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Background Zeaxanthin is a carotenoid pigment found in several fruits and vegetables. Belonging to the xanthophyll family, it is widely present in human and some animals skin and eyes, performing important physiological functions due to its antioxidant and anti-inflammatory effects. Several studies have explored its health benefits against important disorders such as neurological diseases, allergies, and cancer. Scope and approach The aim of this study we to explore the sources, health benefits, and biological properties of zeaxanthin and analyzes its drug interaction with β-carotene. Key findings and conclusion Severela vegetable sources in particularly fruits parts contains zeaxanthin. Biological investigations showed that zeaxanthin has been found to exhibit a protective effect against excessive light and oxidative stress side effects, preventing the development of several neurological, skin, and eye disorders. It exhibits also antioxidant, antiparasitic, anthelmintic activity, and antiosteoporosis effects. Zeaxanthin can also play a role in the inflammatory response, contributing to the treatment or prevention of diseases like allergies and AIDS. Additionally, zeaxanthin can exhibit anticancer, anti-osteoporotic, and ophthalmologic effects. These different properties are mediated by diffetent cellular and molecular mechanisms exhibited by zeaxanthin such as its activation and/or blocker of cell receptors, its actions on signaling pathways, and also its effects on gene expression. Moreover, the safety as a dietary supplement has also been confirmed and its interaction with other carotenoids, such as β-carotene, has been studied and validated in pharmacokinetic investigations. However, further investigations are needed to explore the full potential of zeaxanthin and to elucidate more its molecular pharmacodynamic actions behind its effects on human health, and to investigate also its clinical applications.