This is one of the new discoveries of the application of buckminsterfullerenes.
A derivative of the new class of molecules called buckminsterfullerenes (nicknamed 'buckyballs') is active against HIV-1 and HIV-2, the viruses which cause AIDS, report a team of Emory scientists in the August issue of the journal Antimicrobial Agents and Chemotherapy.
This is the first time buckyballs, so named because of their resemblance to the geodesic domes designed by architect/philosopher Buckminster Fuller, have been shown to have biological activity.
This discovery is believed that it has opened up a whole new avenue for the biological development of buckyballs.
'The finding that these compounds also have virucidal properties (that kill the virus directly before it gets into the cell) without affecting normal cells suggest that they could be used to prevent HIV infection. Nevertheless, it is still early to determine if these compounds will become useful clinically.
About a year ago the scientists theorized that an appropriately modified buckyball might mimic the antiviral properties of the large class of molecules they had been researching for years: polyoxometalates. Buckyballs, they knew, were roughly the same size and shape as polyoxometalates. However, unlike polyoxometalates, buckyballs are insoluble in water.
The team worked with buckyball expert Fred Wudl, Ph.D., of the University of California, Santa Barbara, who was able to design a fulleroid, a water-soluble buckyball. The group then further modified the fulleroid into a derivative dubbed compound 1.
When exposed to three types of human white blood cells infected by the AIDS virus, compound 1 did indeed inhibit two enzymes essential for viral reproduction: reverse transcriptase and HIV-1 protease. Reverse transcriptase is the enzyme blocked by AZT and certain polyoxometalate agents. HIV-1 protease is the enzyme a research team at the University of California, San Francisco, working with Dr. Wudl, has simultaneously reported to be blocked by fulleroids.
Compound 1 appears to break the chain of viral reproduction by serving as a sort of cork to plug up the 'active site' in a cylindrical portion of the HIV-1 protease enzyme. Once clogged, the enzyme has been inactivated and can no longer carry out its job of cutting up pieces of the virus's protein chain necessary for reproduction.
The new compound is not toxic to normal cells but prevents virus growth in infected immune system cells including those infected with HIV resistant to AZT.
Compound 1 is one of only a few agents active against chronically infected immune cells. In the same cells, AZT has no antiviral activity.
'The lack of cross-resistance with AZT suggest that combination studies of the fullerenes with AZT in vitro could be considered,' the team reported.
The research team also identified the virucidal effect the molecule has which blocks the infectivity of HIV without harming its host cell.
* This research was carried out by The Emory team, led by Professor Raymond F. Schinazi of the Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine (based at the Veterans Affairs Medical Center, Decatur), and Craig L. Hill, Ph.D., professor of chemistry. The study was in part supported by the Department of Veterans Affairs and U.S. Public Health Service, and the National Science Foundation.
Ref. Emory Report Homepage (http://www.emory.edu)
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