The Piper caldense is a medicinal plant widely used to treat snake bites, as a sedative and for tooth pain. However, there are few reports about the biological potential of the plant and only two reports on its chemical composition. The objective of the present work was to determine the antimicrobial activity and chemical profiles of P. caldense tissues as well as to isolate their major compounds. The major compound 3-geranylgeranyl-4hydroxybenzoic acid found in all plant tissues, showed antibacterial activity for all tested bacteria including those gram-positive and gram-negative, and especially against gram-positive Staphylococcus aureus, Bacillus subtilis, Enterococcus faecalis with minimum inhibitory concentration of 39.5 µg/mL. The compound was characterized based in the interpretations of spectra data of IR, MS, 1 H and 13 C NMR analysis and chemical profiles of plant tissues obtained by HPLC.