Shikonin and its derivatives are the natural naphthoquinone compounds produced in the roots of the Boraginaceae family. These red pigments have been used for a long time in coloring silk, as food colorants, and in the Chinese traditional system of medicines The resurgence of public interest in natural and plant-based products has led to this category of compounds being in high demand due to their wide range of biological activities including antioxidant, antitumor, antifungal, anti-inflammatory ones. Different researchers worldwide have reported various applications of shikonin derivatives in the area of pharmacology. Nevertheless, the use of these compounds in the food and cosmetics fields needs to be explored more in order to make them available for commercial utilization in various food industries as a packaging material and to enhance their shelf life without any side effects. Similarly, the antioxidant properties and skin whitening effects of these bioactive molecules may be used successfully in various cosmetic formulations. The present review delves into the updated knowledge on the various properties of shikonin derivatives in relation to food and cosmetics. The pharmacological effects of these bioactive compounds are also highlighted. Based on various studies, it can be concluded that these natural bioactive molecules have potential to be used in different sectors, including functional food, food additives, skin, health care, and to cure various diseases. Further research is required for the sustainable production of these compounds with minimum disturbances to the environment and in order to make them available in the market at an economic price. Simultaneous studies utilizing recent techniques in computational biology, bioinformatics, molecular docking, and artificial intelligence in laboratory and clinical trials would further help in making these potential candidates promising alternative natural bioactive therapeutics with multiple uses.