• Title/Summary/Keyword: quinolone

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Anti-inflammatory Constituents of Robinia pseudoacacia Root Bark (아까시나무 뿌리껍질의 항염증활성물질)

  • Kang, Dong-Min;Park, Woo Sung;Kim, Hye-Jin;Jeong, Woo-Jin;Kang, Kwon Kyoo;Ahn, Mi-Jeong
    • Korean Journal of Pharmacognosy
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    • v.53 no.1
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    • pp.8-15
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    • 2022
  • Robinia pseudoacacia L. (Leguminosae) is widely distributed in Asia, North America and Europe. The root bark has been traditionally used for hemostasis, arthritis and hypertension. Therefore, this study was conducted to identify the biological activity and the bioactive constituents of the root bark. We found that the methanol extract obtained from the root bark of R. pseudoacacia reduced the level of ROS and NO production in LPS-induced inflammation of RAW 264.7 cell line. Among the fractions, methylene chloride fraction showed the highest inhibitory activity against the inflammation. Seven constituents (1-7) were isolated from this fraction, and the chemical structures were determined to be medicarpin (1), (-)-vestitol (2), indole 3-carboxaldehyde (3), 3-acetylindole (4), liquiritigenin (5), 4(1H)-quinolone (6) and 8-methoxyononin (7). Among the isolates, medicarpin (1), (-)-vestitol (2), 3-acetylindole (4) and liquiritigenin (5) inhibited ROS and NO production in a dose-dependent manner. This is the first study to show the anti-inflammatory activity of the root bark of R. pseudoacacia, and it is suggested that the four constituents (1, 2, 4, and 5) could play a role in the biological activity.

Use of Antimicrobial Agents for the Treatment of Inpatients in Chonbuk National University Hospital (전북대학교병원 입원환자에서의 항생제 사용 실태)

  • Song, Jae Ho;Kim, Jung Soo
    • Pediatric Infection and Vaccine
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    • v.7 no.2
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    • pp.225-232
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    • 2000
  • Purpose : The use antimicrobial agents is one of the important strategies for the treatment and prophylaxis of microbial infections. But injudicious abuse and misuse of antimicrobial agents is problem to add an extra weight on medical fee, increase of resistant bacteria and side effects according to the antibiotic use. This study was performed to establish the pertinent use of antimicrobial agent in Chonbuk National University Hospital(CNUH). Characteristics of antibiotics use was analysis by reviewing the medical records of patients admitted to CNUH during the period of May 1998. Methods : One thousand eight hundred and thirty three patients were enrolled in this study(medical division 1,014 cases, surgical division 819 cases). Medical records were retrospectively reviewed to classify the rate of antibiotics use, name of antibiotics used, appropriateness of antibiotics use. Results : The overall rate of antibiotic usage in CNUH was 67.2%(1,231/1,833), showing higher rate in surgical division(89.6%) compare to that of medical division(49.0%). Among 1,231 patients to whom antimicrobial agents were given, only 125(10.2%) were treated with single antimicrobial agents. 311(25.3%) were treated with two antimicrobial agents, and 795(64.5%) patients received 3 or more antibiotics. ${\beta}$-lactams(56.4%) were most frequently used followed by aminoglycosides(35.3%), the others(4.9%) and quinolons(3.4%). Amoxicillin-clavulanate was the mostly commonly used antibiotics followed by amoxicillin and unasyn. Prophylactic use of antibiotics was carried in seven hundred six patients(57.4%), mostly in surgical division, which can be considered somewhat inappropriate in the initiation time and duration of antibiotic use. Conclusion : Importance of monotherapy and appropriate prophylactic antibiotic use should be emphasized. Strategies of antibiotics use, such as restriction of drug use, continuous monitoring system, flow sheet system should be considered to reduce antibiotics use and establish the appropriate use of antibiotics as well as inhibiting the occurrence of resistant strains.

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Mutation Patterns of gyrA, gyrB, parC and parE Genes Related to Fluoroquinolone Resistance in Ureaplasma Species Isolated from Urogenital Specimens (비뇨생식기계 검체로부터 분리된 Ureaplasma 종의 Fluoroquinolone 내성과 관련된 gyrA, gyrB, parC, parE 유전자의 돌연변이 양상)

  • Cho, Eun-Jung;Hwang, Yu Yean;Koo, Bon-Kyeong;Park, Jesoep;Kim, Young Kwon;Kim, Sunghyun
    • Korean Journal of Clinical Laboratory Science
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    • v.48 no.2
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    • pp.74-81
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    • 2016
  • Ureaplasma species can normally colonize in the bodies of healthy individuals. Their colonization is associated with various diseases including non-gonococcal urethritis, chorioamnionitis, neonatal meningitis, and prematurity. In 2012, the sum of the resistant and intermediate resistant rates of Ureaplasma spp. to ofloxacin and ciprofloxacin was 66.08% and 92.69%, respectively. DNA point mutations in the genes encoding DNA gyrase (topoisomerase II) and topoisomerase IV are commonly responsible for fluoroquinolone resistance. Each enzyme is composed of two subunits encoded by gyrA and gyrB genes for DNA gyrase and parC and parE genes for topoisomerase IV. In the current study, these genes were sequenced in order to determine the role of amino acid substitutions in Ureaplasma spp. clinical isolates. From December 2012 to May 2013, we examined mutation patterns of the quinolone resistance-determining region (QRDR) in Ureaplasma spp. DNA sequences in the QRDR region of Ureaplasma clinical isolates were compared with those of reference strains including U. urealyticum serovar 8 (ATCC 27618) and U. parvum serovar 3 (ATCC 27815). Mutations were detected in all ofloxacin- and ciprofloxacin-resistant isolates, however no mutations were detected in drug-susceptible isolates. Most of the mutations related to fluoroquinolone resistance occurred in the parC gene, causing amino acid substitutions. Newly found amino acid substitutions in this study were Asn481Ser in GyrB; Phe149Leu, Asp150Met, Asp151Ile, and Ser152Val in ParC; and Pro446Ser and Arg448Lys in ParE. Continuous monitoring and accumulation of mutation data in fluoroquinolone-resistant Ureaplasma clinical isolates are essential to determining the tendency and to understanding the mechanisms underlying antimicrobial resistance.

Clinical Effects of Prothinoamide, Cycloserine, Para-Aminosalicylic Acid, Ofloxasine in Retreatment of Pulmonary Tuberculosis (폐결핵 재치료 환자에서 Prothionamide, Cycloserine, Paraminosalicylic acid, Ofloxasine을 이용한 경구 4제 요법의 임상 효과)

  • Hong, Jae-Rak;Yoo, Min-Kyu;Jeong, Jae-Man;Kim, Young-Jun;Son, Mal-Hyeon
    • Tuberculosis and Respiratory Diseases
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    • v.43 no.5
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    • pp.693-700
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    • 1996
  • Background : Antituberculous therapy is set a short-term therpy used isoniazid(INH), rifampin(RFP), ethambutol(EMB), pyrazinamide(PZA) from 1970s' and treatment rate has been very improved. But drug interruption or irregular medication due to side effects and resistance of drug are serious problem to retreatment cases, specially. Ofloxasine(OFX), developed from Quinolone at 1980's is effective not only other respiratory infectious disease but also pulmonary tube rculosis. And this is useful drug instead of injection agents for retreatment patients who have side effects to other drugs, lived far distance from medical clinics. So, we will evaluate theffectiveness as four oral drugs involving OFX. Method : A retrospective study was made through the regular follow up of smear positive cases,who treated by four drug, namely, prothionamide (PTA) cycloserine(CS), OFX, paraminosalicylic acid(pAS). Results: 1) Out of 66case with positive sputum AFB smear, 42(64%)cases achieved the negative conversion. 2) Considering the negative conversion in all group, 34 case (52%) of sputum conversion occured within first 6 months, on the extent of diease was minimal, moderate, far advanced pulmonary tuberculosis, sputum AFB smear negative response to treatment was 100%, 78%, 46% respectively. 3) The roentgenological improvement occured in 38(58%), extent of diease was minimal, moderately, far advanced pulmonary tuberculosis, Roentgenological improvement to retreatment was 75%, 64%, 46%. 4) When the drnation of patients illness was less than 1 year, 1 to 3 years, 3 10 5 years and more than 5 years, sputum AFB smear negative response to retreatment was 100%, 88%, 80%, 52 %. 5) On side effects, major problems are gastrointestinal troubles, mild liver function abnormality, psychotic problemes, and skin problem(urticaria, itching sensation). Conclusion : The duration & extents of patients illness was shorter & minimal, sputum AFB smear negative response rate was better. Radiologic response is better as shorter duration and minimal extent of diease. But, as diease is longer duration & far advanced, sputum negative conversion & Roentgenological improvement is poor and limited. The adverse reaction was mainly observed gastrointestinal troubles(indigestion, abdominal pain, nausea, vomiting, diarrhea) and are well controled by symptomatic management in most patients, as regard to tolerance to the secondary drugs.

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Antibiotic Resistance for Common Hospital Acquired-pneumonia Pathogens in the Intensive Care Unit of Newly Opened Hospital (새로 개원한 병원 중환자실에서 주요 원내획득 폐렴 감염균의 연도별 항생제 내성율 변화)

  • Lee, Jae-Hyung;Shin, Sung-Joon;Kim, Young-Chan;Oh, Seung-Il;Kim, Mi-Ok;Park, Eun-Joo;Sohn, Jang-Won;Yang, Seok-Chul;Yoon, Ho-Joo;Shin, Dong-Ho;Park, Sung-Soo
    • Tuberculosis and Respiratory Diseases
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    • v.52 no.3
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    • pp.207-218
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    • 2002
  • Background : Intensive care units (ICUs) are generally considered epicenters of antibiotic resistance and the principal sources of multi-resistant bacteria outbreaks. The antibiotic resistance in newly opened intensive care unit that has no microbial colonization on and around the devices was investigated. Materials and Methods : The authors analyzed the antibiotic resistance patterns for common hospital acquired-pneumonia pathogens in the ICUs(Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter spp.) at the newly opened ICU of Hanyang University Medical Center, Kuri Hospital during 6 years(1995-2000). Results : 1) Regarding Staphylococcus aureus, the resistance rate to methicillin was 15% at 1995, 21% at 1996, 20% at 1997, 23% at 1998, 22% at 1999, 55% at 2000. 2) Regarding Pseudomonas aeruginosa, the resistance rate to $3^{rd}$ cephalosporin was 50% at 1995, 50% at 1996, 78% at 1997, 40% at 1998, 77% at 1999, 39% at 2000. Imipenam was 0% at 1995, 27% at 1996, 65% at 1997, 12% at 1998, 16% at 1999, 12% at 2000. Ciprofloxacin was 0% at 1996, 56% at 1997, 36% at 1998, 57% at 1999, 58% at 2000. Tobramycin was 7% at 1995, 10% at 1996, 67% at 1997, 36% at 1998, 65% at 1999, 12% at 2000. Gentamycin was 14% at 1995, 36% at 1996, 67% at 1997, 36% at 1998, 65% at 1999, 12% at 2000. Amikacin was 14% at 1995, 30% at 1996, 61% at 1997, 16% at 1998, 39% at 1999, 18% at 2000. 3) Regarding Acinetobacter spp., the resistance rate to $3^{rd}$ cephalosporin was 92% at 1996, 89% at 1997, 88% at 1998,84% at 1999, 77% at 2000. Imipenem was 50% at 1996, 48% at 1997, 45% at 1998, 49% at 1999, 50% at 2000. Ciprofloxacin was 0% at 1996, 48% at 1997, 33% at 1998, 27% at 1999, 71% at 2000. Tobramycin was 67% at 1995, 100% at 1996, 89% at 1997, 95% at 1998, 87% at 1999, 77% at 2000. Gentamycin was 67% at 1995, 100% at 1996, 89% at 1997, 95% at 1998, 87% at 1999, 83% at 2000. Amikacin was 33% at 1995, 83% at 1996, 82% at 1997, 88% at 1998, 75% at 1999, 69% at 2000. Conclusion : The S.aureus resistance to methicillin, the Pseudomonas aeruginosa resistance to ciprofloxacin, and the Acinetobacter spp. resistance to ciprofloxacin have rapidly increased during 6 years. There is a need to pay speicial attention when using the the antibiotics for the above pathogens. This data may be useful in antibiotic therapy in newly opened intensive care units.

Antioxidative and Hepatoprotective Effects of Injinho-Tang and Osumogwa-Tang (인진호탕(茵蔯蒿湯)과 오수목과탕(吳茱木瓜湯)의 항산화(抗酸化) 및 간세포(肝細胞) 보호효과(保護效果))

  • Lee, Sang-Hyun;Kim, Young-Bok
    • Herbal Formula Science
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    • v.16 no.1
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    • pp.117-130
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    • 2008
  • Korean traditional medicine has been used for the treatment of the various diseases based on both oriental medicinal theory and clinical trials. Thus, the prescriptions of Korean traditional medicine would be useful for the development of new therapeutics. This research focuses on the fundamental study in Korean traditional prescriptions for the development of new hepatoprotective agents. We found two prescriptions. Injinho-Tang and Osumogwa-Tang, showed the significant DPPH free radical scavenging and hepatoprotective effect, respectively. It is well-known that free radical scavenging effect is related to the prevention of various pathological events including liver injury. This paper deals with hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, free radicals scavenging on both DPPH and superoxide of above two prescriptions. Hot water extract of Injinho-Tang did not show the significant hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells, however, it shows the significant scavenging effects for both DPPH and superoxide radicals. On the other hand, all of the hot water extracts of constituent herbal drugs in Injinho-Tang exhibited the promising protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Of these, water extract of Rhei Rhizoma showed the most prominent effect on tacrine-induced cytotoxicity in Hep G2 cells. Bioassay-guided fractionation of Rhei Rhizoma extract has furnished four compounds, and their chemical structures have been identified by comparison of their spectral data with those of literature as chrysophanol (1), emodin (2), 3,5-dihydroxy-4'- methoxystilbene (3), and rhapontigenin (4), respectively. Among the isolated compounds, compounds 2-4 revealed the significant hepatoprotective effect in vitro when their $EC_{50}$ values compare with that of silybin, as a positive control. It also exhibited that emodin possessed the most hepatoprotective effect among these active compounds. In case of Osumogwa-Tang, its hot water extract showed the moderate protective effect on tacrine-induced cytotoxicity in Hep G2 cells. Hot water extract of Chaenomelis Fructus, one of the constituent herbal drug of this prescription, exhibited the significant hepatoprotective effect with $EC_{50}$ value of $7.8{\pm}0.1\;{\mu}g/ml$, however, it showed strong cytotoxicity in Hep G2 cells above the concentration of $25\;{\mu}g/ml$. It was revealed that both hot water extract of Evodiae Fructus and its butanol soluble fraction showed the moderate hepatoprotective effect but concentration-dependent activity in Hep G2 assay system. Two quinolone alkaloids, evocarpine and dihydroevocarpine, also tested for their hepatoprotective effects on tacrine-induced cytotoxicity in Hep G2 cells, however, these two compounds derived from the Evodiae Fructus as the major constituents did not show in vitro hepatoprotective effect. From these results, it would be necessary to further isolation of its hepatoprotective compounds from the butanol soluble fraction of the hot water extract of Evodiae Fructus.

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Control Efficacy of Fungicides on Pepper Bacterial Wilt (고추 풋마름병에 대한 살균제의 방제 효과)

  • Lee, Soo Min;Kwak, Yeon Soo;Lee, Kyeong Hee;Kim, Heung Tae
    • The Korean Journal of Pesticide Science
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    • v.19 no.3
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    • pp.323-328
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    • 2015
  • Control efficacy was investigated with fungicides as 3 copper compound, 3 antibiotic fungicides and one fungicide containing to quinolone against the growth of Ralstonia solanacearum on NA medium and the disease occurrence on pepper seedlings. Among 7 fungicides, oxytetracycline was shown the highest activity against a growth of the pathogen in the agar diffusion method, but validamycin showed no activity against the pathogen. With $1000{\mu}g\;mL^{-1}$ of each copper fungicide as copper hydroxide, copper oxychloride+ dithianone and copper sulfate, 2.2, 1.3 and 1.5 mm in size of clear zone only could be found, respectively. In pepper seedling test, oxytetracycline showed a perfect activity in all treatments 7 days after inoculation. However, its activity was decreased from $500{\mu}g\;mL^{-1}$ of treatment over the time. Copper fungicides showed the control efficacy lower than antibiotic fungicides except for validamycin. Based on the results, it was suggested that it would be better to use antibiotic fungicides than copper fungicides to control pepper bacterial wilt in the fields.

Comparative Analysis of Levofloxacin Resistant Genes in Clinically Isolated Streptococcus pneumoniae (임상에서 분리한 Streptococcus pneumoniae에서 Levofloxacin 내성유전자의 비교 연구)

  • Choi, Jae Min;Park, Seon Hui;Yoon, Ji A;Han, Yang Keum;Lee, In Soo
    • Journal of dental hygiene science
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    • v.12 no.2
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    • pp.109-113
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    • 2012
  • One hundred seventy four Streptococcus pneumoniae clinical isolates were categorized depending on the types of specimens, the age and the gender, respectively. All isolates were analyzed the characteristics of the multi-drug resistance including levofloxacin antibiotics. In the results of analysis depending on the type of samples, it had been confirmed that sputum was the main source of pneumonia infection because 156 of 174 strains (89.7%) were isolated in sputum samples. The opportunity for isolating the S. pneumoniae that had tolerance to levofloxacin was increased in over 51 age patients group compared with other age and male group. Eight strains of isolates were evaluated higher resistant to levofloxacin, and those also showed multi-drug resistant including penicillin, tetracycline, erythromycin, clindamycin and trimethoprim-sulfamethoxazole. In the results of sequence analysis of quinolone resistance determining region in SP32 (MIC $64{\mu}g/mL$) and SP96 (MIC $8{\mu}g/mL$) which were levofloxacin resistant strains, an amino acid substitutions were found Ser-81$\rightarrow$Phe in both GyrA of SP32 and SP96, and Ser-11$\rightarrow$Gly in only SP96. A Ser-79$\rightarrow$Phe substitution of ParC was found in both.

The Antibiotic Resistance Pattern of Gram-Negative Bacteria in Children Younger Than 24 Months with a Urinary Tract Infection: A Retrospective Single-Center Study over 15 Consecutive Years

  • Lee, Yoon Kyoung;Lee, Haejeong;Kim, Jong Min;Kang, Ji-Man;Lee, Sang Taek;Lee, Nam Yong;Kim, Yae-Jean;Cho, Heeyeon
    • Childhood Kidney Diseases
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    • v.19 no.2
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    • pp.148-153
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    • 2015
  • Purpose: We investigated trends in antibiotic resistance for gram-negative bacteria in infants with a urinary tract infection (UTI) over 15 years at a single institution. Methods: A retrospective chart review was conducted for children younger than 24 months who visited the emergency room and were diagnosed with a UTI between January 2000 and December 2014. We selected urine culture data that grew Escherichia coli and Klebsiella pneumoniae. Baseline clinical information and results of antimicrobial susceptibility tests were analyzed by dividing the 15-year study time frame into three periods (A: 2000-2004, B: 2005-2009, and C: 2010-2014). Results: During the study period, 478 applicable children were identified (E. coli, 89.7% and K. pneumoniae, 10.3%). Antibiotic resistance to third-generation cephalosporins was increased from period A to period C (A, 2.1%; B, 8.3%; C, 8.8%; P=0.025). Resistance to quinolones also showed a steady pattern during periods A to C, although it was not statistically significant (A, 7.9%; B, 9.7%; C, 12.4%; P=0.221). The incidence of Extended-spectrum ${\beta}$-lactamase (ESBL)-producing gram-negative bacteria increased from period A to period C (A, 1.4%; B, 7.6%; C, 8.2%; P=0.012). Conclusion: This study revealed that the common uropathogens E. coli and K. pneumoniae experienced increasing resistance rates against third-generation cephalosporins and a constant antibiotic resistance to quinolones in children younger than 24 months. We also showed a recent increased incidence of ESBL-producing gram-negative bacteria in patients with community-acquired UTIs. Therefore, it is necessary to actively surveil resistance in order to properly select empirical antibiotics.

The Clinical Effect of Sparfloxacin for the Treatment of Acute Respiratory Infection (호흡기 감염 질환에서 Sparfloxacin의 임상효과)

  • Lee, Hak-Jun;Park, Hye-Jung;Shin, Chang-Jin;Shin, Kyeong-Cheol;Chung, Jin-Hong;Lee, Kwan-Ho;Lee, Hyun-Woo
    • Journal of Yeungnam Medical Science
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    • v.15 no.2
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    • pp.246-253
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    • 1998
  • Sparfloxacin is a new synthetic quinolone antimicrobial developed at the Research Laboratories of Dainippon Pharmaceutical Co, Ltd. To evaluate the efficacy and safety of sparfloxacin in acute pulmonary infection, we administered sparfloxacina(100mg) twice in a day to 30 patients who had signs and symptoms of acute pulmonary infectious diseases regardless of their underlying lung disease for 7 days. The results were as follows: 1) A total 30 patients were enrolled in the trial. Among them, 24 cases(80%) had underlying lung problems such as chronic obstructive pulmonary disease(36.4%), bronchiectasis(36.4%), bronchial asthma(3.3%), or lung cancer(3.3%). 2) In 26 cases(86.6%), we observed effective improvement, and 4 cases(13.4%) show mildly effective improvement of symptoms and signs of respiratory infection. 3) In 23 cases(73.4%), we observed bacteriological eradication in culture or decreased the number of bacteria by Gram stain which found dominantly in previous Gram stain. 4) The significant side effect was not noted. The above results suggested that sparfloxacin was effective as a first line therapy in patients with acute respiratory infection.

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