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http://dx.doi.org/10.7732/kjpr.2014.27.1.022

Inhibitory Effects of Gardenia jasminoides var. radicans Makino on HIV-1 Enzymes and Prediction of Inhibitory Factor by QSAR  

Yu, Young-Beob (Department of Herbal Pharmaceutical Development, Nambu University)
Publication Information
Korean Journal of Plant Resources / v.27, no.1, 2014 , pp. 22-28 More about this Journal
Abstract
In this study, we conducted the anti-HIV-1 enzymes assay in vitro and its active components were predicted by QSAR in silico for the elucidation of action mechanism on anti-HIV of natural resources. The extracts of Gardenia jasminoides var. radicans Makino were tested for their inhibitory effects on the reverse transcriptase (RT), protease and ${\alpha}$-glucosidase. In the enzyme inhibition assay, the methanol extracts of Gardenia jasminoides var. radicans Makino stem showed a strong activity of 32.5% on the enzyme activity to cleave an oligopeptide, resembling one of the cleavage sites in the viral polyprotein which can only be processed by HIV-1 protease. Moreover the methanol extracts of stem exhibited alpha-glucosidase inhibitory activities of 26.1%. The methanol extracts ($100{\mu}g/ml$) of stem showed a weak activity of 13.4% on anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method. However, all extracts of leaf and stem didn't exhibit the HIV-1-induced cytopathic effects with IC (inhibitory concentration) of $100{\mu}g/ml$ in HIV-1-infected human T-cell line. From these results, it is suggested that Gardenia jasminoides var. radicans Makino extracts may possibly be involved in the inhibition of reverse transcriptase, protease and alpha-glucosidase but can't vitally concerned with the viral replication in vitro.
Keywords
Gardenia jasminoides var. radicans Makino; Anti HIV-1; Reverse transcriptase; Protease; ${\alpha}$-glucosidase; QSAR;
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