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Bacopa monnieri (Brahmi) is described as a ‘brain tonic’ in ancient medical literature, and its formulations such as Brahmi ghrita, Brahmi rasayana, Brahmi vati and Saraswata ghrita are widely used in Ayurvedic medicine. This review describes the comprehensive phytochemistry of B. monnieri and the role of its molecular entities in Ayurvedic formulations. Over the last eight decades phytochemical studies have resulted in the isolation of 98 secondary metabolites from B. monnieri, viz., dammarane type triterpenoid saponins (34), pentacyclic triterpenes (6), phenylethyl glycosides (12), phenylpropanoid glycosides (2), cucurbitacins (7), steroids (8), flavonoids (6), alkaloids (3) and other miscellaneous compounds (20). Bacosides are the major bioactive constituents contributing to the cognitive effects of B. monnieri. However, most Brahmi-based Ayurvedic formulations do not define the chemical entities responsible for their biological activities; instead, their effects are attributed to synergism of their herbal ingredients. Chemical fingerprinting and other quality control measures are critically important in rationalizing the biological effects of Ayurvedic drugs. Similarly, the bioavailability and toxicity of Ayurvedic formulations need to be assessed. Genomic, metabolomic approaches and human trials with valid models on Ayurvedic drugs are so far limited, and these efforts need to be further augmented.

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