Research has shown that C60 Hydrated Fullerenes (HYFNs) inhibit viral reverse transcriptase and blocks other receptor sites (RNA polymerase) needed for viral replication.
Example 1 of 3
Antibiot Khimioter. 2004;49(12):3-8.
[HIV reproduction inhibition by amino acid and dipeptide derivatives of fullerene C60].
[Article in Russian]
Miller GG, Romanova VS, Pokidysheva LN, Titova IV, Kaliberda EN, Rumsh LD, Andreeva OI, Rybalkin NP.
Target-aimed synthesis of a new class of water soluble amino acid and dipeptide derivatives of fullurene (C60 - X) for inhibition of specific virus enzymes, i.e. protease and reverse transcriptase of HIV (P HIV and RT HIV) in cell culture lytic and chronic infections was performed. Out of 13 tested substances, 8 showed inhibitory activity and 5 were effective in pharmacological doses (ID50 varied within 0.46 to 1.0 mcm/ml with respect to the lytic infection and 5.0 to 12.5 mcm/ml with respect to the chronic infection). The activity of (1), (2), (6), (7) and (8) was comparable to that of azidothymidine, a nucleozide inhibitor of RT HIV in the cell culture lytic infection. The substances also showed marked virucidal action. The cytotoxicity (survival, antiproliferative effect) varied from low to very low with respect to the rapidly dividing cells MT4 and HTHIV27 (CD50 > 200-800) and was somewhat higher with respect to PBL (CD50 > 100). The selectivity index (SI = CD50/ID50) was equal to 165-2000 for various samples. The prototype derivatives (1) and (2) had a selective (competitive) inhibitory action on the recombinant protease of HIV with IC50 = 1.25-2.76 mcM, while derivatives (1), (la) and (2) had a noncompetitive inhibitory action on the recombinant reverse transcriptase of HIV (Ki = 7.9-12.1 mM). The pharmacokinetic study of the prototype derivative (1) on laboratory animals revealed no acute or chronic toxicity up to the terminal high concentrations. As for (1), its high interspecies (mice--rabbits) relative bioavailability equal to 110% was shown.
PMID: 16050493 [PubMed - indexed for MEDLINE]
Example 2 of 3
Bioorg Med Chem Lett. 2005 Feb 15;15(4):1107-9.
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.
Mashino T1, Shimotohno K, Ikegami N, Nishikawa D, Okuda K, Takahashi K, Nakamura S, Mochizuki M.
We examined the human immunodeficiency virus-reverse transcriptase and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of cationic, anionic, and amino acid-type fullerene derivatives. Among the fullerene derivatives, the amino acid-type fullerene derivative was the most efficient in human immunodeficiency virus-reverse transcriptase inhibition.
PMID: 15686922 [PubMed - indexed for MEDLINE]
Example 3 of 3
Cytotoxic and antiviral properties of fullerene C60 in the culture of animal cells
Zinaida Klestova, Dr., Ph.D.*, Yuriy Prylutskiy, Dr., Ph.D.,** Marina Marchenko Ph.D. Student ***
*State Scientific-Control Institute of Biotechnology and Strains of Microorganisms (Donetskaya St, 30,Kyiv-151, Ukraine);
**National Taras Shevchenko National University of Kyiv, Volodymyrska Str. 64, 01601 Kyiv, Ukraine
***The Institute of Veterinary Medicine of NAAS (Donetskaya St. 30, Kyiv-151, Ukraine)
One of the urgent problems of modern veterinary biotechnology is to solve the complex task that lies at the intersection of chemistry, physics, materials science, biology, veterinary medicine is focused design, synthesis and study of the functional properties of nanomaterials which characterized by high bioavailability and biocompatibility, low toxicity and high specific biological activity.
In our studies, was used C60 fullerene - fullerene in water-soluble form. This compound molecule is nearly spherical, with a diameter of 0.72 nm , the surface of which consists of 60 carbon atoms connected by single or double chemical called " links. Considered that C60- fullerenes are potential pharmaceutical compounds. However, along with a broad perspective on the use of such substances for the prevention and treatment of diseases, there are certain precautions, particularly with regard to the possible toxic effects on biological objects, including on cell.
Therefore, our research started with the determination of cytotoxic properties of C60 fullerene - on cell line BHK -21, which is continuous line origin from Syrian hamster and which is used in many medical and biological research.
In experiments used at least ten holes in plates with cell culture for each drug dilution in culture medium. The plates with cell culture incubated at +37˚ C with 5% СО2 for 96 hours.
Thus, we have found the maximum cytotoxic concentration of compound that was 0,0375 ±0,003 mg/ml (n=3,).
Determined the antiviral activity of C60 - fullerene, using as a biological model coronovirus (virus of transmissible gastroenteritis of swine). Coronoviruses affect both animals and humans, leading in many cases to a high degree of mortality. Investigation of antiviral activity of fullerene on transmissible gastroenteritis virus of swine in the system in vitro, n = 5 (each concentration: 0,15 , 0,075, 0,0375, 0,019, 0,009, 0,005 was tested in 10 holes).
We found that C60-fullerene reduced the infectious properties of the virus by 2.0 TCID 50/ml which is a significant result.
Therefore, preliminary data suggest recommend this compound for further preclinical and clinical studies.
Source: Lviv Nanotechnology Conference August 2014 http://www.iop.kiev.ua/~nanotwinning/conference2/