The purpose of this research was to examine the preclinical efficacy of a decoction from the roots of as a hypoglycemic, antihyperglycemic, and antihyperalgesic agent using well-known experimental models in mice. Acute oral administration of decoction did not produce toxic effects in mice, according to the Lorke procedure. decoction (31.6-316.2 mg/kg, p. o.) decreased blood glucose levels during acute hypoglycemic and the oral glucose tolerance and oral sucrose tolerance tests, both in normoglycemic and hyperglycemic animals. Phytochemical analysis of roots led to the isolation of perezone (), a mixture of -pipitzol () and -pipitzol (), and 8--D-glucopyranosyloxy-4-methoxy-5-methyl-coumarin (). A pharmacological evaluation of compounds - (3.2-31.6 mg/kg) using the same assays revealed their hypoglycemic and antihyperglycemic actions. Finally, local administration of decoction (31.6-316.2 µg/paw) and compounds- (3.2-31.6 µg/paw) produced significant inhibition on the licking time during the formalin test in healthy and hyperglycemic mice, demonstrating their antinociceptive and antihyperalgesic potential, respectively. Altogether, these results could be related to the use of for treating diabetes and painful complaints in contemporary Mexican folk medicine. A suitable UPLC-ESI/MS method was developed and successfully applied to quantify simultaneously compounds and in decoction.