The effects was studied on the biologically active substances content and antioxidant activity of G. procumbens extracts, which was from different parts of Gynura procumbens(Lour.) Merr, by different drying methods, and with different kinds of solvents. The results showed that: G. procumbens roots compared to its stems and leaves had higher content of phenolic and flavonoids and the antioxidant activity was also stronger, and the ferric reducing ability and ABTS⁺·scavenging capacity and DPPH·scavenging capacity were 21.25±0.31, 35.27±0.26, 56.20±0.22 TEAC（trolox equivalent antioxidant capacity）value (μg Trolox/mL), respectively. Drying methods had significant effect on the content of the biologically active substance of G. procumbens roots extracts, freeze drying and 60 ℃ hot air drying obtained with strong antioxidant activity. Extraction solvents had significant effect on the content of the biologically active substance of G. procumbens roots extracts, and the antioxidant activity (FRAP ferric reducing ability, DPPH·scavenging capacity and ABTS⁺·scavenging capacity) of extracts and their total phenolic content were significantly correlated, with the correlation coefficient R of 0.919, 0.848 and 0.907, respectively. The antioxidant activity (FRAP, DPPH and ABTS) of extracts and their total flavonoids content were significantly correlated, too, with the correlation coefficient R of 0.915, 0.793 and 0.823, respectively. The antioxidant activity (FRAP, DPPH and ABTS) and chlorogenic acid content correlation coefficient R were 0.887, 0.927 and 0.900, respectively, but had less relevant with the vitamin C content was.