CAFFEIC ACID-CONTAINING COMPOUNDS AND LIGNANS DERIVED FROM SPECIES OF THE GENERA ANTHRISCUS, FORSYTHIA AND LINUM
Tim Ausbüttel
Gyógyszertudományok és Egészségügyi Technológiák Tagozat
Dr. Zelkó Romána
SE Bőr-, Nemikórtani és Bőronkológiai Klinika előadóterme
2026-09-25 14:00:00
Modern Trends in Pharmaceutical Scientific Research
Dr. Antal István
Dr. Boldizsár Imre
Arash Mirzahosseini
Móricz M. Ágnes
Dr. Gyires Klára
Dr. Ludányi Krisztina
Dr. Vasanits Anikó
Plant tissues are an important source of pharmacologically relevant natural
products, but their accessibility is often limited by low abundance, instability, and tissuespecific
distribution. These challenges were addressed through a systematic
phytochemical and bioactivity-guided investigation of Forsythia suspensa, Linum
austriacum/L. perenne, and Anthriscus species, combining advanced analytical methods
with controlled conversion strategies to optimize the identification, isolation, and
evaluation of phenylpropanoid-derived metabolites.
In Forsythia suspensa, isomeric CPhEGs (forsythosides A, H, and I) were
identified by mass spectrometry; however, fragmentation analysis confirmed their
structural similarity without enabling their discrimination.
In Linum austriacum and L. perenne, a detailed conversion study of AN lignans
revealed the presence of two previously unknown natural compounds, linadiacin A and
B. Linadiacin A underwent a quantitative two-step conversion via linadiacin B to
justicidin B under acidic conditions. Optimized acidic and enzymatic treatments enabled
the selective enrichment and isolation of linadiacins, diphyllin, and justicidin B, with
structures and fragmentation pathways confirmed by HR-MS and NMR. Biological
evaluation revealed strong in vitro anti-SARS-CoV-2 activity of diphyllin and justicidin
B at low micromolar concentrations with acceptable cytotoxicity, along with pronounced
antiproliferative effects.
In Anthriscus species, comprehensive metabolite profiling established A. nitida and
A. caucalis as new natural sources of AT and DBL lignans. Roots of A. sylvestris and A.
nitida were lignan-rich, enabling efficient one-step isolation and identification of
desmethylyatein in A. nitida provides new insight into lignan biosynthesis. Additionally,
three MDiCQAs were structurally elucidated for the first time as new natural products
from A. sylvestris. Their accumulation was shown to be strongly organ- and developmentstage-
dependent, with early-spring leaves representing optimal raw materials. Although
only one MDiCQA exhibited cytostatic activity, its lack of cancer selectivity underscores
the importance of early toxicity screening.
This work integrates tissue selection, controlled conversion processes, and
advanced analytical techniques to enable efficient access to minor or unstable metabolites
and to support the identification of antiviral and antiproliferative compounds.
