From ancient history, complementary and alternative medicines have played a significant role as holistic therapeutic treatments of various human diseases including cancer, diabetes, neurological diseases, and skin problems. One Indian medicinal plant herb), Bacopa monnieri has been used in many parts of the world as such medicine, particularly for the treatment of various neurological disorders. It is well known as a potent “tonic for the human brain,” which serves as a memory enhancer. Multiple studies proved that this herb contains a plethora of potential bioactive, phytochemical compounds with synergistic properties. The main purpose of the present review is to shed light on the use of Bacopa monnieri and its active principles (bacosides) in the management of neurological disorders. Furthermore, the signaling pathways modulated by bacosides have been critically discussed in this review. Moreover, we have critically summarized the present knowledge of this perennial creeping herb based upon the literature mining from different scientific engines.