Bacosides are the putative bioactive component of the Indian medicinal plant Bacopa monnieri which was placed second in the most important medicinal plants’ list by the Export-Import Bank of India. Among the bacoside components, bacoside A was found to be more pharmacologically active than bacoside B. Traditionally, Bacopa has been used in ayurvedic medicines as a cure for mental disorders and loss of memory. Later on, other pharmacological properties like antioxidant, antidepressant, antiulcer, hepatoprotective, anticancerous, vasodilator, smooth muscle relaxant, mast cell stabilizer, and various other functions are revealed. Increasing clinical trials indicate the potential role of bacosides even in Alzheimer’s disease and in epilepsy. Bacosides attribute to the neuroprotective function mainly through modulating antioxidant enzymes, namely, SOD, catalase, etc. Bacosides also regulate the levels of different neurotransmitters in the brain. Interestingly, bacosides do not exert any side effects as proven both in animal models and in human volunteers. These features render B. monnieri as well as bacosides pharmacologically immensely important. © Springer-Verlag Berlin Heidelberg 2013.