Due to recent lifestyle shifts and health discernments among consumers, synthetic drugs are facing the challenge of controlling disease development and progression. Various medicinal plants and their constituents are recognized for their imminent role in disease management via modulation of biological activities. At present, research scholars have diverted their attention on natural bioactive entities with health-boosting perception to combat the lifestyle-related disarrays. In particular, Zingiber officinale is a medicinal herb that has been commonly used in food and pharmaceutical products. Its detailed chemical composition and high value-added active components have been extensively studied. In this review, we have summarized the pharmacological potential of this well-endowed chemo preventive agent. It was revealed that its functionalities are attributed to several inherent chemical constituents, including 6-gingerol, 8-gingerol, 10-gingerol, 6-shogaol, 6-hydroshogaol, and oleoresin, which were established through many studies (in vitro, in vivo, and cell lines). In this review, we also focused on the therapeutic effects of ginger and its constituents for their effective antioxidant properties. Their consumption may reduce or delay the progression of related diseases, such as cancer, diabetes, and obesity, via modulation of genetic and metabolic activities. The updated data could elucidate the relationship of the extraction processes with the constituents and biological manifestations. We have collated the current knowledge (including the latest clinical data) about the bioactive compounds and bioactivities of ginger. Their detailed mechanisms, which can lay foundation for their food and medical applications are also discussed.