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Twelve new diterpenoids based on two rare skeletal types, namely, paralianones A-D (1-4) and pepluanols A-H (5-12), along with five known compounds, were isolated from an acetone extract of Euphorbia peplus. Their structures were proposed based on 1D and 2D NMR spectroscopic data analysis. These diterpenoids were evaluated for potential anti-inflammatory activity in a lipopolysaccharide-stimulated mouse macrophage cellular model. Compounds 3, 4, 11, 13, and 16 displayed moderate inhibitory effects on NO inhibition, with IC50 values ranging from 29.9 to 38.3 μM.
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http://dx.doi.org/10.1021/acs.jnatprod.6b00206 | DOI Listing |
New Phytol
September 2025
Department of Natural Product Biosynthesis, Max Planck Institute for Chemical Ecology, 07745, Jena, Germany.
The plant family Euphorbiaceae is an abundant source of structurally complex diterpenoids, many of which have reported anticancer, anti-HIV, and anti-inflammatory activities. Among these, ingenol-3-angelate (1a; tradename: Picato®), isolated from Euphorbia peplus, has potent antitumor activity. We report the discovery and characterization of the first genes linked to committed steps of ingenol-3-angelate (1a) biosynthesis in E.
View Article and Find Full Text PDFWellcome Open Res
April 2025
Royal Botanic Gardens Kew, Richmond, England, UK.
We present a genome assembly from a specimen of (petty spurge; Streptophyta; Magnoliopsida; Malpighiales; Euphorbiaceae). The genome sequence has a total length of 277.10 megabases.
View Article and Find Full Text PDFHortic Res
July 2025
State Key Laboratory of Tree Genetics and Breeding, Chinese Academy of Forestry, Beijing 100091, China.
Euphorbiaceae species are renowned not only for horticultural significance but for their production of numerous bicyclic diterpenes with antitumor and antiviral activities. However, the gene clusters responsible for the biosynthesis of these terpenes remain largely unidentified. We here initiated the construction of a comprehensive procedure for terpene gene clusters in Euphorbiaceae species.
View Article and Find Full Text PDFJ Nat Prod
March 2025
School of Pharmaceutical Science, Fujian Provincial Key Laboratory of Innovative Drug Target Research, Xiamen University, Xiamen 361002, China.
Phosphorylation of checkpoint kinase 1 at Ser-345 (p-CHK1(S345)) mediates the replication stress response in cancer cells, leading to chemotherapy resistance. Therefore, finding inhibitors of p-CHK1(S345) is currently a promising strategy to prevent acquired drug resistance. In this study, 14 ingenane diterpenoids (-), involving two undescribed compounds possessing an unprecedented exocyclic double bond Δ, were identified from .
View Article and Find Full Text PDFInt J Mol Sci
December 2024
State Key Laboratory of Functions and Applications of Medicinal Plants & College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang 550014, China.
Euphjatrophanes H-L (-), four new jatrophane-type and one new lathyrane-type diterpenoid, were isolated from , along with eight known diterpenoids (-). Their structures were established on the basis of extensive spectroscopic analysis and X-ray crystallographic experiments. All compounds were subjected to bioactivity evaluation using flow cytometry in autophagic flux assays with HM mCherry-GFP-LC3 cells, the human microglia cells which stably expressed the tandem monomeric mCherry-GFP-tagged LC3.
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