• Advances in Traditional Medicine
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• v.4 no.3
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• pp.179-185
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• 2004

The ethanol extract of Indigofera cordifolia was studied for in vivo gastroprotective activity, cytotoxic activity against oral tumor and normal cells, multidrug resistance (MDR) reversal activity, anti-human immunodeficiency virus (HIV) activity and radical scavenging activity. The extract of I. cordifolia showed potent gastric mucosal protective activity against stomach injury induced by HCl/EtOH solution. However, the gastroprotective activity could not be related to the radical mechanism, because the extract weakly scavenged both OH radical and $O_2*^-$. The extract also showed promising levels of MDR-reversing activity. This study demonstrates the tumor-specific cytotoxic action of the plant extract. However, the extract had no anti-HIV activity. From above results, the study suggests the medicinal importance of I. cordiforia extract.

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.957-962
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• 2006

A novel series of 2-(m-Chlorobenzyl)-4-substituted-1, 1, 3-trioxo-2H, 4H-pyrazolo[4, 5-e][1, 2, 4] thiadiazines (7a-k) were synthesized, and evaluated for their anti-HIV replication in MT-4 cell cultures. Compound (7a) showed activity against HIV-1-induced cytopathicity, with an $EC_{50}$ value of $45.6\;{\mu}M$, but none of the compounds exhibited inhibitory activity against HIV-2.

• Korean Journal of Plant Resources
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• v.27 no.1
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• pp.22-28
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• 2014

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.

• THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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• v.4 no.1
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• pp.199-209
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• 1998

In order to find antiviral effect against Human immunodeficiency virus(HIV), Herpes simplex virus type I(HSV-1) and II(HSV-2) from herb medicines, publicated 29 paters on anti-viral effect of herbal medicines and a convenient virus-induced cytopathic effect (CEP) inhibition assay was introduced. The major virus on experiment are HIV, Hepatitis B virus and HSV-1,2. Those of other studies showed inhibition of infected virus DNA replication and screening test of herbal medicines. More than 15 extractions were prepared by pure water boiling from herbal medicines, and their toxicity of infected cell and anti-viral activities were evaluated. Among them, the major part of herbal medicines showed cell stability compared with the contrast. Cytotoxic concentration (CC) of the $H_2O$ extracts of Padoo against HIV was <4.0, Hyungbangpaedoksan against HIV was 9.3, Whangyonhaedoktang against HIV-1 and HSV-2 was 15.3. These are high level cytotoxic concentration compared with the contrast. But antiviral effect was unable to figure out for selective $index(SI)=CC_{50}/EC_{50}$. The other herbal medicines were unable to showed potent anti-HIV and anti-HSV activity. The antiviral activation using herbs in this thesis have unlimited objects, to select research object will help to show the direction of antiviral drug development that have less side effect and more excellent efficiency.

• Journal of information and communication convergence engineering
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• v.7 no.4
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• pp.576-579
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• 2009

Anti-HIV-1 activities for the extracts (buthanol, hexane, chloroform, and water) of medicinal plants widely used in the folk medicine were evaluated for screening of anti-AIDS agents. The activities of the extracts to inhibit HIV-1 replication were also analyzed. The 50% effective concentration (EC50) of inhibition activity of the p24 production for chloroform extract of Saphora flavescens, chloroform extract of Herba ephedrae, and hexane extract of Pachyma hoelen Rumph showed 5.8, 29.9, and 37.3 2g/ml, respectively, as good activities. Hexane extract of Sophora flavescens, buthanol extract of Tulipa edulis, hexane extracts of Tulipa edulis, Herba ephedra, and Pachyma hoelen Rumph in the 50% cytotoxic concentration ($CC_{50}$) in inhibition activities of recombinant HIV-1 RT showed 12.9, 19.5, 11.6, 12.0, and 36.8 % at concentration of 200 ${\mu}g$/ml, respectively, as good activities. From these results, chloroform extract of Saphora flavescens, chloroform extract of Herba ephedrae, and hexane extract of Pachyma hoelen Rumph were very effective against HIV-1 among all extracts tested. Therefore, we expect these plants will be a useful for anti- HIV-1 therapeutics in future.

• Journal of Physiology & Pathology in Korean Medicine
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• v.18 no.4
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• pp.1129-1133
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• 2004

For the purpose of developing new anti-HIV agents from natural sources, the extracts of Kalopanax pictus were tested for their inhibitory effects on HIV-1 replication and its essential enzymes as the reverse transcriptase (RT). protease and α-glucosidase. In the assay of HIV-1-infected human T-cell line, water extracts of stem and leafstalk inhibited the HIV-1-induced cytopathic effects with Ie (inhibitory concentration) of 25 and 50㎍/㎖, respectively. Moreover water extracts (100㎍/㎖) of stem and leafstalk showed strong activity of 80% and 90% on anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method. 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 58%, but no glucosidase inhibitory activities. 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 protease. 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 α-glucosidase inhibitors.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2574-2580
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• 2012

The discovery that threosyl phosphonate nucleoside (PMDTA, $EC_{50}=2.53{\mu}M$) is a potent anti-HIV agent has led to the synthesis and biological evaluation of 5'-deoxy versions of threosyl phosphonate nucleosides. In the present study, (E)-3'-phosphonoalkenyl and 3'-phosphonoalkyl nucleoside analogues 13, 16, 20 and 23 were synthesized from acetol and tested for anti-HIV activity and cytotoxicity. The adenine analogue 16 was found to exhibit moderate in vitro anti-HIV-1 activity ($EC_{50}=22.2{\mu}M$).

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.868-874
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• 2013

Efficient synthetic route to novel 2'-spirocyclopropanoid 4'-deoxythreosyl phosphonic acid nucleosides was described from 1,4-dihydroxy-2-butene. Cyclopropane moiety was prepared via ester enolate alkylation using (2-chloroethyl)dimethylsulfonium iodide. Synthesized nucleoside analogues 16, 19, 23 and 26 were tested for anti-HIV activity as well as cytotoxicity. However, none of them showed any anti-HIV activity or cytotoxicity up to 100 ${\mu}M$.

• Archives of Pharmacal Research
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• v.22 no.1
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• pp.75-77
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• 1999

Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with $IC_{50}$ values of 360 and $87{\mu}M$, respectively.

• Archives of Pharmacal Research
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• v.29 no.1
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• pp.16-25
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• 2006

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.