Limonene, pinene, and isoprene are abundant and ubiquitous volatile organic compounds (VOCs) which are found in various natural products and also produced from various manufacture processes. Limonene and pinene are major components of food additives and household products for enrichment of good flavors and elimination of malodors, and isoprene is a basal motif of monoterpenes such as limonene and pinene. They have shown many beneficial effects such as chemopreventive, chemotherapeutic, and antioxidant activities. Upon certain conditions, however, adverse effects of these compounds on human health have also been reported. Although they do not seem to have acute and severe toxicity to human, they can easily generate secondary organic aerosols (SOAs) when they react with oxygen and/or ozone, which have shown certain toxic effects on experimental animal models as well as on humans. Numerous household and scented products containing limonene, pinene, and isoprene are widely used in these days. However, biological consequences upon exposure to these products are largely unknown. The aim of this review is to summarize and analyze the current understanding on the biological effects of VOCs, in particular limonene, pinene, and isoprene, as well as their SOAs.