Inhibitory Effects of Scutellarein on Proliferation of Human Lung Cancer A549 Cells through ERK and NFκB Mediated by the EGFR Pathway

Cheng, Chun-Yuan; Hu, Chao-Chin; Yang, Hui-Ju; Lee, Meng-Chih; Kao, Erl-Shyh

doi:10.4077/cjp.2014.bac200

Cited by 34 publications

(28 citation statements)

References 26 publications

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“…The reduction of p-EGFR and p-Akt decreased in the early time point and increased during the late time point, a trend that may be associated with melanogenesis inducer a-MSH. 20,21 These results suggest that the moderate miR-21-induced activation of EGFR/ Akt accounts for the anti-melanogenic effect in UV ray-radiated cells.…”

Section: Discussionmentioning

confidence: 94%

Regulation of miR-21 expression in human melanoma via UV-ray-induced melanin pigmentation

Lin

Chen

et al. 2017

Environmental Toxicology

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Excessive environmental ultraviolet (UV) radiation produces genetic mutations that can lead to skin cancer. This study was designed to assess the potential inhibitory activity of microRNA-21 (miR-21) on the UV irradiation-stimulated melanogenesis signal pathway in melanoma cells. The molecular mechanism of miR-21-induced inhibitory activity on UV-ray-stimulated melanogenesis-regulating proteins was examined in A375.S2 human melanoma and B16F10 mouse melanoma cells. UV irradiation for 30 min induced melanogenesis signal pathway by increasing melanin production and the number of A375.S2 cells. Similarly, UV radiation increased the expression of α-melanocyte-stimulating hormone (α-MSH) protein and decreased the melanogenesis-regulating signal, such as EGFR and Akt phosphorylation. Notably, miR-21 overexpression in UV-ray-stimulated A375.S2 cells decreased α-MSH expression and increased EGFR and Akt phosphorylation levels. Furthermore, miR-21 on UV-ray- induced melanogenesis was down-regulated by the Akt inhibitor and the EGFR inhibitor (Gefitinib). Results suggest that the suppressive activity of miR-21 on UV-ray-stimulated melanogenesis may involve the down-regulation of α-MSH and the activation in both of EGFR and Akt.

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Section: Discussionmentioning

confidence: 94%

Regulation of miR-21 expression in human melanoma via UV-ray-induced melanin pigmentation

Lin

Chen

et al. 2017

Environmental Toxicology

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“…Indeed, it was reported that scutellarein improved micro-circulation and cerebral blood flow 42) and inhibited cancer cell proliferation and metastasis. 43,44) Scutellarein could also decrease platelet aggregation in spontaneously hypertensive rats. 19) In a recent paper published by Yan et al, 45) scutellarein dose-dependently depressed arterial or venous thrombosis in vivo, and restricted the rate of ADP-induced platelet aggregation.…”

Section: Discussionmentioning

confidence: 99%

Delineation of Platelet Activation Pathway of Scutellarein Revealed Its Intracellular Target as Protein Kinase C

Tian

Chang

et al. 2016

Biological & Pharmaceutical Bulletin

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Erigeron breviscapus has been widely used in traditional Chinese medicine (TCM) and its total flavonoid component is commonly used to treat ischemic stroke, coronary heart disease, diabetes and hypertension. Scutellarin is the major ingredient of E. breviscapus and scutellarein is one of the main bioactive metabolites of scutellarin in vivo, but the latter's pharmacological activities have not been fully characterized. Provided evidence that could inhibit platelet aggregation, the effect of scutellarein on rat washed platelets and its underlying mechanisms were evaluated in our research. Scutellarein inhibited platelet adhesion and aggregation induced by multiple G protein coupled receptor agonists such as thrombin, U 46619 and ADP, in a concentration-dependent manner. Furthermore, the mild effect of scutellarein on intracellular Ca 2 mobilization and cyclic AMP (cAMP) level was observed. On the other hand, the role of scutellarein as potential protein kinase C (PKC) inhibitor was confirmed by PKC activity analysis and molecular docking. The phorbol myristate acetate-induced platelets aggregation assay with or without ADP implied that the scutellarein takes PKC(s) as its primary target(s), and acts on it in a reversible way. Finally, scutellarein as a promising agent exhibited a high inhibition effect on ADP-induced platelet aggregation among its analogues. This study clarifies the PKC-related signaling pathway involved in antiplatelet action of scutellarein, and may be beneficial for the treatment of cardiovascular diseases.

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“…It has many biochemical activities, including targeting of the phosphoinositide 3-kinase (PI3K)/ Akt signaling pathway, upregulation of tumor necrosis factor (TNF)-related apoptosisinducing ligand (TRAIL) death receptors DR4/DR5 expression in a p53-dependent manner, inhibition of glutamine metabolism, and induction of the epidermal growth factor receptor (EGFR) pathway. [7][8][9][10] However, the clinical use of apigenin is restricted, owing to its poor biopharmaceutical properties, including water insolubility and poor absorption. 11 Although apigenin is predicted to be safe for lung cancer treatment, similar to the majority of antitumor drugs, resistance could develop during the course of treatment, which could result in therapeutic failure.…”

Section: Introductionmentioning

confidence: 99%

Synergistic apoptotic effects of apigenin TPGS liposomes and tyroservatide: implications for effective treatment of lung cancer

Jin¹,

Yang²,

Zhang³

2017

IJN

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To develop an alternative treatment for lung cancer, a combination of two potent chemotherapeutic agents – liposomal apigenin and tyroservatide – was developed. The therapeutic potential of this combination was investigated using A549 cells. Apigenin and tocopherol derivative-containing D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) liposomes might improve the delivery of apigenin to tumor cells, both in vitro and in vivo. Importantly, compared to either agent alone, the combination of apigenin TPGS liposomes and tyroservatide exhibited superior cytotoxicity, induced stronger G2 arrest, and suppressed A549 cancer cell invasion at a lower dose. The proapoptotic synergistic effects were also observed in A549 cells using terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling, flow cytometry, and Western blot analysis. More importantly, in vivo results showed that the combination of apigenin TPGS liposomes and tyroservatide exhibited tumor-growth inhibitory effects in A549 cell-bearing mice. In conclusion, our study showed that this combination therapy could serve as a promising synergistic therapeutic approach to improve outcomes in patients with lung cancer.

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Inhibitory Effects of Scutellarein on Proliferation of Human Lung Cancer A549 Cells through ERK and NFκB Mediated by the EGFR Pathway

Cited by 34 publications

References 26 publications

Regulation of miR-21 expression in human melanoma via UV-ray-induced melanin pigmentation

Regulation of miR-21 expression in human melanoma via UV-ray-induced melanin pigmentation

Delineation of Platelet Activation Pathway of Scutellarein Revealed Its Intracellular Target as Protein Kinase C

Synergistic apoptotic effects of apigenin TPGS liposomes and tyroservatide: implications for effective treatment of lung cancer

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