Flavonoid treatment of glycogen synthase kinase-based disease
US8802638B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 9, 2009 |
| Grant date | Aug 12, 2014 |
| Priority date | — |
| Expiry date | Apr 9, 2029 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K31/7048
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The flavonoid luteolin reduces amyloid-β peptide (Aβ) generation. Luteolin is also a selective GSK-3 inhibitor that 1) decreases amyloidogenic γ-secretase APP processing, and 2) promotes presenilin 1 (PS1) carboxyl-terminal fragment (CTF) phosphorylation. GSK-3α activity is essential for both PS1 CTF phosphorylation states and PS1-APP interaction. These findings were validated in vivo, using a Tg2576 Alzheimer's Disease model system. Luteolin treatment decreased soluble Aβ levels, reduced GSK-3 activity, and disrupted PS1-APP association. In addition, Tg2576 mice treated with diosmin, a glycoside of a flavone structurally and functionally similar to luteolin (diosmetin), displayed significantly reduced Aβ pathology as well.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.