• 제목/요약/키워드: new antibiotics

검색결과 326건 처리시간 0.025초

Histological Subtype of Ovarian Cancer as a Determinant of Sensitivity to Formamidine Derivatives of Doxorubicin - in Vitro Comparative Studies with SKOV-3 and ES-2 Cancer Cell Lines

  • Denel-Bobrowska, M.;Lukawska, M;Oszczapowicz, I;Marczak, A
    • Asian Pacific Journal of Cancer Prevention
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    • 제17권9호
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    • pp.4223-4231
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    • 2016
  • Background: Development of new apoptosis-inducing drugs is a promising trend in anticancer therapy. For this purpose several formamidinoderivatives of doxorubicin were synthesized. The aim of our study was to investigate effects of the five formamidinodoxorubicins in the ES-2 human ovarian clear cell carcinoma line, for comparison with data obtained previously for SKOV-3 human ovarian adenocarcinoma cells, to answer the question of whether and to what extent the histological cell type is a possible determinant of sensitivity to tested anthracyclines. Materials and Methods: In our experimental work the following methods were used: spectrophotometric assays with MTT; fluorimetric assays - double staining with Hoechst 33258 and propidium iodide (PI), measurement of caspase-3, -8, -9 activity, intracellular accumulation of DOX and analogues, estimation of drug uptake, mitochondrial transmembrane potential; flow cytometry - phosphatidylserine (PS) externalization with annexin V-FITC and PI fluorochromes. Results: Effects of the derivatives of doxorubicin were partially linked with the specific type of cancer cell although intracellular accumulation and cellular uptake of DOX and derivatives were similar in both. All of the investigated derivatives were considerably more cytotoxic than DOX. Formamidinodoxorubicins were able to induce caspase-dependent apoptotic cell death in both cell types. Conclusions: All new formamidine derivatives of DOX were able to induce caspase - dependent apoptosis in human ovarian cancer cell lines SKOV-3 and ES-2. Obtained results suggested that formamidine derivatives of DOX may be promising candidates for the prospective chemotherapeutic agents for the two different histological subtypes of ovarian cancer.

새로운 $\beta$-락탐계 물질의 합성 및 그 항균력 (Synthesis and Antibacterial Activities of New $\beta$-Lactam Compounds)

  • 진정일;장민선;민신홍
    • 약학회지
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    • 제30권6호
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    • pp.294-300
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    • 1986
  • New antibiotics having moieties of penicillanic acid, cephalosporanic acid and ampicillin on both ends of the central polyalkylene were synthesized by reacting 6-aminopenicillanic acid (6-APAl), 7-amino cephalosporanic acid (7-ACA) and ampicillin with hexamethylene diisocyanate and sebacoyl chloride, respecetively. Antibiacterial activities of the compounds were also investigated.

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Taxonomy and Fermentation of Kitasatosporia kimorexae Producing New Thiopeptide Antibiotics, Kimorexins

  • Yeo, Woon-Hyung;Kim, Si-Kwan;Kim, Sang-Seock;Yu, Seung-Hun
    • Journal of Microbiology and Biotechnology
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    • 제4권4호
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    • pp.354-359
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    • 1994
  • An isolate, 90-GT-302, was found to produce antibiotics inducing typical mycelial swelling in Magnaporthe grisea and Fusarium solani. This isolate formed yellow substrate and white rectiflexbiles aerial mycelia in the early stages of growth. The aerial mycelium gradually changed its color to white and finally formed a gray spore mass. Analysis of the cell wall acid hydrolysate revealed the presence of LL- and meso-diaminopimelic acids, glycine, and galactose, which indicated cell wall type X. This result placed our isolate in genus Kitasatosporia. A comparison of isolate 9O-GT-302 with reference strains of Kitasatosporia spp., which not only demonstrated several differences in their physiological properties but also novelty of the active compounds produced by this isolate, led us to designate the isolate as Kitasatosporia kimorexae.

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밀의 항흑수병 항생물질의 연구 1 (Studies on antibiotics against Wheat black rust (I))

  • 정영기
    • 미생물학회지
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    • 제19권3호
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    • pp.108-114
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    • 1981
  • In order to isolate microorganisms which produce antibiotics aganist wheat black rust, some bacteria, molds, and actinomycetes were isolated from soils and screened for the production of antibiptics against wheat black rust. Beacuse wheat black rust-puccinia graminis--is a complete parsitic mold which can't grow in artifical medium, new method for the screening of antibiotic producing microorgsnisms against wheat black rust developed by using live leaves of wheat. With new method, a strain No. $480HS_{20}$ which produces a substnace having strong and Puccinia graminis activity and very narrow antimicrobial spectrum was isolated. the substance produced by the strain No.$480HS_{20}$ had better anti Puccinia graminis activity than any other known antifungal antibotics such as kasurgamycin, balasticidins, actidione, antimycin, ologomycin. And the substance was observed to be very stable at heat and ultraviolet light. The strain was indentified as Bacillus subtilis.

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골수염 치료제인 항생제비드(CJ-40003) 유효성분의 일반약리작용 (General Pharmacology of the Active Ingredients of New Antibiotic Bead (CJ-40003))

  • 김영훈;최재묵;온윤성;연규정;이윤하;김제학;이영수
    • Biomolecules & Therapeutics
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    • 제7권1호
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    • pp.97-104
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    • 1999
  • A new antibiotic bead, CJ-40003 is a combination of three antibiotics, tobramycin, vancomycin and cefazolin embedded in bone cement, for the treatment of osteomyelitis. To evaluate the general pharmacological properties of CJ-40003, the effects of its active ingredients were investigated in mice, rats, dogs and isolated guinea pig ileum. The combination of three antibiotics (CA) did not affect general behavior, central nervous system, smooth muscles, gastrointestinal system, cardiovascular and respiratory system and water and electrolytes excretion when administered intravenously at the doses of 0.3, 1 and 3 mg/kg, respectively, into experimental animals. The CA had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 1, 3 and 10 $\mu\textrm{g}$/ml, respectively. In conclusion, the active ingredients of CJ-40003 showed no pharmacological effect in these studies.

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MRSA에 대한 작약감초탕과 항생제 병용투여의 항균활성에 관한 연구 (A Study on the Antibacterial Activity of Combined Administration of Jakyakgamcho-tang and Antibiotics Against MRSA)

  • 강담희;강옥화;채희성;권동렬
    • 생약학회지
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    • 제54권2호
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    • pp.72-79
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    • 2023
  • MRSA is Staphylococcus aureus resistant to β-lactam antibiotics, and is a worldwide infectious disease. Even with the discovery of new antibiotics, resistance develops rapidly, so new alternatives are needed. Jakyakgamcho-tang (JGT) is a combination of Jakyak and Gamcho, and has been mainly used as an antispasmodic and analgesic in oriental medicine. This study was conducted to find out whether there is an effect on MRSA in relation to the anti-inflammatory effect of JGT and the antibacterial effect of Jakyak and Gamcho found in previous studies. In this study, in order to investigate the antibacterial activity of JGT and the combined effect of existing antibiotics, after extracting JGT with 70% EtoH, the disc diffusion method, minimum inhibitory concentration (MIC), drug combination effect (FICI), and time-kill analysis (Time-kill assay), metabolic inhibition, Western blot and qRT-PCR analysis were used to confirm the antibacterial activity mechanism of MRSA of JGT. As a result of the experiment, all of MRSA showed antibacterial activity in JGT's disc diffusion method, and the MIC was 250-1000 ㎍/mL. When existing antibiotics and JGT were combined with drugs, most had synergy or partial synergy. In addition, it was confirmed that the degree of bacterial growth was suppressed over time when simultaneous administration for 24 hours. JGT showed a synergistic effect when administered together with the ATPase-inhibitor DCCD, suggesting that it affected the inhibition of ATPase. As a result of observing the expression of PBP2a, and hla protein in the JGT-treated group and the untreated control group through wstern blot, it was confirmed that the protein expression of the JGT-treated group was significantly suppressed, and the expression levels of mecA, mecR1 and hla genes were also suppressed during JGT treatment. was observed by qRT-PCR. Combining the results of the experiment, it can be seen that JGT has antibacterial activity in MRSA, and when combined with existing antibiotics, the effect was increased compared to treatment with the drug alone. This suggests that JGT can be an alternative to treatment for antibiotic resistance of MRSA.

세균의 Peptide Deformylase(PDF)를 억제하는 새로운 항균물질의 스크리닝 (Screening of New Antibiotics Inhibiting Bacterial Peptide Deformylase (PDF))

  • 곽진환;김현주;설민정;서병선;이종국;최수영
    • 약학회지
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    • 제47권3호
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    • pp.184-189
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    • 2003
  • Peptide deformylase (PDF) is essential and unique to bacteria, thus making it an attractive target for the discovery of novel antibacterial drugs. PDF deformylates the N-formylmethionine of newly synthesized polypeptides in prokaryotes. In this study, a pdf gene from Staphylococcus aureus 6538p was cloned in pET-14b vector and PDF protein was over-produced in Escherichia coli BL21 (DE3). NH$_2$-terminal His-tagged PDF protein was purified by nickel-nitrilotriacetic acid (Ni-NTA) metal-affinity chromatography. Enzymatic activity of purified 6xHis-tagged PDF was tested on the substrate (formyl-Methionine-Alanine-Serine) by formate dehydrogenase-coupled spectrometric assay of peptide deformylase. For the discovery of new PDF inhibitors from chemical libraries and culture broths of soil bacteria, a target-oriented screening system using a 96-well plate was developed. About 3,000 commercial chemical libraries were tested in this screening system, and 2 chemicals (0.07%) among them showed an inhibitory activity against PDF enzyme. This result showed that a new screening system can be used for the discovery of new PDF inhibitors.

The Development of New Carbacephem Antibiotics

  • Pyun, S.J.;Kim, Y.H.;Lee, Y.S.;Ham, W.H.
    • 대한약학회:학술대회논문집
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    • 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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    • pp.211.1-211.1
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    • 2000
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A New Streptothricin Family Antibiotic Producing Streptomyces Spp. Snus 8810-111 ; Characterization of The Producing Organisms, Fermentation, Isolation, and Structure Elucidation of Antibioitics

  • Goo, Yang-Mo;Kim, Ok-Yun;Joe, Young-Ae;Lee, Young-Bok;Ju, Jeongho;Kim, Beom-Beom-Tae;Lee, Youn-Young
    • Archives of Pharmacal Research
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    • 제19권2호
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    • pp.153-159
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    • 1996
  • A new streptothricin family antibiotic producing Streptomyces spp. SNUS 8810-111 was isolated from a soil sample. Study of its morphological and physiological characters indicated that the antibiotic producing organism was a Streptomyces spp. Taxonomical studies suggested that the organism might belong to the genus streptomyces gougeroti. The organism produced antibiotics most in calcium carbonate-tryptic soy broth. The active principles were recovered from the broth with a cation exchange resin and eluted from the resin with HCI. Cellulose column chromatography gave two active principles.$^1H-^1H$ Homo-COSY study on the first compound revealed four structural components. Total hydrolysis of the antibiotic with HCI allowed isolation of $\beta-lysine$. From these data the antibiotic was found to be streptothricin D. The other compound showed one additional signal in the .$^1H$NMR and the $^{13}C$ NMR spectra. The signal was from a methyl group attached to a nitrogen atom. Comparison of the NMR signals with those of streptothricin D suggested that the compound was N-methyl-streptothricin D which was a new compound in the family of streptothricin antibiotics.

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