Journal
JOURNAL OF NATURAL PRODUCTS
Volume 78, Issue 7, Pages 1618-1623Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.5b00179
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Funding
- European Commission [223736]
- Ph.D. Program on Malaria and Human Development of the University of Camerino
- Italian Ministry for Education, University and Research (MIUR
- PRIN)
- Regione Campania (FarmaBioNet, P.O.R Campania FESR O.O 2.1)
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In addition to known compounds, the leaves of Vernonia amygdalina afforded the new sesquiterpene lactones 14-O-methyl-vernolide (2), 3'-deoxyvernodalol (6), and vernomygdalin (8). These and related compounds were evaluated for modulation of a series of thiol trapping-sensitive transcription factors (NF-kappa B, STAT3, and Nrf2), involved in the maintenance of the chronic inflammatory condition typical of human degenerative diseases. Vernolide (1) emerged as a potent inhibitor of STAT3 and NF-kappa B and showed cytostatic activity toward the prostate cancer cell line DU45, arresting the cell cycle at the S phase. The exomethylene lactones are characterized by multiple Michael acceptor sites, as exemplified by vernolide (1) and vernodalol (5). By using the nuclear magnetic resonance-based cysteamine assay, the most reactive thiophilic site could be identified in both compounds, and competitive experiments qualified vernolide (1) as being more thiophilic than vernodalol (5), in agreement with the results of the pharmacological assays.
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