Oroxylin A reverses CAM-DR of HepG2 cells by suppressing Integrinβ1 and its related pathway

Zhu, Binbin; Zhao, Li; Zhu, Litao; Wang, Hu; Sha, Yunying; Yao, Jing; Li, Zhiyu; Qin, You; Guo, Qinglong

doi:10.1016/j.taap.2012.01.019

Cited by 26 publications

(16 citation statements)

References 26 publications

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“…It is proved that weak‐toxic concentrations (50–200 μM, with an apoptosis rate less than 20%) of oroxylin A could dramatically increase the apoptosis induced by paclitaxel in CAM‐DR model. The mechanism might be because oroxylin A suppressed the expression of integrin β1 and its initiated signal transduction phosphatidyl inositol 3′‐kinas (PI3K)/Akt pathway (Zhu et al, ).…”

Section: Pharmacological Activitymentioning

confidence: 99%

Overview of Oroxylin A: A Promising Flavonoid Compound

Guo

Zhao

2016

Phytotherapy Research

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Oroxylin A is one of the main active components extracted from Scutellariae radix. It has been proved that oroxylin A possesses a broad spectrum of pharmacological functions, including anti-cancer, antiinflammation, neuroprotective, anti-coagulation and so on. The pharmacological activity of oroxylin A has been studied in vitro and on animal models, which reflected its promising potency in disease treatment. This review aims to recapitulate the pharmacological function and the molecular mechanisms of oroxylin A, as well as its sources, extraction, synthesis and toxicity study. These data confirmed the therapeutic potential of oroxylin A and provided reference for further development. Copyright © 2016 John Wiley & Sons, Ltd.

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Section: Pharmacological Activitymentioning

confidence: 99%

Overview of Oroxylin A: A Promising Flavonoid Compound

Guo

Zhao

2016

Phytotherapy Research

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“…The survival rate of cells was calculated using the following formula: survival rate (%)=(absorbance of treated group-absorbance of blank control)/(absorbance of negative control-absorbance of blank control)×100% [23] .…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

The pyrrolidinoindoline alkaloid Psm2 inhibits platelet aggregation and thrombus formation by affecting PI3K/Akt signaling

Wang

et al. 2016

Acta Pharmacol Sin

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Aim: Psm2, one of the pyrrolidinoindoline alkaloids isolated from whole Selaginella moellendorffii plants, has shown a potent antiplatelet activity. In this study, we further evaluated the antiplatelet effects of Psm2, and elucidated the underlying mechanisms. Methods: Human platelet aggregation in vitro and rat platelet aggregation ex vivo were investigated. Agonist-induced platelet aggregation was measured using a light transmission aggregometer. The antithrombotic effects of Psm2 were evaluated in arteriovenous shunt thrombosis model in rats. To elucidate the mechanisms underlying the antiplatelet activity of Psm2, ELISAs, Western blotting and molecular docking were performed. The bleeding risk of Psm2 administration was assessed in a mouse tail cutting model, and the cytotoxicity of Psm2 was measured with MTT assay in EA.hy926 cells. Results: Psm2 dose-dependently inhibited human platelet aggregation induced by ADP, U4619, thrombin and collagen with IC 50 values of 0.64, 0.37, 0.35 and 0.87 mg/mL, respectively. Psm2 (1, 3, 10 mg/kg) administered to rats significantly inhibited platelet aggregation ex vivo induced by ADP. Psm2 (1, 3, 10 mg/mL, iv) administered to rats with the A-V shunt dose-dependently decreased the thrombus formation. Psm2 inhibited platelet adhesion to fibrinogen and collagen with IC 50 values of 84.5 and 96.5 mg/mL, respectively, but did not affect the binding of fibrinogen to GPIIb/IIIa. Furthermore, Psm2 inhibited AktSer473 phosphorylation, but did not affect MAPK signaling and Src kinase activation. Molecular docking showed that Psm2 bound to phosphatidylinositol 3-kinase β (PI3Kβ) with a binding free energy of -13.265 kcal/mol. In addition, Psm2 did not cause toxicity in EA.hy926 cells and produced only slight bleeding in a mouse tail cutting model. Conclusion: Psm2 inhibits platelet aggregation and thrombus formation by affecting PI3K/Akt signaling. Psm2 may be a lead compound or drug candidate that could be developed for the prevention or treatment of thrombotic diseases.

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“…Huh7 cells (Cheng et al, 2012) and HepG2 cells (Zhu et al, 2012) have been described previously. They were maintained in complete Dulbecco's modified Eagle's medium (C-DMEM; Mediatech, Inc.) supplemented with 10% heat-inactivated fetal bovine serum (FBS; Sigma-Aldrich Co. LLC) and 1% penicillin and streptomycin (P/S; Lonza).…”

Section: Cell Lines and Culturesmentioning

confidence: 99%

SelectiveIn VivoTargeting of Human Liver Tumors by Optimized AAV3 Vectors in a Murine Xenograft Model

et al. 2014

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Current challenges for recombinant adeno-associated virus (rAAV) vector-based cancer treatment include the low efficiency and the lack of specificity in vivo. rAAV serotype 3 (rAAV3) vectors have previously been shown to be ineffective in normal mouse tissues following systemic administration. In the present study, we report that rAAV3 vectors can efficiently target and transduce various human liver cancer cells in vivo. Elimination of specific surface-exposed serine and threonine residues on rAAV3 capsids results in further augmentation in the transduction efficiency of these vectors, without any change in the viral tropism and cellular receptor interactions. In addition, we have identified a potential chemotherapy drug, shikonin, as a multifunctional compound to inhibit liver tumor growth as well as to significantly enhance the efficacy of rAAV vector-based gene therapy in vivo. Furthermore, we also document that suppression of tumorigenesis in a human liver cancer xenograft model can be achieved through systemic administration of the optimized rAAV3 vectors carrying a therapeutic gene, and shikonin at a dose that does not lead to liver damage. Our research provides a novel means to achieve not only targeted delivery but also the potential for gene therapy of human liver cancer.

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Oroxylin A reverses CAM-DR of HepG2 cells by suppressing Integrinβ1 and its related pathway

Cited by 26 publications

References 26 publications

Overview of Oroxylin A: A Promising Flavonoid Compound

Overview of Oroxylin A: A Promising Flavonoid Compound

The pyrrolidinoindoline alkaloid Psm2 inhibits platelet aggregation and thrombus formation by affecting PI3K/Akt signaling

SelectiveIn VivoTargeting of Human Liver Tumors by Optimized AAV3 Vectors in a Murine Xenograft Model

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