Three unprecedented thioether-linked dimeric pyrimidines, namely ligusticumines A-C, together with twelve known compounds were isolated and identified from the traditional Chinese medicinal-edible herb, Ligusticum striatum DC. The structures of all the isolated compounds were determined from NMR, HRESIMS and X-ray diffraction spectroscopies. Additionally, a novel 3-step synthetic route was developed to synthesize ligusticumine C by substitution, thiolation and coupling, with an overall yield of 5.4%. The inhibitory activities of the isolated compounds against phosphatidylinositol 3-kinase (PI3K) were tested, of which, (3S)-butylphthalide, a characteristic component of L. striatum, showed a potent inhibitory effect on PI3Kα (IC: 3.6 μg/mL).
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| http://dx.doi.org/10.1016/j.phytochem.2023.113613 | DOI Listing |
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