• Title/Summary/Keyword: Antiviral Activity

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Synthesis of Novel Carboacyclic Nucleosides with Vinyl Bromide Moiety as Open-chain Analogues of Neplanocin A

  • Choi, Myung-Hee;Kim, Hee-Doo
    • Archives of Pharmacal Research
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    • v.26 no.12
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    • pp.990-996
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    • 2003
  • A novel carboacyclic nucleoside analogue, 9-[2-bromo-4-hydroxy-3-hydroxymethyl-2-butenyl] adenine, and its derivatives were designed and synthesized as open-chain analogues of neplanocin A. The syntheses were accomplished via the coupling of adenine or pyrimidine bases to the key intermediate allylic bromide 7. The bromide 7 was prepared from epichlorohydrin in a seven step process in a 54% overall yield. The synthesized compounds were evaluated for their antiviral activity against the polio virus, HSV and HIV.

Synthesis and Antiviral Activity of Novel C-Methyl Branched Cyclopropyl Nucleosides

  • Kwak, Eun-Yee;Hong, Joon-Hee;Park, Young-Jak;Choi, Bo-Gil
    • Archives of Pharmacal Research
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    • v.26 no.9
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    • pp.679-685
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    • 2003
  • A series of novel cyclopropyl nucleosides was synthesized using the highly stereoselective Simmons-Smith reaction starting from 1,2:5,6-di-Ο-isopropylidene-D-mannitol. The structural assignments of these nucleosides were determined by NMR studies and X-ray crystallography. All the synthesized nucleosides were assayed against several viruses.

Newly Designed Six-membered Azasugar-Containing Phosphorothioate Oligonucleotide as a Potent AIDS Therapeutic Drug

  • Bae, Yong-Soo
    • 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.

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Purification and Characterization of an Antiviral Ribosome-inactivating Protein from Chenopodium album L.

  • Cho, Kang-Jin;Lee, Si-Myung;Kim, Yeong-Tae;Hwang, Young-Soo
    • Journal of Applied Biological Chemistry
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    • v.43 no.3
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    • pp.125-130
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    • 2000
  • An antiviral protein (CAP30) with ribosome-inactivating activity was purified from the leaves of Chenopodium album L. through ammonium sulfate precipitation and column chromatography using S-Sepharose, Blue-Sepharose, FPLC Suprose12 HR, and FPLC Mono-S. The molecular wight of CAP30 was estimated to be 30kD. CAP30 was thermostable, maintaing its activity even after incubation at $70^{\circ}C$ for 30 min, and was stable in the pH range of 6 to 9. In a cell-free in vitro translation system using rabbit reticulocyte lysate, protein synthesis was inhibited by the addition of CAP30 with an $IC_{50}$ of 2.26pM. The comparison of N-terminal amino acid sequences of this protein with known ribosome-inactivating proteins (RIPs) revealed that it had some sequence homology with PAP-S and PAP-R from pokeweed (Phytolacca americana)and dodecandrin from P. dodecandra, but had no sequence homology with RIPs from other plants belonging to different orders. The mosaic symptoms on tobacco leaves caused by cucumber mosaic virus infection was completely inhibited by 100 ng/ml of the pure CAP30 protein.

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Repurposing Screens of FDA-Approved Drugs Identify 29 Inhibitors of SARS-CoV-2

  • Ku, Keun Bon;Shin, Hye Jin;Kim, Hae Soo;Kim, Bum-Tae;Kim, Seong-Jun;Kim, Chonsaeng
    • Journal of Microbiology and Biotechnology
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    • v.30 no.12
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    • pp.1843-1853
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    • 2020
  • COVID-19, caused by the novel coronavirus SARS-CoV-2, has spread globally and caused serious social and economic problems. The WHO has declared this outbreak a pandemic. Currently, there are no approved vaccines or antiviral drugs that prevent SARS-CoV-2 infection. Drugs already approved for clinical use would be ideal candidates for rapid development as COVID-19 treatments. In this work, we screened 1,473 FDA-approved drugs to identify inhibitors of SARS-CoV-2 infection using cell-based assays. The antiviral activity of each compound was measured based on the immunofluorescent staining of infected cells using anti-dsRNA antibody. Twenty-nine drugs among those tested showed antiviral activity against SARS-CoV-2. We report this new list of inhibitors to quickly provide basic information for consideration in developing potential therapies.

Innate immune responses of common carp, Cyprinus carpio L. against antiviral activity inducers (항바이러스 활성 유도 물질에 대한 잉어의 선천성 면역 반응)

  • Cho, Mi-Young;Kim, Su-Mi;Kim, Eun-Jeon;Shon, Sang-Gyu;Kim, Jin-Woo;Park, Soo-Il
    • Journal of fish pathology
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    • v.20 no.2
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    • pp.189-200
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    • 2007
  • To investigate the innate immune response involved in early stage of anti-viral defence, carps were injected with UV-inactivated spring viraemia of carp virus (SVCV), poly inosinic:cytidylic acid (Poly I:C) and concanavalin A (Con A), respectively and examined lysozyme activity, serum complement activity and chemiluminescent (CL) response of leucocytes isolated from head kidney at 3 days post-injection. There was no significant difference in plasma lysozyme activities among all experimental groups. However, lysozyme activities of head kidney in the groups injected with antiviral activity inducers were significantly higher than those of the control injected with physiological saline. Bactericidal activities of serum of the groups injected with antiviral activity inducers were not significantly different from control group. However, the CL responses were significantly higher at lower dose of Poly I:C and Con A, whilst dose-dependent increase was shown in UV-inactivated SVCV-injected group. In the challenge test with 1×104 TCID50/fish of SVCV at 4 days post-injection, UV-inactivated SVCV- and Poly I:C-injected groups showed higher relative percent survival (RPS) than Con A-injected group. Furthermore, strong protection was observed in the group injected higher dose of Poly I:C although showed lower activities in lysozyme and CL response. These results suggested that Poly I:C might stimulate other factors belonging to non-specific immune system have induced protective immunity against the SVCV challenged.

Biolagical Activity on Extracts of Japanese Anise(Illicium Anisatum L.) Leaves and Twigs (붓순나무 잎과 가지의 추출물에 대한 생리활성 평가)

  • Shinn, Seong-Whan
    • The Journal of the Convergence on Culture Technology
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    • v.5 no.3
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    • pp.311-316
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    • 2019
  • Japanese anise (Illicium anisatum L.) leaves and twigs were extracted with 50 % aqueous acetone three times. After filtration, the extracts were fractionated with n-hexane, chloroform, ethyl acetate and $H_2O$, and then freeze dried after condensation. Then antioxidation and antiviral activity were evaluated on each fractions. In the antioxidative activities, the results indicated high activity in the EtOAc soluble fraction of the leaves and the EtOAc and $H_2O$ soluble fractions of the twigs. It showed much higher antioxidative value compare to the controls, BHT and ${\alpha}$-tocopherol. In the antiviral activities, the all fractions were negative effects in HRV 1B and EV 71, but good in Influenza PR8. The activities of the crude extracts of the leaves and twigs showed more than 80% activity at the concentration of $10{\mu}g/mL$ and $50{\mu}g/mL$, respectively, and the activities of the EtOAc and $H_2O$ soluble fractions were close to 80%. Based on the above results, the extracts of Japanese anise may be applied for one of the natural biomass sources that can be used as an antioxidant and an antiviral substance.

Synthesis of D-1,3-Dioxolane and L-1,3-Oxathiolane 5-Phenylselenyl Pyrimidine Nucleosides as Potential Antiviral Agents (D-1,3-디옥솔란 및 L-1,3-옥사티올란 5-페닐세레닐 피리미딘 뉴크레오사이드의 합성)

  • Yoo, Jung-Man;Moon, Hyun-Ju;Chung, Byung-Ho;Choi, Bo-Gil;Hong, Joong-Hee;Chun, Moon-Woo
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.46-51
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    • 1996
  • Eight new D-1.3-dioxolanyl and L-1,3-oxathiolanyl nucleosides containing 5-phenyl- selenyl pyrimidine bases which are expected to have antiviral activity were synthesized. Condensation of D-1,3-dioxolane acetate and L-1,3-oxathiolane acetate with 5-phenylselenyl pyrimidines gave anomeric mixtures of their nucleosides which were separated by silicagel column chromatography.

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Synthesis of (-)-Neplanocin A Analogues as Potential Antiviral Agents

  • Shin, Dae-Hong;Lee, Hyuk-Woo;Park, Sung-Soo;Kim, Joong-Hyup;Jeong, Lak-Shin;Chun, Moon-Woo
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.302-309
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    • 2000
  • Based on (-)-neplanocin A with the 5'-hydroxyl substituted with fluoro, azido, or amino group, the corresponding xylo- and arabino derivatives were synthesized from D-ribose using the Mit-sunobu reaction as a key step. None of the final nucleosides did show either significant antiviral activities or cytotoxicities.

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