Sensitivity of Trichomonas vaginalis to metronidazole, tinidazole, and nifuratel in vitro. (1/89)Prompted by the sensitivity of trichomonads to metronidazole and nifuratel in clinical practice, a study was conducted in 1971-1972 of 63 consecutive strains of Trichomonas vaginalis isolated from women with clinically refractory vaginal discharge. Their susceptibility to metronidazole, tinidazole, and nifuratel was tested, using a serial tube dilution technique. The minimum concentrations which in 48 hrs caused immobilization and lysis of trichomonads cultured in Diamond's medium was assessed. No differences in drug potency could be determined. The median trichomonistatic and trichomonicidal concentrations were 0-1 and 0-6 mug/ml. respectively when using an inoculum of 10,000 organisms per ml. An inoculum of 100,000 per ml. resulted in inhibitory concentrations of 1-0 and killing concentrations of 3-3 mug./ml. These levels are readily attained in blood and vaginal tissue after oral ingestion of the two imidazole derivatives. Thus, metronidazole has maintained its efficacy since it was first introduced more than a decade ago. The few therapeutic failures with metronidazole and tinidazole are considered to have been caused by pharmacokinetic deficiencies in the patients, or by re-infection. (+info)
Mutagenicity of nitrofurans, nitrothiophenes, nitropyrroles, nitroimidazole, aminothiophenes, and aminothiazoles in Salmonella typhimurium. (2/89)Thirty-two heterocyclic compounds, including 24 nitroheterocycles, 7 aminoheterocycles and derivatives, and 1 thiophene lacking a nitro group, were tested for mutagenic activity in Salmonella typhimurium TA 98 and TA 100. All the nitroheterocycles (11 new), including nitrofurans, nitrothiophenes, nitropyrroles, and 1 nitroimidazole, were mutagenic in TA 100; 13 were also mutagenic in TA 98. 5-Nitro-2-furoic acid, a noncarcinogen, was mutagenic in TA 100. Seven carcinogenic nitroheterocycles were mutagenic in both strains. Seven aminoheterocycles (4 new), aminothiophenes and aminothiazole derivatives, and 1 thiophene without a nitro group were not mutagenic. Both TA 98 and TA 100 were uvrB and lacked the ability of excision repair of DNA. Among the 24 mutagenic nitroheterocycles, only 13 compounds exhibited bacterial killing effects, suggesting that more than 1 mechanism may be involved in the interaction of nitroheterocycles with bacterial DNA. (+info)
Bactericidal activity of nitrofurans against growing and dormant Mycobacterium bovis BCG. (3/89)Depletion of oxygen triggers the shift-down of Mycobacterium bovis BCG to a state of dormancy. Bacilli in their dormant state are resistant to standard anti-mycobacterials. The nitroimidazole metronidazole was the first compound identified to show bactericidal activity against dormant tubercle bacilli. In contrast to metronidazole's selective toxicity for dormant bacilli, we report here that the nitrofurans nitrofurantoin, furaltadone and nitrofurazone showed bactericidal activity against dormant and growing bacteria. Importantly, the bactericidal effect of nitrofurans on dormant bacilli was 35- to 250-fold higher compared with metronidazole. (+info)
Statistical analysis on toxicity of a nitrofuran derivative, 2-(2-furyl)-3-(5-nitro-2-furyl)acrylamide. (4/89)A food additive, furylfuramide or AF-2, which had been used in Japan since 1965 and structurally is composed of 5-nitro-2-furyl radical and acrylamide, was re-examined mainly on chronic toxicity by statistically reviewing published data. The conclusions are as follows: 1) The maximum safety dosage which shows no demonstrable change in rats must be corrected at least to 1/170 of the value which has been accepted by the Ministry of Health and Welfare of Japan (MHW). 2) The minimum effective dose to bacterial growth in food can not be lowered below the standard usage level with MHW determined, because the inactivation factor in food, decreasing effectivity to 1/20, must be taken into consideration. 3) In view of these two facts, AF-2 is found to be unacceptable as a food additive. 4) Great importance must also be attached to the possibility of mutagenicity and carcinogenicity of AF-2, pointed out recently. Both neurotoxicity and dermatitis observed in tofu (soybean curd) makers are also memtioned. (+info)
Synthesis of styrenes through the biocatalytic decarboxylation of trans-cinnamic acids by plant cell cultures. (5/89)A novel method for producing styrenes from trans-cinnamic acids was developed. When trans-cinnamic acid was incubated with plant cell cultures at room temperature, styrene was obtained. 4-Hydroxy-3-methoxystyrene (2a), 3-nitrostyrene (2f) and furan (2g) were synthesized quantitatively. (+info)
Review article: alternative antibacterial agents for Helicobacter pylori eradication. (6/89)Standard eradication therapies against Helicobacter pylori appear to be effective in most cases, but in clinical practice a failure rate higher than the 5-10% reported in clinical trials is often observed. Among the various reasons responsible for therapeutic failure, antibiotic resistance is becoming a major issue in some countries. A range of different antibacterial agents is currently under investigation: several macrolides, new fluoroquinolones, furazolidone and rifabutin. Although not formally tested in refractory cases, azithromycin, spiromycin, levofloxacin and furazolidone represent the most promising antibacterial agents for possible inclusion in eradication regimens. Rifabutin has been evaluated in H. pylori infections resistant to standard therapies. Although very effective, the drug is expensive and its use should be restricted to the most difficult cases to avoid the development of rifabutin resistance in Mycobacterium spp. (+info)
Damage to mammalian cell DNA by nitrofurans. (7/89)Maximum rates of nitrofuran reduction by intact mammalian cells and homogenates of mouse liver are obtained under anaerobic conditions, although significant reduction does occur with gas mixtures containing 5% oxygen and less. Single-strand breaks in DNA, measured as a decrease in the sedimentation constant on alkaline sucrose gradients, are produced in mammalian L929, KB, AND BHK-21 cells in vitro and Ehrlich ascites cells in vivo by several nitrofuran derivatives under hypoxic conditons. (+info)
Enzymes associated with reductive activation and action of nitazoxanide, nitrofurans, and metronidazole in Helicobacter pylori. (8/89)Nitazoxanide (NTZ) is a redox-active nitrothiazolyl-salicylamide prodrug that kills Helicobacter pylori and also many anaerobic bacterial, protozoan, and helminthic species. Here we describe development and use of a spectrophotometric assay, based on nitroreduction of NTZ at 412 nm, to identify H. pylori enzymes responsible for its activation and mode of action. Three enzymes that reduce NTZ were identified: two related NADPH nitroreductases, which also mediate susceptibility to metronidazole (MTZ) (RdxA and FrxA), and pyruvate oxidoreductase (POR). Recombinant His-tagged RdxA, FrxA, and POR, overexpressed in nitroreductase-deficient Escherichia coli, each rapidly reduced NTZ, whereas only FrxA and to a lesser extent POR reduced nitrofuran substrates (furazolidone, nitrofurantoin, and nitrofurazone). POR exhibited no MTZ reductase activity either in extracts of H. pylori or following overexpression in E. coli; RdxA exhibited no nitrofuran reductase activity, and FrxA exhibited no MTZ reductase activity. Analysis of mutation to rifampin resistance (Rif(r)) indicated that NTZ was not mutagenic and that nitrofurans were only weakly mutagenic. Alkaline gel DNA electrophoresis indicated that none of these prodrugs caused DNA breakage. In contrast, MTZ caused DNA damage and was strongly mutagenic. We conclude that POR, an essential enzyme, is responsible for most or all of the bactericidal effects of NTZ against H. pylori. While loss-of-function mutations in rdxA and frxA produce a Mtz(r) phenotype, they do not contribute much to the innate susceptibility of H. pylori to NTZ or nitrofurans. (+info)
Nitrofurans are a group of synthetic antibacterial agents that have been widely used in the medical field for their antimicrobial properties. The primary use of nitrofurans is to treat urinary tract infections (UTIs) caused by susceptible strains of bacteria. Nitrofurantoin is the most commonly prescribed nitrofuran and is available under various brand names, such as Macrobid and Furadantin.
Nitrofurans have a unique mechanism of action that distinguishes them from other antibiotics. They require an aerobic environment with an adequate concentration of oxygen to be effective. Once inside the body, nitrofurans are rapidly metabolized and concentrated in urine, where they exhibit bactericidal activity against various gram-positive and gram-negative bacteria, including Escherichia coli, Staphylococcus saprophyticus, and Enterococci.
The antibacterial action of nitrofurans is attributed to their ability to inhibit essential bacterial enzymes involved in nucleic acid synthesis, energy production, and cell wall biosynthesis. This multifaceted mechanism of action makes it difficult for bacteria to develop resistance against nitrofurans.
Common side effects associated with nitrofurantoin include gastrointestinal symptoms such as nausea, vomiting, and diarrhea. Less frequently, patients may experience headaches, dizziness, or skin rashes. In rare cases, nitrofurantoin can cause pulmonary reactions, hepatotoxicity, or peripheral neuropathy.
Due to the potential for adverse effects and the risk of developing drug-resistant bacteria, nitrofurans should only be prescribed when there is a strong clinical indication and susceptibility testing has been performed. Patients with impaired renal function, pregnant women in their third trimester, or those with a history of liver or lung disease may not be suitable candidates for nitrofuran therapy due to the increased risk of adverse reactions.
Tritrichomonas is a genus of protozoan parasites that are commonly found in the digestive tracts of various animals, including humans. The most well-known species is Tritrichomonas foetus, which is a significant pathogen in cattle, causing a venereal disease known as bovine trichomoniasis.
In humans, Tritrichomonas vaginalis is the species that is associated with infection, specifically in the urogenital tract of women. It can cause a condition called trichomoniasis, which is typically characterized by vaginitis (inflammation of the vagina) and discharge. However, it's important to note that many people infected with T. vaginalis are asymptomatic, and the infection can sometimes lead to more severe complications such as preterm labor or premature rupture of membranes during pregnancy.
Tritrichomonas species are characterized by having three flagella at the anterior end and one at the posterior end, which they use for movement. They are usually transmitted through direct contact with infected individuals or contaminated fomites. Proper diagnosis and treatment are essential to prevent the spread of infection and potential complications.
Nitroreductases are a group of enzymes that can reduce nitro groups (-NO2) to nitroso groups (-NHOH) or amino groups (-NH2) in various organic compounds. These enzymes are widely distributed in nature and found in many different types of organisms, including bacteria, fungi, plants, and animals.
In medicine, nitroreductases have been studied for their potential role in the activation of certain drugs or prodrugs. For example, some anticancer agents such as CB1954 (also known as 5-(aziridin-1-yl)-2,4-dinitrobenzamide) are relatively inert until they are reduced by nitroreductases to more reactive metabolites that can interact with DNA and other cellular components. This property has been exploited in the development of targeted cancer therapies that selectively deliver prodrugs to tumor cells, where they can be activated by endogenous nitroreductases to kill the cancer cells while minimizing toxicity to normal tissues.
Nitroreductases have also been implicated in the development of bacterial resistance to certain antibiotics, such as metronidazole and nitrofurantoin. These drugs are activated by nitroreductases in bacteria, but overexpression or mutation of the enzyme can lead to reduced drug activation and increased resistance.
Nitro compounds, also known as nitro derivatives or nitro aromatics, are organic compounds that contain the nitro group (-NO2) bonded to an aromatic hydrocarbon ring. They are named as such because they contain a nitrogen atom in a -3 oxidation state and are typically prepared by the nitration of aromatic compounds using nitric acid or a mixture of nitric and sulfuric acids.
Nitro compounds have significant importance in organic chemistry due to their versatile reactivity, which allows for various chemical transformations. They can serve as useful intermediates in the synthesis of other chemical products, including dyes, pharmaceuticals, and explosives. However, some nitro compounds can also be hazardous, with potential health effects such as skin and respiratory irritation, and they may pose environmental concerns due to their persistence and potential toxicity.
It is important to handle nitro compounds with care, following appropriate safety guidelines and regulations, to minimize risks associated with their use.
Metronidazole is an antibiotic and antiprotozoal medication. It is primarily used to treat infections caused by anaerobic bacteria and certain parasites. Metronidazole works by interfering with the DNA of these organisms, which inhibits their ability to grow and multiply.
It is available in various forms, including tablets, capsules, creams, and gels, and is often used to treat conditions such as bacterial vaginosis, pelvic inflammatory disease, amebiasis, giardiasis, and pseudomembranous colitis.
Like all antibiotics, metronidazole should be taken only under the direction of a healthcare provider, as misuse can lead to antibiotic resistance and other complications.
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- The present experiments examined the protective effect of the nitrofuran drugs, furazolidone (FZ) and nitrofurazone (NF), on duodenal ulceration induced by cysteamine or indometacin in rats. (elsevierpure.com)
- Furazolidone is a nitrofuran antibacterial agent. (snpedia.com)
- Hancock gave other examples of cases including nitrofurans in prawns, where a sample was deemed non-compliant because of the presence of furazolidone (AOZ). (foodsafetynews.com)
- Furan2 is a good combo medication that consist of two nitrofuran antibiotics (nitrofurazone and furazolidone) plus good old methylene blue. (seahorse.com)
- Nitrofurans are a class of drugs typically used as antibiotics or antimicrobials. (wikipedia.org)
- Certain drugs have been linked to an increased risk in birth defects, (nitrofuran and sulfonamide classes of antibiotics), but many commonly used antibiotics, such as penicillins, erythromycin, and cephalosporins, have not been found to have an increased risk. (popsugar.com)
- Macrobid belongs to a group of drugs called nitrofuran antibiotics. (rxwiki.com)
- The xerogel material can selectively detect Fe3+ and nitrofuran-based antibiotics (i.e. (bvsalud.org)
- Nitrofurantoin is a nitrofuran antimicrobial agent with activity against certain Gram-positive and Gram-negative bacteria. (nih.gov)
- Nitrofurantoin is a bacteriostatic, nitrofuran antibiotic targeting gram-negative and gram-positive bacteria such as Enterococci , Staphylococci , Streptococci, Corynebacterium , and E. Coli . (goldbio.com)
- Since October 2002, all imports of Brazilian turkey and other poultry meat have been tested for nitrofuran antibiotic residues. (parliament.uk)
- For the simultaneous identification and quantification of five nitrofurans metabolites in farmed shrimp and fish, 3-amino-2-oxazolidinone (AOZ), 3-amino-5-morpholinomethyl-2-oxazolidinone (AMOZ), 1-aminohydantoine (AHD), semicarbazide (SEM), and 3,5-dinitrosalicylic acid hydrazide (DNSH), an accurate, precise, and specific method was developed. (bvsalud.org)
- According to the latest results, among the malachite green tainted samples, 4 freshwater grouper samples and the silver carp sample were also positive for nitrofurans residues. (gov.hk)
- Based on the levels of nitrofurans residues found in the affected freshwater fish samples, risk assessment suggested that the risk to health is low upon usual consumption of the fish. (gov.hk)
- Based on the levels of malachite green/nitrofurans residues detected, risk to health is low upon usual consumption of the fish. (gov.hk)
- Since March 2002, all consignments of shrimps and poultry from Thailand had to be tested for the presence of residues since the presence of nitrofurans had been detected in imported products from the country (see IP/02/436). (thepoultrysite.com)
- In the 2000s, a number of meat imports were destroyed after nitrofurans were found, including chicken imported from Portugal, and chicken imported from Thailand and Brazil. (wikipedia.org)
- However, for the type of nitrofurans detected in this survey, there is inadequate evidence that it can cause cancer in humans. (gov.hk)
- The main concern of nitrofurans in food is that a type of nitrofurans may cause cancer in experimental animals. (gov.hk)
- These findings suggest that 5-nitrofuran-isoxazole analogs are promising in the studies of agents for CD treatment. (bvsalud.org)
- The European Union has banned the use of Nitrofurans in food-producing animals. (wikipedia.org)
- The 5-nitrofuran-isoxazole analogs exhibited relevant in vitro antitrypanosomal activity against the amastigote forms of T. cruzi. (bvsalud.org)
Chloramphenicol and nitrofurans4
- Malaysia has banned the use of chloramphenicol and nitrofurans in seafood farm operations. (foodnavigator.com)
- The fact is the two antibiotics Chloramphenicol and Nitrofurans are banned for use in Malaysia since 1985. (consumer.org.my)
- Toxic and carcinogenic Chloramphenicol and Nitrofurans have no acceptable daily intake (ADI) and maximum residue limits (MRLs) established. (consumer.org.my)
- The presence of Chloramphenicol and Nitrofurans in our meat and fish is not new. (consumer.org.my)
- Comparison of antibacterial activity and biocompatibility of non-leaching nitrofuran bone cement loaded with vancomycin, gentamicin, and tigecycline. (bvsalud.org)
- Non- leaching antibacterial nitrofuran bone cement (NFBC) specimens were prepared with low- dose and high- dose antibiotics . (bvsalud.org)
- Nitrofurazone is an antibacterial drug in the nitrofuran group. (xahnb.com)
- A preliminary screening was done using rapid ELISA kits to test for chloramphenicol, malachite green, nitrofurans, and fluoroquinolones. (lsu.edu)
- Due to concerns that the drug can be cancer causing and harmful to human health, the USFDA banned the use of nitrofurans in food producing animals in 1991 while Furaltadone (another type of nitrofuran) was prohibited earlier in 1985. (consumer.org.my)
- Nitrofurazone is a synthetic topical nitrofuran disinfectant that acts to interfere with bacterial sugar metabolic processes and oxidative enzyme systems, resulting in bacterial inhibition or sterilization. (xahnb.com)
- Some Anti-thyroid and Related Substances, Nitrofurans and Industrial Chemicals. (nih.gov)
- A small set of twelve compounds of a nitrofuran carboxamide chemotype was elaborated from a readily available 2,6-diazaspiro[3.4]octane building block, exploring diverse variants of the molecular periphery, including various azole substituents. (nih.gov)
- In the 2000s, a number of meat imports were destroyed after nitrofurans were found, including chicken imported from Portugal, and chicken imported from Thailand and Brazil. (wikipedia.org)
- The end of testing for Nitrofurans and the reduction in the products tested for in the last two years will save the industry a little money and make it easier for U.S. companies to export meat to the EU. (usmef.org)
- Food survey - using FoodBRAND test methods to detect illegal use of nitrofurans in meat in Europe. (konsumentsamverkan.se)
- In 2002, the Health Ministry Parliamentary Secretary revealed that Nitrofuran and Chloramphenicol had been found in chickens tested. (consumer.org.my)
- Nitrofurans are a group of broad spectrum antibiotics important for use in humans. (consumer.org.my)
- Marine Products Export Development Authority ( mpeda ) director J Bojan reveals that the new maximum permissible limits set by these countries for chloramphenicol and nitrofuran are 0.3 parts per billion (ppb) and 1 ppb, respectively. (org.in)
- The participation in this proficiency test was offered to all the National Reference Laboratories (NRLs) of the European Union (EU) in charge of the analysis of nitrofurans, to Official Laboratories of the then 10 Candidate Countries for entry in EU and to some countries exporting food to the EU. (hal.science)
- The speakers in the workshop recommended import of feed and feed ingredients, free from nitrofuran, chloramphenicol etc, from abroad and test those before marketing or use for producing feed. (thepoultrysite.com)
- This is welcome news for the industry, since Nitrofurans are not permitted in the treatment of food animals in the U.S. and the cost of testing was an unnecessary expense. (usmef.org)
- Porphyria: Treatment with nitrofuran derivatives, such as LAMPIT, may precipitate acute attacks of porphyria. (nih.gov)
- The Nitrofuran testing requirement for beef and pork exports to the European Union (EU) has been removed. (usmef.org)