LOGIN TO YOUR ACCOUNT

Username
Password
Remember Me
Or use your Academic/Social account:

CREATE AN ACCOUNT

Or use your Academic/Social account:

Congratulations!

You have just completed your registration at OpenAire.

Before you can login to the site, you will need to activate your account. An e-mail will be sent to you with the proper instructions.

Important!

Please note that this site is currently undergoing Beta testing.
Any new content you create is not guaranteed to be present to the final version of the site upon release.

Thank you for your patience,
OpenAire Dev Team.

Close This Message

CREATE AN ACCOUNT

Name:
Username:
Password:
Verify Password:
E-mail:
Verify E-mail:
*All Fields Are Required.
Please Verify You Are Human:
fbtwitterlinkedinvimeoflicker grey 14rssslideshare1
Ravishankar, Divyashree; Corona, Giulia; Hogan, Stephanie M.; Spencer, Jeremy P. E.; Greco, Francesca; Osborn, Helen M. I. (2016)
Publisher: Elsevier
Languages: English
Types: Article
Subjects:
Oxidative stress is associated with the pathology of neurodegenerative diseases. Identification of small molecules capable of protecting against oxidative stress is therefore of significant importance. In this context, a library of 76 hydroxy flavones, methoxy flavones and their 4-thio analogues has been evaluated for neuroprotection against H2O2-induced oxidative stress. This revealed the synthetic 7,8-dihydroxy 4-thioflavones as neuroprotective compounds, with 14d and 18d showing highest neuroprotective effects at lower concentrations (0.3 μM). Neuroprotection was found to be mediated via activation of the anti-apoptotic cell survival proteins of the ERK1/2 and PI3K/Akt pathways. Structure-activity relationship analysis revealed the B-ring phenyl group as essential for greater neuroprotection. Replacing the 4-C=O moiety with a 4-C=S moiety also generally enhanced neuroprotection.
  • The results below are discovered through our pilot algorithms. Let us know how we are doing!

    • Neuropharmacol. 2009, 7, 65-74.
    • Rossignol, D. A.; Frye, R. E. Front. Physiol. 2014, 5.
    • Andersen, J. K. Nat. Med. 2004, 10 Suppl, S18-S25.
    • Dajas, F.; Rivera-Megret, A.; Blasina, F.; Arrendondo, F.; AbinCarriquiry, J. A.; Costa, G.; Echeverry, C.; Lafon, L.; Heizen, H.; Ferreira, M.; Morquio, A. Brazilian J. Med. Biol. Res. 2003, 36, 1613-1620.
    • Mecocci, P.; Polidori, M. C. Biochim. Biophys. Acta 2012, 1822, 631-8.
    • Freeman, L. R.; Keller, J. N. Biochim. Biophys. Acta - Mol. Basis Dis. 2012, 1822, 822-829.
    • A. Lapchak, P. Curr. Pharm. Des. 2012, 18, 3694-3703.
    • Nakayama, M.; Aihara, M.; Chen, Y.-N.; Araie, M.; TomitaYokotani, K.; Iwashina, T. Mol. Vis. 2011, 17, 1784-1793.
    • Gutierrez-Merino C, Lopez-Sanchez C, Lagoa R, Samhan-Arias AK, Bueno C, G.-M. V. Curr Med Chem. 2011, 18, 1195-212.
    • Vauzour, D.; Vafeiadou, K.; Rodriguez-Mateos, A.; Rendeiro, C.; Spencer, J. P. E. Genes Nutr. 2008, 3, 115-126.
    • Neurosci. Lett. 2008, 438, 29-33.
    • F. CNS Neurosci. Ther. 2016, 22, 617-24.
    • Gao, L.; Tian, M.; Zhao, H. Y.; Xu, Q. Q.; Huang, Y. M.; Si, Q. C.; Tian, Q.; Wu, Q. M.; Hu, X. M.; Sun, L. B.; McClintock, S. M.; Zeng, Y. J. Neurochem. 2016, 136, 620-636.
    • Gaspar, A.; Silva, T.; Yáñez, M.; Vina, D.; Orallo, F.; Ortuso, F.; Uriarte, E.; Alcaro, S.; Borges, F. J. Med. Chem. 2011, 54, 5165- 5173.
    • Baptista, F. I.; Henriques, A. G.; Silva, A. M. S.; Wiltfang, J.; Da Cruz E Silva, O. A. B. ACS Chem. Neurosci. 2014, 5, 83-92.
    • Spencer, J. P. E. Chem. Soc. Rev. 2009, 38, 1152-1161.
    • Stevenson, D. E.; Hurst, R. D. Cell. Mol. Life Sci. 2007, 64, 2900- 2916.
    • Vauzour, D.; Vafeiadou, K.; Rice-Evans, C.; Williams, R. J.; Spencer, J. P. E. J. Neurochem. 2007, 103, 1355-1367.
    • Med. 2004, 36, 838-849.
    • Spencer, J. P. E. Genes Nutr. 2007, 2, 257-273.
    • Youdim, K. A.; Dobbie, M. S.; Kuhnle, G.; Proteggente, A. R.; Abbott, N. J.; Rice-Evans, C. J. Neurochem. 2003, 85, 180-192.
    • Toxicol. Vitr. 2014, 28, 388-396.
    • Neurosci. 2010, 1, 435-449.
    • Lipinski, C. A. J. Pharmacol. Toxicol. Methods 2000, 44, 235-249.
    • Neuroscience 1995, 67, 921-932.
    • Biochem. Biophys. Res. Commun. 1997, 235, 845-848.
    • L.; Manach, C.; Williamson, G. Am. J. Clin. Nutr. 2004, 80, 15-21.
    • Pietta, P. G. J. Nat. Prod. 2000, 63, 1035-1042.
    • Procházková, D.; Boušová, I.; Wilhelmová, N. Fitoterapia 2011, 82, 513-523.
    • Seyoum, A.; Asres, K.; El-Fiky, F. K. Phytochemistry 2006, 67, 2058-2070.
    • Andjelković, M.; Van Camp, J.; De Meulenaer, B.; Depaemelaere, G.; Socaciu, C.; Verloo, M.; Verhe, R. Food Chem. 2006, 98, 23- 31.
    • Kawabata, T.; Schepkin, V.; Haramaki, N.; Phadke, R. S.; Packer, L. Biochem. Pharmacol. 1996, 51, 1569-1577.
    • Chavarria, D.; Silva, T.; Martins, D.; Bravo, J.; Summavielle, T.; Garrido, J.; Borges, F. Med. Chem. Commun. 2015, 6, 1043-1053.
    • Hwang, S.-L.; Shih, P.-H.; Yen, G.-C. J. Agric. Food Chem. 2012, 60, 877-85.
    • Biochimie 2007, 89, 73-82.
    • Incani, A.; Deiana, M.; Corona, G.; Vafeiadou, K.; Vauzour, D.; Dessì, M. A.; Spencer, J. P. E. Mol. Nutr. Food Res. 2010, 54, 788- 796.
    • Liu, C.; Chan, C. B.; Ye, K. Transl. Neurodegener. 2016, 5, 2.
    • Proc. Natl. Acad. Sci. U. S. A. 2010, 107, 2687-2692.
    • N.; LaFerla, F. M. PLoS One 2014, 9.
    • Wu, C. H.; Hung, T. H.; Chen, C. C.; Ke, C. H.; Lee, C. Y.; Wang, P. Y.; Chen, S. F. PLoS One 2014, 9.
    • Hippocampus 2012, 22, 399-408.
    • Med. Chem. 2010, 53, 8274-8286.
    • Mantilla, C. B.; Ermilov, L. G. Muscle and Nerve 2012, 45, 274- 276.
    • Mol. Cell. Med. 2015, 4, 67-86.
    • Research Centre, Life Sciences Department, University of Roehampton, SW15 4JD, London, UK.
  • No related research data.
  • No similar publications.

Share - Bookmark

Cite this article