Alphastatin, a 24-amino acid fragment of human fibrinogen, is a potent new inhibitor of activated endothelial cells in vitro and in vivo.

摘要: Angiogenesis, the development of new blood vessels from existing vasculature, is crucial for and metastasis solid tumors. Here, we show first time that a 24–amino acid peptide derived amino terminus alpha chain human fibrinogen (termed “alphastatin”) has potent antiangiogenic properties, inhibiting both migration tubule formation dermal microvascular endothelial cells in response to vascular growth factor (VEGF) or basic fibroblast (bFGF) vitro. Moreover, alphastatin markedly inhibits tumors syngeneic murine model. Tumors mice receiving daily injections 12 days exhibited large areas intravascular disruption thrombosis with substantial cellular necrosis. Importantly, administration had no detectable effect on such normal tissues as liver, lungs, kidney. Taken together, these data indicate agent vitro antivascular vivo.