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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| Format: | Article |
| Language: | English |
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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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| author | Ilia Manolov Sevda Raleva Petya Genova Alexey Savov Liliana Froloshka Daniela Dundarova Radka Argirova |
| author_facet | Ilia Manolov Sevda Raleva Petya Genova Alexey Savov Liliana Froloshka Daniela Dundarova Radka Argirova |
| author_sort | Ilia Manolov |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-08e4ba9cda914407a457891387ecfc29 |
| institution | Kabale University |
| issn | 1565-3633 1687-479X |
| language | English |
| publishDate | 2006-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Bioinorganic Chemistry and Applications |
| spelling | doaj-art-08e4ba9cda914407a457891387ecfc292025-02-03T01:00:01ZengWileyBioinorganic Chemistry and Applications1565-36331687-479X2006-01-01200610.1155/BCA/2006/7193871938Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell CultureIlia Manolov0Sevda Raleva1Petya Genova2Alexey Savov3Liliana Froloshka4Daniela Dundarova5Radka Argirova6Department of Organic Chemistry, Faculty of Pharmacy, Medical University, 2 Dunav Street, Sofia 1000, BulgariaDepartment of Virology, National Center of Infectious and Parasitic Diseases, 44A Stoletov Street, Sofia 1233, BulgariaDepartment of Virology, National Center of Infectious and Parasitic Diseases, 44A Stoletov Street, Sofia 1233, BulgariaLaboratory of Molecular Pathology, Medical University, 2 Zdrave Street, Sofia 1606, BulgariaDepartment of Virology, National Center of Infectious and Parasitic Diseases, 44A Stoletov Street, Sofia 1233, BulgariaDepartment of Virology, National Center of Infectious and Parasitic Diseases, 44A Stoletov Street, Sofia 1233, BulgariaDepartment of Virology, National Center of Infectious and Parasitic Diseases, 44A Stoletov Street, Sofia 1233, BulgariaThe 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.http://dx.doi.org/10.1155/BCA/2006/71938 |
| spellingShingle | Ilia Manolov Sevda Raleva Petya Genova Alexey Savov Liliana Froloshka Daniela Dundarova Radka Argirova Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture Bioinorganic Chemistry and Applications |
| title | Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture |
| title_full | Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture |
| title_fullStr | Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture |
| title_full_unstemmed | Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture |
| title_short | Antihuman Immunodeficiency Virus Type 1 (HIV-1) Activity of Rare Earth Metal Complexes of 4-Hydroxycoumarins in Cell Culture |
| title_sort | antihuman immunodeficiency virus type 1 hiv 1 activity of rare earth metal complexes of 4 hydroxycoumarins in cell culture |
| url | http://dx.doi.org/10.1155/BCA/2006/71938 |
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