• The Korean Journal of Nuclear Medicine
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• v.34 no.3
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• pp.252-259
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• 2000

Purpose: The purpose of this study was to compare the radiation adaptive response (RAR) in peripheral lymphocytes (PL) of patients induced by Tc-99m MDP and Tc-99m DTPA scintigraphies. Materials and Methods: Lymphocytes from 45 patients (25 males, 20 females, mean age $44{\pm}18$ years) were collected before and after scintigraphies using 740 MBq Tc-99m MDP (n=22) or Tc-99m DTPA (n=23). Lymphocytes from 20 controls (12 males, 8 females, mean age $43{\pm}7$ years) were also collected. They were exposed to challenge dose of 2 Gy ${\gamma}-rays$ using a Cs-137 cell irradiator Number of ring-form (R) and dicentric (D) chromosomes was counted under the light microscope. From them a representative score, Ydr, was calculated as Ydr=(D+R)/cells. Adaptation index (AI) was defined as difference of Ydr between unconditioned and conditioned lymphocytes. Ydr was also measured after an administration of cycloheximide (CHM), a protein synthesis inhibitor, before challenge dose. Results: RAR was induced in both groups of patients. CHM abolished the adaptive response in both groups. AI of Tc-99m MDP group was significantly higher than that of Tc-99m BTPA group. Conclusion: Tc-99m MDP induced RAR was more prominent than those induced by Tc-99m DTPA.

• The Korean Journal of Pesticide Science
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• v.8 no.3
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• pp.151-161
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• 2004

Three dimensional quantitative structure-activity relationships (3D-QSAR) studies for the protox inhibition activities against root and shoot of rice plant (Orysa sativa L.) and barnyardgrass (Echinochloa crus-galli) by a series of new A=3,4,5,6-tetrahydrophthalimino, B=3-chloro-4,5,6,7-tetrahydro-2H-indazolyl and C=3,4-dimethylmaleimino group, and R-group substituted on the phenyl ring in 1-(5-methyl-3-phenylisoxazolin-5-yl)methoxy-2chloro-4-fluorobenzene derivatives were performed using comparative molecular field analyses (CoMFA) methodology with Gasteiger-Huckel charge. Four CoMFA models for the protox inhibition activities against root and shoot of the two plants were generated using 46 molecules as training set and the predictive ability of the each models was evaluated against a test set of 8 molecules. And the statistical results of these models with combination (SIH) of standard field, indicator field and H-bond field showed the best predictability of the protox inhibition activities based on the cross-validated value $r^2_{cv.}$ $(q^2=0.635\sim0.924)$, conventional coefficient $(r^2_{ncv.}=0.928\sim0.977)$ and PRESS value $(0.091\sim0.156)$, respectively. The activities exhibited a strong correlation with steric $(74.3\sim87.4%)$, electrostatic $(10.10\sim18.5%)$ and hydrophobic $(1.10\sim8.30%)$ factors of the molecules. The steric feature of molecule may be an important factor for the activities. We founded that an novel selective and higher protox inhibitors between the two plants may be designed by modification of X-subsitutents for barnyardgrass based upon the results obtained from CoMFA analyses.

• Korean Journal of Crystallography
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• v.3 no.1
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• pp.9-22
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• 1992

Two crystal structures of bromine sorption complexes of vacuum dehydrated Cd(ll)-exchanged zeolite A have been determined by single-crystal xray diffraction techniques in the cubic space group Pm3m at 21(1) ℃. Both crystals were ion exchanged in flowing streams of exchange solution In which mole ratio of Cd(NO3)2 and Cd(OOCCH3)B was 1:1 with a total concentration of 0.05 M. First crystal was dehydrated at 450℃ and 2 ×10-6 Torr for two days. Second crystal was dehydrated at 650℃ and 2 ×10-6 Torr for two days. Both crystals were then treated with 160 Torr for two days. Second crystal was dehydrated at 650℃ and 2 × 10-6 Torr for two days. Both crystals were then treated with 160 Torr of zeolitically dried bromine vapor at 24℃. Full-matrix least-squares refinements of toe first crystal(a: 12.250(1) A )· and the second crystal(a: 12.204(2) A ) have contecoed to final error indices, Rl:0.075 and Ra:0.079 with 212 reflections, and Rl : 0.089 and Ra = 0.078 with 128 reflections, respectively, for which I >3σ(I). Crystallographic analyses of both crystals show that six Cd2+ ions are located on two different threefold axes of unit cell associated with 6-ring oxygens. Each 4.5 Cd2+ ion is recessed ca.0. 441 A Into the large cavity to complex either with Brsor with Br3from the (111) plane of 0(3), whereas each 1.5 Cd2+ ions recessed ca. 0.678 A into we sodalite unit. Approximately 1.5 Br5-and 1.5 Br3-ions are sorbed per unit cell. Each Brsion interacts and stabilized by complexing with two Cd2+ ions and framework oxide ions, while each Br3ion interacts with one Cd2+ ion and framework oxide ions. Because of residual water molecules the following reactions may be occurred inside of zeolite cavity:

• Journal of Applied Biological Chemistry
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• v.61 no.1
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• pp.83-91
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• 2018

Advances in bacterial and fungal genome mining uncover a plethora of cryptic secondary metabolite biosynthetic gene clusters. Guided by the genome information, targeted transcriptional derepression could be employed to determine the product of a cryptic gene cluster and to explore its biological role. Monascus spp. are food grade filamentous fungi popular in eastern Asia and several genome data belong to them are now available. We achieved transcription activation of a cryptic fungal polyketide synthase-nonribosomal peptide synthase gene Mpfus1 in Monascus purpureus ${\Delta}MpPKS5$ by inserting Aspergillus gpdA promoter at the upstream of Mpfus1 through double crossover gene replacement. The gene cluster with Mpfus1 show a high similarity to those for the biosynthesis of conjugated polyene derivatives with 2-pyrrolidone ring and the mycotoxin fusarin is the representative member of this group. The ${\Delta}MpPKS5$ is incapable of producing azaphilone pigment, providing an excellent background to identify chromogenic and UV-absorbing compounds. Activation of Mpfus1 resulted in a yellow hue on mycelia and its methanol extract exhibit a maximum absorption at 365 nm. HPLC analysis of the organic extracts indicated the presence of a variety of yellow compounds in the extract. This implies that the product of MpFus1 is metabolically or chemically unstable. LC-MS analysis guided us to predict the MpFus1 product and to propose that the Mpfus1-containing gene cluster encode the biosynthesis of a desmethyl analogue of fusarin. This study showcases the genome mining in Monascus and the possibility to unveil new biological activities embedded in it.

• Microbiology and Biotechnology Letters
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• v.7 no.2
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• pp.75-89
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• 1979

One strain of Penicillium sp. (175-66-B), isolated from soil, was able to produce a substance that has a strong inibition activity against the Agkistrodon and Trimeresurus venoms. In this experiment, the chemical and biological properties of the sample were investigated. As an inhibitory substance, it was effective to the proteinase, hemorrhagic and lethal factors of Agkistrodon and Trimeresurus venoms, and also effective to several fractions of the proteinases and hemorrhagic factors of Agkistrodon halys blomhoffi venom. Moreover, in the addition of prednisotone, it was more effective for the cure of the mouse envenomated with the venom amount of two fold of MLD$_{100}$. This substance was very stable to the acid, alkali and heat. Its melting point was high enough to sublime at 222$^{\circ}C$ without any decomposition. This sample was easily dissolved only in hot water, but not in several organic solvents except for a little dissolution in elate. It did not have the chelating activity. It had very strong specificity to the snake venoms. but its activity was depressed by the addition of zinc or cupric salts. This sample had no acute toxicity to the mouse. Its chemical formula was $C_{16}$ $H_{12}$$N_2$ $O_{10}$ with the molecular weight of about 392. It has two epoxy groups and four carboxyl radicals, but amino, nitrite and nitrate radicals, unsaturated bonds and aromatic ring were not detected. Theuchemical configuration of this sample was suggested to be;

• Applied Biological Chemistry
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• v.39 no.1
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• pp.70-76
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• 1996

A series of the herbicidal pyridylsulfonyl areas, none substitutent, 1-(4,6-dimethoxypyrimidine-2-yl)-3-(2-pyridylsulfonyl) urea, 3 and 3-trifluoromethyl substitutent, 1-(4,6-dimethoxypyrimidine-2-yl)-3-(3-trifluoromethyl-2-pyridylsulfonyl) urea, 5(Flazasulfuron) were synthesizied and the rate of hydrolysis of their has been studied in 25%(v/v) aqueous dioxane at $45^{\circ}C$. From the results of solvent effect($m{\ll}1,\;n{\ll}3\;&\;{\mid}m{\mid}{\ll}{\mid}{\ell}{\mid}$), thermodynamic parameter (${\Delta}S^{\neq}=0.54{\sim}\;-2.19\;e.u.\;&\;{\Delta}H^{\neq}=0.025\;Kcal.mol.^{-1}$), hydrolysis product analysis, $pK_a$ constant(3: 4.9 & 5: lit.4.6) and the rate equation, a marked difference in the kinetics of the reaction of 3 and 5(Flazasulfuron) was observed. It may be concluded that the hydrolysis of 5 proceeds through the $A-S_N2Ar$ reaction via conjugate acid$(5H^+)$ below pH 7.0, whereas, above pH 9.0, the hydrolysis proceeds through irreversibly $(E_1)_{anion}$ and reversibly $(E_1CB)_R$ mechanism via conjugate base(CB), respectively. But in case of 5, $A-S_N2Ar,\;(E_1)anion\;and\;(E_1CB)_R$ mechanism involved Smile rearrangement. The mate of rearrangement of 5 to a 3-trifluoromethyl-2-pyridylpyrimidinyl urea(PPU) in acid and 3-trifluoromethyl-2-pyridyl-4.6-dimethoxypyridinyl amine (PPA) in base was increased about 3.5 times by the introduction of trifluoromethyl group in the 3-position on the 2-pyridyl ring. From the basis of these findings, a possible mechanism for the hydrolysis of 5 was proposed and discussed.

• The Korean Journal of Pesticide Science
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• v.3 no.3
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• pp.11-19
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• 1999

A some of synthesized 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenyl propionamide derivativesa substrates were found to selectivity significantly with both rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-galli) for those her- bicidal activities with post emergence in up land. The selectivity of substrates against rice plant better than that of Fenoxaprop-ethyl. The structure activity relationship (SAR) n the selectivity of N-phenyl substituents were analyzed by the Free-Wilson and Hansch method. The SAR approach against barnyard grass is shown that the optimal ($({\pi})_{opt.}=1.60$) hydrophobicity and electron donating effects ($0<{\sigma}$ & 0$(ES)_{opt.}=0.87$) so that the herbicidal activity against rice plant can be decreased. The significance of these results on the selectivity between barnyard grass and rice plant is discussed. And it is assumed that the 2-ethoxy-3-methoxy-4-dimethylamino group substituent ($pI_{50}$=6.60, 1g/ha) is selected as the most highest herbicidal activity against barngard grass in green house.

• Journal of the Korean Applied Science and Technology
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• v.37 no.5
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• pp.1323-1329
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• 2020

To characterize the molecular structure of PhE-gal synthesized using Escherichia coli 𝛽-gal, NMR (¹H- and ¹³C-) spectroscopy and mass spectrometry of PhE-gal were conducted. ¹H NMR spectrum of PhE-gal showed multiple peaks corresponding to the galactosyl group, which is an evidence of galactosylation on 2-phenylethanol (PhE). Downfield proton peaks at 𝛿_H 7.30~7.21 ppm showed the presence of aromatic protons of PhE as well as benzyl CH₂ protons at 𝛿_H 2.88 ppm. Up field proton peaks at 𝛿_H 4.31 ppm, 4.07 ppm and multiple peaks from 𝛿_H 3.86~3.38 ppm are indicative of galactocylation on PhE. ¹³C NMR spectrum revealed the presence of 12 carbons suggestive of PhE-gal. Among 12 carbon peaks from PhE-gal, the four peaks at 138.7, 129.0, 128.6 and 126.5 were assigned aromatic carbons in the phenyl ring. Three peaks at 129.0, 128.6 and 126.5 showed high intensities, indicating CH aromatic carbons. ¹³C NMR data of PhE-gal showed 6 monosaccharide peaks from galactose and 2 peaks from aliphatic chain of PhE, indicating that PhE-gal was galactosyl PhE. The mass value (sodium adduct ion of PhE-gal, m/z = 307.1181) from mass spectrometry analysis of PhE-gal, and ¹H and ¹³C NMR spectral data were in good agreement with the expecting structure of PhE-gal. We are expecting that through future study it will eventually be able to develop a new additive with low cytotoxicity.

• Economic and Environmental Geology
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• v.36 no.4
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• pp.305-312
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• 2003

This study was performed to delineate the subsurface geology, geologic structure, and distribution pattern of the Palgongsan granitic body, and to reveal the relationship between the Kyeongsang basin and Yongnam massif by gravity survey. The study area is located between the latitude of 35$^{\circ}$45'-36$^{\circ}$21'N and longitude of 128$^{\circ}$15'-129$^{\circ}$00'E. Total of 966 gravity data measured by Seoul National University, KlGAM(Korea Institute of Geology, Mining ＆ Materials), Pusan National University and Yonsei University were used. The Bouguer gravity anomaly in the study area ranges from -12.88 to 26.01 mgal with a mean value of 11.27 mgal. A very low anomaly zone is located in the Yongnam massif in west of the study area. The anomaly value increases going from west to east. A low anomaly distribution in Palgongsan granite and Yongnam massif is interpreted as the effect of their lower density than that of Kyeongsang Super Group. Power spectrum analysis is applied to evaluate the average depth of basement the Kyeongsang Basin and Conrad discontinuity from gravity anomaly. The average depths of density discontinuities are calculated 10.45 km and 4.9 km, and these are interpreted as Conrad discontinuity and depth of basement of the Kyeongsang Basin, respectively. The depth of Palgongsan granite is derived by means of 2-dimensional modeling and it decreases gradually toward the east. The gravity anomaly east of the study area decreases abruptly due to Shingryeong fault and Nogosan ring fault. Two deepest and sharp roots of Palgongsan granite are recognized by 2-dimensional modeling of each profiles. The depths of those roots are 5.3 km on a profile AA' and 7 km on a profile BB' which is the maximum depth of Palgongsan granite. Small granitic bodies are also seen to be intruded around the Palgongsan granite. The root of Palgongsan granite is shown by 3-dimensional analysis based on the interpolation of 2-dimensional modeling along each profiles to exist in the southwest vicinity of Palgongsan granite. The total volume of Palgongsan granite is approximately 31.211 $Km^3$.

• Journal of Life Science
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• v.27 no.2
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• pp.139-148
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• 2017

The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.