hexylbiguanide

hexylbiguanide (specifically referring to N1-hexyl-N5-benzyl-biguanide, or HBB) is a novel biguanide derivative developed by researchers at the University of Minnesota as a potent antineoplastic agent and T-lymphocyte activator. Designed using structure-based approaches, HBB binds to the active-site heme of cytochrome P450 3A4 (CYP3A4) with significantly higher affinity than metformin. This binding potently and specifically inhibits CYP3A4 arachidonic acid (AA) epoxygenase activity, suppressing the mitochondrial electron transport chain (ETC) and oxygen consumption rates (OCR), which leads to growth inhibition of breast cancer cells and established mammary tumors. Uniquely, at concentrations that suppress tumor epithelia, HBB promotes the proliferation of CD4+ and CD8+ T lymphocytes without increasing regulatory T cells, suggesting its potential to enhance cancer immunotherapy.

Other names

hexyl-benzyl-biguanideN1-hexyl-N5-benzyl-biguanideN-1-hexyl-N5-benzyl-biguanideN 1-hexyl-N5-benzyl-biguanide