• Title/Summary/Keyword: hydroxylamine

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Synthesis and Importance of Bulky Aromatic Cap of Novel SAHA Analogs for HDAC Inhibition and Anticancer Activity

  • Chun, Pu-Soon;Kim, Won-Hee;Kim, Jung-Su;Kang, Jin-Ah;Lee, Hye-Jin;Park, Ji-Young;Ahn, Mee-Young;Kim, Hyung-Sik;Moon, Hyung-Ryong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.6
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    • pp.1891-1896
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    • 2011
  • On the basis of potent HDAC-inhibitory activity and anticancer activity of SAHA, novel SAHA derivatives 3a-d and 7 with a bulky cap such as p-dimethylaminophenyl, 4-phenylaminophenyl, 4-phenyloxyphenyl, 9H-fluorenyl or naphthalenyl ring were synthesized starting from the corresponding aryl amines or naphthalenyl acetic acid using an EDC-mediated amide coupling reaction in the presence of HOBt followed by a nucleophilic addition-elimination reaction with hydroxylamine. Compounds 3b, 3c and 3d showed more potent inhibitory activity on total HDACs (14~27-fold), HDAC1 (8~15-fold), HDAC2 (1.3~25-fold) and HDAC7 (1~3-fold) and more potent anticancer activity (2~22-fold) against MCF-7, MDA-MB-231, MCF-7/Dox, MCF-7/Tam, SK-OV-3, LNCaP and PC3 human cancer cell lines than SAHA.

Partial Nitrification of Wastewater with Strong N for Anaerobic Nitrogen Removal (혐기성 질소제거를 위한 고농도 질소폐수의 부분질산화)

  • Hwang, In-Su;Min, Kyung-Sok
    • Journal of Korean Society of Environmental Engineers
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    • v.28 no.4
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    • pp.414-420
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    • 2006
  • Effluent from an anaerobic digestion system with an elutriated phased treatment(ADEPT, Anaeorbic Digestion Elutriated Phase Treatment) for piggery waste treatment using anaerobic ammonium oxidation(ANAMMOX) process was used as a substrate of partial nitrification reactor. In mesophilic condition($35^{\circ}C$), controlling parameters of nitrite accumulation were HRT, pH, free ammonia(FA) and hydroxylamine rather than dissolved oxygen. Bicarbonate alkalinity consumption ratio including bicarbonate stripping and buffering was 8.78 g $Alk._{comsumed}/g\;NH_4-N_{converted}$. In steady state for 1 day of HRT and $2.7{\sim}4.4mg/L$ of DO, $NO_2-N/NH_4-N$ ratio of partial nitrification effluent was about $1{\sim}3$, which was applicable to ANAMMOX reactor influent for the combined partial nitrification-ANAMMOX process.

Production, isolation and characterization of the antibiotic from Pseudomonas aeruginosa 3120 (Pseudomonas aeruginosa 3120으로부터 항생물질의 생산,분리 및 특성)

  • Ko, Hack-Ryong;Chun, Hyo-Kon;Kho, Yung-Hee;Sung, Nack-Kie
    • Applied Biological Chemistry
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    • v.36 no.6
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    • pp.428-433
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    • 1993
  • A strain that inhibited the growth of Pellicularia sasakii was isolated from the soil and identified as Pseudomonas aeruginosa 3120. A dark brownish antibiotic, MRL3120 isolated and purified from the culture broth of P. aeruginosa 3120 was soluble in ethylacetate, chloroform and methanol, and it was active against gram-positive and negative bacteria as well as fungi. The structure of MRL3120 was identified as a chelate compound consisting of two N-methyl-N-thioformyl-hydroxylamine and a copper ion by the analysis of UV, IR, and EI-MS spectra and other physico-chemical properties and supposed to have a structure of fluopsin C related compound. Addition of $CuSO_4$ into the fermentation medium containing soybean meal increased antifungal activity but no activity was found in the presence of EDTA (0.1%, v/v). However antibiotic MRL3120 was not produced in the fermentation medium containing soytone instead of soybean meal but it was rapidly produced by the addition of $CuSO_4$.

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A Solid Phase Synthesis of Dihydro-1,4-dioxin and Dihydro-1,4-oxathiin Carboxanilides Using Polymer-bound Oxime Ester (고체상에 연결된 옥심 에스테르를 이용한 다이하이드로-1,4-다이옥신 및 다이하이드로-1,4-옥사티인 카르복스아닐라이드 유도체의 고체상 합성)

  • Hahn, Hoh-Gyu;Bae, Su-Yeal;Nam, Kee-Dal
    • The Korean Journal of Pesticide Science
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    • v.10 no.1
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    • pp.1-6
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    • 2006
  • A methodology for the syntheses of carboxanilides using solid support of 4-chloro-3-nitorbenzophenone oxime resin 5 was developed. Condensation of 4-chloro-3-nitorbenzophenone resin 6 with hydroxylamine hydrochloride salt gave oxime resin 5. The reaction of oxime resin 5 with dioxin and oxathiin derivatives 7a-d afforded the corresponding polymer-bound dioxin and oxathiin derivatives 9a-d. These polymer-bound resins 9a-d were treated respectively with aniline in the presence of acetic acid resulted in the corresponding dioxin carboxanilides 10a-d (yield, 5%-quantitative).

Purification and Characterization of a Maltopentaose-producing Amylase from Bacillus megaterium KSM B-404. (Bacillus megaterium KSM B-404으로부터 생산되는 Maltopentaose생성 Amylase의 정제 및 특성)

  • 박제원;김병주;이재우;김영배
    • Microbiology and Biotechnology Letters
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    • v.30 no.4
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    • pp.352-358
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    • 2002
  • An amylase that hydrolyzes starch into maltopentaose as a main product was found in the culture supernatant of a strain of Bacillus megaterium KSM B-404 isolated from local soil. The enzyme was purified 129-fold by ammonium sulfate precipitation, DEAE-Toyopearl and Superdex 75 HR 10/30 column using a FPLC system. The molecular weight of the amylase was determined as about 68 kDa by using SDS-PAGE. Optimum pH and temperature of amylase were found to be $50^{\circ}C$ and pH 6.0~7.0, respectively. The enzyme was stable up to $60^{\circ}C$ by addition of $Ca^{2+}$ and its pH stability was in the range of 6.0~10.0. The activity of enzyme was inhibited by $Cu^{2+}$ $Hg^{2+}$ , and $Fe^{3+}$ and maintained by $Ca^{2+}$ and $Mg^{2+}$ . EDTA and pCMB also showed inhibitory effect to the enzyme. TLC and HPLC analysis of the products of the enzyme reaction showed the presence of maltopentaose(52%), maltotriose (25%), maltose (11%), glucose, and maltotetraose in the starch hydrolysates.

Developement of novel enzyme system for production of enantiomerically pure ${\beta}-amino$ acids : Kinetic resolution of racemic 3-amino-n-butanoic acid using transaminase from Alcaligenes denitrificans Y2k-2

  • Im, Seong-Yeop;Jo, Byeong-Gwan;Kim, Byeong-Gi
    • 한국생물공학회:학술대회논문집
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    • 2000.11a
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    • pp.579-582
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    • 2000
  • (R,S)-3-amino-n-butanoic acid$(DL-\;{\beta}\;-homoalanine)$ has been kinetically resolved using Alcaligenes denitrificans Y2k-2 as a biocatalyst, which was isolated from soil by enrichment culture, which was carried out with minimal media containing (R,S)-3-amino-n-butanoic acid as a sole nitrogen source. The enzyme which peformed this kinetic resolution assumed to belong to the ${\omega}-transaminase$ family, because A. denitrificans used pyruvate as amino acceptor and its transaminase activity was inhibited by gabaculine, aminooxy acetic acid and hydroxylamine. In whole cell reaction, (R,S)-3-amino-n-butanoic acid was kinetically resolved to the corresponding (R)-3-amino-n-butanoic acid with excellent E (>100) in the presence of pyruvate as an amino acceptor at $37^{\circ}C$. (S-specific) We observed the substrate inhibition for pyruvate at 100mM. In this study, characteristics of transaminase activity of Alcaligenes denitrificans Y2k-2, such as substrate specificity and thermostability, are carried out for the development of (R)-3- amino-n-butanoic acid production system.

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Biochemical characterization of Alanine racemase- a spore protein produced by Bacillus anthracis

  • Kanodia, Shivani;Agarwal, Shivangi;Singh, Priyanka;Agarwal, Shivani;Singh, Preeti;Bhatnagar, Rakesh
    • BMB Reports
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    • v.42 no.1
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    • pp.47-52
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    • 2009
  • Alanine racemase catalyzes the interconversion of L-alanine and D-alanine and plays a crucial role in spore germination and cell wall biosynthesis. In this study, alanine racemase produced by Bacillus anthracis was expressed and purified as a monomer in Escherichia coli and the importance of lysine 41 in the cofactor binding octapeptide and tyrosine 270 in catalysis was evaluated. The native enzyme exhibited an apparent $K_m$ of 3 mM for L-alanine, and a $V_{max}$ of $295\;{\mu}moles/min/mg$, with the optimum activity occurring at $37^{\circ}C$ and a pH of 8-9. The activity observed in the absence of exogenous pyridoxal 5'-phosphate suggested that the cofactor is bound to the enzyme. Additionally, the UV-visible absorption spectra indicated that the activity was pH independece, of VV-visible absorption spectra suggests that the bound PLP exists as a protonated Schiff's base. Furthermore, the loss of activity observed in the apoenzyme suggested that bound PLP is required for catalysis. Finally, the enzyme followed non-competitive and mixed inhibition kinetics for hydroxylamine and propionate with a $K_i$of $160\;{\mu}M$ and 30 mM, respectively.

Isolation of Methylotrophic Actionmycetes Capable of Producing Antagonistic Activity Against Oral Resident Bacteria and Screening of Mutants (구강상재균을 중심으로 항균력을 나타내는 메탄올 자화방선균의 분리 및 변이주 생산)

  • Park, Myoung-Ho;Lee, Hwa-Sik;Bae, Bong-Jin;Kim, Joung
    • Journal of Technologic Dentistry
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    • v.22 no.1
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    • pp.145-152
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    • 2000
  • In order to select an effective antibiotic substance against oral resident bacteria, we were isolated from soil and texonomically analyzed. Seven hundred and eighteen strains were isolated on humic acid- vitamin agar(HV agar) and 220 strains were on methanol medium from three each paddy forest, field and riverside soil samples. So, during the screening of antibiotics from soil, we isolated microorganisms showing powerful antagonistic activity against oral resident bacteria. Microorganism was tested against 25 strains of bacteria, yeast and fungi. Among them, No. 248 strain exhibited the most strongly growth inhibition. So, the taxonomical analysis the isolated strain was found to be unknown Actinomyces sp. and was named No 248. A production of the antibiotics from No. 248 begins at the early exponential phase developed at the 72th hour under the optinum conditions. The property of No. 248 antimicrobial compound was very stable under acid(pH 3.0) and alkali(pH 10.0) treatment, but it was instable in heat treatment at $120^{\circ}C$. For the improvement of antibiotic activity, two mutants were isolated from strain No. 248 by the treatment of mutagenic agents, NTG and hydroxylamine. As a result, the mutant strains excreted the potent antibiotics to inhibit the growth of Candida albicans.

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Construction of Yeast Vectors Potentially Useful for Expression of Eukaryotic Genes as ${\beta}$-galactosidase Fusion Proteins

  • Chung, Kyung-Sook;Choi, Won-Ja;Lee, Hee-Won;Kim, Kyu-Won;Yoo, Hyang-Sook
    • BMB Reports
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    • v.29 no.4
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    • pp.359-364
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    • 1996
  • By both in vitro hydroxylamine mutagenesis of the wild type 3-phosphoglycerate kinase gene (PGK) promoter DNA and insertion of the leu2-d gene, we have created yeast expression vectors potentially useful for production of eukaryotic genes in yeast. The guanine (G) to adenine (A) change at the -3 position from the ATG start codon of the PGK promoter-based vector rendered a 6~7 times elevated expression of the adjacent eukaryotic gene, and insertion of the leu2-d gene in the vector containing the mutated PGK promoter further enhanced the expression of the gene. When expression of the AIDS virus HIV1-gagP17 gene in a lacZ fusion form was examined with this new vector, a 15 times higher level of expression than that from the original PGK promoter was observed. Northern and Southern analysis showed that this elevated expression is due to the production of a high copy number of mRNA by leu2-d gene functioning and by efficient translation of the produced mRNA. Thus, the vector that contained the A at the -3 position from the ATG start codon in the promoter region and the leu2-d gene shows increased expression capability and will be potentially useful for production of eukaryotic genes in yeast.

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Fabrication of Size-Controlled Hole Array by Surface-Catalyzed Chemical Deposition (표면 촉매 화학 반응을 이용한 크기 조절이 가능한 홀 어레이 제작)

  • Park, Hyung Ju;Park, Jeong Won;Lee, Dae-Sik;Pyo, Hyeon-Bong
    • Journal of Sensor Science and Technology
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    • v.27 no.1
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    • pp.55-58
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    • 2018
  • Low-cost and large-scale fabrication method of nanohole array, which comprises nanoscale voids separated by a few tens to a few hundreds of nanometers, has opened up new possibilities in biomolecular sensing as well as novel frontier optical devices. One of the key aspects of the nanohole array research is how to control the hole size following each specific needs of the hole structure. Here, we report the extensive study on the fine control of the hole size within the range of 500-2500 nm via surface-catalyzed chemical deposition. The initial hole structures were prepared via conventional photo-lithography, and the hole size was decreased to a designed value through the surface-catalyzed chemical reduction of the gold ion on the predefined hole surfaces, by simple dipping of the hole array device into the aqueous solution of gold chloride and hydroxylamine. The final hole size was controlled by adjusting reaction time, and the optimal experimental condition was obtained by doing a series of characterization experiments. The characterization of size-controlled hole array was systematically examined on the image results of optical microscopy, field emission scanning electron microscopy(FESEM), atomic-force microscopy(AFM), and total internal reflection microscopy.