This study was undertaken to evaluate possible antiallergic effects of an extract of pigments from green sea urchin (Strongylocentrotus droebachiensis) shells. Effects were studied on animal models - guinea pig ileum contraction, rabbit eyes allergic conjunctivitis, and rabbit local skin irritation. The extract significantly reduced, in a dose-dependent manner, the histamine-induced contractions of the isolated guinea pig ileum with ID50 =1.2 µg/mL (in equivalents of spinochrome B), had an inhibitory effect on the model of ocular allergic inflammation surpassing the reference drug olopatadine, and did not show any irritating effect in rabbits. The extract predominantly contained polyhydroxy-1,4-naphthoquinone which would be responsible for the pharmacological activity. The active compounds of the extract were evaluated in silico with molecular docking. Molecular docking into H1R receptor structures obtained from molecular dynamic simulations showed that all spinochrome derivatives bind to the receptor active site, but spinochrome monomers fit better to it. The results of the present study suggest possibilities for the development of new agents for treating allergic diseases on the base of pigments from sea urchins shells.
- MeSH
- alergická konjunktivitida farmakoterapie MeSH
- antialergika chemie izolace a purifikace farmakologie MeSH
- biologické pigmenty chemie MeSH
- dibenzoxepiny farmakologie MeSH
- histamin farmakologie MeSH
- ileum účinky léků MeSH
- králíci MeSH
- kůže účinky léků MeSH
- modely nemocí na zvířatech MeSH
- morčata MeSH
- naftochinony chemie izolace a purifikace farmakologie MeSH
- olopatadin MeSH
- simulace molekulového dockingu MeSH
- skořápky zvířat chemie MeSH
- Strongylocentrotus chemie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- králíci MeSH
- morčata MeSH
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1,4-naphthoquinone MeSH Prohlížeč
- antialergika MeSH
- biologické pigmenty MeSH
- dibenzoxepiny MeSH
- histamin MeSH
- naftochinony MeSH
- olopatadin MeSH
- spinochrome A MeSH Prohlížeč
