6533b7d8fe1ef96bd126adb5

RESEARCH PRODUCT

Tigliane diterpenes from the latex of Euphorbia obtusifolia with inhibitory activity on the mammalian mitochondrial respiratory chain

Ernesto EstornellJ. Alberto MarcoEmilio PalomaresLiliana Betancur-galvis

subject

LatexStereochemistryRespiratory chainIn Vitro TechniquesMitochondria HeartElectron Transportchemistry.chemical_compoundEuphorbiaRotenoneDrug DiscoveryAnimalsNADH NADPH OxidoreductasesSubmitochondrial particlePharmacologyEuphorbiaOxidase testbiologyPlant ExtractsUncoupling AgentsEuphorbiaceaeBiological activitybiology.organism_classificationMitochondrial respiratory chainchemistryBiochemistryCattleDiterpenesDiterpene

description

Abstract Six diterpenes isolated from the latex of Euphorbia obtusifolia Poir. (Euphorbiaceae) were evaluated for their inhibition of the NADH oxidase activity in submitochondrial particles from beef heart. 4,20-Dideoxyphorbol-12,13-bis(isobutyrate) was the most potent inhibitor and showed an inhibitory concentration with IC 50 value of 2.6±0.3 mM. In the present study, some structure–activity trends are suggested for the inhibitory activity of the mammalian mitochondrial respiratory chain of these natural product derivatives of 4-deoxyphorbol esters.

https://doi.org/10.1016/s0378-8741(03)00010-2