The cerium , lanthanum , and neodymium
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, NMR, 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.
demonstrated anti-HIV
activity (IC50=21.4 μM) close to maximal
nontoxic concentration. ,
, and demonstrated
limited anti-HIV potency, so none of the complexes seems
appropriate to be used in clinic. Further targeting of HIV-1
inhibition by is under progress.
Sialyltransferases (ST) are a family of enzymes specifically transporting sialic acids (SAs) onto nascent glycoproteins and glycolipids, so participating in glycoprotein synthesis. The envelope of human immunodeficiency virus -type 1 (HIV-1) is highly glycosylated and sialylated. Here we report for the first time data on ST-activity in acutely and chronically HIV-1 infected cells in cell culture. The results demonstrated higher ST activity in cytosols of both acutely and chronically infected cells compared to uninfected ones. Data fit well toour earlier assumption about the virus specific character of sialylation, found by using of direct radioactive precursor of biosynthesis of SAs as terminal moieties of sialoglycoproteins (Sgps) of HIV-1 in cell culture.
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