Abstract:The physiological functions and pharmacological activities of betaine were reviewed in this paper. Betaine could be used as a methyl donor for methionine metabolism and osmosis-regulator for cell response under hypertonic stress. It also showed pharmacological activities towards the diseases of heart, nerve and liver, and hyperhemicysteinuria. The functions and activities of betaine provided a basis for the application of netaine as vessel additives and human drug candidate.