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1.
Acta Virol ; 61(3): 341-346, 2017.
Article in English | MEDLINE | ID: mdl-28854799

ABSTRACT

Activity of three photosensitizing phthalocyanine derivatives was tested for photodynamic inactivation towards two coated and two non-enveloped viruses - bovine viral diarrhea virus (BVDV), influenza virus A(H3N2), poliovirus type 1 (PV-1) and human adenovirus type 5 (HAdV5). In the case of coated viruses, a combination of virucidal and irradiation effects was registered by octa-methylpyridyloxy-substituted Ga phthalocyanine (Ga8) toward BVDV, whereas tetra-methylpyridyloxy-substituted Ga phthalocyanine (Ga4) revealed a marked photoinactivation only. No such effect was observed towards influenza A virus. In contrast, the photoinactivating potential of Ga4 and Ga8 marked very high values on naked viruses, especially on HAdV5, at which both the virucidal as well as the irradiation effects became combined.


Subject(s)
Adenoviruses, Human/drug effects , Diarrhea Viruses, Bovine Viral/drug effects , Indoles/pharmacology , Influenza A Virus, H3N2 Subtype/drug effects , Photosensitizing Agents/pharmacology , Poliovirus/drug effects , Animals , Cattle , Cell Line , Dogs , Humans , Isoindoles , Madin Darby Canine Kidney Cells
2.
Drug Res (Stuttg) ; 66(12): 639-643, 2016 Dec.
Article in English | MEDLINE | ID: mdl-27552486

ABSTRACT

Anti-enteroviral chemotherapeutics for clinical use are not registered so far, mainly due to the rapid development of drug-resistance. One of the possible approaches to overcome this problem is the use of combined chemotherapy. However, its application consisting of simultaneously given drugs, is not efficacious because of the development of multiple resistance. Here we present a novel approach for combined application of anti-enteroviral compounds, consisting of a consecutive alternating administration (CAA) course. CAA was tested on 2 in vivo models of Coxsackievirus B3 infection in newborn mice at inoculation dose of 20 MLD50 (50% mouse lethal dose): neurotropic (Nancy strain) and cardiotropic (Woodruff strain) infections. Compounds partnering in a triple combination were selected as enterovirus (EV) replication inhibitors with different mode of action - disoxaril (a VP1 blocker), guanidine.HCl (targeting 2C protein) and oxoglaucine (attacking 3A coding region). The application of this combination by CAA course resulted in around 40 and 60% survival rate in mice infected with Nancy and Woodruff virus, respectively, accompanied by a marked lengthening of the mean survival time (MST). The results obtained are proofs for the prospect of the treatment course by a triple combination through the CAA scheme as an approach interfering the occurrence of drug resistance at EV infections.


Subject(s)
Antiviral Agents/administration & dosage , Coxsackievirus Infections/drug therapy , Enterovirus B, Human/drug effects , Animals , Animals, Newborn , Apomorphine/administration & dosage , Apomorphine/analogs & derivatives , Drug Therapy, Combination/methods , Guanidine/administration & dosage , Isoxazoles/administration & dosage , Mice , Mice, Inbred ICR
3.
Antiviral Res ; 110: 104-14, 2014 Oct.
Article in English | MEDLINE | ID: mdl-25111906

ABSTRACT

The plant-derived polyphenolic compounds castalagin, vescalagin and grandinin (C-glucosidic ellagitannins containing nonahydroxyterphenoyl) manifested a strong inhibitory effect on the replication of acyclovir-resistant strains of herpes simplex viruses (HSV) type 1 and 2 in MDBK cells in focus forming units (i.e., microscopically registered microplaques) reduction assay and in two variants of cytopathic effect inhibition test. The effect on the acyclovir (ACV)-resistant herpes simplex virus type 1 (HSV-1) strain was markedly higher compared to that on the ACV-resistant herpes simplex virus type 2 (HSV-2). The three compounds showed comparable levels of antiviral activity against ACV-resistant HSV strains, in contrast with previous results where castalagin exerted the highest degree of activity against wild type HSV strains (Vilhelmova et al., 2011). Combinations of ellagitannins and ACV were tested on the ACV-resistant strains of both HSV-1 and 2 and produced synergistic effects that were revealed by applying the three-dimensional approach of Prichard and Shipman (1990). The ellagitannin(s)-ACV combination applied against ACV-resistant HSV-1 produced a much stronger synergistic effect compared to the effect observed against ACV-resistant HSV-2. The study of the effects of the combination ellagitannin(s)-ACF on intact cell monolayers did not show any toxicity resulting from interaction between the two substances. Altogether, the results obtained in this study demonstrate the highly promising potential of these plant polyphenols as antiherpetic agents.


Subject(s)
Acyclovir/pharmacology , Glycosides/pharmacology , Herpesvirus 1, Human/growth & development , Herpesvirus 2, Human/growth & development , Heterocyclic Compounds, 4 or More Rings/pharmacology , Hydrolyzable Tannins/pharmacology , Animals , Antiviral Agents/pharmacology , Cattle , Cell Line , Drug Resistance, Viral , Drug Synergism , Microbial Sensitivity Tests , Virus Replication/drug effects
4.
Phytomedicine ; 21(11): 1432-8, 2014 Sep 25.
Article in English | MEDLINE | ID: mdl-25022206

ABSTRACT

UNLABELLED: Propolis Extract ACF(®) (PPE) is a purified extract manufactured from propolis collected in a Canadian region rich in poplar trees, and it is the active substance of a topical ointment used against herpes labialis (cold sores or fever blisters). Aim of this study was to analyze the chemical composition of PPE in order to understand the plant origin and possible relations between compounds and antiviral activity, and to characterize the antiviral activity of the extract against herpes simplex virus in vitro. MATERIAL AND METHODS: The analysis of the propolis extract samples was conducted by Gas Chromatography-Mass Spectrometry (GC-MS). The antiviral activity was tested against herpes simplex viruses type 1 and type 2 in MDBK cell cultures by treating the cells with PPE at the time of virus adsorption, and by incubating the virus with the extract before infection (virucidal assay). RESULTS: Results from the GC-MS analyses revealed a dual plant origin of PPE, with components derived from resins of two different species of poplar. The chemical composition appeared standardized between extract samples and was also reproduced in the sample of topical ointment. The antiviral studies showed that PPE had a pronounced virucidal effect against herpes simplex viruses type 1 and type 2, and also interfered with virus adsorption.


Subject(s)
Antiviral Agents/pharmacology , Herpesvirus 1, Human/drug effects , Herpesvirus 2, Human/drug effects , Propolis/pharmacology , Animals , Antiviral Agents/chemistry , Canada , Cattle , Cell Line , Gas Chromatography-Mass Spectrometry , Ointments/chemistry , Populus/chemistry , Propolis/chemistry
5.
Antiviral Res ; 89(2): 174-81, 2011 Feb.
Article in English | MEDLINE | ID: mdl-21134403

ABSTRACT

The effects of combinations of three nonahydroxyterphenoyl-bearing C-glucosidic ellagitannins (castalagin, vescalagin and grandinin) with acyclovir (ACV) on the replication of type-1 and type-2 herpes simplex viruses in MDBK cells were tested by the focus-forming units reduction test. Ellagitannins included in these combinations possess a high individual antiviral activity: selectivity index of castalagin and vescalagin versus HSV-1 was similar to that of ACV, and relatively lower against HSV-2. The three-dimensional analytical approach of Prichard and Shipman was used to evaluate the impact of drug-drug interactions. The combination effects of ellagitannins with acyclovir were markedly synergistic.


Subject(s)
Acyclovir/pharmacology , Antiviral Agents/pharmacology , Herpesvirus 1, Human/drug effects , Herpesvirus 2, Human/drug effects , Hydrolyzable Tannins/pharmacology , Animals , Cattle , Cell Line , Drug Synergism , Microbial Sensitivity Tests/methods , Virus Replication/drug effects
6.
Acta Virol ; 53(1): 57-60, 2009.
Article in English | MEDLINE | ID: mdl-19301953

ABSTRACT

Standard therapies such as surgery and chemotherapy offer only minimal improvement in pancreatic cancer. However, the viruses killing cancer cells and substances like some antibiotics and phytoalexins with anticancer potential may represent a candidate non-conventional mean of cancer treatment in the future. In this study, the effect of infection with oncolytic H-1 parvovirus (H-1PV) combined with antibiotic norfloxacin (NFX) or phytoalexin resveratrol on the survival of cell lines Panc-1 and BxPC3 derived from human pancreatic carcinoma was tested. Whereas H-1PV with NFX exerted a synergistic effect, H-1PV with resveratrol resulted in an additive effect only. All the effects were partial, but they were more pronounced in Panc-1 compared to BxPC3 cells.


Subject(s)
Antineoplastic Agents/pharmacology , H-1 parvovirus/growth & development , Oncolytic Viruses/growth & development , Cell Line, Tumor , Cell Survival/drug effects , Drug Interactions , Humans , Norfloxacin/pharmacology , Resveratrol , Stilbenes/pharmacology
7.
Bioorg Med Chem ; 16(15): 7457-61, 2008 Aug 01.
Article in English | MEDLINE | ID: mdl-18590964

ABSTRACT

The aporphine alkaloid glaucine has been converted into 3-aminomethylglaucine and its free amino group has been linked to cinnamic, ferulic, sinapic, o-, and p-coumaric acids. The antioxidative potential of the synthesized amides was studied against DPPH(*) test. All of the tested compounds demonstrated higher radical scavenging activity than glaucine and 3-aminomethylglaucine, and lower antioxidative effect than the free hydroxycinnamic acids. The newly synthesized compounds were tested in vitro for antiviral activity against viruses belonging to different taxonomic groups.


Subject(s)
Antioxidants/chemistry , Antiviral Agents/chemistry , Aporphines/chemistry , Cinnamates/chemistry , Coumaric Acids/chemistry , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antioxidants/pharmacology , Antiviral Agents/pharmacology , Cell Line , Dogs , Humans , Molecular Structure , Structure-Activity Relationship , Viruses/drug effects
8.
J Hosp Infect ; 62(1): 98-106, 2006 Jan.
Article in English | MEDLINE | ID: mdl-16307826

ABSTRACT

A new formula with reduced ethanol content (55%) in combination with 10% propan-1-ol, 5.9% propan-1.2-diol, 5.7% butan-1.3-diol and 0.7% phosphoric acid exhibited a broad spectrum of virucidal activity. In quantitative suspension tests, with and without protein load, this formulation reduced the infectivity titre of seven enveloped (influenza A and B, herpes simplex 1 and 2, bovine corona, respiratory syncytial, vaccinia, hepatitis B, bovine viral diarrhoea) and four non-enveloped (hepatitis A, polio, rota, feline calici) viruses >10(3)-fold within 30s. In comparative testing, only 95% ethanol showed similar levels of activity. In fingerpad tests, the formulation produced a log10 reduction factor of the titre of poliovirus type 1 (Sabin) of 3.04 in 30s compared with 1.32 by 60% propan-2-ol. Testing against feline calicivirus produced a log10 reduction factor of 2.38 by the test formulation; in contrast, the log10 reduction factors with 70% ethanol and 70% propan-1-ol were 0.68 and 0.70, respectively.


Subject(s)
Antiviral Agents/pharmacology , Disinfectants/pharmacology , Ethanol/analysis , Hand Disinfection/methods , Viruses/drug effects , 1-Propanol/analysis , Adult , Animals , Antiviral Agents/chemistry , Butanols/analysis , Calicivirus, Feline/drug effects , Cats , Cattle , Cell Line , Disinfectants/chemistry , Drug Synergism , Female , Fingers/virology , Humans , Male , Phosphoric Acids/analysis , Poliovirus/drug effects , Propylene Glycol/analysis
9.
Methods Find Exp Clin Pharmacol ; 25(7): 521-4, 2003 Sep.
Article in English | MEDLINE | ID: mdl-14571281

ABSTRACT

The present study provides direct experimental proof that the combination of influenza virus infection A/Aichi/2/68 (H3N3) with different models of oxidative stress, such as immobilization, cold and cold-restraint, is associated with graduated oxidative disturbances in the stomach of mice, despite the absence of virus replication and inflammation in this tissue. It was found that experimental influenza virus infection is accompanied with significant changes in gastric mucosal integrity, as well as an increase in the products of lipid peroxidation in the stomachs of mice. Preliminary exposure of mice to immobilization stress and subsequent inoculation of influenza virus did not significantly influence gastric ulceration or lipid peroxidation compared with infected mice. Cold stress resulted in a significant decrease in the index of stomach ulceration and did not influence the fluorescent products of lipid peroxidation and MDA compared with infected animals. The simultaneous application of cold-restraint stress and influenza virus infection provoked synergism in the activity of all factors on the parameters under investigation. Ulceration increased approximately two-fold, as did the amount of fluorescent products of lipid peroxidation and MDA, compared with influenza virus-infected and non-stressed animals.


Subject(s)
Gastric Mucosa/metabolism , Gastric Mucosa/pathology , Influenza A virus , Lipid Peroxidation , Orthomyxoviridae Infections/complications , Stomach Ulcer/metabolism , Animals , Cold Temperature , Immobilization , Male , Mice , Mice, Inbred ICR , Orthomyxoviridae Infections/metabolism , Orthomyxoviridae Infections/virology , Oxidative Stress , Restraint, Physical , Stomach Ulcer/etiology , Stomach Ulcer/pathology , Stress, Psychological/complications
10.
Methods Find Exp Clin Pharmacol ; 25(4): 259-64, 2003 May.
Article in English | MEDLINE | ID: mdl-12808470

ABSTRACT

Successful antioxidant treatment of the so-called "free radical diseases" has been reported in the literature. In this study we examined the preventive effect of vitamin E and vitamin C, alone and in combination, on the damage caused by influenza virus infection (IVI). Male mice (ICR), infected with influenza virus A/2/68/(H3N2) (1.5 of LD(50)), were administered single once-daily doses of vitamin E (60 mg/kg b.w.) and vitamin C (80 mg/kg b.w.) intraperitoneally (3 days before virus inoculation). On the 5th and 7th day, respectively, after virus inoculation, animals were decapitated. Monooxygenase enzyme activity (ethylmorphine N-demethylase, amidopyrin N-demethylase, analgin N-demethylase, aniline hydroxylase, cytochrome P-450 content and NADPH-cytochrome C reductase [CCR]) was determined in liver 9000 x g supernatant. Primary and secondary products of lipid peroxidation (LPO; conjugated dienes [CD] and TBA-reactive substances) were measured in blood plasma, lung and liver 9000 x g supernatant. Vitamin E effectively restored LPO-levels increased by IVI. The effect of vitamin C was similar, but slighter. The combination (vitamin E + C) had greater effect on LPO levels than their separate administration. P-450-dependent monooxygenase activity was significantly restored and more pronounced cytochrome P-450 content and NADPH-CCR activity was noted. The preventive effect of vitamin E was stronger than the effect of vitamin C, but the combination (vitamin E + C) had the strongest effect. The superior protective effect of the combination is probably due to vitamin C's repairing effect on vitamin E's tocopheroxyl radical.


Subject(s)
Antioxidants/therapeutic use , Ascorbic Acid/therapeutic use , Orthomyxoviridae Infections/prevention & control , Vitamin E/therapeutic use , Animals , Cytochrome P-450 Enzyme System/metabolism , Drug Therapy, Combination , Influenza A virus , Injections, Intraperitoneal , Lipid Peroxidation/drug effects , Liver/enzymology , Liver/metabolism , Lung/metabolism , Male , Mice , Mice, Inbred ICR , Mixed Function Oxygenases/metabolism , Orthomyxoviridae Infections/enzymology , Orthomyxoviridae Infections/metabolism , Thiobarbituric Acid Reactive Substances/metabolism
12.
Z Naturforsch C J Biosci ; 55(9-10): 824-9, 2000.
Article in English | MEDLINE | ID: mdl-11098838

ABSTRACT

Influenza virus infection is associated with development of oxidative stress in lung and blood plasma, viz. increase of primary and secondary lipid peroxidation products. It was established that rimantadine treatment led to a decrease of the products of lipid peroxidation in tissues of mice experimentally infected with influenza virus A/Aichi/2/68 (H3N2). The effect is strongest in blood plasma (a decrease of about 50%) and weaker in the lung (about 20%). To elucidate the mechanism of this action of rimantadine, experiments were carried out with some model systems. The capability of rimantadine to scavenge superoxide radicals (scavenging properties) was studied in a system of xanthine-xanthine oxidase to generate superoxide. The amount of superoxide was measured spectrophotometrically by the NBT-test and chemiluminesce. Rimantadine does not show scavenging properties and its antioxidant effect observed in vivo, is not a result of its direct action on the processes of lipid peroxidation and/or interaction with antioxidant enzymes. The antioxidant properties of rimantadine were investigated by measurement of induced lipid peroxidation in a Fe2+ and (Fe2+ - EDTA) system with an egg liposomal suspension. Our findings with model systems do not prove an antioxidant or prooxidant effect of the drug on the processes of lipid peroxidation. Apparently, the observed antioxidant effect of rimantadine in vivo is not connected directly with free radical processes in the organism.


Subject(s)
Antioxidants/pharmacology , Lipid Peroxidation/drug effects , Lung/physiology , Orthomyxoviridae Infections/physiopathology , Rimantadine/pharmacology , Animals , Free Radical Scavengers/pharmacology , Influenza A virus , Lung/drug effects , Lung/physiopathology , Male , Mice , Mice, Inbred ICR , Orthomyxoviridae Infections/blood , Rats , Rats, Wistar , Superoxides/metabolism , Thiobarbituric Acid Reactive Substances/analysis , Xanthine , Xanthine Oxidase
13.
Acta Virol ; 44(2): 73-8, 2000 Apr.
Article in English | MEDLINE | ID: mdl-10989697

ABSTRACT

Effects of enviroxime and disoxaril, inhibitors of replication of some picornaviruses with known mechanisms of action, alone or in combination, on replication of coxsackievirus B1 (CVB1) in FL cells and on experimental CVB1 infection in newborn mice were tested. The combination of enviroxime and disoxaril resulted in vitro in a synergistic interaction. Both compounds were administered in vivo, alone or in combination, daily by subcutaneous (s.c.) route since the day of virus inoculation till the 5th day post inoculation (p.i.). Our findings about the in vivo antiviral effects of the individual compounds correlated with those of other authors, i.e. disoxaril significantly reduced the virus-induced death (the minimum 50% effective dose (ED50) was 12.5 mg/kg; P = 0.0037), while enviroxime was not effective even when applied at a dose as high as 100 mg/kg (P = 0.264). However, when both the substances were combined, the same protective effect was achieved with concentrations of disoxaril two to four times lower than those of the drug administered alone. In this way a higher selectivity ratio was achieved. Namely, the combination of 50 mg/kg enviroxime and 3.125-6.25 mg/kg disoxaril was synergistic. Along with reduction in mortality a marked delay in the course of the disease was observed.


Subject(s)
Antiviral Agents/pharmacology , Benzimidazoles/pharmacology , Coxsackievirus Infections/prevention & control , Enterovirus B, Human/drug effects , Isoxazoles/pharmacology , Animals , Cell Line , Drug Synergism , Humans , Mice , Mice, Inbred ICR , Oximes , Sulfonamides , Virus Replication/drug effects
14.
Z Naturforsch C J Biosci ; 55(3-4): 292-4, 2000.
Article in English | MEDLINE | ID: mdl-10817222

ABSTRACT

1-(4-Morpholinomethyl)-tetrahydro-2(1H)-pyrimidinone (mopyridone) exhibited a marked activity against rubella virus (Judith and RA27/3 strains), a MIC50 value of 0.9 microM and selectivity ratio of 557.7 been found in the case of Judith strain. These data, in addition to the previous ones about its anti-alphavirus effects suggest the compound to be considered as a broad spectrum inhibitor of togavirus replication.


Subject(s)
Antiviral Agents/pharmacology , Pyrimidinones/pharmacology , Rubella virus/drug effects , Virus Replication/drug effects , Animals , Cell Line , Cricetinae
15.
Z Naturforsch C J Biosci ; 54(1-2): 75-83, 1999.
Article in English | MEDLINE | ID: mdl-10097408

ABSTRACT

New 3'-, 5'-, 5-bromo-2'-deoxyuridine (3a-g) and 3'-, 5'-thymidine (4a-i) analogues with amino acid and peptide residues were synthesized and evaluated for antiviral activity. The influence of long peptide chains, essential amino acids and the effect of this structural modification on the antiviral activity has been also reported. Three 5-bromo-2'-deoxyuridine derivatives containing glycyl-, glycyl-glycyl- and glycyl-glycyl-glycyl- residues (3a, 3b, 3c) showed a strong activity against the herpes virus PsRV and a moderate one vs. HSV-1. The corresponding thymidine analogues were considerably less effective, and only compounds 4d and 4h showed a borderline effect against PsRV.


Subject(s)
Anti-HIV Agents/chemical synthesis , Antiviral Agents/chemical synthesis , Bromodeoxyuridine/analogs & derivatives , Bromodeoxyuridine/chemical synthesis , Thymidine/analogs & derivatives , Thymidine/chemical synthesis , Amino Acids , Animals , Anti-HIV Agents/chemistry , Anti-HIV Agents/pharmacology , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Bromodeoxyuridine/chemistry , Bromodeoxyuridine/pharmacology , Cells, Cultured , Chick Embryo , Chickens , Drug Design , Fibroblasts/cytology , Fibroblasts/virology , HIV/drug effects , Herpesvirus 1, Human/drug effects , Herpesvirus 1, Suid/drug effects , Humans , Influenza A virus/drug effects , Microbial Sensitivity Tests , Peptides , Structure-Activity Relationship , Thymidine/chemistry , Thymidine/pharmacology
16.
Acta Virol ; 43(5): 303-11, 1999 Oct.
Article in English | MEDLINE | ID: mdl-10757231

ABSTRACT

To assess the possible interactions among picornavirus replication inhibitors, inhibitory effects of dual combinations of enviroxime, disoxaril, arildone, S-7, guanidine, PTU-23, and HBB on poliovirus type 1 (Mahoney) replication in FL cells were tested. Beforehand, the 50% inhibitory concentration (IC50) in the plaque inhibition test was been determined for each individual compound, i.e. enviroxime-0.2 micromol/l, disoxaril-0.3 micromol/l, arildone-2.7 micromol/l, (S-7)-100 micromol/l, guanidine-200 micromol/l, (PTU-23)-200 micromol/l, and HBB-300 micromol/l. Each of the dual combinations, in which enviroxime or HBB was one of the partners, showed synergistic or additive effects. Combining disoxaril with enviroxime, HBB or PTU-23 resulted in synergism, while combining it with guanidine, S-7 or arildone led to antagonism. Arildone showed additive or synergistic effects when combined with enviroxime, HBB and PTU-23, and antagonistic ones when combined with disoxaril, S-7 or guanidine. All dual combinations of PTU-23 were synergistic with the exception of the pair of PTU-23 + guanidine that was antagonistic. Guanidine had additive to synergistic interactions with HBB or enviroxime but antagonistic ones with disoxaril, arildone and PTU-23. Guanidine or PTU-23 when combined with S-7 showed an unusual effect - synergistic one with an antagonistic zone. The combinations of S-7 with enviroxime or HBB were synergistic but those with disoxaril or arildone were antagonistic. Research on interactions of picornavirus replication inhibitors could possibly contribute to the development of efficient chemotherapy of infectious diseases caused by picornaviruses as well as to the better understanding of the mode of action of those inhibitors.


Subject(s)
Antiviral Agents/pharmacology , Poliovirus/drug effects , Virus Replication/drug effects , Benzimidazoles/pharmacology , Cell Line , Drug Combinations , Drug Interactions , Drug Synergism , Guanidine/pharmacology , Humans , Isoxazoles/pharmacology , Ketones/pharmacology , Oximes , Phenylthiourea/analogs & derivatives , Phenylthiourea/pharmacology , Poliovirus/physiology , Pyrimidines/pharmacology , Sulfonamides
17.
Acta Virol ; 43(4): 263-5, 1999 Aug.
Article in English | MEDLINE | ID: mdl-10749374

ABSTRACT

When combined, enviroxime and disoxaril, two selective picornavirus inhibitors, exert a marked synergistic inhibitory effect on poliovirus type 1 replication in FL cells. The cytotoxicity of the compounds applied individually and in combination to the same cells was examined. The quantitative assay of the cytotoxic effect was made by determination of the growth curve of uninfected FL cells in the presence of increasing concentrations of the compounds applied alone and in combination. The obtained results indicate lack of a synergic cytotoxic effect of the combination of enviroxime and disoxaril. The previously established synergistic antiviral effect, and the lack of cross-resistance and synergic cytotoxic effect classify the combination of enviroxime and disoxaril as a very promising chemotherapeutic.


Subject(s)
Antiviral Agents/pharmacology , Benzimidazoles/pharmacology , Isoxazoles/pharmacology , Poliovirus/drug effects , Cells, Cultured , Drug Synergism , Humans , Oximes , Poliovirus/physiology , Sulfonamides , Virus Replication/drug effects
18.
Z Naturforsch C J Biosci ; 53(9-10): 883-7, 1998.
Article in English | MEDLINE | ID: mdl-9825543

ABSTRACT

Cholesteryl 3",4"-dimethoxycinnamate (7) and a new synthesized o-coumaroyl ester of 3 beta-(2'-hydroxyethoxy)-cholest-5-en (13) exhibited a marked activity against poliovirus type 1 (Mahoney). Compound 7 showed an approximately 20-fold greater selectivity in its antiviral activity than compound 13. These compounds were selected from thirteen steryl esters of cinnamic acid derivatives through an in vitro antiviral screening against viruses belonging to taxonomic groups with causative agents of important human infectious diseases to which chemotherapy is indicated, i.e. Picornaviridae, Orthomyxoviridae, Paramyxoviridae and Herpesviridae.


Subject(s)
Antiviral Agents/chemical synthesis , Cholesterol Esters/chemical synthesis , Cinnamates/chemical synthesis , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Cholesterol Esters/chemistry , Cholesterol Esters/pharmacology , Cinnamates/chemistry , Cinnamates/pharmacology , Herpesviridae/drug effects , Humans , Microbial Sensitivity Tests , Molecular Structure , Orthomyxoviridae/drug effects , Paramyxoviridae/drug effects , Picornaviridae/drug effects , Poliovirus/drug effects , Structure-Activity Relationship , Virus Diseases
19.
Z Naturforsch C J Biosci ; 52(7-8): 516-21, 1997.
Article in English | MEDLINE | ID: mdl-9309880

ABSTRACT

Steroid esters of cynnamic acid derivatives have been synthesized by a heterogeneous Wittig reaction under sonochemical conditions from the corresponding triphenylphosphonium bromides and unprotected phenolic aldehyds using K2CO3 as a base. 5 beta-Cholan-3 alpha, 7 alpha, 12 alpha, 24-E-ferulate (11') exhibited a marked inhibitory effect on influenza virus A. The synthetic 3 alpha, 24-E-diferulates of 5 beta-cholan-3 alpha, 24- diol, 5 beta-cholan-3 alpha, 12 alpha, 24-triol and 5 beta-cholan-3 alpha, 7 alpha, 12 alpha, 24-tetrol (8, 9 and 12) showed antitumor activity on leukemia P-388 in mice.


Subject(s)
Antineoplastic Agents/chemistry , Antiviral Agents/chemistry , Cholic Acids/chemistry , Cinnamates/chemistry , Cinnamates/therapeutic use , Leukemia P388/drug therapy , Viruses/drug effects , Animals , Antineoplastic Agents/therapeutic use , Antineoplastic Agents/toxicity , Antiviral Agents/pharmacology , Cell Line , Cinnamates/toxicity , Influenza A virus/drug effects , Male , Mice , Mice, Inbred DBA , Microbial Sensitivity Tests , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular
20.
Z Naturforsch C J Biosci ; 51(7-8): 558-62, 1996.
Article in English | MEDLINE | ID: mdl-8810095

ABSTRACT

Esculetin (6,7-dihydroxycoumarin) and its diacetate exhibited a marked inhibitory effect on Newcastle disease virus replication in cell cultures at concentrations of 36 microM and 62 microM, respectively. These compounds were selected from ten hydroxycoumarin derivatives through an in vitro antiviral screen involving viruses of the picorna-, orthomyxo-, paramyxo-, and herpes virus families.


Subject(s)
Antiviral Agents/isolation & purification , Coumarins/isolation & purification , Trees , Virus Replication/drug effects , Animals , Antiviral Agents/chemistry , Antiviral Agents/pharmacology , Bulgaria , Cell Line , Cell Survival/drug effects , Cells, Cultured , Chick Embryo , Coumarins/chemistry , Coumarins/pharmacology , Herpesvirus 1, Suid/drug effects , Influenza A virus/drug effects , Magnetic Resonance Spectroscopy , Molecular Structure , Newcastle disease virus/drug effects , Newcastle disease virus/physiology , Plant Extracts , Plant Stems , Poliovirus/drug effects , Spectrophotometry, Infrared
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