A comparative test of fifteen compounds against all known human rhinovirus serotypes as a basis for a more rational screening program

Andries, Koen; Dewindt, B.; Snoeks, Jos; Willebrords, R.; Stokbroekx, Raymond A.; Lewi, Paul

doi:10.1016/0166-3542(91)90001-8

Cited by 49 publications

(20 citation statements)

References 16 publications

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“…HRV-1B and -14 were selected as representative serotypes for HRV groups A and B, respectively. In fact, a differential susceptibility of HRV serotypes to a panel of antiviral compounds allowed the identification of two groups of HRVs, designated antiviral group A and group B (Andries et al, 1990(Andries et al, , 1991. Antiviral group B contains twice as many serotypes as group A and accounts for five times as many colds (Andries et al, 1990(Andries et al, , 1991.…”

Section: Resultsmentioning

confidence: 99%

“…In fact, a differential susceptibility of HRV serotypes to a panel of antiviral compounds allowed the identification of two groups of HRVs, designated antiviral group A and group B (Andries et al, 1990(Andries et al, , 1991. Antiviral group B contains twice as many serotypes as group A and accounts for five times as many colds (Andries et al, 1990(Andries et al, , 1991. The cytotoxicity of compounds was monitored in preliminary studies by evaluating the effects produced on the morphology, viability and growth of HeLa (Ohio) cells, a human cell line suitable for the replication of the three picornaviruses.…”

Section: Resultsmentioning

confidence: 99%

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Anti-Picornavirus Activity of Synthetic Flavon-3-yl Esters

Conti

Mastromarino

Sgro

et al. 1998

Antivir Chem Chemother

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Members of the family Picornaviridae, which comprise rhinoviruses and enteroviruses, are responsible for several human diseases. It is estimated that over 100 serotypes of human rhinoviruses (HRV) cause approximately half of all cases of the common cold. Also, poliomyelitis still represents a relevant health problem in some countries of the world, despite a dramatic decrease in its incidence as a result of intensive vaccination programmes in developed countries. There therefore exists a need to search for effective chemotherapeutic agents for picornavirus infections.Several classes of flavonoids, isolated from plants utilized in traditional medicine, possess a well recognized anti-picornavirus activity (Van Hoof et al.,1984;Kaul et al., 1985;Tsuchiya et al., 1985). Among polyhydroxylated flavones, quercetin was originally described to reduce the infectivity and the intracellular replication of poliovirus type 1 (PV-1), but not of PV-2 or PV-3. Hesperetin, a flavanone, was able to interfere with PV-1 infection of cell monolayers without affecting virus infectivity (Kaul et al., 1985). 3-Methoxylated flavones, such as chrysosplenol B and C, and axillarin, were found to have potent anti-HRV activity, whereas flavones without a methoxyl group at the 3-position had no anti-rhinovirus activity (Tsuchiya et al., 1985). Beside an effect on HRVs, 4′,5-dihydroxy-3,3′,7-trimethoxyflavone (Ro-09-0179) also exerted an inhibitory activity against coxsackieviruses in tissue cultures (Kaul et al., 1985). The mechanism of action of flavonoids has been attributed to interference with an early stage of viral infection, probably represented by viral RNA synthesis (Castrillo et al., 1986;Gonzales et al., 1990).The study of various synthetic flavones, structurally related to natural flavonoids, confirmed the anti-picornavirus activity of this class of compounds (De Meyer et al., 1991;Desideri et al., 1995). Among the derivatives studied by us, flavanones were generally less effective against picornaviruses than flavones, and 3-hydroxy or 3-methoxyflavones were more active than 3-unsubstituted flavones. The presence of a 3-hydroxy group increased the anti-PV potency, whereas a 3-methoxy group enhanced the effect against HRV-1B ( Desideri et al., 1995). In order to further study the influence on anti-picornavirus activity of the substituent in position 3 of synthetic flavones, we extended our research to esters of chloroflavon-3-ols with natural occurring hydroxybenzoic and hydroxycinnamic acids, i.e. gallic, syringic, caffeic, vanillic and ferulic acids (compounds 2 a-h, 3 a-l). Materials and Methods: VirologyCells HeLa (Ohio) cells were routinely grown at 37°C in 75 cm 2 tissue culture flasks using Eagle's MEM supplemented with 100 µg/ml of streptomycin and 100 U/ml of penicillin G. Eight percent heat-inactivated fetal calf serum (FCS) was added for cell growth (growth medium); the concentration was reduced to 2% for cell maintenance (maintenance medium). The in vitro antiviral activity against picornaviruses (rhinovirus serotype 1B ...

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Anti-Picornavirus Activity of Synthetic Flavon-3-yl Esters

Conti

Mastromarino

Sgro

et al. 1998

Antivir Chem Chemother

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“…An additional structural feature observed in all enteroviruses examined to date is a hydrophobic cavity, at the heart of VP1 beneath the canyon, that contains cellularly derived lipids, known as "pocket factors," which would stabilize the virus during its spread from cell to cell and would always be expelled upon interaction with the receptor. Antiviral compounds have been discovered that bind tightly to the VP1 pocket replacing the pocket factor and stabilizing the capsids to such an extent that uncoating is blocked (1,19,48).…”

Section: Swine Vesicular Disease Virus (Svdv) Is a Member Of Thementioning

confidence: 99%

Structure of Swine Vesicular Disease Virus: Mapping of Changes Occurring during Adaptation of Human Coxsackie B5 Virus To Infect Swine

Verdaguer

Jiménez‐Clavero

Fita

et al. 2003

J Virol

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The structure of swine vesicular disease virus (SVDV) was solved and refined at a 3.0-Å resolution by X-ray crystallography to gain information about the role of sequence changes that occurred as this virus evolved from the parental human pathogen coxsackievirus B5 (CVB5). These amino acid substitutions can be clustered in five distinct regions: (i) the antigenic sites, (ii) the hydrophobic pocket of the VP1 ␤-sandwich, (iii) the putative CAR binding site, (iv) the putative heparan sulfate binding site, and (v) the fivefold axis. The VP1 pocket is occupied by a branched pocket factor, apparently different from that present in the closely related virus CVB3 and in other picornaviruses. This finding may be relevant for the design of new antiviral compounds against this site. Density consistent with the presence of ions was observed on the fivefold and threefold axes. The structure also provided an accurate description of the putative receptor binding sites.

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“…Several capsid-binding inhibitorsmolecules (CIs) are being investigated as promising drug candidates (Andries et al, 1991;Diana, 2003;Makarov et al, 2005;Watson et al, 2003) (Andries et al, 1991;Diana, 2003;Makarov et al, 2005;Watson et al, 2003), the most developed ones being pleconaril and vapendavir (Diana et al, 1995;Feil et al, 2012) (Diana et al, 1995;Feil et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

“…As of today no therapeutics have been approved for the treatment of these infections (De Palma et al, 2008;Rollinger and Schmidtke, 2011). Several capsid-binding molecules (CIs) are being investigated as promising drug candidates (Andries et al, 1991;Diana, 2003;Makarov et al, 2005;Watson et al, 2003), the most developed ones being pleconaril and vapendavir (Diana et al, 1995;Feil et al, 2012).…”

Section: Introductionmentioning

confidence: 99%