• Archives of Pharmacal Research
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• v.14 no.3
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• pp.199-203
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• 1991

7H-thiazolo-[3,2-a]-pyridines as potential antimicrobial agents were prepared by reaction of $\alpha,\beta$-unsaturated nitriles and thioglycolic acid.

• Natural Product Sciences
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• v.20 no.3
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• pp.160-169
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• 2014

44 compounds and 9 minerals were isolated from and detected in the New Zealand deer velvet antler Cervus elaphus var. scoticus L$\ddot{o}$nnberg. The chemical structures of (1 - 26) were identified on the basis of the spectroscopic methods and comparisons with literature, respectively. The structures were identified as cholesterol (CS, 6), 7-keto-CS (7), $7{\beta}$-hydroxy-CS (8), and $7{\alpha}$-hydroxy-CS (9), and included 12 steroid $3{\beta}$-O-(palmitic/stearic/myristic acid esters; PM/SA/MS) [CS-$3{\beta}$-O-PM (1 - 1), CS-$3{\beta}$-O-SA (1 - 2), CS-$3{\beta}$-O-MR (1 - 3), 7-keto-CS-$3{\beta}$-O-PM (2 - 1), 7-keto-CS-$3{\beta}$-O-SA (2 - 2), 7-keto-CS-$3{\beta}$-O-MR (2 - 3), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-SA (3 -1), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-PM (3 - 2), $7{\beta}$-hydroxy-CS-$3{\beta}$-O-MR (3 - 3), $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-SA (4 - 1), $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-PM (4 - 2), and $7{\alpha}$-hydroxy-CS-$3{\beta}$-O-MR (4 - 3)], dinonyl phthalate (5), 8 nucleic acids analogues [uracil (10), deoxyguanosine (11), deoxyuridine (12), uridine (13), deoxyadenosine (14), adenosine (15), inosine (16), and guanosine (17)], and the 9 free amino acids [L-phenylalanine (18), L-isoleucine (19), L-leucine (20), L-tyrosine (21), L-valine (22), L-proline (23), L-threonine (24), L-alanine (25), and L-hydroxyproline (26)]. Also, there are 8 kinds of amino acids [asparagine, serine, glutamine, glycine, histidine, arginine, methionine, and lysine], 2 sialic acids [N-acetylneuraminic acid (27), ketodeoxynonulosonic acid (28)], and 9 minerals [Na > K > Ca > Mg > Fe > Zn > B > Al > Cu] were detected from the autoaminoacid analyzer and ICP spectrometer, HPAEC-PAD/HPLC-FLD, respectively. 9 kinds of oxycholesterol-$3{\beta}$-O-fatty acid ester (2 - 1, 2 - 2, 2 - 3, 3 - 1, 3 - 2, 3 - 3, 4 - 1, 4 - 2, and 4 - 3) and 3 nucleic acids (12, 14, and 15) were isolated from the velvet antler for the first time. 6 kinds of steroids (7, 8, 9, 2 - 1, 3 - 1, and 4 - 1) were examined for their anti-proliferative effects against L1210, P388D1, K562, MEG-01, KG-1, MOLT-4, A549, HepG2, MCF-7, SK-OV-3, and SW-620 cancer cell lines. They showed anti-proliferative effects with $IC_{50}$ values of 0.06, 2.16, 2.42, > 50.0, 1.66 and $8.31{\mu}M$ against L1210, while the values were 24.05, 9.44, 5.22, 0.25. 9.48 and $49.77{\mu}M$ against P388D1, respectively. The others were inactive.

• Journal of Microbiology and Biotechnology
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• v.3 no.3
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• pp.174-180
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• 1993

A strain SMF14 producing an extracellular $\beta$-lactamase was isolated from soil and identified to be a strain of Streptomyces aureofaciens. $\beta$-Lactamase was purified from the cell free culture broth through batchwise hydroxyapatite adsorption, anion exchange chromatography on DEAE Sephadex A-50, gel filtration on Sephadex G-75, and adsorption chromatography on hydroxyapatite. The molecular mass was estimated to be about 43 kDa by SDS-PAGE. The $\beta$-lactamase had substrate specificity to penicillins and it was inhibited by clavulanic acid, being classified to the group 2a of penicillinase.. The optimal reaction pH and temperature were pH 6.0~7.5 and $50^{\circ}C$. The $K_m, and V_{max}$ values of $\beta$-lactamase for penicillin G were calculated to be 1.72 mM and 5.4$\times$$10^5 \mu M \cdot min^{-1}$, respectively.

• The Korean Journal of Pharmacology
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• v.20 no.2
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• pp.35-47
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• 1984

Contents of immunoreactive ${\beta}-endorphin$ and maximum of $^3H-morphine$ binding was measured in the rat midbrain homogenates from different subgroups at 24 hour interval over 24 hours. Animals were adapted to the light-dark cycle(L : D, 12: 12) or constant darkness (D : D, 12 : 12) for 3 weeks. After the adaptation, 0.5ml of physiologic saline or drug was administered twice a day for 2 weeks. A highly significant circadian rhythm with the peak$(94.8{\pm}7.7\;fmole/mg\;protein)$ at 06:00 and the nadir $(27.6{\pm}2.4\;fmole/mg\;protein)$ at 18:00 was observed in constant of group. Constant dark or treatment of reserpine, pargyline, imipramine, amphetamine and chlorpromazine modified the diurnal rhythm in the time of peak and nadir, shape, phase amplitude and 24 hour mean of ${\beta}-endorphin$ contents. Opiate receptor binding by $^3H-morphine$ also showed highly significant diurnal change in control and constant dark adapted rats. Statistical analysis by one-way analysis of variance and two-way analysis of variance indicates that the·re are highly significant differences between the diurnal change of ${\beta}-endorphin$ in control and those constant dark adapted and drug treated groups. However diurnal change of Maximum $^3H-morphine$ binding is closely related to the change of ${\beta}-endorphin$ contents. The results are interpreted with regard to the circadian rhythm of beta-endorphin contents, its modification by psychoactive drugs and possible mechanism of diurnal change of opiate receptor in brain.

• Archives of Pharmacal Research
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• v.27 no.2
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• pp.164-168
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• 2004

The chromatographic separation of the MeOH extract of the aerial parts of Solidago virga-aurea var. gigantea $M_{IQ}$ . (Compositae) led to the isolation of six terpenoids and four phenolic compounds, trans-phytol (1), ent-germacra-4(15),5,10(14 )-trien-1$\alpha$-ol (2), $\beta$-amyrin acetate (3), ent-germacra-4(15),5,10(14)-trien-1$\beta$-ol (4), $\beta$-dictyopterol (5), oleanolic acid (6), kaempferol (7), kaempferol-3-O-rutinoside (8), methyl 3,5-di-O-caffeoyl quinate (9), and 3,5-di-O-caffeoyl quinic acid (10). Their structures were established by chemical and spectroscopic methods. Compounds 4, 5, and 10 showed moderate cytotoxicity against five cultured human tumor cell lines in vitro with its E $D_{50}$ values ranging from 1.52∼18.57 $\mu\textrm{g}$/mL.L.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.48 no.6
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• pp.469-472
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• 2003

The rice bran has been known to contain tocopherols and tocotrienols carrying antioxidant and cholesterol-lowing activities. The content of 8 isomers of vitamin E : $\alpha\textrm{-}$, $\beta\textrm{-}$, $\gamma\textrm{-}$, $\delta\textrm{-}$tocoperols (T) and tocotrienols ($\textrm{T}_3$) were extracted from 18 major rice varieties and quantified with an HPLC. Tested varieties exhibited T, $\textrm{T}_3$ and total vitamin E ($\textrm{TT}_3$) contents ranging 9.1-14.8, 22.4-37.1, 34.9-46.5 mg/100g with averages of 11.1, 28.0, 39.2 mg/100g, respectively. Among tested varieties, Seojinbyeo and Hwasungbyeo showed high T contents and Andabyeo, Damakum were high in $\textrm{T}_3$, and Andabyeo and Seojinbyeo were high in total $\textrm{TT}_3$ contents. Regardless of varieties, the average 8 isomer contents (in mg/100g) were in descending order of $\gamma\textrm{-}$$\textrm{T}_3$(17.9) ＞$\alpha\textrm{-}$$\textrm{T}_3$(8.8) ＞$\alpha\textrm{-}$T (7.8) ＞$\gamma\textrm{-}$T(2.6) ＞$\delta\textrm{-}$$\textrm{T}_3$ (0.9)＞$\beta\textrm{-}$T (0.7)＞$\beta\textrm{-}$$\textrm{T}_3$ (0.4)＞$\delta\textrm{-}$T (0.1). In most varieties, $\gamma\textrm{-}$$\textrm{T}_3$, a strong antioxidant and anticancer compound, consisted 64% of total tocotrienol and 46% of total vitamin E in vice bran.

• Journal of environmental and Sanitary engineering
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• v.21 no.2 s.60
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• pp.57-68
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• 2006

This study was designed to provide basic data on preventive plans by affecting factors that have analysed on musculoskeletal diseases. The survey were conducted from July 1 to 30, 2004 among 600 hair dressers working in Seoul and Gwangju using self-administration questionnaire. The results of this study are summarized as follows: The pain experience rate of musculoskeletal diseases. in the last one yea was 55.2%. 35.7% of respondents answered they had pain on shoulders, 30.6% had pain on legs and feet, 28.9% had pain on waist, 26.8% had hands, fingers and wrist, 22.3% had pain on necks and 17.6% had pain arms and elbows more than disease on necks, shoulders, arms and elbows, hands, fingers and wrists, waist, shoulders legs and feet. The prevalence rate of the last week was 40.3%. The prevalence rate in each body parts of the last week was 23.3% on legs and feet, 21.2% on shoulders, 20.8% on waist, 14.9% on hands, fingers and wrists, 14.4% on necks, 9.3% on arms. The affecting factors on musculoskeletal disease index were analysed by multiple linear regression analysis. there are working posture$(\beta=0.27)$; authority of task$(\beta=0.18)$, self-conscious stress $(\beta=0.16)$, age$(\beta=0.14)$, physical burden from work$(\beta=0.13)$, and task required$(\beta=0.10)$. Determinant coefficients was 22.7%. Based on the results above, working posture, job stress and physical burden from task are highly related with pain. In order to prevent musculoskeletal disease of hairdressers, working posture shall be improved and leisure opportunities to relieve stress, and health management education shall be provided.

• Journal of the Korean Chemical Society
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• v.31 no.4
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• pp.334-343
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• 1987

The Chemical reactions between $NiL_m{^{2+}}\{$Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;Ni(1[14]4-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{\beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}$}\and\ CN^-$ ion were studied by the spectrophotometric method. The equilibrium constants (K_1$) for the 1:1 complex ion, $[NiL_m(CN)]^+\;with\;NiL_m{^{2+}}\;and\;CN^-$ ion were determined in the range of 3 to $25^{\circ}C$. The $K_1\;for\;Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;Ni(1[14]4-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}\;at\;15^{\circ}C$ was 4.7, 5.3, 6.2, 7.5, 9.4, and 9.8, respectively. The values of $K_1$ decreased with increasing temperature. From the temperature effect on equilibrium constant ($K_1$), thermodynamic parameters $({\Delta}H^{\circ},\;{\Delta}S^{\circ},\;{\Delta}G^{\circ})$ for reaction were evaluated and the reaction of $NiL_m{^{2+}}\;and\;CN^-$ ion was exothermic. $NiL_m{^{2+}\;reacts\;with\;CN^-$ ion to give $Ni(CN)_4{^{2-}}$ ion and macrocyclic ligand $(L_m)$. The kinetics of formation of the $Ni(CN)_4{^{2-}}$ ion of varying the $[CN^-],\;[HCN],\;and\;[OH^-]$ have been investigated at 3∼$25^{\circ}C\;and\;0.5M\;NaClO_4$. Maintaining a constant $[CN^-],\;k_{obs}/[CN^-]^2$ increases linearly with increasing [HCN]. In the presence of large quantities of $[OH^-],\;k_{obs}/[CN^-]^2$ also increases linearly with $[OH^-]$. From the temperature effect on kinetic constant (k_{obs})$, parameter of activation $({\Delta}H^{\neq},\;{\Delta}S^{\neq})$ of reaction of $NiL_m{^{2+}}\;with\;CN^-$ ion were determined. For the $Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{\beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}\;series\;{\Delta}H^{\neq}$ gradually decrease as the d-d transition energy, $ν(cm^{-1})$ decrease. And the reaction of the five $NiL_m{^{2+}}\;with\;CN^-$ ion take place by way of equal paths.

• The Korean Journal of Pharmacology
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• v.21 no.2
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• pp.128-141
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• 1985

To investigate the influence of phenobarbital sodium on the action of morphine and on the diurnal rhythms of both opiate receptor binding and ${\beta}-endorphin$ contents, the amount of specifically bound $(^3H)$-morphine and immunoreactive ${\beta}-endorphin$ were measured in the midbrain of phenobarbital-treated rats at 4h intervals in a day. Rats were housed and adapted to a controlled cycle of either 12 h light-12 h dark or 24 h constant dark. After 3 weeks of adaptation, 0.5 ml of physiological saline or phenobarbital sodium (20mg/kg/day, i.p.) were administered twice a day for 2 weeks. Highly significant diurnal rhythms of opiate receptor binding and ${\beta}-endorphin$ were present in rat midbrain. In control group, the peak of maximum $(^3H)$-morphine binding was observed at 22:00 h, whereas the peak of ${\beta}-endorphin$ content was found at 06:00 h. Even in the absence of time cues these diurnal rhythms persisted, but they were highly modified with respect to the wave form as well as differences in the timing of peak and nadir. In the phenobarbital-treated group, these diurnal rhythms were also modified in shape, phase and amplitude, as well as in timing of peak and nadir. In this group, 24 h mean of opiate receptor binding was significantly decreased, while the 24 h mean level of ${\beta}-endorphin$ content was highly increased. However, Kd values in all experimental groups did not change. This indicates that differences in binding were not due to changes in the affinity, but in the number of binding sites. Statistical analysis of regression line indicates that changes of receptor binding were closely correlated with the changes of ${\beta}-endorphin$ content. These results suggest that phenobarbital may influence the action of morphine by changing the number of opiate receptors and that the modification of diurnal rhythm of opiate receptor by the agent is possibly due to changes of ${\beta}-endorphin$ content.

• Food Science and Biotechnology
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• v.17 no.5
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• pp.1060-1065
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• 2008

A novel benzoyl glucoside (4) and 13 known phenolic compounds were isolated from the leaves of Camellia japonica by a guided 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay. The structure of 4 was determined to be 4-hydroxy-2-methoxyphenol 1-O-$\beta$-D-(6'-O-p-hydroxylbenzoyl)-glucopyranoside (camelliadiphenoside). The 13 known compounds were identified as (E)-coniferyl alcohol (1), (-)-epicatechin (2), 4-hydroxyphenol 1-O-$\beta$-D-(6-O-p-hydroxybenzoyl) glucopyranoside (3), naringenin 7-O-$\beta$-D-glucopyranoside (5), quercetin 3-O-$\beta$-L-rhamnopyranosyl(1$\rightarrow$6)-$\beta$-D-glucopyranoside (6), kaempferol 3-O-$\beta$-L-rhamnopyranosyl(1$\rightarrow$6)-$\beta$-D-glucopyranoside (7), (+)-catechin (8), 1,6-di-O-p-hydroxybenzoyl-$\beta$-D-glucopyranoside (9), phloretin 2'-O-$\beta$-D-glucopyranoside (10), quercetin 3-O-$\beta$-D-glucopyranoside (11), quercetin 3-O-$\beta$-D-galactopyranoside (12), kaempferol 3-O-$\beta$-D-galactopyranoside (13), and kaempferol 3-O-$\beta$-D-glucopyranoside (14). Their chemical structures were determined by the spectroscopic data of fast atom bondardment mass spectrometry (FABMS) and nuclear magnetic resonance (NMR). Flavonoids having the catechol moiety showed significantly higher DPPH radical scavenging activity than other isolated compounds having monohydroxy phenyl group.