Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture
<p>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) (<bold>W</bold>) and 3,<mml:math alttext="$3'$"> <mml:msup> <mml:mn>3</mml:mn> <mml:mo>...
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| Format: | Article |
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| Language: | English |
| Published: |
Wiley
2006-01-01
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| Series: | Bioinorganic Chemistry and Applications |
| Online Access: | http://www.hindawi.com/GetArticle.aspx?doi=10.1155/BCA/2006/71938 |
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| Summary: | <p>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) (<bold>W</bold>) and 3,<mml:math alttext="$3'$"> <mml:msup> <mml:mn>3</mml:mn> <mml:mo>′</mml:mo> </mml:msup> </mml:math>-benzylidenebis[4-hydroxycoumarin] (<bold>1</bold>) 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-<mml:math alttext="$1_{LAI}$"> <mml:mrow> <mml:msub> <mml:mn>1</mml:mn> <mml:mrow> <mml:mtext>LAI</mml:mtext> </mml:mrow> </mml:msub> </mml:mrow> </mml:math> virus. La(<bold>W</bold>) demonstrated anti-HIV activity (IC50=21.4μM) close to maximal nontoxic concentration. Nd(<bold>W</bold>), Ce(<bold>1</bold>), and Nd(<bold>1</bold>) 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(<bold>W</bold>) is under progress.</p> |
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| ISSN: | 1565-3633 |