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Methods in Molecular Biology (Clifton,... 2006To identify new genes in an organism, a genetic approach can be used to screen for mutations that display a particular phenotype. Genotoxic agents, such as ultraviolet...
To identify new genes in an organism, a genetic approach can be used to screen for mutations that display a particular phenotype. Genotoxic agents, such as ultraviolet (UV) light, ionizing radiation, or chemicals can be used to randomly induce DNA lesions in the genome. Most efficient mutagenesis occurs when a mutagen confers a high frequency of mutations with low lethality, in the range of 10 to 50% survival. These mutations can be in the form of frameshifts, deletions, or rearrangements. To initiate a mutagenesis, a fresh subculture of cells grown into log phase is collected, washed, and resuspended in potassium phosphate buffer. The mutagen is added to the culture for a predetermined time, deactivated, and washed from the cells. The cells are allowed to recover from the treatment by incubating in liquid or on solid medium. Mutants can be isolated by screening individual colonies or by using direct selection of cells from the mutagenized cell population.
Topics: 4-Nitroquinoline-1-oxide; Aminacrine; Ethyl Methanesulfonate; Genes, Fungal; Methylnitronitrosoguanidine; Mutagenesis; Mutagens; Mycology; Nitrogen Mustard Compounds; Quinolones; Saccharomyces cerevisiae; Ultraviolet Rays
PubMed: 16118430
DOI: 10.1385/1-59259-958-3:121 -
Journal of the National Cancer Institute Mar 2000
Topics: Aminacrine; Animals; Antineoplastic Agents; Base Pair Mismatch; Colonic Neoplasms; DNA Damage; DNA Repair; DNA, Neoplasm; Drug Resistance; Frameshift Mutation; Genetic Predisposition to Disease; Humans; Mutagens; Neoplasms; Neoplasms, Experimental; Nitrogen Mustard Compounds
PubMed: 10716953
DOI: 10.1093/jnci/92.6.440 -
Sexually Transmitted Diseases Mar 1997Trichomonas vaginalis is a common vaginal pathogen. Oral metronidazole is the drug of choice for the treatment of trichomoniasis. Oral metronidazole, however, may cause... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Multicenter comparison of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine hydrochloride, and allantoin in the treatment of symptomatic trichomoniasis.
BACKGROUND AND OBJECTIVES
Trichomonas vaginalis is a common vaginal pathogen. Oral metronidazole is the drug of choice for the treatment of trichomoniasis. Oral metronidazole, however, may cause unpleasant side effects and is contraindicated during the first trimester of pregnancy. In vitro studies and preliminary clinical data have suggested that intravaginal clotrimazole may be effective against this pathogen.
GOALS
To compare the efficacy of clotrimazole vaginal tablets, oral metronidazole, and vaginal suppositories containing sulfanilamide, aminacrine, and allantoin (AVC suppositories) in the treatment of women with symptomatic trichomoniasis.
STUDY DESIGN
In a multicenter, open-label trial conducted in 1982 and 1983, 168 symptomatic women with microscopically evident vaginal trichomoniasis were randomized to receive any of 2 g of metronidazole as a single oral dose, two 100-mg clotrimazole vaginal tablets once a day for 7 days, or vaginal suppositories containing 1.05 g of sulfanilamide, 14 mg of aminacrine hydrochloride, and 140 mg of allantoin (AVC suppositories) twice a day for 7 days. Wet mounts and cultures were repated at 1 to 2 and 4 to 6 weeks after completion of treatment.
RESULTS
The number of patients who had positive cultures after treatment were 40/45 (88.9%) in the clotrimazole group, 35/43 (81.4%) in the AVC suppository group, and 9/45 (20%) in the metronidazole group (P < 0.001). All treatments were associated with a reduction in reported symptoms. Oral metrohidazole was more effective in reducing symptoms than either of the topical preparations. Adverse events, mostly mild or moderate in severity, were reported by 7 (14.6%) of 48 patients who had received oral metronidazole and 4 (7.8%) of 51 women who used AVC suppositories. There were no adverse events reported by the 50 women who used clotrimazole vaginal tablets.
CONCLUSIONS
Oral metronidazole was more effective in eradicating T. vaginalis than clotrimazole vaginal tablets or AVC vaginal suppositories. All three regimens reduced symptoms; oral metronidazole was more effective in reducing symptoms than either topical preparation.
Topics: Administration, Intravaginal; Administration, Oral; Adolescent; Adult; Allantoin; Aminacrine; Antitrichomonal Agents; Clotrimazole; Female; Humans; Metronidazole; Middle Aged; Sulfanilamide; Sulfanilamides; Trichomonas Vaginitis
PubMed: 9132982
DOI: 10.1097/00007435-199703000-00006 -
Journal - Association of Official... 1987A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by...
A previously reported visible spectrophotometric method for the analysis of aminacrine hydrochloride in creams, jellies, and suppositories was studied collaboratively by 8 laboratories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbance of the minima at about 389 and 412 nm. Each collaborator received 4 creams (0.2%), 1 jel (0.2%), 1 molded suppository (6 mg/3.198 g), and 2 gelatin-encapsulated suppository samples (12 mg/6.661 g and 14 mg/6.863 g). The cream samples included blind duplicates prepared to contain 0.212% aminacrine hydrochloride, 15% sulfanilamide, and 2% allantoin. Mean recovery for the authentic cream was 104.7% with a coefficient of variation (CV) of 9.22%. The commercial products contained these respective amounts (CVs): creams, 100.0% (2.48%) and 101.5% (2.16%); jel, 118.0% (9.58%); molded suppository, 102.7% (1.88%); and gelatin encapsulated suppositories, 93.1% (1.0%) and 94.3% (1.60%). Standard aminacrine hydrochloride provided for the study was 99.6% pure by nonaqueous titration. Thin layer chromatographic identification of aminacrine hydrochloride was also tested collaboratively. The method was not adopted by AOAC.
Topics: Aminacrine; Aminoacridines; Chromatography, Thin Layer; Drug Stability; Indicators and Reagents; Ointments; Spectrophotometry, Ultraviolet; Suppositories
PubMed: 3610970
DOI: No ID Found -
Journal - Association of Official... Jan 1983A visible spectrophotometric method has been developed for the quantitation of aminacrine hydrochloride in creams, jellies, and suppositories. Aminacrine hydrochloride...
A visible spectrophotometric method has been developed for the quantitation of aminacrine hydrochloride in creams, jellies, and suppositories. Aminacrine hydrochloride was extracted into acidic ethanol and its visible spectrum was recorded. The amount present was calculated by determining the net absorbance between the absorbance maximum at about 402 nm and one-half the sum of the absorbances of the minima at about 389 and 412 nm. Aminacrine and a trace contaminant, 9(10H)-acridone, were independently identified by different thin layer chromatographic systems.
Topics: Aminacrine; Aminoacridines; Chromatography, Thin Layer; Spectrophotometry; Spectrophotometry, Ultraviolet; Suppositories; Vaginal Creams, Foams, and Jellies
PubMed: 6826500
DOI: No ID Found -
Journal - Association of Official... Jan 1983Utilizing the fluorescent property of aminacrine hydrochloride and a filter fluorometer, a fluorometric method for aminacrine hydrochloride in drug combinations was...
Utilizing the fluorescent property of aminacrine hydrochloride and a filter fluorometer, a fluorometric method for aminacrine hydrochloride in drug combinations was developed, collaboratively studied, and adopted as official first action in the 11th edition of Official Methods of Analysis. Identity was confirmed by thin layer chromatography (TLC). Additional analytical work was undertaken with a grating fluorometer to support a change in the method status to official final action. The grating instrument recorded the aminacrine hydrochloride spectrum as opposed to the total fluorescence emission measured by the filter instrument. The spectrum of aminacrine hydrochloride showed that the molecule was exhibiting self-absorption of the emitted radiation even at concentrations of 10(-6)M and that the ratio of the 2 peaks in the emission spectrum varied with concentration. Additional analyses of an authentic cream preparation that also contained sulfanilamide gave an average recovery of 86.0% for aminacrine hydrochloride in 10 replicate portions. Because of these observations, the current Associate Referee's recommendation to delete the fluorometric procedure from the 13th edition of Official Methods of Analysis was adopted. A recommended deletion of the TLC identification test was also adopted.
Topics: Aminacrine; Aminoacridines; Chromatography, Thin Layer; Ethanol; Spectrometry, Fluorescence; Suppositories; Vaginal Creams, Foams, and Jellies
PubMed: 6826501
DOI: No ID Found -
European Journal of Medicinal Chemistry Oct 2023A novel family of 4-aminoacridine derivatives was obtained by linking this heteroaromatic core to different trans-cinnamic acids. The 4-(N-cinnamoylbutyl)aminoacridines...
A novel family of 4-aminoacridine derivatives was obtained by linking this heteroaromatic core to different trans-cinnamic acids. The 4-(N-cinnamoylbutyl)aminoacridines obtained exhibited in vitro activity in the low- or sub-micromolar range against (i) hepatic stages of Plasmodium berghei, (ii) erythrocytic forms of Plasmodium falciparum, and (iii) early and mature gametocytes of Plasmodium falciparum. The most active compound, having a meta-fluorocinnamoyl group linked to the acridine core, was 20- and 120-fold more potent, respectively, against the hepatic and gametocyte stages of Plasmodium infection than the reference drug, primaquine. Moreover, no cytotoxicity towards mammalian and red blood cells at the concentrations tested was observed for any of the compounds under investigation. These novel conjugates represent promising leads for the development of new multi-target antiplasmodials.
Topics: Animals; Aminacrine; Aminoacridines; Antimalarials; Mammals; Plasmodium berghei; Plasmodium falciparum; Primaquine
PubMed: 37390511
DOI: 10.1016/j.ejmech.2023.115575 -
Scientific Data Oct 2022Viruses are genetically and structurally diverse, and outnumber cells by orders of magnitude. They can cause acute and chronic infections, suppress, or exacerbate...
Viruses are genetically and structurally diverse, and outnumber cells by orders of magnitude. They can cause acute and chronic infections, suppress, or exacerbate immunity, or dysregulate survival and growth of cells. To identify chemical agents with pro- or antiviral effects we conducted arrayed high-content image-based multi-cycle infection screens of 1,280 mainly FDA-approved compounds with three human viruses, rhinovirus (RV), influenza A virus (IAV), and herpes simplex virus (HSV) differing in genome organization, composition, presence of an envelope, and tropism. Based on Z'-factors assessing screening quality and Z-scores ranking individual compounds, we identified potent inhibitors and enhancers of infection: the RNA mutagen 5-Azacytidine against RV-A16; the broad-spectrum antimycotic drug Clotrimazole inhibiting IAV-WSN; the chemotherapeutic agent Raltitrexed blocking HSV-1; and Clobetasol enhancing HSV-1. Remarkably, the topical antiseptic compound Aminacrine, which is clinically used against bacterial and fungal agents, inhibited all three viruses. Our data underscore the versatility and potency of image-based, full cycle virus propagation assays in cell-based screenings for antiviral agents.
Topics: Aminacrine; Anti-Infective Agents, Local; Antiviral Agents; Azacitidine; Clobetasol; Clotrimazole; Herpes Simplex; Humans; Influenza A virus; Mutagens; Rhinovirus
PubMed: 36209289
DOI: 10.1038/s41597-022-01733-4 -
Nucleic Acids Research Apr 2023
Topics: Humans; Aminacrine; Peptide Nucleic Acids; Tumor Suppressor Protein p53; Down-Regulation; HeLa Cells; Neoplasms; Proto-Oncogene Proteins c-mdm2
PubMed: 36864743
DOI: 10.1093/nar/gkad166 -
Przeglad Lekarski Sep 1982
Comparative Study Review
Topics: Aminacrine; Antineoplastic Agents; Aspartic Acid; Cisplatin; Etoposide; Humans; Ifosfamide; Interferons; Medroxyprogesterone; Medroxyprogesterone Acetate; Methyltestosterone; Neoplasms; Phosphonoacetic Acid; Razoxane; Tamoxifen; Teniposide; Vinca Alkaloids
PubMed: 6182581
DOI: No ID Found