• Archives of Pharmacal Research
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• v.3 no.1
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• pp.7-12
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• 1980

Ampliciline was synthesized from 6-amino-pencillanic acid (6-APA) and D-.alpha. phenylglycine methyl ester by using amplicilin synthesizing enzyme from Peudomonas melanogenum (IAM 1655). The whole cell enzyme was immobilized by entrapping it in the polyacrylamide gel lattices. The polymer used in the enzyme entrapment was made from 150 mg per ml of acrylamide monomer and 8 mg per ml of N, N'-methylenebisacrylamide. About 200 mg/whole cell enzyme was mixed in the polymer for entrapment. The maximal activity retention after immobilization was 56%. The optimal pH values for the whole cell enzyme and the immobilized whole cell enzyme were 6.0 and 5.9, respectively. The optimal temperature for the enzyme activity were the same for both type of preparations. The enzyme stabilities against pH and heat increased for immobilized whole cell enzyme. Immobilized cell was more stable especially in the acidic condition while both type were found to be very suceptible to thermal inactivation at a temperature above 4.deg.C. The kinetic constants obtained from Lineweaver-Burk plot based on two substate reaction mechanism showed somewhat higher value for immobilized whole cell enzyme as compared to the whole cell enzyme : the Km value for 6-APA were 7.0 mM and 12.5 mM while Km values for phenylglycine methyl ester were 4.5 mM and 8.2 mM, respectively. Using the immobilized whole cell enzyme packed in a column reactor, the productivity of ampiciline was studied by varying the flow rate of substrate solution. At the space velocity, SV, 0.14 hr$^{-1}$ the conversion was 45%. Operational stability found in terms of half life was 30 hr at SV = 0.2 hr.

• Archives of Pharmacal Research
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• v.15 no.3
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• pp.251-255
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• 1992

A number of 4-hydroxy-2H (or alkyl)-N-(3-aralkyl-2-thio-1-hydantoinyl)-1, 2-benzothiazine3-carboxamide 1, 1-dioxides were synthesized through the reaction of 4-hydroxy-2H (or alkyl)1, 2-benzothiazine-3-carboxylic methyl ester 1, 1-dioxide and 1-amino-2-thio-3-aralkyl-4-imidazolones in xylene. The compounds synthesized were screened for antinflammatory effect on carrageenin-induced edema in rat and for analgesic effect on acetic acid-induced Writhing syndrome in mice. Most compounds were inhibots of carrageenin-induced rat foot edema and some showed significant antinflammatory activity comparable to that of indomethacin and significant analgesic activity comparable to that of indomethacin and aspirin.

• The Korean Journal of Food And Nutrition
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• v.2 no.2
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• pp.65-71
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• 1989

Deer horn has been used in oriental medicine and folk remedy. It has had much effects on 'health and tonic efficacy' But this word, 'health and tonic efficacy', is very obscure in modern sense This report attempts to investigate their scientific and objective effects among many papers. The biochemical components of antler are composed of pentoses, hexoses, acid mucopolysaccharides, free and ester fatty acids, glycolipids, phospholipids, prostaglandins, sterols, protein and peptides, free amino acids, minerals, hormones etc. Deer horn extract especially increases body weight gain and feed efficiency, and it stimulates the ability of spermatogenesis of animal. However, a few papers have reported concerning the toxicity and side effects of antler.

• Fisheries and Aquatic Sciences
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• v.3 no.3_4
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• pp.188-194
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• 2000

A protease purified from hepatopancreas of shrimp, Penaeus japonicus, had maximum activity at $70^{\circ}C$ and in neutral and alkaline pH ranges. Specific activity at optimum reaction condition of the protease was estimated to be approximately 12 U/mg/min. The protease was stable in neutral and alkaline pH ranges and activity was retained after heat treatment at $50^{\circ}C$ for 30 min. Apparent $K_m$ and $V_{max}$ value against casein substrate were estimated to be $0.29\%$ and $7.8see^{-1}$, respectively, and those against N-CBZ-L-tyrosine p-nitropheny1 ester (CBZ­Tyr-NE) were 0.38 mM and $2,400 see^{-1}$, respectively. The N-termina1 sequence of the protease showed high homology to the trypsin from same species and the proteases from shrimp. Myosin heavy chain (MHC) from shrimp tail meat was the most susceptible to the protease and actin/tropomyosin were degraded progressively during 4 hr incubation, but to a lesser degree than MHC.

• Applied Chemistry for Engineering
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• v.25 no.4
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• pp.392-395
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• 2014

(2S,3S,4S)-3,4-Dihydroxyglutamic acid (DHGA), a biologically active ${\alpha},{\beta}$-dihydroxy-${\gamma}$-amino acid, was efficiently synthesized from a readily available D-serine derivative in 30% overall yield over 11 steps. The key stereoselective $OsO_4$-catalyzed dihydroxylation reaction controlled by an N-diphenylmethylene group on the amino group of ${\gamma}$-amino-${\alpha},{\beta}$-unsaturated (Z)-ester successfully introduced the diol moiety of the intermediate 5a in 86% with more than 10 : 1 diastereomeric ration. Then it was in turn successfully converted to the desired target compound, (2S,3S,4S)-3,4-DHGA, via simple oxidation and hydrolysis in a highly stereoselective manner and a higher yield than the previous syntheses. This result strongly supports that our synthetic methodology of stereoselective $OsO_4$-catalyzed dihydroxylation should be useful in stereoselctive synthesis of various bioactive compounds with an amino diol moiety.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.2
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• pp.319-325
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• 1999

Volatile flavor compounds in Korean salt fermented shrimp on the market were analyzed by vacuum simultaneous distillation solvent extraction/gas chromatography/mass spectrometry/olfac tometry(V SDE/GC/MS/O) and aroma extract dilution anlaysis(AEDA). A total of 32 volatile com pounds were detected by GC/O analysis. Of these, 18 were positively identified, and composed of S containing compounds(5), aldehydes(4), ketones(3), N containing compounds(3), ester(1), alcohol(1) and aromatic hydrocarbon(1). Predominant odorants(Log3FD$\geq$4) in salt fermented shrimp were 2,3 butanedione(sour/buttery), 1 octen 3 one(earthy/mushroom like), dimethyl trisulfide(cooked cabbage /soy sauce like) and 2 acetylthiazole(grainy/nutty). Predominant free amino acids were aspartic acid, glutamic acid(sour and umami taste), arginine, methionine(bitter) and lysine(sweet and bitter) in evaluation of taste value.

• Journal of agriculture & life science
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• v.46 no.3
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• pp.109-118
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• 2012

The gene encoding an esterase enzyme was cloned from a metagenomic library of cow rumen bacteria. The esterase gene (est2R) was 2,120 bp in length, encoding a protein of 516 amino acid residues with a calculated molecular weight of 57,286 Da. The molecular weight of the enzyme was estimated to be 57,000 Da by SDS-PAGE. Est2R shared 35.6% amino acid identity with esterase (CAH19079) of uncultured prokaryote. The Est2R was most active at $20-40^{\circ}C$, and showed optimum at $30^{\circ}C$ and pH 8.0. The most activity of Est2R for the different chain length of p-nitrophenyl ester group as substrate was p-nitrophenyl acetate. Moreover, the enzyme was found to be most active without organic solvent, followed by 98% active with ethanol, and the enzyme activity was highly affected by the acetonitrile. The enzyme was significantly inhibited by $Zn^{2+}$ but stimulated by $Ca^{2+}$. So, novel esterase gene est2R is likely to obtain from cow rumen metagenome and supposed to use for industrial purpose.

• Bulletin of the Korean Chemical Society
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• v.30 no.2
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• pp.435-440
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• 2009

19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a~2l, 3a~3g were synthesized and preliminarily evaluated in vitro against influenza virus $A_3$,B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus $A_3\;(TC_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;19.2\;{\mu}$mol/L, SI = 6.3) and B (T$C_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;29.9\;{\mu}$mol/L, SI = 4.0); 2g was more active against influenza $A_3$ virus at very low cytotoxicity ($TC_{50}\;>\;2092.1\;{\mu}mol/L,\;IC_{50}=\;143.7\;{\mu}mol/L,$ SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;11.3\;{\mu}mol$/L, SI = 17.7 ) and HSV-2 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;20.7\;{\mu}mol$/L , SI = 9.7).

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.24
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• pp.10819-10824
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• 2015

Aims: To explore the effect and probable mechanism of a synthetic retinoid 4-amino-2-tri-fluoromethylphenyl ester (ATPR) on apoptosis of MDA-MB-231 breast cancer cells. Materials and Methods: MTT assays were performed to measure the proliferation of MDA-MB-231 cells treated with different concentrations of all-trans retinoic acid (ATRA) and ATPR. Morphologic changes were observed by microscopy. The apoptosis rates and cell cycling of MDA-MB-231 cells treated with ATRA or ATPR were assessed using flow cytometry analysis. Expression of retinoic acid receptor and phosphorylation of ERK, JNK, p38 proteins were detected by Western blotting. Results: Treatment of the cells with the addition of $15{\mu}mol/L$ ATPR for 48 h clearly demonstrated reduced cell numbers and deformed cells, whereas no changes in the number and morphology were observed after treatment with ATRA. The apoptosis rate was 33.2% after breast cancer MDA-MB-231 cells were treated by ATPR ($15{\mu}mol/L$) whereas ATRA ($15{\mu}mol/L$) had no apoptotic effect. ATPR inhibited the phosphorylation of ERK, JNK, and p38 while ATRA had no significant effect. ATPR inhibited the expression of BiP and increased the expression of Chop at the protein level compared with control groups, ATRA and ATPR both decreased the protein expression of $RXR{\alpha}$, ATPR reduced the protein expression of $RAR{\beta}$ and $RXR{\beta}$ while ATRA did not decrease $RAR{\beta}$ or $RXR{\beta}$. Conclusions: ATPR could induce apoptosis of breast cancer MDA-MB-231 cells, possible mechanisms being binding to $RAR{\beta}/RXR{\beta}$ heterodimers, then activation of ER stress involving the MAPK pathway.

• Journal of Food Hygiene and Safety
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• v.26 no.3
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• pp.242-247
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• 2011

A greening phenomenon has been observed in some plant foods such as chestnut, sweet potato, burdock, and others during processing. The formation of the pigments was postulated as reactions of primary amino compounds with chi orogenic acid or caffeic acid ester, yielding acridine derivatives. Acridine derivatives have been regarded as mutagenetic agents. For the reason, the bacterial reverse mutation test was carried out to evaluate the genotoxicity of green pigment using Salmonella typhimurium TA98 and TA100. Alanine, arginine, aspartic acid, glycine, lysine, and phenylalanine were reacted repectively with chlorogenic acid to synthesize model compound. Green pigment was extracted from sweet potato. Maximum concentration of 2 and 50 mg/plate was tested for the synthetic green pigments and extracted green pigment respectively, taking bacterial survival, solubility, and color intensity into consideration. There was no signigicant increase in the reverse mutation either with or without S9 activation system by any test material. Though further studies with other genotoxicity test system are necessary, both synthetic and sweet potato green pigments seemed not to cause mutation despite the acridine moiety in their structures.