It is a flavone found in a variety of fruits and vegetables, including oranges, parsley, and onions, as well as tea. Although its cancer-preventing benefits are recognized (1), it does not have adequate bioavailability, like most polyphenols, to be able to have a strong effect when ingested organically in vegetables and fruits.
In the case of anti-angiogenesis, like resveratrol, the Apigenin negatively regulates hypoxia-inducible factor-1 (HIF-1) in lung, prostate and pancreatic cancer cell lines (7). Apigenin, like curcumin, inhibits angiogenesis in lung and breast cancer by lowering VEGF expression (8). Apigenin's other anti-angiogenic mechanisms target the signalling pathways of proinflammatory transcription factors NF-κB and COX-2 (9). Apigenin also suppresses the phosphorylation of VEGFR-2 (10).
In cancer prevention, this isoflavone reduces the risk of occurrence of both hormone-dependent and hormone-independent cancers, including prostate cancer, breast cancer, gastric cancer, colon cancer, non-small cell lung cancer and leukaemia (11). The antitumor effects of genistein are largely due to its anti-angiogenic action. This soy isoflavone inhibits endothelial cell proliferation, as well as tube migration and formation (12). Genistein's suppressive effects on MMP-2, as well as those it shares with resveratrol on the hypoxia-inducible factor HIF-1 and the vascular endothelial growth factor VEGF, are thought to be responsible for its anti-angiogenic properties (13). Genistein also blocks angiogenesis by inhibiting the activity of protein tyrosine kinase and the activation of mitogen-activated protein kinase (MAPK) (14).
The powerful antioxidant and anti-inflammatory effects of quercetin make it a champion in cancer prevention (15), including colon cancer, prostate cancer, lung cancer, breast cancer, leukaemia (16), etc. At higher doses, however, quercetin proves to be an unbeatable enemy of cancer. Quercetin's anticancer properties include inhibiting cancer cell invasion, progression, and metastasis, as well as having a strong anti-angiogenic effect (17).
Regular consumption of green tea is one of the best known ways to prevent several types of cancer (24). The compound that plays the most important role in cancer prevention, however, is epigallocatechin-3-gallate, abbreviated EGCG. This green tea extract has been shown to be beneficial in suppressing tumor growth, invasion, metastasis, and apoptosis in several malignancies. These include pancreatic cancer (25), prostate cancer, colon cancer (26), breast cancer (27), cervical cancer (28), etc. No less important, however, is the anti-angiogenic effect of EGCG, perhaps one of the most effective polyphenols in combating tumour angiogenesis.
To begin with, EGCG suppresses the expression of HIF-1, the nuclear transcription factor NFB, and the vascular endothelial growth factor VEGF (29). Following that, studies show an inhibition of the dimerization of VEGF receptors, which play an essential role in angiogenesis (30). Additionally, EGCG negatively regulates the PI3K/Akt signalling pathway, which deactivates the metalloproteinase MMP-9 and the pro-inflammatory factor NF-κB (31). Epigallocatechin-3-gallate suppresses liver metastasis in colorectal cancer by inhibiting the AKT signalling pathway and the expression of the endothelial growth factor receptor 2 VEGFR-2 (32).
Major anti-angiogenesis signalling pathways targeted by phytochemicalsRajasekar, Janani, Madan Kumar Perumal, and Baskaran Vallikannan. "A critical review on anti-angiogenic property of phytochemicals." The Journal of Nutritional Biochemistry 71 (2019): 1-15.
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- Zhao, Guangming, et al. "Apigenin inhibits proliferation and invasion, and induces apoptosis and cell cycle arrest in human melanoma cells." Oncology Reports 37.4 (2017): 2277-2285.
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