Human Immunodeficiency Virus‐Reverse Transcriptase Inhibition and Hepatitis C Virus RNA‐Dependent RNA Polymerase Inhibition Activities of Fullerene Derivatives.

Mashino, Tadahiko; Shimotohno, K; Ikegami, Noriko; Nishikawa, Dai; Okuda, K; Takahashi, Kyoko; Nakamura, Shigeo; Mochizuki, Masahito

doi:10.1002/chin.200525096

Cited by 21 publications

(38 citation statements)

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“…We report here, for the first time, HCV-RdRp-inhibitory activity of demethylzeylasteral (compound 5) from T. hypoglaucum. Due to HCV-RdRp-inhibitory activity of compound 5 and based on the previous research showing increased HCV-RdRp-inhibitory activity following alteration of functional groups in synthesized compounds [28], additional modification of the functional groups R1, R2, R3, and R4 (see Fig. 1) of compound 5 for leading to more potent HCV-RdRp-inhibitory substances would be a valuable step toward finding anti-HCV agents based on natural products.…”

Section: Discussionmentioning

confidence: 99%

Inhibitory effect of Yunnan traditional medicines on hepatitis C viral polymerase

Nakamura

Kakiuchi

et al. 2006

J Nat Med

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For the purpose of developing novel anti-hepatitis C virus (HCV) agents from natural resources, 93 Yunnan crude drugs were screened for their inhibitory effects on RNA-dependent RNA polymerase (RdRp) of HCV. Although 71 methanol extracts and 50 water extracts inhibited HCV-RdRp by more than 50% at a concentration of 50 μg/ml, the majority of them contained a high percentage of tannins. However, methanol extracts of Plumbago zeylanica (branch), Maytenus fookerii (leaf) and Huashidancha (Y61, branch and leaf), and water extracts of Potentilla griffithii (whole plant) and Salvia yunnanensis (underground part), having IC values of less than 10 μg/ml, showed less than 10% tannin content. In addition, from a methanol extract of Tripterygium hypoglaucum (root bark), demethylzeylasteral was isolated as a strongly inhibitory substance against HCV-RdRp.

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Section: Discussionmentioning

confidence: 99%

Inhibitory effect of Yunnan traditional medicines on hepatitis C viral polymerase

Nakamura

Kakiuchi

et al. 2006

J Nat Med

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“…Results indicated that the amino acid modified fullerenes strongly inhibited HIV-RT with the IC 50 of 0.029 M [38]. A series of C 60 derivatives were synthesized, and the inhibition efficiency of fullerene to HIV-1 strain was improved with the increased positive charges near to the C 60 backbone [39].…”

Section: Anti-virus Activitymentioning

confidence: 98%

“…C 60 didn't possess a specific affinity to the virions and it seemed that ROS was contributed for it [44]. Hepatitis C virus (HCV) inhibition effects of three fullerenes derivatives were not significantly different [38].…”

Section: Anti-virus Activitymentioning

confidence: 99%

Fullerenes as unique nanopharmaceuticals for disease treatment

Liang

2010

Sci. China Chem.

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As unique nanoparticles, fullerenes have attracted much attention due to their unparalleled physical, chemical and biological properties. Various functionalized fullerenes with OH, NH 2 , COOH, and peptide modifications were developed. It summarized the biological activities of fullerenes derivatives in cancer therapy with high efficiency and low toxicity, as reactive oxygen species scavenger and lipid peroxidation inhibitor, to inhibit human immunodeficiency virus and to suppress bacteria and microbial at low concentration. In addition, the mechanism for fullerene to enter cells and biodistribution of fullerene in vivo was also discussed. This research focuses on the current understanding of fullerenes-based nanomaterials in the potential clinical application as well as biological mechanism of fullerenes and its derivatives in disease therapy. fullerene, nanoparticle, nanomedicine, clinical application, biological effect

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“…However, much potential research and many applications in biological systems are greatly hindered because the unique cage structure of fullerene made it highly hydrophobic and hardly soluble in hydrophilic solvents. The water-solubility of fullerene and its derivatives has been improved in several ways, including: (1) chemical functionization to obtain soluble derivatives [4] ; (2) utilization of stabilizer to make aqueous solution [5,6] ; (3) formation of a uniform dispersion of aqueous nanoparticle suspension by a specific procedure which includes dissolving fullerene or its derivative in some organic solvents (e.g., tetrahydrofuran and toluene), mixing with water, and finally removing organic solvents [7,8] .…”

Section: Introductionmentioning

confidence: 99%

Inhibition of DNA restrictive endonucleases by aqueous nanoparticle suspension of methanophosphonate fullerene derivatives and its mechanisms

Song

Huang

et al. 2009

Sci. China Ser. B-Chem.

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Aqueous nanoparticle suspension of fullerene and its derivatives are currently attracting much attention. To determine the effects of aqueous nanoparticle suspension of a mono-methanophosphonate fullerene and bis-methanophosphonate fullerene (denoted as n-MMPF and n-BMPF, respectively) on the activities of DNA restrictive endonucleases, plasmid pEGFP-N1 was cleaved at a single but differently restrictive site by EcoR I, BamH I, and isozymes Cfr9 I and Xma I, respectively. Both n-MMPF and n-BMPF inhibited the activity of EcoR I, while n-BMPF exhibited stronger inhibition than n-MMPF. Addition of n-BMPF into reaction mixtures inhibited the activities of all the four enzymes, and IC 50 values for EcoR I, BamH I, Cfr9 I and Xma I were 4.3, >30, 11.7 and 8.3 μmol/L, respectively. When EcoR I was completely inhibited by n-BMPF, addition of excess amounts of pEGFP-N1 could not produce the product linear plasmid; however, increase of EcoR I amounts antagonized EcoR I inhibition of n-BMPF. Two scavengers of reactive oxygen species (ROS), mannitol and sodium azide at the concentrations of 2−10 mmol/L, did not reverse inhibition of n-BMPF, implying that this inhibition probably is not correlated to ROS. These results suggested that aqueous nano-fullerenes might act as inhibitors of DNA restrictive endonucleases. mono-and bis-methanophosphonate fullerene, aqueous nanoparticle suspension, DNA restrictive endonucleases, reactive oxygen species

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Human Immunodeficiency Virus‐Reverse Transcriptase Inhibition and Hepatitis C Virus RNA‐Dependent RNA Polymerase Inhibition Activities of Fullerene Derivatives.

Abstract: Derivatives. -(MASHINO*, T.; SHIMOTOHNO, K.; IKEGAMI, N.; NISHIKAWA, D.; OKUDA, K.; TAKAHASHI, K.; NAKAMURA, S.; MOCHIZUKI, M.; Bioorg. Med. Chem. Lett. 15 (2005) 4, 1107-1109; Kyoritsu Coll. Pharm., Minato, Tokyo 105, Japan; Eng.) -A. Forchert 25-096

Cited by 21 publications

References 1 publication

Inhibitory effect of Yunnan traditional medicines on hepatitis C viral polymerase

Inhibitory effect of Yunnan traditional medicines on hepatitis C viral polymerase

Fullerenes as unique nanopharmaceuticals for disease treatment

Inhibition of DNA restrictive endonucleases by aqueous nanoparticle suspension of methanophosphonate fullerene derivatives and its mechanisms

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