RSC Medicinal Chemistry Blog

One of the difficulties in vaccinating against annual flu pandemics is the myriad of different virus strains and the ability of the virus to rapidly mutate – which occurs so much faster than vaccine development.

Excitingly, however, Aharon Gedanken from Bar-Ilan University and colleagues from the Israeli Ministry of Health have developed a method of virus inhibition effective against several different strains, including H1N1 (swine flu). By using gold nanoparticles with anionic surface functional groups mercaptoethanesulfonate or mercaptosuccinic acid, the researchers were able to inhibit infection in MDCK cells, with no cytotoxic side effects.  They believe the mode of action is due to the nanoparticles preventing the virus from attaching to the cell surface, but further research is currently under way to determine the exact mechanism.

This HOT article is currently free to access – download it today!

Effective multi-strain inhibition of influenza virus by anionic gold nanoparticles
Matias Sametband, Sourabh Shukla, Tal Meningher, Shira Hirsh, Ella Mendelson, Ronit Sarid, Aharon Gedanken and Michal Mandelboim
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00229A

Current treatments for heart attacks usually involve restoring blood flow to the heart and and removing the blockage that caused it in the first place.     But what treatments are there for the oxygen-starved muscle? Well, currently, none.

The correct name for the damage caused to tissue by a lack of oxygen and nutrients is reperfusion injury, largely caused by the production of reactive oxygen species.  Naturally occurring flavonoids – antioxidants found in fruit, tea, wine and chocolate – have been shown to have a positive effect on cardiovascular health and have been highlighted as promising treatments for heart disease.   To date however, the poor aqueous solubility of the most promising flavonol candidates has prevented further therapeutic development – probably because the FDA has strong views on DMSO as an injecting solvent.

Now, researchers from Melbourne, Australia have synthesised water soluble prodrugs of some of those flavonols.  Owen Woodman and co-workers synthesised phosphate and hemiadipate derivatives of flavonol, 4′-hydroxyflavonol and 3′,4′-dihydroxyflavonol which were shown to significantly decrease reperfusion injury in two distinct animal models.  The group hopes this work will make a meaningful  step towards the clinical application of hydroxylated flavonols.

Read the full details of this interesting study online – the article is currently free to access:

Water soluble flavonol prodrugs that protect against ischaemia-reperfusion injury in rat hindlimb and sheep heart
Spencer J. Williams, Colleen J. Thomas, Mirna Boujaoude, Carlie T. Gannon, Shannon D. Zanatta, Bevyn Jarrott, Clive N. May and Owen L. Woodman
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C0MD00240B