• Journal of Microbiology and Biotechnology
• /
• v.23 no.2
• /
• pp.184-188
• /
• 2013

In the continued search for inhibitors of enoyl-acyl carrier protein (ACP) reductase, we found that four acylbenzenediol sulfate metabolites from Streptomyces sp. AN1761 potently inhibited bacterial enoyl-ACP reductases of Staphylococcus aureus, Streptococcus pneumoniae, and Mycobacterium tuberculosis. Their structures were identified as panosialins A, B, wA, and wB by MS and NMR data. They showed stronger inhibition against S. aureus FabI and S. pneumoniae FabK with $IC_{50}$ of 3-5 ${\mu}M$ than M. tuberculosis InhA with $IC_{50}$ of 9-12 ${\mu}M$. They also exhibited a stronger antibacterial spectrum on S. aureus and S. pneumoniae than M. tuberculosis. In addition, the higher inhibitory activity of panosialin wB than panosialin B on fatty acid biosynthesis was consistent with that on bacterial growth, suggesting that they could exert their antibacterial activity by inhibiting fatty acid synthesis.

• BMB Reports
• /
• v.42 no.2
• /
• pp.81-85
• /
• 2009

Early and accurate detection of drug resistant Mycobacterium tuberculosis can improve both the treatment outcome and public health control of tuberculosis. A number of molecular-based techniques have been developed including ones using probe molecules that target drug resistance-related mutations. Although these techniques are highly specific and sensitive, mixed signals can be obtained when the drug resistant isolates are mixed with drug susceptible isolates. In order to overcome this problem, we developed a new drug susceptibility test (DST) for one of the most effective anti-tuberculosis drug, isoniazid. This technique employed a microplate hybridization assay that quantified signals from each probe molecule, and was evaluated using clinical isolates. The evaluation analysis clearly showed that the microplate hybridization assay was an accurate and rapid method that overcame the limitations of DST based on conventional molecular techniques.

• Journal of the Korean Chemical Society
• /
• v.20 no.5
• /
• pp.358-363
• /
• 1976

Kinetic studies on solvolytic reactions of 1-and 2-naphthalene sulfonyl chlorides in ethanol-water mixtures have been carried out by means of conductometry at several temperatures. The rate constant for 2-naphthyl compound was larger than that for 1-naphthyl compound. This was contrary to the prediction of MO theory and could be rationalized as due to the peri-hydrogen effect in the transition state for 1-naphthyl compound. Based on m values of Winstein plots and n values of Kivinen pacolots it was concluded that the solvolytic displacement of the two naphthalene sulfonyl chlorides in ethanol-water mixtures proceed via $S_N2$ process.

• Koreanishche Zeitschrift fur Deutsche Sprachwissenschaft
• /
• v.1
• /
• pp.141-163
• /
• 1999

Im Rahmen der Prinzipien und Parametertheorie ist die $koh\"{a}rente$ Konstruktion umstritten in bezug auf die Frage, ob sie yon der satzwertigen, $inkoh\"{a}renten$ Konstruktion(i.e. Small Clause) herleitbar ist oder nicht. Die derivationellen Analysen wie Evakuierungsanalyse, Verbanhebungsanalyse und Reanalyse gehen von der Annahme aus, $da{\ss}\;die\;koh\"{a}rente$ Konstruktion eine von der $inkoh\"{a}renten$ Konstruktion derivierte Variation ist. Im Gegensatz dazu ist nach der Unifikationsanalyse die $koh\"{a}rente$ Konstruktion die basisgenerierte monosententiale Konstruktion. In der vorliegenden Arbeit wird versucht, die empirische und theoretische $Unad\"{a}quatheit$ der derivationellen Analysen zu zeigen. Wenn die derivationellen Analysen korrekt $w\"{a}ren,\;mu{\ss}te$ auch nach der Derivaton beim langen Passiv das Akkusativkomplement der Infinitivkonstruktion ohne Kasuskonversion bleiben. Aber in der Tat wird der Nominativkasus dem Komplement der Infinitivkonstruktion zugewiesen. In der empirischen Gesichtspunkten steht das lange Passiv nicht im Einklang rnit den derivationellen Analysen. Ferner $mu{\ss}$ nach Chomskys $\"{O}konomieprinzip$ die Derivation obligatorisch sein. Aber die derivationellen Analysen, nach denen der grammatische Satz vom grammatischen Satz deriviert wird, ist nicht obligatorisch, sondern fakultativ. Sie sind theoretisch nicht $ad\"{a}quat$. In dieser Arbeit wird die Resultativkonstruktionen als weitere $koh\"{a}rente$ Konstruktion vorgeschlagen. Dabei wird die Evidenz gegen die Small Clause Struktur, die nach den derivationellen Analysen als $urspr\"{u}ngliche$ Struktur der koharenten Konstruktion angenommen wurde, zweierlei wie folgt gezeigt: Skopus und Idiomatisierung. Wenn die Resultativkonstruktionen als Small Clause analysiert werden, kann ein Adverb innerhalb des Small Clause auftreten, das den weiten Skopus $\"{u}ber$ den Gesamtsatz hat. Aber unter der Small Clause Analyse kann $tats\"{a}chlich$ das Adverb wegen der K-Kommandobedingung keinen weiten Skopus. D.h. das Adverb kann das finite Verb nicht k-kommandieren. Idiomatisierung bildet vor der Transformation im Lexikon eine syntaktische Einheit. In der Resultativkonstruktion, die das $inh\"{a}rente$ Reflexivum enthalt, $k\"{o}nnen\;das\;Resultativpr\"{a}dikat$ und das Verb wie ein reflexives Verb analysiert werden. Aber unter der Small Clause Analyse ist Idiomatisierung des $Resultativpr\"{a}dikats\;und\;Verbs\;nicht\;m\"{o}glich$, weil sie in der D-Struktur keine syntaktische Einheit bilden.

• Koreanishche Zeitschrift fur Deutsche Sprachwissenschaft
• /
• v.1
• /
• pp.69-90
• /
• 1999

Die vorliegende Arbeit setzte sich zum Ziel, deutsche verbale Phraseolexeme(vPL) auf der Grundlage einer Mehrebenenbeschreibung syntaktisch sowie semantisch zu untersuchen. Dabei $st\"{u}tzten$ wir uns vor allem auf die Valenz- und Kasustheorie sowie das 6-Stufen-Modell von G. Helbig(1983) und das Mehrebenenmodell $f\"{u}r$ vPL von B. Wotjak(1992), das seinerseits vom methodischen Ansatz her in engem Zusammenhang zu dem Beschreibungsansatz steht. Aber Wir modifizierten teilweise das Modell yon B. Wotjak(1992) und stellten einige vPL exemplarisch dar. Dieser Untersuchung lag eine verbozentrische Auffassung des Satzes zugrunde: Das Verb bildet das organisierende Zentrum des Satzes und ist fur die Grundstruktur des Satzes verantwortlich. Das Verb als $Valenztr\"{a}ger\;er\"{o}ffnet$ um sich herum bestimmte Leerstellen, deren Zahl und Art letztlich von der Verbbedeutung her determiniert sind. Auch vPL kann als $Valenztr\"{a}ger$ - wie das Verb - das strukturelle Zentrum des Satzes darstellen, d.h. vPL bildet als Ganzes das $Pr\"{a}dikat$, das wendungsextern eine bestimmte Zahl von Leerstellen $er\"{o}ffnet$ und determiniert im Satz mit seinen $inh\"{a}renten$ semantischen Merkmalen seine semantische und syntaktische Umgebung. Bei der Analyse von vPL gingen wir von der Auffassung von B. Wotjak aus, $da\ss$ Modelle zur Beschreibung von Verben prinzipiell auch auf die Beschreibung von verbalen PL anwendbar sind. In dieser Untersuchung verwendeten wir - in Anlehnung an B. Wotjak(1996:4f.) - den Terminus 'Phraseologismus' als Oberbegriff, der a) Kollokationen, $b)\;Funktionsverbgef\"{u}ge\;(FVG)$, c) Wortidiome (wortwertige idiomatische Redewendungen oder Phraseolexeme), d) Satzidiome(satzwertige idiomatische Redewendungen bzw. kommunikative Formeln/ Routineformeln), e) $Sprichw\"{o}rter\;umfa{\ss}t$. Wir $beschr\"{a}nkten$ uns den Gegenstand unserer Untersuchung auf verbale Phraseolexeme(vPL), d.h. wie oben genannte Wortidiome. VPL lassen sich $prim\"{a}r$ in bezug auf das wendungsexterne ($\"{a}u{\ss}ere$) Aktantenpotential(PLe) und $sekund\"{a}r$ in bezug auf die interne Kom­ponentenstruktur des PL(PLi) klassifizieren. Unsere Studie soil nicht nur Hintergrundwissen $f\"{u}r$ Lexikonein­tragungen vertiefen helfen, sondern auch $f\"{u}r$ den Fremdsprachen­unterricht von Nutzen sein.

• Journal of Microbiology and Biotechnology
• /
• v.17 no.5
• /
• pp.761-768
• /
• 2007

Serratia proteamaculans HY-3 isolated from the digestive tract of a spider produces an extracellular protease named arazyme, with an estimated molecular mass of 51.5 kDa. The purified enzyme was characterized as having high activities at wide pH and temperature ranges. We further characterized biochemical features of the enzymatic reactions under various reaction conditions. The protease efficiently hydrolyzed a broad range of protein substrates including albumin, keratin, and collagen. The dependence of enzymatic activities on the presence of metal ions such as calcium and zinc indicated that the enzyme is a metalloprotease, together with the previous observation that the proteolytic activity of the enzyme was not inhibited by aspartate, cysteine, or serine protease inhibitors, but strongly inhibited by 1,10-phenanthroline and EDTA. The araA gene encoding the exoprotease was isolated as a 5.6 kb BamHI fragment after PCR amplification using degenerate primers and subsequent Southern hybridization. The nucleotide sequence revealed that the deduced amino acid sequences shared extensive similarity with those of the serralysin family of metalloproteases from other enteric bacteria. A gene(inh) encoding a putative protease inhibitor was also identified immediately adjacent to the araA structural gene.

• Archives of Pharmacal Research
• /
• v.29 no.1
• /
• pp.26-33
• /
• 2006

Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

• Development and Reproduction
• /
• v.6 no.1
• /
• pp.31-35
• /
• 2002

The major urinary proteins(MUPs) of mice that bind hydrophobic molecules known as pheromones are regulated in part by the actions of growth hormone. The expression of the MUPs was therefore investigated in transgenic mice that express a human growth hormone-releasing factor gene from a metallothionein gene promoter(MT-GRF) and as a result have elevated growth hormone levels. MUPs were severely down-regulated in the urine of these animals compared to normal mice or to control transgenic mice expressing another gene(the inhibin a subunit) from the same metallothionein promoter(MT-Inh) and more MUPs disappeared in male mice than female ones. MUPs were also down-regulated in the urine of the UT-GRF-injected mice. In addition, it was observed that the urine of the MT-GRF mice included a high molecular weight protein that co-migrates with the major serum protein albumin, indicating an impairment in glomerular filtration within the kidney. The urinary loss of serum proteins was more severe in male MT-GRF mice than female ones. Thus the overexpression of human GRF mimics changes observed in MUP protein expression and glomerular function in other models of growth hormone hypersecretion with sex-dependent differential effects.

• Tuberculosis and Respiratory Diseases
• /
• v.53 no.1
• /
• pp.17-26
• /
• 2002

Background : The detection and early elimination of the causes for acute respiratory distress syndrome(ARDS) at the initial stage can result in a more favorable prognosis. Miliary tuberculosis as a cause of the ARDS is quite rare. A diagnosis of miliary tuberculosis is difficult due to the diversity of radiological patterns and non-specific clinical finfings, and low sensitivity of sputum examinations for acid-fast bacilli(AFBs). An analysis of the clinical data is the first step in diagnosing these unusual, rare cases. Materials and Methods : In this study the clinical features, laboratory data, radiological findings and diagnostic methods were analyzed in 9 cases with an initial presentation of ARDS due to miliary tuberculosis. The ARDS was defined by the definition of the American-Europian consensus conference 1992. Results : The mean age of the patients was $67{\pm}18$ years (F:M=7:2). The chief complaints were dyspnea(5/9), coughing (3/9) and fever(5/9). On a physical examination, fine or coarse crackles were noted(6/9). The ARDS developed on average 6.7 days after the initial respiratory symptoms. The mean $PaO_2/FiO_2$ of the patients was $133.5{\pm}53.4$, the number of cases with a WBC<5000/$mm^3$ was 4 out of 9 cases. A platelet count<70,000/$mm^3$ was observed in 2 out of 9 cases, and the serum albumin level was $2.6{\pm}0.6$ g/dL. The initial simple chest PA showed ground glass appearances and consolidation in all cases, However, the miliary nodular densities were observed in only 4 out of the 9 cases. HRCT revealed alveolar densities and a consolidation in 5 out of 6 cases, and miliary nodules in 5 out of 6 cases, The diagnosis of tuberculosis was made by a liver biopsy (4/4, 100% sensitivity), a bone marrow biopsy (1/2, 50% sensitivity), and an open lung biopsy (1/1), the sputum AFB was positive in only 2 out of 9 cases. The patient was treated with INH, RFP, EMB, PZA, and steroids. The survival rate was 55.5%. Conclusion : Miliary tuberculosis should be considered as one of the causes for ARDS in areas where there is a high prevalence of tuberculosis. The chief complaints of the patients on admission are dyspnea, fever and coughing without any specific riskfactors. A liver biopsy is particularly useful in ARDS patients with mechanical ventilation to determine the causes of the ARDS if miliary tuberculosis is suspected as being the underlying disease.

• Tuberculosis and Respiratory Diseases
• /
• v.63 no.5
• /
• pp.435-439
• /
• 2007

Standard antituberculous therapy, including isoniazid (INH), rifampin, ethambutol, and pyrazinamide (PZA), is widely used to treat active tuberculosis. The most important side effect is hepatotoxicity. In a standard four-drug regimen, PZA was the most common cause of drug-induced hepatitis and was dose-related. The incidence of drug-induced hepatitis is high at doses of 40~70 mg/kg per day but has fallen significantly since the recommended dose was reduced. Liver toxicity induced by PZA is rare at doses of 25 mg/kg per day or less. PZA-induced fulminant hepatic failure is also rare but fatal. We report a case of fulminant hepatic failure caused by a re-challenge of PZA.