The aging of the population and exposure to pollutants have led to the emergence of diseases such as tumors and cancers, public health problems worldwide. An increase in cancer incidence is expected, especially in low-and middle-income countries. In this context, drugs are sought to inhibit the proliferation of tumor cells. One such compound is Piperlongumine (PLN) from Piper longum Linn, which has demonstrated significant biological properties. It exhibits the capacity to modulate crucial cellular signaling pathways, prompting the death of tumor cells through apoptosis and autophagy, while inhibiting their proliferation. Notably, the induction of apoptosis is specifically targeted towards tumor cells, avoiding non-tumor cells. These events correlate with the ability of PLN to elevate reactive oxygen species (ROS), which are toxic to cells. It also has synergistic effects when combined with other compounds, including doxorubicin in leukemic cells. However, further research is required to confirm these results and determine the efficacy and safety of PLN in clinical practice. It is crucial to fully understand its mechanisms of action and its interaction with other therapies before it can be used safely and effectively.