Arsenic is a ubiquitous element found in several forms in environment. Although certain foods, such as marine fish, contain substantial levels of organic arsenic forms, they are relatively low in toxicity compared to inorganic forms. In contrast, arsenic in drinking water is predominantly inorganic and very toxic. Chronic ingestion of arsenic-contaminated drinking water is therefore the major pathway posing potential risk to human health. World populations are exposed to low to moderate levels of arsenic of parts per billion (ppb) to thousands of ppb. When exposed to human, it could metabolize into monomethylarsonous acid (MMA<SUP>Ⅲ</SUP>) and dimethylarsinous acid (DMA<SUP>Ⅲ</SUP>), which are highly toxic. Lots of stuides have been recently focused how MMA<SUP>Ⅲ</SUP> and DMA<SUP>Ⅲ</SUP> induce toxic insults in various target tissues. Epidemiological studies revealed that chronic arsenic exposure caused cancer, cardiovascular diseases, and diabetes etc. In this review, the current understanding of arsenic on health effects will be discussed.