Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells - Archive ouverte HAL
Journal Articles Bioorganic and Medicinal Chemistry Letters Year : 2023

Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells

Etienne Buscail

Abstract

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 diter-penes 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 & PRIME;,5 & PRIME;-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 un-derlying mechanism of 4 and 6 was further investigated revealing the involvement of PKC & zeta;in the cytostatic activity.
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Dates and versions

hal-04244338 , version 1 (19-10-2023)

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Elise Crossay, Valérie Jullian, Manon Trinel, David Sagnat, Dimitri Hamel, et al.. Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells. Bioorganic and Medicinal Chemistry Letters, 2023, 90, pp.117366. ⟨10.1016/j.bmc.2023.117366⟩. ⟨hal-04244338⟩
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