• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.97-97
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• 1995

On the combination of antacid, the pharmacokinetics and gastric adhesion of $\^$14/C-aceglutamide aluminum complex($\^$14/C-AGA) were examined in rats. Specially, This study was focused on the drug interaction that the coadministration of antacid may affect the oral absorption and gastric adhesion of aceglutamide aluminum complex(AGA). After the oral administration of $\^$14/C-AGA and antacid to rats, the radioactivity of plasma and urinary recovery was lower than that of $\^$14/C-AGA administered group. Relatively, the cumulative recovery of radioactivity in feces was increased significantly. The comparative bioavailability of $\^$14/C-AGA from the plasma concentration-time curve and urinary recovery was about 60%. in vitro, the effect of antacid in the gastric adhesion of AGA was not significantly different between AGA and AGA/antacid treatment. And it accorded well with the result of in vivo experiment. In conclusion, on the combination of antacid, the oral absorption of AGA was decreased but the gastric adhesion was not affected in respect of drug interaction.

• Journal of Microbiology and Biotechnology
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• v.32 no.8
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• pp.1047-1053
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• 2022

When ptsG, a glucose-specific phosphotransferase system (PTS) component, is deleted in Escherichia coli, growth can be severely poor because of the lack of efficient glucose transport. We discovered a new PTS transport system that could transport glucose through the growth-coupled experimental evolution of ptsG-deficient E. coli C strain under anaerobic conditions. Genome sequencing revealed mutations in agaR, which encodes a repressor of N-acetylgalactosamine (Aga) PTS expression in evolved progeny strains. RT-qPCR analysis showed that the expression of Aga PTS gene increased because of the loss-of-function of agaR. We confirmed the efficient Aga PTS-mediated glucose uptake by genetic complementation and anaerobic fermentation. We discussed the discovery of new glucose transporter in terms of different genetic backgrounds of E. coli strains, and the relationship between the pattern of mixed-acids fermentation and glucose transport rate.

• Journal of Microbiology and Biotechnology
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• v.19 no.3
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• pp.257-264
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• 2009

A $\beta$-agarase gene, agaB34, was functionally cloned from the genomic DNA of a marine bacterium, Agarivorans albus YKW-34. The open reading frame of agaB34 consisted of 1,362 bp encoding 453 amino acids. The deduced amino acid sequence, consisting of a typical N-terminal signal peptide followed by a catalytic domain of glycoside hydrolase family 16 (GH-16) and a carbohydrate-binding module (CBM), showed 37-86% identity to those of agarases belonging to family GH-16. The recombinant enzyme (rAgaB34) with a molecular mass of 49 kDa was produced extracellularly using Escherichia coli $DH5{\alpha}$ as a host. The purified rAgaB34 was a $\beta$-agarase yielding neoagarotetraose (NA4) as the main product. It acted on neoagarohexaose to produce NA4 and neoagarobiose, but it could not further degrade NA4. The maximal activity of rAgaB34 was observed at $30^{\circ}C$ and pH 7.0. It was stable over pH 5.0-9.0 and at temperatures up to $50^{\circ}C$. Its specific activity and $k_{cat}/K_m$ value for agarose were 242 U/mg and $1.7{\times}10^6/sM$, respectively. The activity of rAgaB34 was not affected by metal ions commonly existing in seawater. It was resistant to chelating reagents (EDTA, EGTA), reducing reagents (DTT, $\beta$-mercaptoethanol), and denaturing reagents (SDS and urea). The E. coli cell harboring the pUC18-derived agarase expression vector was able to efficiently excrete agarase into the culture medium. Hence, this expression system might be used to express secretory proteins.

• Journal of Microbiology and Biotechnology
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• v.22 no.11
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• pp.1532-1539
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• 2012

The ${\alpha}$-galactosidase-coding gene agaAJB13 was cloned from Sphingomonas sp. JB13 showing 16S rDNA (1,343 bp) identities of ${\leq}97.2%$ with other identified Sphingomonas strains. agaAJB13 (2,217 bp; 64.9% GC content) encodes a 738-residue polypeptide (AgaAJB13) with a calculated mass of 82.3 kDa. AgaAJB13 showed the highest identity of 61.4% with the putative glycosyl hydrolase family 36 ${\alpha}$-galactosidase from Granulicella mallensis MP5ACTX8 (EFI56085). AgaAJB13 also showed <37% identities with reported protease-resistant or Sphingomonas ${\alpha}$-galactosidases. A sequence analysis revealed different catalytic motifs between reported Sphingomonas ${\alpha}$-galactosidases (KXD and RXXXD) and AgaAJB13 (KWD and SDXXDXXXR). Recombinant AgaAJB13 (rAgaAJB13) was expressed in Escherichia coli BL21 (DE3). The purified rAgaAJB13 was characterized using p-nitrophenyl-${\alpha}$-D-galactopyranoside as the substrate and showed an apparent optimum at pH 5.0 and $60^{\circ}C$ and strong resistance to trypsin and proteinase K digestion. Compared with reported proteaseresistant ${\alpha}$-galactosidases showing thermolability at $50^{\circ}C$ or $60^{\circ}C$ and specific activities of <71 U/mg with or without protease treatments, rAgaAJB13 exhibited a better thermal stability (half-life of >60 min at $60^{\circ}C$) and higher specific activities (225.0-256.5 U/mg). These sequence and enzymatic properties suggest AgaAJB13 is the first identified and characterized Sphingomonas ${\alpha}$-galactosidase, and shows novel protease resistance with a potential value for basic research and industrial applications.

• Archives of Pharmacal Research
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• v.17 no.3
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• pp.145-149
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• 1994

Intravenous administration of hydro-methanolic extract of Cyperus scariosus (3-10 mg/kg) produced hypotensive and bradcardiac effects. These effects remianed unaltered in atropinized animals indicating that cardiovascular effects of the plant extract are not medliated through activation of muscarinic receptors. In the in vitro studies, it suppressed the spontaneous contractions of guinea-pig paired atria, rat ulterus and rabbit jejunum in a concentration-dependent (0.1-1 mg/ml) manner. It also inhibited histanmine or acetylcholine-induced contractions of guinea-pig ieum indicating non-sepcific spasmolytic action. In rabbit aorta, it inhibited norepinephrine $(10\;mu{M)}$ as well as $K^+$ (80mM)-induced contractions at similar concentrations (0.1-1 mg/ml). These data indicate that cyperus scariosus contains $Ca^{2+}$ channel blocker-like constituent(s) which may explain hypotensive effect observed in vivo and the general spasmolytic activity of plant explain its folkloric use in diarrhoea.

• YAKHAK HOEJI
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• v.38 no.6
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• pp.800-805
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• 1994

Antacid(AM, 600 mg/kg=aluminium hydroxide, magnesium hydroxide, and simethicone with a ratio of 1 : 1 : 0.1) and aceglutamide aluminium(AGA, 263 mg/kg)-Effect of the combined preparation containing on the gastric mucosal hexosamine, sialic acid, and aluminium contents adhered to the gastric wall of the rat was investigated. Severe ulcers were produced in rats by injecting of $30\;{\mu}l$ acetic acid(30%) into the subserosal layer of one position in the corpus. When given orally for 15 consecutive days, AM(1,200 mg/kg), AGA(525, 1,050 mg/kg), and the combined preparation significantly decreased the ulcer area. AGA(525, 1,050 mg/kg) and the combined preparation also increased the amount of hexosamine and sialic acid in the intact and ulcerated areas. On the other hand, the contents of hexosamine and sialic acid were not affected by AM (600, 1,200 mg/kg). The amount of aluminium adhered to the gastric wall of the rat was higher in the combined preparation when compared to the AM(600 mg/kg) and AGA(263 mg/kg). The aluminium contents adhered may play an important role protecting mucosa from aggresive action of gastric juice and potenting defensive factors through the increase of mucosa-forming components by AGA.

• Korean Journal of Clinical Pharmacy
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• v.25 no.3
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• pp.171-177
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• 2015

Background: Androgenetic alopecia (AGA), one of alopecias, requires continuous treatment in order to prevent or stop it, and patient's compliance is very important. Currently, only two drugs (finasteride, minoxidil) have been approved for AGA by Food and Drug Administration of United States (US FDA). However, another ${\alpha}-2$ reductase inhibitor, dutasteride, is approved by Korea Ministry of Food and Drug Safety (MFDS) through a phase III trial. For treatment, pharmacotherapy of AGA usually combines topical minoxidil 7% with one of oral <${\alpha}-2$ reductase inhibitor. Objectives: We evaluated the comparative efficacy and adverse effect between topical minoxidil 7%/finasteride 1 mg and topical minoxidil 7%/dutasteride 0.5 mg pharmacotherapy for outpatients with AGA. Also we evaluated the relationship between therapeutic effect and regular hospital visit. Method: This study was performed retrospectively based on electronic medical record (EMR) data of total 98 patients (topical minoxidil 7% with dutasteride 0.5 mg ($Avodart^{(R)}$) or finasteride 1 mg ($Alopecia^{(R)}$, $Propecia^{(R)}$) with diagnosis of AGA from department of dermatology at a secondary hospital from January $1^{st}$, to May $31^{st}$, 2014. Results: The efficacy and adverse event of topical minoxidil 7%/dutasteride 0.5 mg (DUTA group) were 100% and 45.7%, and of topical minoxidil 7%/finasteride 1 mg (FINA group) were 92.1% and 33.3%, respectively. The mean onset time of responses and adverse events in the FINA group were 3.86 months and 4.43 months. Those in the DUTA group were 3.97 months and 5.06 months. Conclusion: Both FINA and DUTA group were highly effective, but the DUTA group showed higher efficacy and adverse effects than those in the FINA group. Dutasteride may be another alternative in AGA treatment.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.17
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• pp.7125-7128
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• 2014

Background: Acquired genetic alterations and presence of sensitizing mutations in the tyrosine kinase domain of EGFR and other signaling molecules have been found in different subsets of primary lung adenocarcinoma. The commonest EGFR mutations are small in frame deletions of exon 19 and a point mutation (L858R) in exon 21, having a combined occurrence of around 90%. The objective of this study was to determine the frequency and types of EGFR mutations in primary lung adenocarcinomas in Pakistan. Materials and Methods: EGFR mutations in tumor samples were screened by multiplex real time PCR. Briefly, DNA from formalin fixed paraffin-embedded tissue was amplified with primers and probes specific to 43 different EGFR mutations in a Cobas z 480 instrument. The assay detects mutations in four exons (18-21) of the EGFR gene. Results: Out of 94 patients, 65 were males and 29 females with a M:F ratio of 2.2: 1. The median age was 62 years (range, 28 - 85 years). In our biopsy samples 70 (74%) cases were of primary lung adenocarcinoma, whereas 24 (26%) were confirmed metastatic adenocarcinoma of primary lung origin. EGFR mutation was positive in 29% of the patients. The highest frequency of L858R was observed in 48% of these, followed by deletion in exon 19 (44%). In addition, other rare mutations such as compound G718X:S768I and insertions in exon 20 insertion were detected in approximately 4% of the patients. Conclusions: This study showed that Del 19 and L858R are the most frequent mutations in Pakistani lung adenocarcinoma patients and around 29% of the patients were found eligible for erlotinib therapy.

• YAKHAK HOEJI
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• v.38 no.5
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• pp.496-503
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• 1994

The combined products of antacids(AM) composed of aluminium hydroxide, magnesium hydroxide, and simethicone with a ratio of 1 : 1 : 0.1 and aceglutamide aluminium(AGA) were assayed for the antiulcer activity. The effect of the antacids(AM) in concurrent treatment with AGA was studied in acute gastric lesion induced by Shay's method, stress, ethanol, and indomethacin, in chronic gastric ulcers induced by acetic acid, and in duodenal ulcer induced by mepirizole. In all experimental models, the combined treatment of AM and AGA in the ratio of 2.3:1 showed significant potentiation in inhibition against acute gastric and duodenal ulcer and revealed a significant potentiation of the healing of chronic gastric ulcer.

• Journal of Microbiology and Biotechnology
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• v.15 no.4
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• pp.800-808
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• 2005

Leuconostoc mesenteroides SY1, an isolate from kimchi, was able to ferment $\alpha$-galactosides, such as melibiose and raffinose. $\alpha$-Galactosidase ($\alpha$-Gal) activity was higher in cells grown on melibiose and raffinose than cells grown on galactose, sucrose, and fructose. $\alpha$-Gal activity was not detected in cells grown on glucose, indicating the operation of carbon catabolite repression (CCR). A 6 kb DNA fragment was PCR amplified using a primer set based on the nucleotide sequence of a putative $\alpha$-galactosidase gene (aga) from L. mesenteroides ATCC 8293. Nucleotide sequencing of the 6 kb fragment confirmed the presence of aga and other genes involved in the galactosides utilization, and the gene order was galR (transcriptional regulator)-aga-gaIK (galactokinase)-gaIT (galactose-1-phosphate uridylyltransferase). Northern blotting experiment showed that aga, gaIK, and gaIT constituted the same operon, that the transcription was induced by galactosides, such as melibiose and raffinose, whereas gaIR was independently transcribed as a monocistronic gene, and that the level of transcription was fairly constant. The aga was overexpressed in E. coli BL21 (DE3) using pET26b(+) vector, and $\alpha$-Gal was accumulated in E. coli as an inclusion body.