Journal
JOURNAL OF NATURAL PRODUCTS
Volume 85, Issue 11, Pages 2557-2569Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.2c00471
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Funding
- DBM Microscopy Core Faci l i t y (Department of Biomedicine)
- Swiss National Science Foundation [MM121224]
- University Hospital of Zurich [205321-176008]
- Swiss National Science Foundation (SNF) [205321_176008] Funding Source: Swiss National Science Foundation (SNF)
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A screening of over 2500 plant extracts in melanoma cells revealed that the ethyl acetate extract from Artemisia argyi displayed significant inhibition of the PI3K/AKT pathway. Through activity profiling, 21 active compounds were isolated, including one novel dimerosequiterpenoid, one new disesquiterpenoid, three new guaianolides, 12 known sesquiterpenoids, and four known flavonoids.
A library of more than 2500 plant extracts was screened for activity on oncogenic signaling in melanoma cells. The ethyl acetate extract from the aerial parts of Artemisia argyi displayed pronounced inhibition of the PI3K/AKT pathway. Active compounds were tracked with the aid of HPLC-based activity profiling, and altogether 21 active compounds were isolated, including one novel dimerosequiterpenoid (1), one new disesquiterpenoid (2), three new guaianolides (3-5), 12 known sesquiterpenoids (6-17), and four known flavonoids (19-22). A new eudesmanolide derivative (13b) was isolated as an artifact formed by methanolysis. Compound 1 is the first adduct comprising a sesquiterpene lactone and a methyl jasmonate moiety. The absolute configurations of compounds 1 and 3-18 were established by comparison of their experimental and calculated ECD spectra. The absolute configuration for 2 was determined by X-ray diffraction analysis. Guaianolide 8 was the most potent sesquiterpene lactone, inhibiting the PI3K/AKT pathway with an IC50 value of 8.9 +/- 0.9 mu M.
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