Water soluble fullerenes with antiviral activity
AssigneeThe Regents of the University of California
InventorsSimon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Abstract
A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
Claims43
A compound comprising a water soluble derivative of buckministerfullerene (C60) with virucidal properties, and water soluble salts thereof.
A method for inhibiting retrovirus in cells infected therewith comprising contacting the cells with a pharmaceutically effective amount of a water soluble buckminsterfullerene or salt thereof.
A method for therapeutic treatment of HIV infection, AIDS or ARC comprising administering to a subject a pharmaceutically effective amount of a pharmaceutical composition comprising a water soluble buckminsterfullerene, or salt thereof.
A method for assaying compounds capable of inhibiting growth of a retrovirus comprising:
- a) activating a cell containing the virus;
- b) measuring the production of reverse transcriptase or p24 produced by the activated cell;
- c) contacting the cell with an inhibition effective amount of a water soluble buckministerfullerene compound, or salt thereof;
- and
- d) determining the decrease in production of reverse transcriptase or p24 of the contacted cell as compared with that of the activated cell.
A method for identifying a fullerene compound that inactivates HIV protease comprising:
- a) establishing a model of the HIVP molecule having an open active site containing Asp25 and Asp125;
- b) establishing a model of a fullerene derivative symmetrically substituted with a polar organic moiety containing from 1 to 20 carbon atoms;
- c) comparing the fit of the fullerene model with the active site of the HIV protease model to determine binding therebetween.
Dependencies are inferred from the claim text.