Houttuynia cordata Thunb. (Saururaceae), a widely used herbal medicine and popularly consumed as a healthy vegetable, exhibits anti-inflammatory, antioxidant, and antitumor activities. In particular, H. cordata contains a lot of alkaloids and flavonoids, such as quercitrin and quercetin. So, research on the preparation of food and functional cosmetics, such as the ones used for anti-aging and hair loss prevention, using H. cordata is in progress. Therefore, this study identified the active compounds of H. cordata using HPCL and evaluated the acetylcholinesterase (AChE) inhibitory and antioxidant activities of these compounds. In particular, cryptochlorogenic acid, which is a phenolic compound, and apigenin, afzelin, quercitrin, and hyperoside, which are flavonoids, were detected in H. cordata. Among them, quercitrin was the major content of H. cordata at 1.326 mg/g, followed by the hyperoside, afzelin, and cryptochlorogenic acid contents of 0.678, 0.157, and 0.140 mg/g, respectively. Likewise, only apigenin did not show any antioxidant activity, but other active compounds showed very good scavenging activity. Finally, apigenin, afzelin, cryptochlorogenic acid, quercitrin, and hyperoside had an AChE inhibitory activity of 98.49, 79.77, 64.13, 61.97, and 27.4 % in 100 μg/mL, respectively. So, in the future, the results of this study will be used to develop and commercialize functional tea products.