Bioactive natural products have always played a significant role as novel therapeutical agents irrespective of their source of origin. They have a profound effect on human health by both direct and indirect means and also possess immense medicinal properties. Fruit species are largely appreciated and highly consumed throughout the world. Epidemiologic information supports the association between high intake of fruits and low risk of chronic diseases. There are several biological reasons why the consumption of fruits might reduce or prevent chronic diseases. Fruits are rich sources of nutrients and energy, have vitamins, minerals, fiber and numerous other classes of biologically active compounds. Moreover, parts of the fruit crops like fruit peels, leaves and barks also possess medicinal properties and have been included in this review. The most important activities discussed in this review include antidiabetic, anticancer, antihypertensive, neuroprotective, anti-inflammatory, antioxidant, antimicrobial, antiviral, stimulation of the immune system, cell detoxification, cholesterol synthesis, anticonvulsant and their ability to lower blood pressure. Several phytochemicals involved in this context are described with special emphasis on their structural properties and their relativity with human diseases.