Daphnanes diterpenes from the latex of Hura crepitans L. And activity against human colorectal cancer cells Caco-2

Trinel M.; Le Lamer A.-C.; Jullian V.; Jacquemin D.; Graton J.; Cristofoli V.; Crossay E.; Yassine M.; Rolland C.; Vergnolle N.; Mejia K.; Joel Cabanillas B.; Racaud-Sultan C.; Fabre N. · Bioorganic Chemistry (2020) · DOI: 10.1016/j.bioorg.2020.104132

Resumen

Hura crepitans (Euphorbiaceae) is a tree from South America that produces an irritant latex used as a fish poison. A bio-guided fractionation of an ethanolic extract of the latex led to the isolation and structural identification of three known daphnane-type diterpenes (1–3) including huratoxin (1), together with two new analogs (4, 5). Compound 1 was found to exhibit significant and selective cell growth inhibition against the colorectal cancer cell line Caco-2, with morphological modifications suggesting formations mimicking the intestinal crypt architecture. The underlying mechanism of 1 was further investigated, in comparison with 12-O-tetradecanoylphorbol-13-acetate (TPA), revealing two different mechanisms.

Instituciones: Universidad Peruana Cayetano Heredia