• Title/Summary/Keyword: anti-HIV-1 activity

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Anti-HIV-1 Protease Activity and in Vivo Anti-lipid Peroxidative Effect on Rosa davurica (생열귀나무의 항 HIV-1 protease 작용과 생체내 과산화지질생성 저해효과)

  • Kim, Suk-Nam;Chang, Kwang-Jin;Choi, Jong-Won;Park, Jong-Cheol
    • Korean Journal of Pharmacognosy
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    • v.31 no.3
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    • pp.264-267
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    • 2000
  • Anti-human immunodeficiency virus (HIV) type I protease (PR) and anti-lipid peroxidation effects on Rosa davurica were investigated. Of the various parts tested from R. davurica, the water extracts of stem and leaves inhibited the HIV-1 PR activity by more than 45% at a concentration of $100\;{mu}g/mL$. Hyperoside from the percarp of title plant showed 25% inhibition on HIV-1 PR at $200\;{mu}M$. The methanol extract of the root of R. davurica reduced the level of lipid peroxides induced by bromobenzene in vivo.

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The Extracts of Solanum nigrum L. for Inhibitory Effects on HIV-1 and Its Essential Enzymes (Human Immunodeficiency Virus Type I에 대한 용규(龍葵) 추출물의 억제활성)

  • Yu, Young-Beob
    • Korean Journal of Oriental Medicine
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    • v.10 no.1
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    • pp.119-126
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    • 2004
  • For the purpose of developing new anti-HIV agents from natural sources, the extracts of Solanum nigrum L. were tested for their inhibitory effects on HIV-1 replication and its essential enzymes as the reverse transcriptase (RT), protease and ${\alpha}$-glucosidase. In the assay of HIV-1-infected human T-cell line, water extracts inhibited the HIV- 1 -induced cytopathic effects with IC (inhibitory concentration) of 100 ug/ml. Moreover water extracts (100ug/ml) of aerial parts showed strong activity of 32.6% on anti-HIV-1 PR using the activity of the enzyme to cleave an oligopeptide. In the HIV-1 reverse transcriptase inhibition assay, aqueous extract a inhibited 17.4%, 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 PR and RT. 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 PR, RT and ${\alpha}$-glucosidase inhibitors.

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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 (다래나무 추출물의 HIV-1 효소억제활성과 구조활성상관(QSAR)예측)

  • Yu, Young-Beob
    • The Korea Journal of Herbology
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    • v.21 no.4
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    • pp.115-121
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    • 2006
  • 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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Inhibitory Effects of Campsis grandiflora on HIV-1 reverse Transcriptase, HIV-1 Protease and α-glucosidase (능소화 잎 및 줄기 추출물의 Human Immunodeficiency Virus Type I 억제활성)

  • Yu, Young-Beob
    • Korean Journal of Plant Resources
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    • v.25 no.2
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    • pp.169-175
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    • 2012
  • For the elucidation of action mechanism on anti-HIV of natural resources, the extracts of $Campsis$ $grandiflora$ were tested for their inhibitory effects on HIV-1 replication and its essential enzymes as the reverse transcriptase (RT), protease and ${\alpha}$-glucosidase. In the assay of HIV-1-infected human T-cell line, water extracts of stem inhibited the HIV-1-induced cytopathic effects with IC (inhibitory concentration) of 100 ${\mu}g$/ml. Moreover water extracts (100 ${\mu}g$/ml) of stem showed strong activity of 37.9% on anti-HIV-1 RT using Enzyme Linked Oligonucleotide Sorbent Assay (ELOSA) method. In the HIV-1 protease inhibition assay, methanol extracts of stem and leaf extract showed 33.6% and 31.5% inhibition of 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, but did not exhibited glucosidase inhibitory activities. From these results, it is suggested that the inhibition of the viral replication $in$ $vitro$ is due to the inhibition of reverse transcriptase by water extracts of stem of $Campsis$ $grandiflora$.

In vitro Evaluation of Anti-Human Immunodeficiency Virus Activity of Nucleoside Derivatives and Studies on Their Mode of Action (핵산유도체들의 항 Human Immunodeficiency Virus in vitro 약효평가와 작용기전연구)

  • Lee, Chong-Kyo;Kim, Dong-Ki;Kim, Jee-Hyun;Kim, Hae-Soo;Pi, Mi-Kyoung;Park, Jong-Beak;Kim, Baek
    • 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.

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Anti-Human Immunodeficiency Virus-Type 1 Activity of Constituents from Juglans mandshurica

  • Min, Byung-Sun;Lee, Hyeong-Kyu;Lee, Sang-Myung;Kim, Young-Ho;Bae, Ki-Hwan;Otake, Toru;Nakamura, Norio;Hattori, Masao
    • Archives of Pharmacal Research
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    • v.25 no.4
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    • pp.441-445
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    • 2002
  • Three naphthalene glycosides (1-3), four flavonoids (4-7), and two galloyl glycosides (8-9) were isolated from the stem-bark of Juglans mandshurica (Juglandaceae). Their structures were determined by chemical and spectral means, including to 2D-NMR (COSY, HMQC, and HMBC) experiments. Amongst the isolated compounds, taxifolin (4) showed the most potent HIV-induced cytopethic activity against MT-4 cells with complete inhibitory concentration ($IC_{100}$) value of $25{\;}{\mu\textrm{g}}/ml$ and maximum cytotoxic concentration ($CC_{100}$) value of above $100{\;}{\mu\textrm{g}}/ml$. However, naphthalene glycosides (1-3), flavonoids (5-7)), and galloyl tannins (8-9) were inactive against anti-HIV-1 activity.

Inhibitory Effects of Ricinus communis on HIV-1 Essential Enzymes in vitro and Prediction of Inhibitory Factor Using QSAR in silico (구조활성상관(QSAR)에 의한 피마엽 추출물의 HIV-1 효소억제활성인자 예측)

  • Han, Chang-Ho;Yu, Young-Beob
    • The Journal of Internal Korean Medicine
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    • v.27 no.4
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    • pp.888-894
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    • 2006
  • Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Ricinus communis were tested for their inhibitory effects on essential enzymes reverse transcriptase (RT), protease and alpha-glucosidase. Inhibition activity of major compounds of Ricinus communis were predicted from quantitative structure activity relationships (QSAR) in silico. Methods and Results : In the anti-HIV-1 RT using enzyme-linked oligonucleotide sorbent assay (ELOSA) method, water and methanol extracts (100ug/ml) of Ricinus communis showed strong activity of 94.2% and 82.7%, respectively. In the HIV-1 protease and alpha-glucosidase inhibition assay, neither water nor methanol extracts of Ricinus communis inhibited the activity of the enzyme to cleave any substrates as oligopeptides and oligosaccharides. Conclusions : We found that for these samples it is possible that the inhibition of the RT in vitro is due to the secondary metabolites of Ricinus communis such as ricinine and quercetin. It would beof great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agents up to date are RT inhibitors.

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Synthesis and Anti-HIV Evaluation of the Novel 2-(m-Chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines

  • Yan, Ren-Zhang;Liu, Xin-Yong;Xu, Wen-Fang;Pannecouque, Christophe;Witvrouw, Myriam;Clercq, Erik De
    • 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.

Inhibitory Effects of Gardenia jasminoides var. radicans Makino on HIV-1 Enzymes and Prediction of Inhibitory Factor by QSAR (꽃치자나무 추출물의 HIV-1 효소 억제 활성과 QSAR에 의한 활성인자 예측)

  • Yu, Young-Beob
    • 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.

Anti-HIV Activity of Dehydroaltenusin- a Metabolite from a Streptomyces sp.

  • Jabbar, Abdul;Shresta, Ajude Prashad;Hasan, Choudhury Mahmood;Rashid, Mohammad Abdur
    • Natural Product Sciences
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    • v.5 no.4
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    • pp.162-164
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    • 1999
  • Dehydroaltenusin (1) was isolated from the chloroform extract of the culture filtrate of a Streptomyces sp. and its structure was determined from spectral data as well as by comparison with published values. In an XTT-based in vitro anti-HIV assay, dehydroaltenusin effectively inhibited the cytopathic effects of HIV infection at a concentration of $1-5\;{\mu}g/mL$.

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