The genus Garcinia is composed of around 200 species distributed in the tropics and subtropics. Out of 36 species from India, Garcinia gummi-gutta (L.) Roxb. is an important non-timber forest product (NTFP) from the southwestern ghats of India. It is a small- or medium-sized fruit tree valued for its fruits as a condiment. Moreover, the plant is a better source of phytochemicals such as xanthones, benzophenones, organic acids, and amino acids. Among these phytochemicals, hydroxycitric acid (HCA), an important organic acid enriched in fruit rinds, has the mechanism for regulation of lipid metabolism and obesity control. HCA helps to regulate serotonin synthesis and thereby suppresses food intake in our body. Also, it competitively inhibits the ATP-citrate lyase meant for the conversion of citrate to oxaloacetate and acetyl coenzyme A, a building block of fatty acid synthesis. Furthermore, an array of pharmacological effects such as antioxidant, antitumor, anti-allergic, anti-inflammatory, antibacterial, antifungal, antiviral, neuroprotective, anti-HIV, enzyme inhibition, and hypoglycemic effects has been well elucidated based on in vitro as well as in vivo experimental models. A generous portion of phytoconstituents with therapeutic potentialities has been contributed by the fruits, followed by leaf and bark. An array of health, wellness, and nutraceutical supplements are being produced from the plant by reputed pharma companies all over the world. To fulfil the needs of pharmaceutical industries, breeding approaches could be enhanced to improve the genome of G. gummi-gutta. Thus, underutilized plants, in turn, may contribute significantly to plant-based industry, thus benefiting the rural people who engage in the collection, processing, and marketing of such resources.