| In vitro: |
| Nat Prod Commun. 2015 Dec;10(12):2037-9. | | Macrocyclic Diterpenoids from the Latex of Euphorbia helioscopia.[Pubmed: 26882659] |
METHODS AND RESULTS:
One new jatrophane diterpenoid, 7α,9β,15β-triacetoxy-3β-benzoyloxy-14β-hydroxyjatropha-5E,11E-diene (3), together with four known macrocyclic diterpenoids, euphoheliosnoid A (1), epieuphoscopin B (2), Euphohelioscopin A (4) and euphoscopin C (5), were isolated from the stem latex of Euphorbia helioscopia. Their structures were established by spectroscopic analyses.
CONCLUSIONS:
In the anti-inflammatory assay, Euphohelioscopin A (4) exhibited moderate inhibitory activity on the release of cytokine TNF-α (IC50 = 23.7 ± 1.7 μM), IL-6 (IC50 = 46.1 ± 1.1 μM) and chemokine MCP-1 (IC50 = 33.7 ± 3.8 μM) in lipopolysaccharide (LPS) induced RAW 264.7 macrophages without notable cytotoxicity (IC50 > 80 μM). | | Chem Biol. 2012 Aug 24;19(8):994-1000. | | Euphohelioscopin A is a PKC activator capable of inducing macrophage differentiation.[Pubmed: 22921066 ] | To identify small molecules that selectively control hematopoietic stem cell differentiation, we performed an unbiased screen using primary human CD34(+) cells.
METHODS AND RESULTS:
We identified a plant-derived natural product, Euphohelioscopin A, capable of selectively differentiating CD34(+) cells down the granulocyte/monocytic lineage. Euphohelioscopin A also inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60.
CONCLUSIONS:
Mechanistic studies revealed that Euphohelioscopin A is an activator of protein kinase C (PKC), and that the promonocytic effects of this natural product are mediated by PKC activation. In addition to shedding insights into normal hematopoiesis, this work may ultimately facilitate the application of stem cell therapies to a host of myeloid dysfunctions. |
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