Euphorbiaceae Diterpenes

Members of the Euphorbiaceae plant family have been employed in traditional herbal folk medicine around the world, mainly to treat cancerous conditions, swellings, and warts. Since the isolation of jatrophone in 1970, Euphorbia species became of interest for phytochemists as well as synthetic chemists.

A vast number of biologically active terpenoids, mainly diterpenes have been isolated in the following years. A small selection of structurally complex natural products is shown below.

We are currently engaged in the synthesis of Euphorbiaceae diterpenes, in particular euphosalicin, Pl-3, and Eser-2. These structurally fascinating natural products selectively inhibit P-glycoprotein and show pronounced levels of multi-drug-resistance (mdr) reversal effects. As overexpression of P-glycoprotein in cancer cells reduces the efficiency of modern cancer-chemotherapy, jatrophane diterpenes might become novel lead structures for the development of cancer therapeutics.