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Pharmacokinetics and in vitro blood-brain barrier screening of the plant-derived alkaloid tryptanthrin

Autor/Autorin
Jähne, Evelyn A.
Eigenmann, Daniela E.
Sampath, Chethan
Butterweck, Veronika
Culot, Maxime
Cecchelli, Roméo
Gosselet, Fabien
Walter, Fruzsina R.
Deli, Maria A.
Smiesko, Martin
Hamburger, Matthias
Oufir, Mouhssin
Datum
2016
Metadata
Zur Langanzeige
Type
01 - Zeitschriftenartikel, Journalartikel oder Magazin
Zusammenfassung
The indolo[2,1-b]quinazoline alkaloid tryptanthrin was previously identified as a potent anti-inflammatory compound with a unique pharmacological profile. It is a potent inhibitor of cyclooxygenase-2, 5-lipooxygenase-catalyzed leukotriene synthesis, and nitric oxide production catalyzed by the inducible nitric oxide synthase. To characterize the pharmacokinetic properties of tryptanthrin, we performed a pilot in vivo study in male Sprague-Dawley rats (2 mg/kg bw i. v.). Moreover, the ability of tryptanthrin to cross the blood-brain barrier was evaluated in three in vitro human and animal blood-brain barrier models. Bioanalytical UPLC-MS/MS methods used were validated according to current international guidelines. A half-life of 40.63 ± 6.66 min and a clearance of 1.00 ± 0.36 L/h/kg were found in the in vivo pharmacokinetic study. In vitro data obtained with the two primary animal blood-brain barrier models showed a good correlation with an immortalized human monoculture blood-brain barrier model (hBMEC cell line), and were indicative of a high blood-brain barrier permeation potential of tryptanthrin. These findings were corroborated by the in silico prediction of blood-brain barrier penetration. P-glycoprotein interaction of tryptanthrin was assessed by calculation of the efflux ratio in bidirectional permeability assays. An efflux ratio below 2 indicated that tryptanthrin is not subjected to active efflux.
Link
https://www.ncbi.nlm.nih.gov/pubmed/27093249
URI
http://hdl.handle.net/11654/23688
DOI der Originalausgabe
https://doi.org/10.1055/s-0042-105295
Übergeordnetes Werk
Planta Medica
Jahrgang
82
Ausgabe
11-12
Seiten
1021-1029
Zitation

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