Seven new tetrasaccharide glycosides, tyrianthins 1-7 (1-7), along with six known glycolipids were isolated from the roots of Ipomoea tyrianthina, and their structures were elucidated by spectroscopic and chemical methods. The content of resin glycosides in samples collected in three different regions was analyzed and compared, and the results showed that the flowering or dry season did not have any effect on the chemical composition for the same locality, but the growing location itself did affect the chemical composition of resin glycosides. Intraperitoneal administration to mice of tyrianthin 6 (6) resulted in antidepressant activity. Tyrianthin 6 (6), scammonin 1 (8), and scammonin 2 (9) exhibited dose-dependent protective effects against pentylenetetrazole-induced seizures. Also, tyrianthin 6 (6) and scammonin 2 (9) produced relaxant effects on spontaneous contractions in the isolated rat ileum.