Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture
The cerium Ce(III), lanthanum La(III), and neodymium Nd(III) complexes with 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one (warfarin) (W) and 3,3′-benzylidenebis[4-hydroxycoumarin] (1) were synthesized and studied for the first time for cytotoxicity (on MT-2 cells) and as anti-HIV agents un...
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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Wiley
2006-01-01
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| Series: | Bioinorganic Chemistry and Applications |
| Online Access: | http://dx.doi.org/10.1155/BCA/2006/71938 |
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| Summary: | The cerium Ce(III), lanthanum La(III), and neodymium Nd(III) complexes with
4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one (warfarin)
(W) and 3,3′-benzylidenebis[4-hydroxycoumarin]
(1) were synthesized and studied for the first time
for cytotoxicity (on MT-2 cells) and as anti-HIV agents under
acute and chronic infection. The complexes were characterized by different physicochemical methods:
mass spectrometry, ¹H NMR, ¹³C NMR, and IR
spectroscopy. The spectra of the complexes were interpreted on the
basis of comparison with the spectrum of the free ligands.
Anti-HIV effect of the complexes/ligands was measured in MT-2
cells by microtiter infection assay. Detection of endogenous
reverse transcriptase (RT) activity and RT processivity by PCR
indicative for proviral DNA synthesis demonstrated that anti-HIV
activity has not been linked to early stages of viral replication.
No effect on late steps of viral replication has been found using
cells chronically producing HIV-1LAI virus. La(W) demonstrated anti-HIV
activity (IC50=21.4μM) close to maximal
nontoxic concentration. Nd(W), Ce(1), and Nd(1) demonstrated
limited anti-HIV potency, so none of the complexes seems
appropriate to be used in clinic. Further targeting of HIV-1
inhibition by La(W) is under progress. |
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| ISSN: | 1565-3633 1687-479X |