Anti-angiogenic activity

Paris D, Ait-Ghezala G, Mathura VS, Patel N, Quadros A, Laporte V, et al. Anti-angiogenic activity of the mntant Dntch A(beta) peptide on human brain microvascular endothelial cells. Brain Res Mol Brain Res 2005 136 212-30. 

Figure 4 Anti-angiogenic activity of 1 and 3. (A) Angiographic images of the developmental CAM (EDD 9) treated with 0.9% NaCl (control) and 1 and 3 (150 pM/day). The vasculature is visualized by FITC-dextran fluorescence angiography (25 mg/kg, 20 kDa, XCK = 470 nm, Xem = 520 nm).

In 2006, Jung et al. described the anti-angiogenic activity of the artemisinin monomers 52-60 using vascularized chorioallantoic membranes of chicken embryo as an in vivo model. These compounds, at concentrations as low as 5 nmol/egg, inhibited angiogenesis process by 29-75%. Monomer 60 was found to be the most effective among the tested compounds. ... 

Sorafenib is a kinase inhibitor with both antiproliferative and anti-angiogenic activity. Approved for the treatment of advanced renal cell carcinoma and for the treatment of patients with hepatocellular carcinoma. Peak plasma levels of sorafenib are generally observed 3 hours after oral administration. The... 

Furthermore, sulfated 0-CD mimicked heparin in the augmentation of anti-angiogenic activity of angiostatic steroids, but used alone promoted blood vessel cell growth (angiogenesis) [58]. 

Shi J, et al. (2003) Structure-activity relationship studies of the anti-angiogenic activities of linomide. Bioorg Med Chem Lett 13(6) 1187—1189... 

Sunitinib maleate (1, Sutent, SU11248) was discovered by Sugen, which later became part of Pfizer. It is an orally active drug that exhibits potent anti-angiogenic activity through the inhibition of multiple RTKs. Specifically, 1 inhibits vascular... 

S-FP13P (53)] (Fig. 8-13) [1-3,7,8,44,45]. Some of the TNF-a production regulators prolong the life span of mice with cachexia indnced by lipopolysac-charide injection and show more potent anti-angiogenic activity than that of thahdomide (48) at a much lower dose than thalidomide (48) [2]. However, the... 

For anti-angiogenic activity, thymidine phosphorylase (TP)/platelet-derived endothelial ceU growth factor (PD-ECGF) was considered as a putative... 

The peptide CXCR4 antagonist TN14003 has demonstrated antitumor efficacy in two animal models of metastatic breast and head and neck cancer [48, 103]. Animals were treated with the CXCR4 peptide by intraperitoneal injection for 35 days. Tumors at the primary subcutaneous site of injection as well as the number of lung metastasis were inhibited. In the head and neck animal model, antitumor activity was correlated with anti-angiogenic activity of the anti-CXCR4 treatment. 

It has been demonstrated that EGCG can inhibit the matrix metalloproteinase activity at a relatively low dose. EGCG inhibits the activity of secreted MMP-2 and MMP-9 at concentrations of 8-13 pM. Meanwhile, 1 pM EGCG increased the expression of TIMP-1 and TIMP-2, proteins that inhibit the activity of activated MMPs. Because such concentrations of tea polyphenols are physiologically significant, this is an attractive mechanism for the observed anti-invasive and anti-angiogenic activities of EGCff and other tea polyphenols in vivo. Recently, similar observations of the inhibitory effects of tea polyphenols on the activities of MMPs have been made TE-3 appears to be the most active of the compounds examined in this respect (unpublished results). 

M. Sasaki, Depudecin, a microbial metabolite containing two epoxide groups, exhibits anti-angiogenic activity in vivo, Biol. Pharm. Bull. 1995, 18,1305-1307. 

Hydrazinocurcuminoids modified from curcuminoids by Shim et al. [64] showed greater anti-proliferative potency than curcuminoids in bovine aortic endothelial cells (BAECs) (Table 7). In contrast to curcumin, which inhibited the proliferation of several epithelial and fibroblast cells non-selectively, hydrazinocurcuminoids showed specificity against endothelial cells. Thus, proper modification on the linker between the two phenyl rings cannot only enhance the anti-angiogenic activity but also the specificity. The rank order of the potencies of the curcuminoids was 1 > 2 > 3. The hydrazinocurcuminoids showed the same trend. Therefore, the elimination of methoxy groups from the phenyl rings resulted in decreased anti-angiogenic potency. 

Anti-angiogenic activity of selected receptor tyrosine kinase inhibitors, PD 166285 and PD 173074, implications for combination treatment with photodynamic therapy. Invest New Drugs, 17, 121-135. 

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