• Title/Summary/Keyword: Nitrofurantoin

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In Vitro and in Vivo Effects of Nitrofurantoin on Experimental Toxoplasmosis

  • Yeo, Seon-Ju;Jin, ChunMei;Kim, SungYeon;Park, Hyun
    • Parasites, Hosts and Diseases
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    • v.54 no.2
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    • pp.155-161
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    • 2016
  • Toxoplasma gondii is an important opportunistic pathogen that causes toxoplasmosis, which has very few therapeutic treatment options. The most effective therapy is a combination of pyrimethamine and sulfadiazine; however, their utility is limited because of drug toxicity and serious side effects. For these reasons, new drugs with lower toxicity are urgently needed. In this study, the compound, (Z)-1-[(5-nitrofuran-2-yl)methyleneamino]-imidazolidine-2,4-dione (nitrofurantoin), showed anti-T. gondii effects in vitro and in vivo. In HeLa cells, the selectivity of nitrofurantoin was 2.3, which was greater than that of pyrimethamine (0.9). In T. gondii-infected female ICR mice, the inhibition rate of T. gondii growth in the peritoneal cavity was 44.7% compared to the negative control group after 4-day treatment with 100 mg/kg of nitrofurantoin. In addition, hematology indicators showed that T. gondii infection-induced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels, biochemical parameters involved in liver injury, were reduced by nitrofurantoin significantly. Moreover, nitrofurantoin exerted significant effects on the index of antioxidant status, i.e., malondialdehyde (MDA) and glutathione (GSH). The nitrofurantoin-treated group inhibited the T. gondii-induced MDA levels while alleviating the decrease in GSH levels. Thus, nitrofurantoin is a potential anti-T. gondii candidate for clinical application.

Effects of Nitrofurantoin on Lipid Peroxidation and Reactive Oxygen Radical Generation in Porcine Lung Microsome (Nitrofurantion이 폐장 미크로솜 지질과산화와 반응성 산소 라디칼 생성에 미치는 영향)

  • Paick, Jae-Seung;Kim, Si-Whang;Kim, Hae-Won;Chung, Myung-Hee;Kim, Myung-Suk
    • The Korean Journal of Pharmacology
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    • v.21 no.1
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    • pp.34-48
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    • 1985
  • In vitro effects of nitrofurantoin, an antimicrobial agent for acute and chronic urinary tract infection, on the lung microsomal lipid peroxidation and the generation of reactive oxygen radicals were investigated to elucidate the biochemical mechanisms of its in vivopulmonary toxicity. The interaction of nitrofurantoin with porcine lung microsome resulted in significant lipid peroxidation. In addition, nitrofurantoin stimulated the generation of reactive oxygen radicals, $O^{-}_{2}{\cdot},\;H_2O_2$ as well as a highly reactive secondary oxygen species, $OH{\cdot}$. The stimulation of lipid peroxidation was inhibited not only by superoxide dismutase and catalase, but also by hydroxyl radical scavengers, mannitol and thiourea. Neither singlet oxygen $({^1}O_{2})$ was detected during the incubation of microsome with nitrofurantoin, nor lipid peroxidation was inhibited by singlet oxygen scavengers. When incubated anaerobically under the nitrogen atmosphere, the ability of nitrofurantoin to stimulatle lipid peroxidation was abolished. It appears that NADPH-dependent metaboliam of nitrofurantoin in pulmonary microsome under aerobic condition is accompanied by the stimulation of lipid peroxidation through the mediation of reactive oxygen radicals, particularly hydroxyl radical. It is strongly suggested from these results that the stimulation of pulmonary microsomal lipid peroxidation by the reactive oxygen radical may be a in vivo mechanism of pulmonary toxicity caused by nitrofurantoin.

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Protective Effects of Plant Extracts against Isoniazid- and Nitrofurantoin-Induced Cytotoxicity in HepG2 Cells (Isoniazid와 Nitrofurantoin으로 유발되는 간 세포독성에 대한 식물추출물의 보호효과)

  • Byun, Erisa;Jeong, Gil-Saeng;Lee, Dong-Sung;Li, Bin;Yang, Suk-Hyun;Beom, Jin-Seon;Lv, Hui-zi;An, Ren-Bo;Kim, Youn-Chul
    • Korean Journal of Pharmacognosy
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    • v.40 no.2
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    • pp.137-142
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    • 2009
  • Isoniazid was discovered in 1950's and since then it has been widely used as a synthetic bactericidal agent in the treatment of tuberculosis. However, the adverse effect of isoniazid has been reported to show significant hepatotoxicity in approximately 1-2% of patients. Nitrofurantoin {1-(5-nitro-2-furfurylideneamino)-hydantoin} is a synthetic nitrofuran that is commonly used for the treatment and prophylaxis of urinary tract infections, but its use is associated with liver cirrhosis and fatal liver necrosis. Therefore, studies for natural products with protective effect on the isoniazid- and/or nitrofurantoin-induced hepatotoxcity would be valuable as the potential therapeutic use. 107 plants sources were collected at Mt. Baekdu, and extracted with methanol. These extracts had been screened for the protective effects against isoniazid- and/or nitrofurantoin-induced cytotoxicity in HepG2 cells at the both 100 and $300{\mu}g/ml$. Five methanolic extracts, Acanthopanax senticosus, Acer mono, Asparagus schoberioides, Fagopyrum tataricum, Potentilla centigrana, showed significant protective effects against isoniazidinduced hepatotoxicity. Two methanolic extracts, Acer mono and Leonurus artemisia, showed significant protective effects against nitrofurantoin-induced cytotoxicity in HepG2 cells.

Gene Expression Profiling of Human Bronchial Epithelial (BEAS-2B) Cells Treated with Nitrofurantoin, a Pulmonary Toxicant

  • Kim, Youn-Jung;Song, Mee;Ryu, Jae-Chun
    • Molecular & Cellular Toxicology
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    • v.3 no.4
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    • pp.222-230
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    • 2007
  • Some drugs may be limited in their clinical application due to their propensity towards their adverse effects. Toxicogenomic technology represents a useful approach for evaluating the toxic properties of new drug candidates early in the drug discovery process. Nitrofurantoin (NF) is clinical chemotherapeutic agent and antimicrobial and used to treatment of urinary tract infections. However, NF has been shown to result in pulmonary toxic effects. In this research, we revealed the changing expression gene profiles in BEAS-2B, human bronchial epithelial cell line, exposed to NF by using human oligonucleotide chip. Through the clustering analysis of gene expression profiles, we identified 136 up-regulated genes and 379 down-regulated genes changed by more than 2-fold by NF. This study identifies several interesting targets and functions in relation to NF-induced toxicity through a gene ontology analysis method including biological process, cellular components, molecular function and KEGG pathway.

Isolation of the Pathogenic Bacteria from Chicken and Antimicrobial Drug Sensitivity of the Strain Isolated (가금유래 주요병원성세균의 분리와 분리균주에 대한 약제감수성조사)

  • 박근식;김기석;남궁선
    • Korean Journal of Poultry Science
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    • v.7 no.1
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    • pp.53-64
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    • 1980
  • A total of 1503 specimens were submitted to the Poultry Disease Diagnostic Service Laboratory during the year 1966 and 1978. The most frequently diagnosed diseases in order of prevalence were avian mycoplasmosis, staphylococcosis, colibacillosis, salmonellosis and pullorum disease, the percentages of the conditions being 24.6%, 20.0%, 18.0%, 12.6% and 6.4%, respectively, The drug resistance of pathogenic mirnoorganisms isolated during the year 1978 from chicken with colicabacillosis, staphylococcosis or salmonellosis were investigated by the use of disc diffusion technique, the results being as follow. 1) Drug resistance of 63 strains of Escherichia coli More than 95% of the strains tested were sensitive to colistin and gentamicin. The percentages of strains sensitive to kanamycin, chloramphenicol, ampicillin and nitrofurantoin were 66.7%, 60.3%, 60.3% and 47.6%, respectively. Majority of the strains were highly resistant to streptomycin and tetracyline. All the strains were resisistant to bacitracin lincomycin, oleandomycin, penicillin and erythromycin. All the strains tested were resistant to more than two among 10 drugs in common use such as penicillin, erythromycin, streptomycin, tetracycline, neomycin, chloramphenicol, kanamycin, ampicillin and gentamicin, and 27 different resistance patterns were noted. The most frequent multiple resistance pattern was PC, EM, SM and TC (11.1%). 2) Drug resistance of 48 strains of Salmonella More than 95% of the strains tested were sensitive to colistin, gentamicin ana ampicillin. The percentages of st rains sensitive to kanamycin, tetracycline, neomycin and nitrofurantoin were 81,3%, 79%, 72.9%, and 68.0% respectively. None of them was sensitive to streptomycin, oleandomycin, erythromycin, lincomycin and bacitracin. All the strains were resistant to more than one among 7 drugs in common use such as streptomycin, erythromycin, neomycin, tetracycline, kanamycin, ampicillin and gentamicin. The most frequent resistance pattern was SM and EM(66.7%). 3) Drug resistance of 54 strains of Staphylococci All the strains tested were sensitive to gentmaicin, kanamycin and cephalothin. Majority of them were highly sensitive to bacitracin, methicillin, nitrofurantoin and chloramphenicol. The Percentages of strains sensitive to streptomycin, ampicillin, lincomycin and tetracycline were 66.7%, 55.6%, 44.4% and 27.8%, respectively. Among them, 51 strains were resistant to more than one among 11 drugs in common use such as tetracycline, lincomycin, ampicillin, penicillin, streptomycin, erythromycin, neomycin, oleandomycin, chloramphenicol, methicillin and bacitracin, and thirty one different resistance patterns were noted.

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Autoimmune hepatitis and thyroiditis associated with antituberculous medications : A case report (항결핵약으로 유발되고 갑상선염이 동반된 자가면역간염 1례)

  • Yu, Seong Keun;Kim, Sara;Moon, Jin Soo;Kim, Han Seong
    • Clinical and Experimental Pediatrics
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    • v.51 no.5
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    • pp.528-532
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    • 2008
  • Drug-induced toxic hepatitis is a relatively common hepatic disease in children, and it is usually self-limiting upon cessation of the offending drugs. Antituberculous drugs are well known for inducing hepatitis. Some cases of drug-induced hepatitis with autoimmune features have been reported; in these cases, the offending drugs were usually methyldopa, nitrofurantoin, minocycline, and interferon. The authors report the first case in Korea of drug-induced autoimmune hepatitis associated with thyroiditis and multiple autoantibodies that was induced by the antituberculous drugs isoniazid and rifampin.

Mutagenicity of Nitrofuran, Nitroimidazole and Nitrothiazole Derivatives on Salmonella/Microsome System (Nitrofuran, Nitroimidazole 및 Nitrothiazole 유도체들의 Salmonella/Microsome System에 대한 돌연변이 유발성)

  • 변우현;현형환;이세영
    • Korean Journal of Microbiology
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    • v.14 no.4
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    • pp.151-158
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    • 1976
  • Using Ames'Salmonella/microsome system, mutagenicity of antirichomonal nitrofuran, nitroimidazole, and nitrothiazole derivatives was examined. Nitrofurantoin, nifuratel, furazolidone, metronidazole, nimorazole, ornidazole, and aminitrozole showed potent mutagenicity en $TA_100$ strain which is a base substitute mutant and contains R-factor plasmid pKM101 without microsomal enzyme activation. In addition, nifuratel, furazolidone, metronidazole, and ornidazole also induced frameshift mutation in $TA_98$ strain.

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Bacteriological Identification of Strains Isolated from Diarrheal Patients at Ham Yang Gun, Kyeongsang-Namdo in July 1971 (1971년(年) 경남(慶南) 함양군(咸陽郡)에서 유행(流行)한 설사환자(患者)에서 분리(分離)한 Salmonella.Shigella 균(菌)의 세균학적(細菌學的) 연구(硏究))

  • Kim, Je-Soo;Ju, Byung-Chil;Park, Soo-Yeon;Ju, Jin-Woo;Yang, Hak-Do
    • The Journal of the Korean Society for Microbiology
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    • v.7 no.1
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    • pp.1-8
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    • 1972
  • The authors made a study on the bacteriological identification about unidentified strains which were roughly screened by local health center, which an epidemic diarrhea was outbreak at Ham Yang Gun, Kyeongsang-Namdo in July 1971. And the authors made an attempt to bacteriological Identification, serotyping with slide agglutination, and determination of the susceptibility of identified strains to various chemotherapeutic agents. The results Were obtained as follows: 1. The isolated strains identified Shigella flexneri type 2b(2 strains) and Salmonella paratyphi B(4 strains). 2. Sensitivity test using with three concentrations chemotherapeutic agents(Paper disk used; Eiken chemical Co., Tokyo, Japan): (1) Shigella flexneri type 2b isolated strains were sensitive to kanamycin, colistin(100%) and penicllin(50%) respectively, but resistant to erythromycin, oleandomycin, leucomycin, chloramphenicol, tetracycline, dihydrostreptomycin and sulfadimethoxin(100%) respectively. (2) Salmonella paratyphi B isolated strains were sensitive to chloramphenicol, tetracycline, dihydrostreptomycin, kanamycin, sulfadimethoxine(100%) and colistin(50%) respectively, but resistant to penicillin, erythromycin, oleandomycin and leucomycin(100%) respectively. 3. Sensitivity test using with multodisk urinary code(Paper disk used; Oxoid, London): (1) Shigella flexneri type 2b isolated strains were sensitive to Bactrim, ampicillin, nitrofurantoin, nalidixic add and gentamicin(100%) respectively, but resistant to chloramhpenicol, tetracycline, sulfadiazine and Fanasil(100%) respectively. (2) Salmonell paratyphi B isolated strains were sensitive to Bactrim, chloramphenicol, ampicillin, nitrofurantoin, tetracycline, nalidixic acid, gentamicin(100%) and sulfadiazine(50%) respectively, but resistant to Fanasil(100%) and sulfadiazine(50%) respectively.

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A report on the Shigella cultures isolated in Korea(1974) (1974년 한국에서 분리된 이질균에 관한 보고)

  • Kim, Soon-Hit;Chun, Nam-Ho;Ryu, Young-Hat
    • The Journal of the Korean Society for Microbiology
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    • v.10 no.1
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    • pp.13-17
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    • 1975
  • The authors identified fourty-seven Shigella cultures among 1504 suspectable cultures of enteric pathogens collected from all over the country in 1974. Fourty-three out of fourty-seven cultures belonged to Shigella flexneri, three to Shigella sonnei and the rest to Shigella dysenteriae, and none of cultures belonging to subgroup C was detected in 1974. Three Shigella flexneri 2a cultures were isolated in Seoul area, but the others in Kangwon-Do. All the Shigella cultures were sensitive to nitrofurantoin, cephalosporin, ampicillin and penicillin G $1{\mu}g$, but resistant to bacitracin, lincomycin and penicillin V. $10{\mu}g$ by means of the In-Vitro tests.

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Biochemical Properties of NAD(P)H-Quinone Oxidoreductase from Saccharomyces cerevisiae

  • Kim, Kyung-Soon;Suk, Hee-Won
    • BMB Reports
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    • v.32 no.2
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    • pp.127-132
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    • 1999
  • The NAD(P)H-quinone oxidoreductase (EC 1. 6. 99. 2) was purified from S. cerevisiae. The native molecular weight of the enzyme is approximately 111 kDa and is composed of five identical subunits with molecular weights of 22 kDa each. The optimum pH of the enzyme is pH 6.0 with 1,4-benzoquinone as a substrate. The apparent $k_m$ for 1,4-benzoquinone and 1,4- naphthoquinone are 1.3 mM and $14.3\;{\mu}M$, respectively. Its activity is greatly inhibited by $Cu^{2+}$ and $Hg^{2+}$ ions, nitrofurantoin, dicumarol, and Cibacron blue 3GA. The purified NAD(P)H-quinone oxidoreductase was found capable of reducing aromatic nitroso compounds as well as a variety of quinones, and can utilize either NADH or NADPH as a source of reducing equivalents. The nitroso reductase activity of the purified NAD(P)H-quinone oxidoreductase is strongly inhibited by dicumarol.

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