Margatoxin - Medicinal Significance

Medicinal Significance

Neointimal hyperplasia is the movement and proliferation of smooth muscle cells into the luminal area of a blood vessel. This generates a new inner structure that can block blood flow. This is commonly seen to cause failure of interventional clinical procedures that include placement of stents and bypass grafts.
Due to changes in potassium channel type the vascular smooth muscle cells switch from the contractile to proliferating phenotype. It is suggested that Kv1.3 is important in proliferating vascular smooth muscle cells. Inhibitors of such channels suppress vascular smooth muscle proliferation, stenosis following injury, and neointimal hyperplasia. Studies shows that margatoxin is a high potency inhibitor of vascular cell migration, with an IC50 (half maximal inhibitory concentration) of 85 pM. In this study, a negative effect was also found. There have been vasoconstrictor effects observed in some arteries, but elevated blood pressure has not appeared as a significant concern.