The chemical constituents of some species of Euphorbia, which grow mostly in semi-desert areas in Iran and on the Alborz Mountains in the north of Tehran, have been found to include chemotaxonomically important myrsinane diterpenoids and cycloartane triterpenoids. The Euphorbia plants collected in province of Azarbaijan in the northwestern part of Iran contained mostly derivatives of skin-irritating ingenol esters. Some of the diterpenoids with myrsinane carbon skeleton inhibited enzymes such as a-glycosidase, urease, HIV-1 reverse transcriptase, and prolyl endopeptidase. They also showed analgesic and DNA-damaging activities. The present review describes the chemistry and biological activity of several compounds isolated from different species of Iranian Euphorbia: diterpenoids with myrsinane skeletons, flavonoids, tannins, alkanes, sterols, mono-, sesqui- and triterpenoids, skin-irritating and tumor-promoting latexes and their active ingenol diterpenoids