Flavonoids are the important class of phytochemicals, which are mainly present in the various parts of plant such as fruits, leaves, flowers and specially berries. In earlier days, flavonoids have been known for their antioxidant properties only. Among all flavonoids, quercetin and rutin are the most usable flavonoids reported. Day to day, their demand is increasing in the realm of pharmaceuticals, biotechnological and nutraceutical industries due to their significant features in healthcare applications. Some important plants such as apples, tea plant, onions, red grapes, citrus fruits, curly kale, leeks, broccoli, cherries, raspberry, cranberry, blueberry, tomatoes, soya and blackberries contain flavonoid in maximum quantification limits and are so called the best sources for them. Flavonoids containing two basic nuclei such as flavan and flavones, which are further categorized into flavones, flavonols, flavanones, flavan-3-ols, isoflavones and anthocyanidins. Rhamnazin’ or 5,4’- dihydroxy-7,5’-dimethoxyflavonol is commonly found in Artemisia, Alnus, Betula, Aesculus and Rhamnus spp. Rhamnazin gained wider acceptance among bio-actives for healthcare benefits due to its antioxidant, antibacterial, antiangiogenic and anti-tumor properties. Furthermore, anti-infective and anti-proliferative properties are not much explored yet, which have attracted the attention of the researchers. Therefore, the present review extensively discussed the scientific aspects of ‘rhamnazin’ and its derivatives with respect to its medicinal uses, pharmacological activities, separation, isolation and various analytical techniques.