Abstract
We previously identified the alkaloids tryptanthrin (1), indirubin (2) and indolinone (3) as pharmacologically active compounds in woad (Isatis tinctoria L.). They inhibit COX-2, 5-LOX catalyzed leukotriene synthesis, and mast cell degranulation at low µM to nM concentrations, and they possess drug-like physico-chemical properties. A pilot pharmacokinetic study in rats (2 mg/kg i.v. b.w.) showed that 1 and 2 have half-lives of 30 – 40 min, whereas 3 was rapidly eliminated. In silico predictions for 1 – 3 indicated high oral absorption and favourable blood-brain transport. In animal and human in vitro blood-brain-barrier (BBB) models 1 and 3 displayed high BBB permeation. In the Caco-2 intestinal absorption model, 1 showed high permeation, while the recovery of 3 was low.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.