• 제목/요약/키워드: anti-HIV-1 activity

검색결과 75건 처리시간 0.018초

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

  • 김석남;장광진;최종원;박종철
    • 생약학회지
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    • 제31권3호
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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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Human Immunodeficiency Virus Type I에 대한 용규(龍葵) 추출물의 억제활성 (The Extracts of Solanum nigrum L. for Inhibitory Effects on HIV-1 and Its Essential Enzymes)

  • 유영법
    • 한국한의학연구원논문집
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    • 제10권1호
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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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다래나무 추출물의 HIV-1 효소억제활성과 구조활성상관(QSAR)예측 (Inhibitory Effects of Actinidia arguta on HIV-1 Reverse transcriptase, HIV-1 Protease and alpha-glucosidase in vitro and in silico)

  • 유영법
    • 대한본초학회지
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    • 제21권4호
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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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능소화 잎 및 줄기 추출물의 Human Immunodeficiency Virus Type I 억제활성 (Inhibitory Effects of Campsis grandiflora on HIV-1 reverse Transcriptase, HIV-1 Protease and α-glucosidase)

  • 유영법
    • 한국자원식물학회지
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    • 제25권2호
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    • pp.169-175
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    • 2012
  • 능소화 추출물의 HIV-1에 대한 항바이러스 효과를 복제 관련 효소에 대한 억제실험과 바이러스 복제억제 실험을 통하여 살펴보았다. 역전사효소 억제활성을 ELOSA 방법으로 실험한 결과 능소화 줄기의 물 추출물이 100 ${\mu}g$/ml 농도에서 각각 37.9%의 활성을 나타내었고, 능소화 잎과 줄기의 메탄올 추출물에서 33.6% 및 31.5%의 HIV-1 protease 억제활성 나타 내었다. 그리고 HIV-1 복제 억제활성은 MT-4 세포에 대한 HIV-1 유도 세포변성억제를 광학현미경으로 관찰하여 살펴본 결과 줄기의 물 추출물이 100 ${\mu}g$/ml 농도에서 HIV-1 바이러스 증식을 완전히 억제하였다.

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

  • 이종교;김동기;김지현;김해수;피미경;박종백;김백
    • 대한바이러스학회지
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    • 제27권1호
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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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    • 제25권4호
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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.

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

  • 한창호;유영법
    • 대한한방내과학회지
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    • 제27권4호
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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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    • 제29권11호
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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.

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

  • 유영법
    • 한국자원식물학회지
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    • 제27권1호
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    • pp.22-28
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    • 2014
  • 꽃치자나무 추출물의 HIV-1 reverse transcriptase, protease 및 alpha-glucosidase에 대한 억제활성실험을 실시하였다. ELOSA 방법으로 실험한 역전사효소 억제활성 실험에서는 꽃치자나무 잎 MeOH 추출물 $100{\mu}g/ml$ 농도에서 13.4%의 약한 억제활성이 관찰되었고, 줄기의 메탄올추출물에서는 32.5%의 높은 HIV-1 protease 억제활성과 줄기의 메탄올 추출물에서는 26.1%의 alpha-glucosidase 억제활성이 관찰되었다. 그리고 HIV-1 복제 억제활성은 MT-4 세포에 대한 HIV-1 유도 세포변성억제를 광학현미경으로 관찰하여 살펴본 결과 잎과 줄기의 모든 추출물에서 HIV-1 바이러스 증식억제에 억제활성이 관찰되지 않았다. In silico 실험결과 주요성분인 crocetin이 81.8%의 높은 역전사 효소활성이 예측되었으며, genipin이 55.39%, geniposidic acid aglycone이 64.5% 역전사효소 활성이 예측되었다. 주로 aglycone의 활성이 높게 예측되었으며 배당체의 경우 활성이 현저하게 저하되는 것으로 나타났다.

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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    • 제5권4호
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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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