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Bioorg Med Chem ; 90: 117366, 2023 07 15.
Artículo en Inglés | MEDLINE | ID: mdl-37329676

RESUMEN

Hura crepitans L. (Euphorbiaceae) is a thorn-covered tree widespread in South America, Africa and Asia which produces an irritating milky latex containing numerous secondary metabolites, notably daphnane-type diterpenes known as Protein Kinase C activators. Fractionation of a dichloromethane extract of the latex led to the isolation of five new daphnane diterpenes (1-5), along with two known analogs (6-7) including huratoxin. Huratoxin (6) and 4',5'-epoxyhuratoxin (4) were found to exhibit significant and selective cell growth inhibition against colorectal cancer cell line Caco-2 and primary colorectal cancer cells cultured as colonoids. The underlying mechanism of 4 and 6 was further investigated revealing the involvement of PKCζ in the cytostatic activity.


Asunto(s)
Neoplasias Colorrectales , Diterpenos , Euphorbiaceae , Humanos , Látex , Células CACO-2 , Diterpenos/farmacología , Neoplasias Colorrectales/tratamiento farmacológico
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