Studies involving mechanism of emodin, an herbal extract, has revealed its potential as anti-inflammatory, antioxidant and anti-cancer agent. Emodin has been shown to successfully induce apoptosis, down-regulate cancer inducing genes, proving it to be a therapeutically significant pharmacophore. Modification of emodin and synthesis of various derivatives have successfully increased efficacy of the molecule in regulating various cellular pathway like MAPK signaling pathway, NF-κβ signaling pathway, ROS mediated pathways and apoptotic pathways. With the advent of various, anti-bacterial properties of emodin may come in rescue to combat emerging drug resistant microbial and parasitic strains. Different emodin derivatives, including the recently reported haloemodin, which inhibits bacterial topoisomerases, can be designed to generate future drugs against resistant pathogens. Emodin derivatives can also inhibit proteases and microtubule-associated proteins, which play an important role in Alzheimer’s disease. Properly designed drug delivery systems like liposomes and nanoparticles have been reported as efficient emodin carriers and to enhance emodin activity in cancer cell inhibition. Exploitation of these newly reported properties of this age-old drug could prove to be a promising solution for anti-microbial chemoresistance menace and other prevalent non-communicable diseases.