• Title/Summary/Keyword: CVB

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Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

  • Wubulikasimu, Reyila;Yang, Yanbing;Xue, Fei;Luo, Xianjin;Shao, Dongping;Li, Yuhuan;Gao, Rongmei;Ye, Weidong
    • Bulletin of the Korean Chemical Society
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    • v.34 no.8
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    • pp.2297-2304
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    • 2013
  • A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4- or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 ($IC_{50}=1.08{\mu}g/mL$, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.

Antiviral activity of ginsenosides against coxsackievirus B3, enterovirus 71, and human rhinovirus 3

  • Song, Jae-Hyoung;Choi, Hwa-Jung;Song, Hyuk-Hwan;Hong, Eun-Hye;Lee, Bo-Ra;Oh, Sei-Ryang;Choi, Kwangman;Yeo, Sang-Gu;Lee, Yong-Pyo;Cho, Sungchan;Ko, Hyun-Jeong
    • Journal of Ginseng Research
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    • v.38 no.3
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    • pp.173-179
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    • 2014
  • Background: Ginsenosides are the major components responsible for the biochemical and pharmacological actions of ginseng, and have been shown to have various biological activities. In this study, we investigated the antiviral activities of seven ginsenosides [protopanaxatriol (PT) type: Re, Rf, and Rg2; protopanaxadiol (PD) type: Rb1, Rb2, Rc, and Rd)] against coxsackievirus B3 (CVB3), enterovirus 71 (EV71), and human rhinovirus 3 (HRV3). Methods: Assays of antiviral activity and cytotoxicity were evaluated by the sulforhodamine B method using the cytopathic effect (CPE) reduction assay. Results: The antiviral assays demonstrated that, of the seven ginsenosides, the PT-type ginsenosides (Re, Rf, and Rg2) possess significant antiviral activities against CVB3 and HRV3 at a concentration of $100{\mu}g/mL$. Among the PT-type ginsenosides, only ginsenoside Rg2 showed significant anti-EV71 activity with no cytotoxicity to cells at $100{\mu}g/mL$. The PD-type ginsenosides (Rb1, Rb2, Rc, and Rd), by contrast, did not show any significant antiviral activity against CVB3, EV71, and HRV3, and exhibited cytotoxic effects to virus-infected cells. Notably, the antiviral efficacies of PT-type ginsenosides were comparable to those of ribavirin, a commonly used antiviral drug. Conclusion: Collectively, our findings suggest that the ginsenosides Re, Rf, and Rg2 have the potential to be effective in the treatment of CVB3, EV71, and HRV3 infection.

Cinnamaldehyde Derivatives Inhibit Coxsackievirus B3-Induced Viral Myocarditis

  • Li, Xiao-Qiang;Liu, Xiao-Xiao;Wang, Xue-Ying;Xie, Yan-Hua;Yang, Qian;Liu, Xin-Xin;Ding, Yuan-Yuan;Cao, Wei;Wang, Si-Wang
    • Biomolecules & Therapeutics
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    • v.25 no.3
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    • pp.279-287
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    • 2017
  • The chemical property of cinnamaldehyde is unstable in vivo, although early experiments have shown its obvious therapeutic effects on viral myocarditis (VMC). To overcome this problem, we used cinnamaldehyde as a leading compound to synthesize derivatives. Five derivatives of cinnamaldehyde were synthesized: 4-methylcinnamaldehyde (1), 4-chlorocinnamaldehyde (2), 4-methoxycinnamaldehyde (3), ${\alpha}$-bromo-4-methylcinnamaldehyde (4), and ${\alpha}$-bromo-4-chlorocinnamaldehyde (5). Neonatal rat cardiomyocytes and HeLa cells infected by coxsackievirus B3 (CVB3) were used to evaluate their antiviral and cytotoxic effects. In vivo BALB/c mice were infected with CVB3 for establishing VMC models. Among the derivatives, compound 4 and 5 inhibited the CVB3 in HeLa cells with the half-maximal inhibitory concentrations values of $11.38{\pm}2.22{\mu}M$ and $2.12{\pm}0.37{\mu}M$, respectively. The 50% toxic concentrations of compound 4 and 5-treated cells were 39-fold and 87-fold higher than in the cinnamaldehyde group. Compound 4 and 5 effectively reduced the viral titers and cardiac pathological changes in a dose-dependent manner. In addition, compound 4 and 5 significantly inhibited the secretion, mRNA and protein expressions of inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 in CVB3-infected cardiomyocytes, indicating that brominated cinnamaldehyde not only improved the anti-vital activities for VMC, but also had potent anti-inflammatory effects in cardiomyocytes induced by CVB3.

Antiviral Activity of Hot-Water Extract and Its Ethanol Precipitate of Phellinus pini Fruiting Body (낙엽진흙버섯 자실체 유래 열수 추출물과 메탄을 침전물의 항바이러스활성)

  • Lee, Sae-Mi;Kim, Sung-Min;Lee, Yoon-Hee;Kim, Woo-Jung;Na, Ye-Seul;Kim, Hyun-Guell;Nam, Jae-Hwan;Shin, Hyun-Dong;Kwon, Doo-Han;Park, Yong-Il
    • Microbiology and Biotechnology Letters
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    • v.37 no.1
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    • pp.33-41
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    • 2009
  • The crushed fruiting body of Alaskan Porodaedalea pini (Brot.) Murrill (syn. Phellinus pini) was extracted in boiling water for 4 h with the yield of 20.5% in dry mass. This hot-water extract showed significant antiviral activity by inhibiting the plaque formation in HeLa cells by coxackievirus B3 (CVB3) and also showed highest inhibitory effect against neuraminidase activity among water extracts of various mushrooms. From the water extract, the ethanol precipitate (EP) and supernatant fraction (ES) were obtained through 75% ethanol precipitation with the yield of 43.3% and 28.3% in dry mass, respectively. Whereas ES did not show any detectable level of antiviral activity, EP showed significant dose-dependent inhibition of plaque formation by CVB3 in HeLa cells with an $EC_{50}$ (50% effective concentration) of 0.45 mg/mL. The cytotoxicity on HeLa cells by EP was relatively low with the $CC_{50}$ (50% cytotoxic concentration) of 2.25 mg/mL. EP also effectively inhibited neuraminidase activity in a dose-dependent manner showing up to 75% inhibition at 1.7 mg/mL. These results suggest that the hot-water extract and its EP of P. pini fruiting body can be a candidate for the development of a potent broad-range antiviral agent against influenza virus(Flu) as well as CVB3. The major active component of EP was shown to be a heteropolysaccharide-protein complex containing glucose as the main sugar residue with mole percentage of 79.8% and other sugars like galactose (19.2%), xylose (17%), mannose (5.8%), and fucose (4.6%) and a small portion (12.7%, in mass) of protein.

Molecular identification and clinical features of enteroviral infection in children of central Korea: An overview of enteroviral epidemiology between spring 2005 and autumn 2006 (2005년 봄부터 2006년 가을까지 국내 중부지역의 enterovirus 감염의 분자유전학 조사와 임상양상)

  • Roh, Eui Jung;Jin, Yong Man;Chung, Eun Hee;Chang, Young Pyo;Park, Woo Sung;Park, Kwisaung;Jee, Young Mee
    • Clinical and Experimental Pediatrics
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    • v.52 no.11
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    • pp.1234-1240
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    • 2009
  • Purpose:Enteroviruses (EVs) are commonly known to cause infection, especially in infants and children. This report presents an overview of enterovirus epidemiology in central Korea. Methods:From the spring of 2005 to the autumn of 2006, we collected the cerebrospinal fluid (CSF) and stool samples from the pediatric patients with a febrile illness or suspected meningitis who were admitted to hospitals in central Korea. In order to test for EVs, cell lines were derived from pretreated susceptible specimen, and the cytopathic effects were observed. Seminested real time-polymerase chain reaction (RT-PCR) and direct sequencing were performed for genotypic and phylogenetic analyses. Results:Of the 305 patients examined, 51 (16.7%) tested positive for EV. Of these 51 patients, 44 showed the following serotypes: Echovirus (ECV) 18 (18 cases, 35.2%), Coxsackievirus B (CVB) 5 (13 cases, 25.4%), ECV25 (5 cases, 9.8%), ECV9 (4 cases, 7.8%), ECV5 (3 cases, 5.8%), and EV74 (1 case, 1.9%). In 2005, between June and August, ECV18 and CVB5 were mostly responsible for the enteroviral infections among the patients in central Korea. In 2006, between July and August, ECV25 was mostly the cause of enteroviral infection. Conclusions:There is a need for continuous surveillance of enteroviral infection and its clinical manifestations, particularly for EV74, which was first identified in Korea.

Growth Performance of Early Finishing Gilts as Affected by Different Net Energy Concentrations in Diets

  • Lee, Gang Il;Kim, Kwang-Sik;Kim, Jong Hyuk;Kil, Dong Yong
    • Asian-Australasian Journal of Animal Sciences
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    • v.28 no.11
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    • pp.1614-1623
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    • 2015
  • The objectives of the current experiment were to study the response of the growth performance of early finishing gilts to different net energy (NE) concentrations in diets, and to compare the NE values of diets between calculated NE values and measured NE values using French and Dutch CVB (Centraal Veevoederbureau; Central Bureau for Livestock Feeding) NE systems. In a metabolism trail, the NE concentrations in five diets used for the growth trial were determined based on digestible nutrient concentrations, digestible energy, and metabolizable energy using a replicated $5{\times}5$ Latin square design with 10 barrows (initial body weight [BW], $39.2{\pm}2.2kg$). In a growth trial, a total of 60 early finishing gilts (Landrace${\times}$Yorkshire; initial BW, $47.7{\pm}3.5kg$) were allotted to five dietary treatments of 8.0, 9.0, 10.0, 11.0, and 12.0 MJ NE/kg (calculated, as-is basis) with 12 replicate pens and one pig per pen in a 42-d feeding experiment. The NE and amino acid (AA) concentrations in all diets were calculated based on the values from NRC (2012). Ratios between standardized ileal digestible AA and NE concentrations in all diets were closely maintained. Pigs were allowed ad libitum access to feed and water. Results indicated that calculated NE concentrations in diets (i.e., five dietary treatments) were close to measured NE concentrations using French NE system in diets. The final BW was increased (linear and quadratic, p<0.05) with increasing NE concentrations in diets. Furthermore, average daily gain (ADG) was increased (linear and quadratic, p<0.01) with increasing NE concentrations in diets. There was a quadratic relationship (p<0.01) between average daily feed intake and NE concentrations in diets. Feed efficiency (G:F) was also increased (linear, p<0.01) as NE concentrations in diets were increased. The NE intake per BW gain (kcal NE/kg of BWG) was increased (linear, p<0.01) with increasing NE concentrations in diets that were predicted from both French and Dutch CVB NE systems. Linear regression indicated that predictability of daily NE intake from the BW of pigs was very low for both French ($R^2$, 0.366) and Dutch CVB ($R^2$, 0.374) NE systems. In conclusion, increasing NE concentrations in diets increase BW, ADG, G:F, and NE intake per BW gain of early finishing gilts. The BW of early finishing gilts is not a good sole variable for the prediction of daily NE intake.

Effect of Resveratrol on Coxsackie Virus B3m-induced Myocarditis in Mice

  • Dong Hao-Han;He-Li Ren
    • Proceedings of the Korean Society of Food Science and Nutrition Conference
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    • 2004.11a
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    • pp.116-121
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    • 2004
  • To observe the intervening effect of resveratrol on coxsackie virus B3m-induced myocarditis in Balb/c mice and explore the mechanism of intervening effect. Using an animal model of viral myocarditis induced by coxsackie virus B3m (CVB3m), with Ribavirin and Astragalan as comparison, to examine the changes of general condition, mortality, the weights of heart, liver and spleen, serum MDA and NO levels, and cardiac histology in Balb/c mice. By comparison with Ribavirin and Astragalan, it was found that in the mice model of viral myocarditis induced by coxsackie virus B3m resveratrol significantly improved the changes of general condition, mortality, the weights of heart, liver and spleen, serum MDA and NO levels, and cardiac histology. It suggested that resveratrol may have some chemopreventive and chemotherapeutic effects in the treatment of viral myocarditis.

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