Degradable poly(apigenin) polymer inhibits tumor cell adhesion to vascular endothelial cells

Cochran, David B.; Gray, Lindsay N.; Anderson, Kimberly W.; Dziubla, Thomas D.

doi:10.1002/jbm.b.33486

Cited by 17 publications

(11 citation statements)

References 30 publications

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“…Apigenin-loaded lipid nanocapsules prepared with phase inversion method showed high efficacy in restricting breast and liver cancer growth [237]. Cochran et al [238] demonstrate that a long-term releasing apigenin-based polymer and subsequent nanoparticle delivery system has ability to inhibit tumor cell adhesion through the suppression of endothelial cell adhesion molecule expression. These studies show promise that nano-formulations of apigenin could become an effective drug-delivery system.…”

Section: 0 Major Limitations Of Apigeninmentioning

confidence: 99%

Plant Flavone Apigenin: an Emerging Anticancer Agent

et al. 2017

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Research in cancer chemoprevention provides convincing evidence that increased intake of vegetables and fruits may reduce the risk of several human malignancies. Phytochemicals present therein provide beneficial anti-inflammatory and antioxidant properties that serve to improve the cellular microenvironment. Compounds known as flavonoids categorized anthocyanidins, flavonols, flavanones, flavonols, flavones, and isoflavones have shown considerable promise as chemopreventive agents. Apigenin (4′, 5, 7-trihydroxyflavone), a major plant flavone, possessing antioxidant, anti-inflammatory, and anticancer properties affecting several molecular and cellular targets used to treat various human diseases. Epidemiologic and case-control studies have suggested apigenin reduces the risk of certain cancers. Studies demonstrate that apigenin retain potent therapeutic properties alone and/or increases the efficacy of several chemotherapeutic drugs in combination on a variety of human cancers. Apigenin’s anticancer effects could also be due to its differential effects in causing minimal toxicity to normal cells with delayed plasma clearance and slow decomposition in liver increasing the systemic bioavailability in pharmacokinetic studies. Here we discuss the anticancer role of apigenin highlighting its potential activity as a chemopreventive and therapeutic agent. We also highlight the current caveats that preclude apigenin for its use in the human trials.

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Section: 0 Major Limitations Of Apigeninmentioning

confidence: 99%

Plant Flavone Apigenin: an Emerging Anticancer Agent

et al. 2017

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“…Apigenin has demonstrated suppression of cancer signalling pathways and tumour cell adhesion on endothelial cells. Signalling pathways thought to be involved include JNK, ERK and AP‐1 . In other research studies, apigenin has exhibited anti‐inflammatory effects and demonstrated benefit in metabolic syndrome via inhibition of the enzyme NAD+ase .…”

Section: Introductionmentioning

confidence: 99%

The antiproliferative and apoptotic effects of apigenin on glioblastoma cells

Stump

Santee

Williams

et al. 2017

Journal of Pharmacy and Pharmacology

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Objectives Glioblastoma (GBM) is highly proliferative, infiltrative, malignant and the most deadly form of brain tumour. The epidermal growth factor receptor (EGFR) is overexpressed, amplified and mutated in GBM and has been shown to play key and important roles in the proliferation, growth and survival of this tumour. The goal of our study was to investigate the antiproliferative, apoptotic and molecular effects of apigenin in GBM. Methods Proliferation and viability tests were carried out using the trypan blue exclusion, MTT and lactate dehydrogenase (LDH) assays. Flow cytometry was used to examine the effects of apigenin on the cell cycle check-points. In addition, we determined the effects of apigenin on EGFR-mediated signalling pathways by Western blot analyses. Key findings Our results showed that apigenin reduced cell viability and proliferation in a dose-and time-dependent manner while increasing cytotoxicity in GBM cells. Treatment with apigenin-induced is poly ADP-ribose polymerase (PARP) cleavage and caused cell cycle arrest at the G2M checkpoint. Furthermore, our data revealed that apigenin inhibited EGFR-mediated phosphorylation of mitogen-activated protein kinase (MAPK), AKT and mammalian target of rapamycin (mTOR) signalling pathways and attenuated the expression of Bcl-xL. Conclusion Our results demonstrated that apigenin has potent inhibitory effects on pathways involved in GBM proliferation and survival and could potentially be used as a therapeutic agent for GBM.

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“…In terms of blood pressure reduction and vasodilation, research has indicated that apigenin can dilate the contracted aortic ring of rats caused by phenylephrine in vitro . Experiments have shown that apigenin can inhibit the proliferation of vascular smooth muscle cells in a dose-dependent manner within a certain concentration range (17), suggesting that apigenin is important in preventing cardiovascular diseases such as hypertension and atherosclerosis.…”

Section: Introductionmentioning

confidence: 99%

“…The results indicated that the antioxidant effect of apigenin and its role in protecting vascular endothelial cells occurred by increasing the activity of intracellular superoxide dismutase (SOD) and the secretion of NO. In addition, apigenin can inhibit the proliferation of vascular smooth muscle cells in a dose-dependent manner and may have the potential to inhibit thickening of vascular walls (17). …”

Section: Introductionmentioning

confidence: 99%

Apigenin in the regulation of cholesterol metabolism and protection of blood vessels

Zhang

Song

et al. 2017

Experimental and Therapeutic Medicine

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Hyperlipidemia is a major independent risk factor for atherosclerosis. Seeking natural compounds in medicinal plants capable of reducing blood fat and studying their mechanisms of action has been the focus of research in recent years. The aim of the present study was to analyze the mechanisms of apigenin in regulating cholesterol metabolism and protecting blood vessels, and to provide a theoretical basis for the clinical application of apigenin. The mouse model of hyperlipidemia was established to verify the efficacy of apigenin in improving hyperlipidemia and to observe the mechanism of action of apigenin in reducing cholesterol content. In vitro cell experiments were conducted to evaluate the role of apigenin in mediating reverse cholesterol transport. Additionally, H2O2-injured human umbilical venous endothelial cells (EA.hy926 cells) were used for further study on the roles of apigenin in resisting oxidization and protecting vascular endothelial cells. Apigenin significantly regulated blood fat, reduced animal weight, and reduced total cholesterol (P=0.024), triglyceride (P=0.031) and low-density lipoprotein cholesterol (P=0.014) in the serum of the high-fat diet mice. Apigenin improved the blood lipid metabolism of the hyper-lipidemia model mice. Body weight and serum cholesterol content increased abnormally (P=0.003) as a consequence of high-fat diet. Apigenin increased the activity of superoxide dismutase in EA.hy926 cells (P=0.043) and increased the amount of nitric oxide secreted by the cells (P=0.038). Apigenin also inhibited the proliferation of vascular smooth muscle cells in a dose-dependent manner (P=0.036). In conclusion, apigenin can regulate cholesterol metabolism in vivo and plays a role in reducing the level of blood fat by promoting cholesterol absorption and conversion, and accelerating reverse cholesterol transport. Apigenin also has a role in resisting oxidization and protecting blood vessels.

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Degradable poly(apigenin) polymer inhibits tumor cell adhesion to vascular endothelial cells

Cited by 17 publications

References 30 publications

Plant Flavone Apigenin: an Emerging Anticancer Agent

Plant Flavone Apigenin: an Emerging Anticancer Agent

The antiproliferative and apoptotic effects of apigenin on glioblastoma cells

Apigenin in the regulation of cholesterol metabolism and protection of blood vessels

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