In vitro activity: Doxazosin-induced apoptosis is blocked by specific caspase-8 inhibitors, supporting the functional involvement of caspase-8 in doxazosin-induced apoptosis. Doxazosin increases FADD recruitment and subsequent caspase-8 activation, implicating Fas-mediated apoptosis as the underlying mechanism of the effect of Doxazosin in prostate cells. Doxazosin and cholestyramine similarly decreases plasma total and LDL plus VLDL cholesterols, and total triglycerides on average by 46%, 61% and 45% respectively. Doxazosin induces DNA damage and cell death in HL-1 cell line. Doxazosin treatment decreases cell viability in primary cultures of neonatal rat cardiomyocytes, and Hoechst dye vital staining demonstrates doxazosin-induced apoptosis in primary cultures of human adult cardiomyocytes. Doxazosin antagonizes the VEGF-mediated angiogenic response of HUVEC cells, by abrogating cell adhesion to fibronectin and collagen-coated surfaces and inhibiting cell migration, via a potential downregulation of VEGF expression.

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