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Natural bioactive compounds from plants are of great importance in modem therapeutics,which are used to prepare antibiotics,growth supplements or some other therapeutics.L-theanine is such a bioactive amide amino acid presented in different plants and fungi,especially in tea.Theanine has influential effects on lifestyle associated diseases,such as diabetes,cardiovascular disorders,hypertension,stress relief,tumor suppression,menstruation and liver injury.This amino acid can maintain normal sleep and improve memory function and nullify effect of the neurotoxins.The rate of bioavailability and its medium of ingestion in the body is one of the great concs for its additional antioxidant properties.Pharmacokinetics of the bioactive compound and its mode of action are described herewith.The biosynthesis and industrial synthesis are also reviewed to promote accelerated production of this bioactive compound in the pharmaceutical industries.