• Molecules and Cells
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• v.24 no.2
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• pp.294-300
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• 2007

The mammalian glycosylphosphatidylinositol (GPI) anchor consists of three mannoses attached to acylated GlcN-(acyl)PI to form $Man_3$-GlcN-(acyl)PI. The first of the three mannose groups is attached to an intermediate to generate Man-GlcN-(acyl)PI by the first mannosyltransferase (GPI-MT-I). Mammalian and protozoan GPI-MT-I have different substrate specificities. PIG-M encodes the mammalial GPI-MT-I which has 423 amino acids and multiple transmembrane domains. In this work we cloned PIG-M homologues from humans, Plasmodium falciparum (PfPIG-M), and Saccharomyces cerevisiae (GPI14), to test whether they could complement GPI-MT-I-deficient mammalian cells, since this biosynthetic step is likely to be a good target for selective screening of inhibitors against many pathogenic organisms. PfPIG-M partially restored cell surface expression of the GPI-anchored protein CD59 in PIG-M deficient mammalian cells, and first mannose transfer activity in vitro; however, this was not the case for GPI14.

• Bulletin of the Korean Chemical Society
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• v.13 no.4
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• pp.407-413
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• 1992

The chromatographic separation of the stereoisomers of the N-(3,5-dinitrobenzoyl) derivatives of fifteen dipeptide methyl esters and nine dipeptide alkyl esters was investigated on three different chiral stationary phases derived from N-acylated ${\alpha}-arylalkylamines$. Two of these CSPs contain second stereogenic centers. These secondary stereogenic centers of CSPs were proposed to provide secondary effects in terms of chiral recognition. From the elution orders of the four dipeptide stereoisomers and the separation factors of the enantiomeric pairs of the N-(3,5-dinitrobenzoyl) derivatives of the dipeptide alkyl esters having different alkoxy substituents, it was proposed that the intercalation of the alkoxy substituents of dipeptide derivatives between the connecting arm of CSPs may control the magnitude of chiral separations of dipeptide derivatives.

• Archives of Pharmacal Research
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• v.13 no.3
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• pp.257-260
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• 1990

Hantzch's type reaction of methyl acetopyruvate (2a), methyl 3-aminocrotonate (3) and 3-nitrobenzaldehyde (4) led to dimethyl 3-acetyl-6-methyl-4-(3'-nitrophenyl)-2, 5-dicarboxylate (5a) and methyl 2, 6-dimethyl-5-(1', 2'-dioxo-2'-methoxyethyl)-4-(3' nitrophenyl)- 2, 5-dicarboxylate (5a) and methyl 2, 6-dimethyl-5-(1', 2'-dioxo-2'methoxyethyl_4-(3' nitrophenyl)1, 4-dihydropyridine-3-carboxylate (6a) in 26.7 and 9.2% yield, respectively. On the other hand, methyl 2, 60dimethyl-4-(3'-nitrophenyl)-1, 4-dihydropyridine 3-carboxylate (9) was acylated by ethyl oxaly chloride to give methyl 2, 6-dimethyl-5-(1', 2'-dioxo-2'-ethoxyethyl)-4-(3'-nitrophenyl)-a, 4-dihydropyridine-3-carboxylate (6b) in 76.8% yield.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.193.1-193.1
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• 2003

Activity-guided separation for the aerial parts of Rodgersia podophylla A. Gray gave a new acylated flavonoid, quercetin 3-O-${\alpha}$-L-(5$^2$-acetyl)-arabinofuranoside (1), together with six known flavonoids (2-7). Their hepatoprotective activities were determined by using the primary cultures of rat hepatocytes injured by H$_2$O$_2$. Quercetin 3-O-${\alpha}$-L-(3$^2$-acetyl)-arabinofuranoside (3), kaempferol 3-O-${\alpha}$-L-rhamnopyranoside (5) and quercetin 3-O-${\alpha}$-L-rhamnopyranoside (6) exhibited hepatoprotective activities comparable to silybin at the concentration of 50 mM (45.7, 50.8 and 57.3 %, respectively), and the new flavonoid 1 showed hepatoprotective activity at the concentration of 100mM (50.1%).

• Korean Journal of Food Science and Technology
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• v.25 no.2
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• pp.123-129
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• 1993

Physico-chemical properties of the acetylated and raw starch were Investigated with the chucheongbyeo and samkangbyeo. The solubility and swelling power was increased by acylation reaction. The light transmittance was higher in the acetylated rice starch. The blue value of chucheongbyeo and samkangbyeo rice starches were lowered to 10.9% and 16.0%, respectively, by the acylation reaction. The alkali number was 7.6 in the chucheongbyeo rice starch and 7.2 in the samkangbyeo rice starch, whereas acylated starch in the same orders was 55 and 52, respectively. The hardness, adhesion, cohesion of starch gel was increased by the acylation reaction. The temperature of initial gelatinization of the acetylated chucheongbyeo and samkangbyeo rice starch was shown to $59^{\circ}C\;and\;62^{\circ}C$, respectively, lowering $5{\sim}6^{\circ}C$ in temperature by the acylation. The viscosity as well as by the acylation reaction was raised 38% and 14%, respectively. The rice starch particles were shown to plygonal structure. But it were deformed in the acylated starch, and was completely destroyed in the starch which is by gelatinized for 30 min. at $70^{\circ}C$.

• Horticultural Science & Technology
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• v.16 no.3
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• pp.381-384
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• 1998

Intersectional differences in anthocyanin composition were observed in a survey of floral anthocyanins of 27 species in genus Hibiscus (Malvaceae). The most common suits of floral anthocyanins were 3-xylosylglucosides and 3-glucosides of delphinidin and cyanidin in species of section Trichospermum, Fucaria, Trionum, Abelmoschus, and Ketmia. Cyanidin 3-sophoroside was the predominant anthocyanin in species of section Lilibiscus. Six common anthocyanidin 3-glucosides and corresponding malonates were detected only in the species of section Bombycella. These intersectional variation coincided generally with proposed sectional boundaries based on morphological characteristics. Anthocyanin composition was more complicated in self-incompatible species than in self-compatible species. The systematic significance of diverse anthocyanin profile was discussed in the aspect of pollination ecology.

• Journal of Microbiology and Biotechnology
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• v.23 no.5
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• pp.652-655
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• 2013

Diverse p-terphenyl compounds, named curtisians, have been isolated from the fungus Paxillus curtisii, and degradation of wood by this fungus is thought to be progressed by iron chelation of p-terphenyl curtisians. In this study, the iron chelation ability of p-terphenyls has been proved by chrome azurol S (CAS) assay, reducing power, and UV-visible spectroscopic analyses. The catechol moiety of p-terphenyl is an essential factor for the potent iron chelation ability, and thus deacylated curtisian with a tetrahydroxyl moiety in the central ring of p-terphenyl is more effective than acylated curtisians.

• Archives of Pharmacal Research
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• v.27 no.8
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• pp.878-883
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• 2004

Tacrolimus (FK506), which is isolated from Streptomyces tsukubaensis, is a new potent immu-nosuppressant. Because of poor solubility in water, the conventional intravenous dosage forms of tacrolimus contain surfactants such as cremophor EL (BASF Wyandotte Co.) or hydroge-nated polyoxy 60 castor oil (HCO-60) which may cause adverse effects. This study relates to a polymer-tacrolimus conjugate, which can be dissolved in water, formed by chemically binding the sparingly soluble drug, tacrolimus, with the water soluble polymer, methoxypoly(ethylene glycol) (mPEG). Water soluble tacrolimus-mPEG conjugates have been synthesized and shown to be function in vitro as prodrugs. These conjugates are in the form of an ester wherein the 24-, 32- or 24,32-positions are esterified. The desired 24-, 32- or 24,32-esterified com-pounds were obtained by initially acylating of tacrolimus with iodoacetic acid at the 24-,32-, or 24,32-positions and then reacting the resulting acylated tacrolimus with a mPEG in the pres-ence of a base such as sodium bicarbonate. These conjugates were converted again into tac-rolimus by the action of enzymes in human liver homogenate, and the half-lives of the conjugates are approximately 10 min in the homogenate, indicating that the esterified tacroli-mus derivatives may be practically applicable as a prod rug for the immunosuppressant.

• Bulletin of the Korean Chemical Society
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• v.35 no.12
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• pp.3609-3617
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• 2014

A series of compounds containing both 1,3,4-oxadiazole and thiohydantoin were synthesized as a promising scaffold for application in medicinal chemistry. The key step of the synthesis is a microwave-assisted cyclization of semicarbazides possessing a thiohydantoin moiety at one of the acyl termini using $POCl_3$ as a dehydrating reagent. A wide range of semicarbazides were prepared through the substitution of hydrazides with an N-acylated thiohydantoin derived from the cyclization of the corresponding isothiocyanate with an amino acid and subsequent N-acylation of the resultant thiohydrantion. Consequently, the 58 number of 1,3,4-oxadiazole derivatives having a thiohydantoin substituent were prepared in good overall yields.

• Applied Chemistry for Engineering
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• v.3 no.1
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• pp.156-171
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• 1992

Chitin was isolated from crab shell. Chitosan, which was prepared by the deacetylation of chitin, was acylated to obtain N-acetyl(regenerated chitin), N-propionyl, N-butyryl, N-hexanoyl, N-decanoyl and N-maleated chitosans and their metal ion adsorption characteristics of N-acylchitosans were investigated. In order to enhance the adsorptivity, their porous beads were prepared and their adsorptivity with respect to the porosity and the adsorptivities for metal ions($Cu^{2+}$, $Ni^{2+}$, $CO^{2+}$, $Mn^{2+}$, $Ag^{+}$)were investigated. Their metal ion adsorptivities were remarkably imporved compared to those of chitin. As the larger acyl groups were introduced, adsorptivity increased, but that of N-decanoyl chitosan showed some decrease because of steric hindrance of the bulky N-decanoyl group. N-Maleated chitosan containing carboxyl group showed highly improved adsorptivity, and N-acylchitosans showed the good selective adsorption in the mixed metal ions($Cu^{2+}$, $Ni^{2+}$, $CO^{2+}$, $Mn^{2+}$ and $Ag^{+}$). They also showed excellent adsorption characteristics as chelating polymers.