Ocimum sanctum L. a benevolent herb has been integrated into the traditional medicine practice from ancient times. The phytochemical analysis signifies the presence of polyphenols, flavonoids, terpenoids, amino acids, unsaturated fatty acids, and essential elements (vitamins and minerals). Polyphenols and flavonoids are the major essential components present in the various form of tulsi extract and responsible for different pharmacological activities such as anticancer, antioxidant, antimicrobial, anti-inflammation, etc. These activities were mediated through altering the functionality associated with the nF-κβ, ERK, p38, and MPK pathways. Further, the antimicrobial activity is amplified by the presence of unsaturated fatty acids such as linolic acid and linoleic acid which manipulate the membrane integrity of microbial. The molecular mechanism for such activity is mediated through destabilization of the microbial membrane by interfering with the electron transport chain and oxidative phosphorylation process. An extensive literature survey was carried out through various scientific search engine such as PubMed, Google scholar, science Direct, Medline, Embase, Cochrane library, and Indian medical databases. Diversified phenolic and flavonoid phytoconstituents of tulsi are responsible for anti-oxidant, antimicrobial, hypolipidemic, immunomodulatory, hepatoprotective, neuroprotective, antistress, antidiabetic, antiulcer, anticancer, anti-inflamatory, etc. Further, therapeutic potency of tulsi reflects in clinical trail reports provide satisfactory results with negligible adverse effects, which might be emerge as a green medicine to lessen the global burden of microbial, inflammation, metabolic associated disorders, etc. However, alteration in the composition and variation in the percentage yield of secondary metabolites due to phenotypic and genotypic disparity are the critical challenges that need to address in future. • From ancient times, Ocimum sanctum L . commonly known as holy basil or tulsi is considered one of the core pillars of the traditional practice of herbal medicine. • Presences of therapeutically active polyphenols and flavonoid enriched phytoconstituents are responsible for potent antioxidant, anticancer, anti-inflammatory, antimicrobial activity, etc. • Encouraging preclinical results brings 11 clinical trials on exploring the antimicrobial activity in the maintenance of oral hygiene, metabolic associated, inflammatory mediated disorders, neuroprotection, antistress activity, etc. • Translationally major portions of the osmium-based formulations are intended for the treatment of cold and cough (29.1%) and food supplement/functional food (14.5%) which remains the witness for its strong antimicrobial, antimicrobial, and anti-inflammatory activity and balance composition of macro and micronutrient.