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KMID : 0861020060210040115
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Korea Journal of Herbology
2006 Volume.21 No. 4 p.115 ~ p.121
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Inhibitory Effects of Actinidia arguta on HIV-1 Reverse transcriptase, HIV-1 Protease and alpha-glucosidase in vitro and in silico
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Yu Young-Beob
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Abstract
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Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Actinidia arguta were tested for their inhibitory effects on essential enzymes as the reverse transcriptase (RT), protease and {alpha}-;glucosidase. And we predicted inhibition activity of major compounds of Actinidia arguta using Quantitative Structure Activity Relationships (QSAR).
Methods : In this assay the activity of HIV-1 reverse transcriptase is measured as the formation of a strand of copy-DNA (cDNA) using RNA as a template. The activity of HIV-1 protease is measured as the cleavage of an oligopeptide by HIV-1 protease.
Results : In the anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method, water extracts (100ug/ml) of stem and leaf showed strong activity of 93.9% and 91.9%, respectively. In the HIV-1 protease inhibition assay, aqueous stem extract inhibited the activity of the enzyme to cleave an oligopeptide, resembling one of the cleavage sites in the viral polyprotein which can only be processed by HIV-1 protease with 56.8%. In the {alpha}-glucosidase inhibition assay, aqueous stem extract showed activity of 73.1%.
Conclusion : We found out this result, for these samples it is possible that the inhibition of the viral replication in vitro is due to the inhibition at least one of RT and {alpha}-glucosidase. It would be of great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agent up to date are RT, PR and {alpha}-glucosidase inhibitors.
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KEYWORD
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Actinidia arguta, HIV-1 essential enzymes, QSAR
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