As the most common cancer among women around the globe, breast cancer is currently the leading cause of cancer-related deaths in the world. The search for new and effective drugs to treat breast cancer is thus of central importance, given the drawbacks involved in current treatment methods that compromise their effectiveness. In this search for new drugs, medicinal plant extracts may be a potential source for alternative novel treatments of breast cancer. Notably, there has been growing interest in one particular plant as a source for anti-cancer drugs due to its diverse medicinal uses in traditional folk medicines. Vernonia amygdalina (VA) is a woody shrub that can grow up to 5 m tall, belonging to the family of Asteraceae. Native to Nigeria (West Africa) and widely grown in Africa, VA is also found in Asia, and is especially common in Singapore and Malaysia. The leaves exhibit a characteristic odor and bitter taste, explaining its common English name of 'bitter leaf'. Owing to the lack of documentation of this plant, different local names have been used in various countries, such as Etidod or Ewuro in Nigeria, South African leaf in Malaysia and Kenya, as well as Non-tree South in China. The medicinal properties of the plant, however, are widely recognized. As one of the plants that forms a major portion of the naturalist's pharmacopeia in Nigeria, VA has been shown to possess diverse therapeutic effects such as anti-malarial, anti-microbial (anti-bacterial, anti-fungal, anti-plasmodial, etc.), anti-diabetic and anti-cancer effects. The anti-cancer effect of VA was first shown in human carcinoma of nasopharynx and later in leukemia cells P-388 and L-1210 using the chloroform extract of VA.