Planta Med 2019; 85(18): 1542
DOI: 10.1055/s-0039-3400070
Main Congress Poster
Poster Session 2
© Georg Thieme Verlag KG Stuttgart · New York

Permeability of lichen compounds through the blood brain barrier as an important argument for their potential neuroprotective action

Sroka E Studzińska
1   Department of Pharmacognosy, Poznan University of Medical Sciences,, Święcickiego 4, 60-781Poznań, Poland
,
K Grzanka
1   Department of Pharmacognosy, Poznan University of Medical Sciences,, Święcickiego 4, 60-781Poznań, Poland
,
P Zalewski
1   Department of Pharmacognosy, Poznan University of Medical Sciences,, Święcickiego 4, 60-781Poznań, Poland
,
M Paczkowska
1   Department of Pharmacognosy, Poznan University of Medical Sciences,, Święcickiego 4, 60-781Poznań, Poland
,
T Plech
2   Department of Pharmacology, Medical University,, Chodzki 1, 20-093 Lublin, Poland
,
J Cielecka-Piontek
1   Department of Pharmacognosy, Poznan University of Medical Sciences,, Święcickiego 4, 60-781Poznań, Poland
› Institutsangaben
Weitere Informationen

Publikationsverlauf

Publikationsdatum:
20. Dezember 2019 (online)

 

Lichens are an association of fungi and algae or cyanobacteria. Lichens contain many compounds with multidirectional activities (e.g. antiinflammatory, antibacterial or neuroprotective) [1], [2], [3]. In order to define a pharmacological activity also in central nervous system, the permeability of selected lichen compounds through the blood-brain barrier was assessed.

Blood brain barrier permeability studies were conducted using PAMPA-BBB (the blood-brain barrier specific parallel artificial membrane permeability assay). Acetone extracts from the thallus of Hypogymnia physodes, Parmelia sulcata, Evernia prunatri, Cladonia uncialis were produced. The concentration of lichen acids was determined using the HPLC-DAD method.

A gradient HPLC method with UV detection and the Kinetex C18 column (100 × 2.1 mm, 5 μm) was used. The mobile phase consisted of acetonitrile and 0.5 % formic acid with a flow rate of 0.3 mL/min. The detection wavelength was 254 nm and column. temperature was set at 40oC. The method meets all required validation parameters (selectivity, linearity, precision, accuracy).The concentrations of lichen compounds in fluids simulating blood and brain fluids were expressed as apparent permeability coefficients (P e ).

The results showed that the high permeability for physodic acid (P e = 5.6 cm s-1), evernic acid (P e = 4.7 cm s-1), (-)-usnic acid (P e = 36.1 cm s-1) was confirmed. The permeability of salazinic acid was determined to be low (P e = 0.5 cm s-1). Reference value is P e < 2*10-6 cm s-1 [4].

This results show that for the examined lichen compounds, pharmacological effects within the central nervous system are possible.

The project “Universal modular platform for conducting release tests simulating physiological conditions for oral dosage forms” is supported by the National Center for Research and Development in the program EUROSTARS-2.

 
  • References

  • 1 Studzińska-Sroka E, Hołderna-Kędzia E, Galanty A, Bylka W, Kacprzak K, Ćwiklińska K. In vitro antimicrobial activity of extracts and compounds isolated from Cladonia uncialis . Nat Prod Res 2015; 29: 2302-2307
  • 2 Studzińska-Sroka E, Dubino A. Lichens as a source of chemical compounds with anti-inflammatory activity. Herba polonica 2018; 64: 56-64
  • 3 Fernández-Moriano C, Divakar PK, Crespo A, Gómez-Serranillos MP. In vitro neuroprotective potential of lichen metabolite fumarprotocetraric acid via intracellular redox modulation. Toxicol Appl Pharmacol 2017; 316: 83-94
  • 4 Di L, Kerns EH, Fan K, McConnell OJ, Carter GT. High throughput artificial membrane permeability assay for blood-brain barrier. Eur J Med Chem 2003; 38: 223-32