One new cerebroside, macaocerebroside A (1), and 15 known compounds (2-16) were isolated from Solanum macaonense for the first time. In an antineutrophilic inflammatory assay, four caffeic acid derivatives (2-5) were active against superoxide anion generation with IC50 values of 3.3-4.8 μM; especially, 3 inhibited elastase release with an IC50 value of 4.0 μM. Additionally, kaempferol (8) also showed inhibition against elastase release with an IC50 value of 4.0 μM. In a cytotoxic assay, rutin (14) had selective moderate cytotoxicity toward human lung (A549), bladder (NTUB1), and prostate (DU145) cancer cell lines with IC50 values of 34.6, 41.3, and 31.8 μM, respectively.