-sensitive cells. Taken together, our results indicated that IS potentiated TRAIL-induced apoptosis through ROS-mediated down-regulation of STAT3/cFLIP signaling.

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Section: Discussionmentioning

confidence: 99%

Icariside II overcomes TRAIL resistance of melanoma cells through ROS-mediated downregulation of STAT3/cFLIP signaling

et al. 2016

Oncotarget

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“…The results showed that the metabolized mainly via desugarisation, dehydrogenation, hydrogenation, hydroxylation, demethylation, glucuronidation, dehydration, and glycosylation pathways in vivo . Specific hydrolysis of 7-O glucoside in the gut lumen and glucuronic acid conjugation in the liver was considered as the main physiologic processes of icariside II (Sun et al, 2014). …”

Section: Components Isolated From Tcms That Target Epidermal Growth Fmentioning

confidence: 99%

Development of Certain Protein Kinase Inhibitors with the Components from Traditional Chinese Medicine

et al. 2017

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Traditional Chinese medicines (TCMs) have been used in China for more than two thousand years, and some of them have been confirmed to be effective in cancer treatment. Protein kinases play critical roles in control of cell growth, proliferation, migration, survival, and angiogenesis and mediate their biological effects through their catalytic activity. In recent years, numerous protein kinase inhibitors have been developed and are being used clinically. Anticancer TCMs represent a large class of bioactive substances, and some of them display anticancer activity via inhibiting protein kinases to affect the phosphoinositide 3-kinase, serine/threonine-specific protein kinases, pechanistic target of rapamycin (PI3K/AKT/mTOR), P38, mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinases (ERK) pathways. In the present article, we comprehensively reviewed several components isolated from anticancer TCMs that exhibited significantly inhibitory activity toward a range of protein kinases. These components, which belong to diverse structural classes, are reviewed herein, based upon the kinases that they inhibit. The prospects and problems in development of the anticancer TCMs are also discussed.

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“…IT was the structural parent nucleus of ICA and BHG-I, and the glycosylation number of IT, BHG-I, and ICA were 0, 1, 2, respectively (Figure 1). Previous studies revealed that higher concentrations of IT were discovered in rat plasma, urine, and feces after oral administration of ICA or BHG-I (Sun et al, 2014;Sun et al, 2016). Pharmacological studies confirmed that ICA increased bone mass and prevent glucocorticoid-induced apoptosis in osteocytes (Feng et al, 2013;Wang et al, 2018).…”

Section: Introductionmentioning

confidence: 97%

Prediction and Verification of Epimedium Flavonoids With Different Glycosylation Numbers in Reversing Glucocorticoid-Induced Bone Formation Inhibition by Molecular Docking and Zebrafish

Jiang

Xiao

et al. 2022

Front. Environ. Sci.

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Glucocorticoids have been detected in environmental waters, and their biological potency has raised concerns on their impact on aquatic vertebrates especially fish. Numerous researches showed that the continuous and direct contact of aquatic vertebrates with glucocorticoid contaminants in environmental water will cause bone formation inhibition. The aim of this study is to predict and verify the effect of icaritin (IT), icariin (ICA), and baohuside-I (BHG-I) in reversing glucocorticoid-induced bone formation inhibition (GIBFI) by molecular docking and zebrafish model. We contrasted their activity in reversing GIBFI from their affinity to bone metabolism proteins (OPG, RANKL, BMP-2, BMP-4, Runx-2) by molecular docking. Subsequently, zebrafish model was adopted to evaluate their reverse effects on GIBFI. Alizarin red staining coupled with image quantification were performed to evaluate the effects of ICA, IT, and BHG-I on skeleton stained area (SSA) and cumulative optical density (COD). Inductively coupled plasma-mass spectrometry was applied to determine the contents of bone mineral elements (CBME, Mg, K, Ca, Fe, Zn) in zebrafish bones. Docking results showed the receptors (BMP-2, BMP-4, and Runx2) all combined well to ICA, while BHG-I bound well to OPG, the affinity between IT and the above targets were the weakest. Fortunately, IT, ICA, and BHG-I significantly increased the SSA, COD, and the contents of Ca compared with the model group (p < 0.05) in the order of IT>ICA>BHG-I. In conclusion, the glycosyl groups increased the H-bond affinity between flavonoids and target sites, which weakened bone formation. IT, BHG-I, and ICA all alleviated GIBFI, but their intensity order was IT>ICA>BHG-I.

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Ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry analysis of icariside II metabolites in rats

Cited by 12 publications

References 9 publications

Icariside II overcomes TRAIL resistance of melanoma cells through ROS-mediated downregulation of STAT3/cFLIP signaling

Icariside II overcomes TRAIL resistance of melanoma cells through ROS-mediated downregulation of STAT3/cFLIP signaling

Development of Certain Protein Kinase Inhibitors with the Components from Traditional Chinese Medicine

Prediction and Verification of Epimedium Flavonoids With Different Glycosylation Numbers in Reversing Glucocorticoid-Induced Bone Formation Inhibition by Molecular Docking and Zebrafish

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