Anthocyanins are water-soluble naturally occurring pigments that are therapeutically beneficial and that have gained considerable interests by researchers in the field of phytopharmaceuticals and pharmacology. The evidence based scientific reports on the potential and efficacy of anthocyanins has caused an upsurge in their testing in clinical trials and formulation of herbal drug supplements since the past few decades. Their structural attributes enable them to be absorbed and react with various biomolecules in the human body, to provide beneficial physiological benefits. The anthocyanins are 2-phenylbenzopyrylium derivatives of dietary phenolics and exhibit antioxidant, anti-inflammatory and protective effects against metabolic and cardiovascular conditions. The metabolism of anthocyanins and their stability in-vivo in human body and during post-harvest storage still needs extensive investigation to fully explore their benefits. In the present chapter, we discuss the chemistry, medicinal uses in folklore/traditional medicine and the natural sources of their occurrence. The pre-clinical, clinical and pharmaceutical applications are also discussed, to emphasize the consumer demands and medicinal value of anthocyanins.