dc.contributor.author |
Gama, Ntombenhle Hlengiwe
|
|
dc.contributor.author |
Kumar, Kamlesh
|
|
dc.contributor.author |
Ekengard, Erik
|
|
dc.contributor.author |
Haukka, Matti
|
|
dc.contributor.author |
Darkwa, James
|
|
dc.contributor.author |
Nordlander, Ebbe
|
|
dc.contributor.author |
Meyer, Debra
|
|
dc.date.accessioned |
2016-06-24T06:23:21Z |
|
dc.date.issued |
2016-06 |
|
dc.description.abstract |
HIV infection is known for replication in proliferating CD+ T-cells. Treatment of these cells
with cytostatic (anti-proliferation) compounds such as hydroxyurea interferes with the cells’s
ability support HIV replication. Combinations of such cytostatic compounds with proven
anti-retroviral drugs (like ddI) are known as virostatic , and have been shown to aid in the
control of the infection. The use of two different drugs in virostatic combinations however,
carries the risk of adverse effects including drug-drug interactions, which could lead to
augmented toxicities and reduced efficacy. Here, a novel digold(I) complex of ferrocenequinoline
(3) was investigated for cytostatic behaviour as well as anti-viral activity which if
demonstrated would eliminate concerns of drug-drug interactions. The complex was
synthesized and characterized by NMR, FT-IR and mass spectroscopy and the molecular
structure was confirmed by X-ray crystallography. Bio-screening involved viability dyes, real
time electronic sensing and whole virus assays. The complex showed significant (p = 0.0092)
inhibition of virus infectivity (83%) at 10 ug/mL. This same concentration caused cytostatic
behaviour in TZM-bl cells with significant (p<0.01) S and G2/M phase cell cycle arrest.
These data supports 3 as a virostatic agent, possessing both anti-viral and cytostatic
characteristics. |
en_ZA |
dc.description.department |
Biochemistry |
en_ZA |
dc.description.embargo |
2017-06-30 |
|
dc.description.librarian |
hb2016 |
en_ZA |
dc.description.sponsorship |
National Research Foundation (NRF) and the Technology
Innovation Agency (TIA), South Africa. NRF Innovation Doctoral Scholarship. European Commission (Erasmus Mundus Europe Asia, EMEA) and University of Johannesburg, South Africa |
en_ZA |
dc.description.uri |
http://link.springer.com/journal/10534 |
en_ZA |
dc.identifier.citation |
Gama, N, Kumar, K, Ekengard, E, Haukka, M, Darkwa, J, Nordlander, E & Meyer, D 2016, 'Gold(I) complex of 1,1′-bis(diphenylphosphino) ferrocene–quinoline conjugate : a virostatic agent against HIV-1', BioMetals, vol. 29, no. 3, pp. 389-397 |
en_ZA |
dc.identifier.issn |
0966-0844 (print) |
|
dc.identifier.issn |
1572-8773 (online) |
|
dc.identifier.other |
10.1007/s10534-016-9921-9 |
|
dc.identifier.uri |
http://hdl.handle.net/2263/53384 |
|
dc.language.iso |
en |
en_ZA |
dc.publisher |
Springer |
en_ZA |
dc.rights |
© Springer Science+Business Media New York 2016. The original publication is available at : http://link.springer.com/journal/10534. |
en_ZA |
dc.subject |
HIV infection |
en_ZA |
dc.subject |
Hydroxyurea interferes |
en_ZA |
dc.subject |
Cytostatic (anti-proliferation) compounds |
en_ZA |
dc.subject |
Human immunodeficiency virus (HIV) |
en_ZA |
dc.title |
Gold(I) complex of 1,1′-bis(diphenylphosphino) ferrocene–quinoline conjugate : a virostatic agent against HIV-1 |
en_ZA |
dc.type |
Postprint Article |
en_ZA |