Orally bioavailable stilbenoids—compositions and therapeutic applications thereof
US9056074B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 17, 2012 |
| Grant date | Jun 16, 2015 |
| Priority date | — |
| Expiry date | May 28, 2033 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C43/23
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A novel, bioavailable and safe stilbenoid 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 with an unexpected enhanced ability to prevent the accumulation of lipids accompanying the terminal differentiation of adipocytes, thereby inhibiting adipogenesis, and nutraceutical and cosmeceutical compositions comprising 3,5-dimethoxy-3,4′-dihydroxystilbene useful for anti-obesity and anti-cellulite therapy, are disclosed. Further the enhanced SIRT-1 activation ability of 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#1 and 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are disclosed. The enhancement of SIRT-1 polypeptide activity of the said compounds is unexpectedly much higher than resveratrol or its natural analog pterostilbene. Sirtuin modulating compositions comprising an orally bioavailable SIRT-1 enhancing compounds (i) 3,5-dimethoxy-3,4′-dihydroxystilbene represented by STR#I and (ii) 2,3′,5′,6-tetrahydroxy-trans-stilbene represented by STR#II are also disclosed. An additional embodiment, also discloses the enhanced anti-Propionibacterium acnes activity of 3,5-dimethoxy-3,4′-dihydroxystilbenes represented by STR#I and compositions thereof.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.