• Journal of Applied Biological Chemistry
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• 제42권4호
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• pp.161-165
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• 1999

The antiviral activity of CAP30 from Chenopodium album, a type1 ribosome-inactivating protein (RIP), was examined against 5 different plant viral pathogens, and its activity against Tobacco mosaic virus was compared to those of well known antiviral proteins such as Pokeweed Antiviral protein from leaves and seeds. When the inoculating concentration of Tobacco mosaic virus was varied from 0.4 to $400{\mu}g/ml$, it was observed that CAP30 at the concentration of $1{\mu}g/ml$ suppressed the viral infection of C. amaranthicolor and C. quinoa almost completely up to $40{\mu}g/ml$ Tobacco mosaic virus. Results from the assays for the inhibitions of in vitro translation of rabbit reticulocyte lysate and the suppression of Tobacco mosaic virus infection ($10{\mu}g/ml$) to C. quinoa indicated that CAP30 is a strong inhibitor of protein synthesis and virus infection. The infection of several viruses other than Tobacco mosaic virus to host plants were also inhibited by $5{\mu}g/ml$ CAP30, suggesting that a gene encoding CAP30 can be used to develop transgenic virus-resistant plants.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.233.2-233.2
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• 2002

Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand. neplanocin A is the representative of the carbocyclic nucleosides and has been recognized as a potent antitumor and antiviral agent. Based on these findings. it was of great interest to design apio neplanocia A which combined the properties of apio nucleosides and neplanocin A. (omitted)

• Bulletin of the Korean Chemical Society
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• 제26권9호
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• pp.1366-1368
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• 2005

The first synthesis of a 4'-branched carbocyclic C-nucleoside 11 was achieved via the key intermediate 6, which was prepared using Knovenagel type condensation from ketone derivative 4.

• 생약학회지
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• 제30권1호
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• pp.34-39
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• 1999

To search for less toxic antiherpetic agents, the inhibitory effects of twelve kinds of flavonoids including chrysin, quercetin, quercitrin, rutin, fisetin, gossypin, kaempferol, morin, naringenin, naringin, hesperetin and hesperidin on the plaque formation of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in Vero cells were examined by plaque reduction assay in vitro. Some flavonoids tested in this study showed potent antiherpetic activity, reducing intracellular replication of herpes simplex viruses when Vero cell monolayers were infected and subsequently cultured in medium containing flavonoids. Naringenin showed the most potent antiviral activity against HSV-1 with selectivity index (SI) of 19.1 and hesperetin showed the most potent antiviral activity against HSV-2 with SI of 9.8. These results suggest that some flavonoids may be a potential therapeutic agent for the treatment and prevention of herpes simplex virus infections.

• 약학회지
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• 제48권1호
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• pp.88-92
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• 2004

In this study; a series of 2',4'-doubly branched carbocyclic nucleosides (8,9,10) were synthesized from simple acyclic ketone derivative as starting material. The installation of the 4'-quaternary carbon needed was carried out using a 〔3,3〕-sigmatropic rearrangement. In addition, the introduction of a methyl group in the 2'-position was accomplished by Grig-nard reaction. Bis-vinyl was successfully cyclized using a Grubbs' catalyst II. The natural bases (adenine, cytosine, uracil) were efficiently coupled with the use of a Pd(0) catalyst. Although all the synthesized compounds were assayed against several viruses, only cytosine analogue 9 showed weak antiviral viral activity (EC$_{50}$=45.4 $\mu$M) against CoxB3 virus.s.

• Archives of Pharmacal Research
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• 제17권2호
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• pp.93-99
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• 1994

Macrtophages play an important role in defense against virus infection by intrinsic resistance and by extrinsic resistance. Since interferon-induced enzymes which are 2'-5' oligoadenylate synthetase and p1/eIF-2 protein kinase have been shown to be involved in the inhibition of viral replication, I examined the mechanism by which poly I:C, an interferon inducer, exerts its antiviral effects in inflammatory macrophages infected with herpes simplex virus type 1 (HSV-1). The data presented here demonstrate that poly I:C-induced antiviral activity is partially due to the activation of 2'-5' pligoadenylate synthetase. The activation of 2'-5' oligoadenlate A synthetase by poly I:C is also at least mediated via the production of interferon-.betha.. Taken together, these data indicate that interferon-.betha. produced in response to poly I:C acts in an autocrine manner to activate the 2'-5' oligoadenylate synthetase and to induce resistance to HSV-1.

• Bulletin of the Korean Chemical Society
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• 제29권9호
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• pp.1723-1728
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• 2008

An efficient synthetic route for carbocyclic versions of stavudine analogues and their evaluation on antiviral activity are described. The construction of an ethynylated quaternary carbon at the 4'-position of carbocyclic nucleosides was accomplished using Claisen rearrangement of 11 and ring-closing metathesis (RCM) of dienyne 14 as key transformations. An antiviral evaluation of the synthesized compounds, 20, 21, 22, and 25 against HIV-1, HSV-1, HSV-2, and HCMV showed that only the guanine analogue 25 is moderately active against HIV-1 in the MT-4 cell line ($EC_{50}$ = 11.91 $\mu$mol).

• Bulletin of the Korean Chemical Society
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• 제30권11호
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• pp.2626-2630
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• 2009

2'($\beta$)-Hydroxymethylated adenosine is a potent and selective inhibitor of hepatitis C virus (HCV) replication. It targets the RNA-dependent RNA polymerase of HCV, NS5B. Synthesis and antiviral evaluation of carbocyclic versions are described. The cyclopentene intermediate ($9\beta$) was successfully synthesized through sequential Johnson-Claisen orthoester rearrangement and ring-closing metathesis (RCM). Coupling of bases via a Pd(0) catalyst, selective dihydroxylation, and desilylation yielded the target nucleoside analogues. The compounds 17 and 18 were assayed for their ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line and showed moderate antiviral activity with toxicity up to 20.0 and 24.7 ${\mu}g/mL$, respectively.

• Advances in Traditional Medicine
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• 제9권2호
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• pp.192-199
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• 2009

Bioactivity-directed isolation has led to the isolation of (-)-ent-costunolide (1) as the major active compound from Hepatostolonophora paucistipula. This compound (1) was determined by spectroscopic data interpretation. This sesquiterpene lactone (1) inhibited the growth of the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185, (4 mm inhibition zone at $15{\mu}g$/disc), cytotoxic activity to murine leukaemia cell lines ATCC CCL 46 P 388D1 ($IC_{50}$ 687 ng/ml, at $0.075{\mu}g$/disk), BSC monkey kidney cell lines (100% of well at $15{\mu}g$/disk) and antiviral activity to Herpes simplex virus (0.25 mg/ml, 100% of well at $7.5{\mu}g$/disk) and Polio virus (0.125 mg/ml, 100% of well at $3.75{\mu}g$/disk). These results suggest that (-)-ent-costunolide (1) has potential antimicrobial and cytotoxic agents.

• Archives of Pharmacal Research
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• 제26권11호
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• pp.960-966
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• 2003

Macrophages play an important role in host defenses by killing tumors and virus infections and producing secretory products. High mannuronic acid (HMA) containing alginate was examined to determine the mechanisms by which HMA-activated macrophages resist infection with HSV-1 and inhibit the growth of tumor cells. The ability of macro phages to resist infection with HSV-1 or to inhibit the growth of tumor cells was assessed following treatment with HMA alginate in the presence of either antibodies to various cytokines or inhibitors/scavengers of toxic macrophage products. Only antibodies to IFN-$\alpha$/$\beta$ were able to abrogate the protective effects of HMA alginate in macrophages infected with HSV-1, suggesting that the antiviral activity induced by this immunomodulator was mediated by the production of IFN-$\beta$. In contrast, anti-TNF-$\alpha$, anti-IFN and inhibitors of nitric oxide and reactive oxygen species were all able to partially abrogate HMA-induced cytostatic activity, suggesting that multiple mechanisms are involved in macrophage cytostasis. These results indicate that the HMA-induced intrinsic antiviral and extrinsic cytotoxic activites are mediated by different mechanisms.