• 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.

• 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.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.155-160
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• 2002

A series of modified oligonucleotides containing a phosphorothioate (P=S) backbone and a six-membered azasugar (6-AZS) as a sugar substitute in a nucleotide were synthesized and tested for their ability to inhibit the human immunodeficiency virus type I(HIV-l) in vitro without the aid of any transfecting agents. While P=S oligonucleotides with natural nucleotides had little anti-HIV-l activity, the six-membered azasugar nucleotide (6-AZN)-containing P=S oligonucleotides (AZPSONs) potently inhibited the HIV-l/SHIV replication and syncytium formation (ECso = 0.02-0.2 /lM) without cytotoxicity up to 100 /lM. DBM-2198, the most effective in anti-HIV-l activity among the AZPSONs, consists of random sequence and five 6¬AZNs evenly distributed in 18 nucleotides. DBM-2198 showed strong antiviral activity against, not only laboratory strains, but also primary isolates and even drug-resistant strains of HIV-I. DBM-2198 was much more effective than ddI or ddC in its anti-HIV-l activity in vitro. Particularly noteworthy is that the anti-HIV-l activity of DBM-2198 was better than that of AZT with respect to its long-lasting efficacy after a single treatment. Nevertheless, the antiviral activity of the AZPSONs was very specific to HIV-I. Poliovirus, or even simian immunodeficiency virus (SIV), was not inhibited by the AZPSONs. Taken together, our results strongly suggest that AZPSON can be used as a safe and effective AIDS-therapeutic drug against a broad spectrum of HIV -1 strains.

• Parasites, Hosts and Diseases
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• v.54 no.1
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• pp.93-96
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• 2016

Toxoplasmosis, a neglected tropical disease caused by the protozoan parasite Toxoplasma gondii, occurs throughout the world. Human T. gondii infection is asymptomatic in 80% of the population; however, the infection is life-threatening and causes substantial neurologic damage in immunocompromised patients such as HIV-infected persons. The major purpose of this study was to investigate the seroprevalence of T. gondii infection in subjects infected with HIV/AIDS in eastern China. Our findings showed 9.7% prevalence of anti-T. gondii IgG antibody in HIV/AIDS patients, which was higher than in intravenous drug users (2.2%) and healthy controls (4.7%), while no significant difference was observed in the seroprevalence of anti-Toxoplasma IgM antibody among all participants (P>0.05). Among all HIV/AIDS patients, 15 men (7.7%) and 10 women (15.9%) were positive for anti-T. gondii IgG antibody; however, no significant difference was detected in the seroprevalence of anti-Toxoplasma IgG antibody between males and females. The frequency of anti-Toxoplasma IgG antibody was 8.0%, 13.2%, 5.5%, and 0% in patients with normal immune function ($CD4^+$ T-lymphocyte count ${\geq}500cells/ml$), immunocompromised patients (cell count ${\geq}200$ and <500 cells/ml), severely immunocompromised patients (cell count ${\geq}50$ and <200 cells/ml), and advanced AIDS patients, respectively (cell count <50 cells/ml), while only 3 immunocompromised patients were positive for anti-T. gondii IgM antibody. The results indicate a high seroprevalence of T. gondii infection in HIV/AIDS patients in eastern China, and a preventive therapy for toxoplasmosis may be given to HIV/AIDS patients based on $CD4^+$ T lymphocyte count.

• 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.

• Archives of Pharmacal Research
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• v.29 no.10
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• pp.826-833
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• 2006

Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

• The Journal of Korean Society of Virology
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• v.27 no.1
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• pp.69-75
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• 1997

To evaluate in vitro anti-HIV efficacies of nucleoside derivatives, MT-4 cell line was infected with HIV-1 and HIV-2 respectively and treated with various compounds and the formerly approved drugs such as AZT, d4T, ddC and ddI. CPE method was used to evaluate their antiviral activity. Most dideoxynucleosides, AZT, d4T, ddC and ddI, showed anti-HIV activities against both viruses but no other compounds including anti-herpesvirus drugs did any. Further experiments were carried out to study their inhibitory mechanism of viral adsorption. The results showed no inhibition of syncytium formation due to an interaction between the gp120 expressed in HIV -infected cell surface and CD4 receptor on the uninfected cell surface in the presence of AZT. AZT showed no activity up to $100\;{\mu}g/ml$. Inhibition of reverse transcriptase (RT) in the presence of AZT-triphosphate was tested by using RT expressed in E. coli and purified and its $IC_{50}$ was 4.5 nM.

• Archives of Pharmacal Research
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• v.26 no.6
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• pp.441-445
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• 2003

New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.

• 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.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.591-597
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• 1993

Two new 6-azauracil dioxolane nucleosides which are related to Dioxolane T and expected to have anti-HIV activity were asymmetrically synthesized. The key intermediate 8 have been synthesized in ten steps from D-mannose and condensed with 6-azauracil to give 13 and 14 after desilylation, respectively.