Though some secondary metabolites from fungi have found application as antibiotics in modern medicine, majority of these compounds are however known to be hazardous to livestock and human systems. About 400 mycotoxins have been characterized in recent times with each potentially toxic to a biological or human system. Exposure of humans to airborne toxins-carrying spores produced by several species of fungi in water damaged buildings and damp indoor environments have been linked with allergies and sick building syndrome. Contamination of cereals, grains or tubers in the field, transit or store with a broad spectrum of noxious mycotoxins is well reported in literature. Scientific evidences have implicated consumption of such contaminated agricultural products with diseases such as nephropathy, immuno-deficiency, stunted growth, weight loss, onyalai, neural tube defect, CNS depression, kwashiorkor, hepatocellular carcinoma, jaundice, diarrhoea, beriberi and even death. Inhibition of protein synthesis and cell proliferation, inhibition of peptide chain elongation, binding to DNA and uncoupling oxidative phosphorylation, inactivation of ceramide synthase, transferases and other enzymes, and cell wall disruption etc are some of the mechanisms adduced for their toxic activity. With increasing incidence of mycotoxin-related diseases in the developing countries of Africa and other third world economies, concerns about their public health impacts are rife and heightening given that both chronic intermittent and acute exposures are deemed injurious. Therefore an understanding of their modes/mechanisms of injury in biological and human systems will help in tailoring their management in a broad scale.