• Applied Biological Chemistry
• /
• v.48 no.1
• /
• pp.82-88
• /
• 2005

3D QSAR studies for the fungicidal activities against resistive phytophthora blight (RPC; 95CC7303) and sensitive phytophthora blight (Phytopthora capsici) (SPC; 95CC7105) by a series of new 2-alkoxyphenyl-3-phenylthioisoindoline-1-one derivatives (X: A=propynyl & B=2-chloropropenyl) were studied using comparative molecular field analyses (CoMFA) methodology. The CoMFA models were generated from the two different alignment, atom based fit (AF) alignment and field fit (FF) alignment. The atom based alignment exhibited a higher statistical results than that of field fit alignment. The best models, A3 and A7 using combination fields of H-bond field, standard field, LUMO and HOMO molecular orbital field as additional descriptors were selected to improve the statistic of the present CoMFA models. The statistical results of the two models showed the best predictability of the fungicidal activities based on the cross-validated value $q^2\;(r^2_{cv.}=RPC:\;0.625\;&\;SPC:\;0.834)$, non cross-validated value $(r^2_{ncv.}=RPC:\;0.894\;&\;SPC:\;0.915)$ and PRESS value (RPC: 0.105 & SPC: 0.103), respectively. Based on the findings, the predictive ability and fitness of the model for SPC was better than that of the model for RPC. The fugicidal activities exhibited a strong correlation with steric $(66.8{\sim}82.8%)$, electrostatic $(10.3{\sim}4.6%)$ and molecular orbital field (SPC: HOMO, 12.6% and RPC: LUMO, 22.9%) factors of the molecules. The novel selective character for fungicidal activity between two fungi depend on the positive charge of ortho, meta-positions on the N-phenyl ring and size of hydrophilicity of a substituents on the S-phenyl ring.

• Clinical and Experimental Pediatrics
• /
• v.52 no.2
• /
• pp.159-166
• /
• 2009

Purpose : Iron deficiency anemia (IDA) is one of the most common nutritional deficiencies in children on a weaning diet. We investigated weaning practices in infants and children, as well as their mothers' knowledge about weaning. Methods : We investigated 129 children with IDA and 166 without IDA (aged 6-36 months) who had visited 10 university hospitals between March 2006 and July 2007. We investigated the hematologic values of both groups. A questionnaire on weaning was answered by the mothers of these children. Results : The hematologic values in the IDA group showed a significant difference from those in the comparison group (P<0.05). Children who were solely breastfed until 6 months of age were 85%, 34% (P<0.05), and weaning was started by 6.3, 6.4 months, respectively (P>0.05). Rice gruel, boiled rice, and fruit juice accounted for approximately 80% of the starting foods in both groups (P>0.05). Only 40% of the children in the IDA group had a balanced diet within a month, versus 38% in the comparison group. In response to questions about the necessity of iron-fortified foods for breast-fed infants, less than 50% of mothers in both groups answered correctly. In the IDA group, 42% showed serum ferritin less than 10 ng/mL, while 92% showed serum MCV less than 72 fL. Conclusion : In conclusion, collection of information on history should be thorough for feeding and selective examinations for IDA in high-risk groups. Considering the adaptation period, we suggest beginning children on a weaning diet at 45 months. In addition, we need to educate mothers on weaning practice, especially on the necessity of iron-fortified foods for breast-fed infants.

• The Korean Journal of Pharmacology
• /
• v.28 no.2
• /
• pp.129-136
• /
• 1992

As it has been reported that the depolarization-induced acetylcholine (ACh) release is modulated by activation of presynaptic $A_1-adenosine$ heteroreceptor in hippocampus and various lines of evidence indicate the involvement of adenylate cyclase system in $A_1-adenosine$ post-receptor mechanism in hippocampus, it was attempted to delineate the role of adenylate cyclase system in the $A_1-receptor-mediated$ control of ACh release in this study. Slices from rat hippocampus were incubated with $[^3H]-choline$ and the release of the labelled products was evoked by electrical stimulation $(3\;Hz,\;5\;Vcm^{-1},\;2\;ms,\;rectangular\;pulses)$, and the influence of various agents on the evoked tritium-outflow was investigated. $N^6-cyclopentyladenosine$ (CPA), a specific $A_1-adenosine$ receptor agonist, in concentrations ranging from 0.1 to $10\;{\mu}M$, decreased the $[^3H]-ACh$ release in a dose-dependent manner without the changes of basal rate of release. 8-cyclopentyl-1,3-dipropylxanthine $(DPCPX,\;1{\sim}10\;{\mu}M)$, a selective $A_1-receptor$ antagonist, increased the $[^3H]-ACh$ release in a dose-related fashion with slight increase of basal tritium-release. And the CPA effects were significantly inhibited by DPCPX $(2\;{\mu}M)$ pretreatment and the dose-response curve produced by CPA was shifted to the right. The responses to N-ethylmaleimide $(NEM,\;10\;&\;30\;{\mu}M)$, a SH-alkylating agent of G-protein, were characterized by increments of the evoked ACh-release and the basal release, and the CPA effect were completely abolished by NEM pretreatment. Forskolin, a specific adenylate cyclase activator, in concentrations ranging from 0.3 to $10\;{\mu}M$, increased the evoked ACh-release in a dose-dependent manner and the CPA effects were inhibited by forskolin. These results indicate that the $A_1-adenosine$ heteroreceptor plays an important role in ACh-release via nucleotide-binding protein Gi in the rat hippocampus and that the adenylate cyclase system might be participated in this process.

• The Korean Journal of Physiology and Pharmacology
• /
• v.22 no.2
• /
• pp.203-213
• /
• 2018

Tumor undergo uncontrolled, excessive proliferation leads to hypoxic microenvironment. To fulfill their demand for nutrient, and oxygen, tumor angiogenesis is required. Endothelial progenitor cells (EPCs) have been known to the main source of angiogenesis because of their potential to differentiation into endothelial cells. Therefore, understanding the mechanism of EPC-mediated angiogenesis in hypoxia is critical for development of cancer therapy. Recently, mitochondrial dynamics has emerged as a critical mechanism for cellular function and differentiation under hypoxic conditions. However, the role of mitochondrial dynamics in hypoxia-induced angiogenesis remains to be elucidated. In this study, we demonstrated that hypoxia-induced mitochondrial fission accelerates EPCs bioactivities. We first investigated the effect of hypoxia on EPC-mediated angiogenesis. Cell migration, invasion, and tube formation was significantly increased under hypoxic conditions; expression of EPC surface markers was unchanged. And mitochondrial fission was induced by hypoxia time-dependent manner. We found that hypoxia-induced mitochondrial fission was triggered by dynamin-related protein Drp1, specifically, phosphorylated DRP1 at Ser637, a suppression marker for mitochondrial fission, was impaired in hypoxia time-dependent manner. To confirm the role of DRP1 in EPC-mediated angiogenesis, we analyzed cell bioactivities using Mdivi-1, a selective DRP1 inhibitor, and DRP1 siRNA. DRP1 silencing or Mdivi-1 treatment dramatically reduced cell migration, invasion, and tube formation in EPCs, but the expression of EPC surface markers was unchanged. In conclusion, we uncovered a novel role of mitochondrial fission in hypoxia-induced angiogenesis. Therefore, we suggest that specific modulation of DRP1-mediated mitochondrial dynamics may be a potential therapeutic strategy in EPC-mediated tumor angiogenesis.

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

• The Korean Journal of Pesticide Science
• /
• v.4 no.2
• /
• pp.21-28
• /
• 2000

A new fourty six 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)-N-phenylpro- pionamide derivatives were synthesized and the herbicidal activities against rice plant and barnyard grass with pre-emergence in down land were measured. The structure activity relationships (SAR) between the activities and physicochemical parameters of the substituted(X) N-phenyl group in substrates were analyzed and discussed by Free- Wilson and Hansch method from the basis on the former study (Sung. et. al., 1999). The conditions of selective herbicide activity both the barnyard grass and rice plant are shown that the optimal hydrophobicity, $({\pi})_{opt.}=1.34$ and electron donating with field effect (F<0) of meta and ortho, para-substituted mono or disubstituent on the N-phenyl ring were found to contribute significantly. The herbicidal activities against barnyard grass are roughly the same as the results in up land whereas damage to rice plant in down land more increase than that of up land. Degradation products in water are 2-(4-(6-chloro-2-benzoxazolyloxy)phenoxy)propionic acid ((A)) (obs. pKa=4.35 & obs. logP=4.77) and 6-chloro-2-benzoxazolone (B) (obs. pKa=8.40 & obs. logP=2.90). These results were supposing that the hydrolysis product of substrates, (A) is comparatively absorbed in rice plant but not in barnyard grass. And it is assumed from the SAR equations that the 2,6-dimethyl-4-methoxymethyl group substituent ($pI_{50}=5.41$, 3g/ha) is selected as the most highest herbicidal activity against barnyard grass in green house.

• The Korean Journal of Pesticide Science
• /
• v.13 no.4
• /
• pp.256-261
• /
• 2009

Molinate (S-ethyl hexahydro-1H-azepine-1-carbothioate), a selective, preemergence thiocarbamate herbicide used for grass weed control in rice fields, is being most widely used in Korea. This study was conducted to assess the comparative toxicity of molinate on two aquatic insects, Chironomus riparius and Cloeon dipterum in four larval stages. First-instar larvae of C. riparius appeared to be the most sensitive to acute exposure of molinate with a 48-h $EC_{50}$ of 7.8 mg/L, followed by third instar (48-h $EC_{50}\;=\;22.9\;mg/L$), second instar (48-h $EC_{50}\;=\;25.0\;mg/L$) and fourth instar (48-h $EC_{50}$ > 50 mg/L) larvae. Also, the sensitivity of the larvae of C. dipterum was presented as the same manner of the larvae of C. riparius. The youngest group of larvae of C. riparius appeared to be the most sensitive to molinate, with 96-h $EC_{50}$ values ranged from 14.3 to 24.1 mg/L. The authors assume that the young instar lavae of aquatic insects, Chironomus riparius and Cloeon dipterum are more sensitive to molinate. Also, the authors propose that Mayfly, Cloeon dipterum is well suited as a bioassay organism because it is one of the most vulnerable aquatic insects inhabiting agricultural ecosystem in Korea.

• The Journal of Korean Society for Radiation Therapy
• /
• v.27 no.2
• /
• pp.107-113
• /
• 2015

Purpose : The measurement of skin dose is very important that treatment of breast cancer. On account of the cold or hot dose as compared with prescription dose, it is necessary to analyse the skin dose occurring during the various plan of the breast cancer treatment. At our hospital, we want to apply various analyses using a diversity of dosimeters to the breast cancer treatment. Subjectss and Methods : In the study, the anthropomorphic phantom is used to find out the dose difference of the skin(draining site), scar and others occurring from the tangential treatment plan of breast cancer. We took computed tomography scan of the anthropomorphic phantom and made plans for the treatment planing using open and wedge, Field-in-Field, Dose fluence. Using these, we made a comparative analysis of the dose date points by using the Eclipse. For the dose comparison, we place the anthropomorphic phantom in the treatment room and compared the measurement results by using the TLD and MOSFET on the dose data points. Results : On the central point of treatment planing basis, the upward and downward skin dose measured by the MOSFET was the highest when the fluence was used. The skin dose of inner and outer was distinguished from the figure(5.7% ~ 10.3%) when the measurements were fulfilled by using TLD and MOSFET. The other side of breast dose was the lowest in the open beam, on the other hand, is highest in the Dose fluence plan. In the different kinds of treatment, the dose deviation of inner and outer was the highest, and so this was the same with the TLD and MOSFET measurement case. The outer deviation was highest in the TLD, and the Inner'was highest in the MOSFET. Conclusion : Skin dose in relation to the treatment plan was the highest in the planing using the fluence technique in general and it was supposed that the high dose had been caused by the movement of the MLC. There's some differences among the all the treatment planning, but the sites such as IM node occurring the lack of dose, scar, drain site are needed pay close attention. Using the treatment planning of dose fluence is good to compensate the lack of dose, but It increases the dose of the selective range rather than the overall dose. Therefore, choosing the radiotherapy technique is desirable in the lights of the age and performance of the patient.

• Restorative Dentistry and Endodontics
• /
• v.33 no.6
• /
• pp.537-544
• /
• 2008

Polymerase chain reaction (PCR) can detect bacteria more rapidly than conventional plate counting. However DNA-based assays cannot distinguish between viable and dead cells due to persistence of DNA after cells have lost their vitality. Recently, propidium monoazide (PMA) treatment has been introduced. The purpose of this study is to evaluate the applicability of the PMA treatment and real-time PCR method for cell counting in comparison with plate counting and to evaluate the antibacterial efficacy of 2% CHX on E. faecalis using PMA treatment in combination with real-time PCR. Firstly, to elucidate the relationship between the proportion of viable cells and the real-time PCR signals after PMA treatment, mixtures with different ratios of viable and dead cells were used. Secondly, relative difference of viable cells using PMA treatment in combination with real-time PCR was compared with CFU by plate counting. Lastly, antibacterial efficacy of 2% CHX on E. faecalis was measured using PMA treatment in combination with real-time PCR. The results were as follows : 1. Ct value increased with decreasing proportion of viable E. faecalis. 2. There was correlation between viable cells measured by real-time PCR after PMA treatment and CFU by plate counting until Optical density (OD) value remains under 1.0. However, viable cells measured by real-time PCR after PMA treatment have decreased at 1.5 of OD value while CFU kept increasing. 3. Relative difference of viable E. faecalis decreased more after longer application of 2% CHX.

• The Korean Journal of Pharmacology
• /
• v.30 no.3
• /
• pp.263-272
• /
• 1994

Since it was been reported that the depolarization-induced ACh release is inhibited by activation of presynaptic $A_1-adenosine$ heteroreceptor in hippocampus, a large body of experimental data on the post-receptor mechanism of this process has been accumulated. But, the post-receptor mechanism of presynaptic $A_1-adenosine$ receptor on the ACh release has not been clearly elucidated yet. Therefore, it was attempted to clarify the post-receptor mechanisms of the $A_1-adenosine$ receptor-mediated control of ACh release in this study. Slices from rat hippocampus were equilibrated with $^3H-choline$ and the release of the labelled products was evoked by electrical stimulation (3 Hz, 5 $VCm^{-1}$, 2ms, rectangular pulses), and the influence of various agents on the evoked tritium-outflow was investigated. Adenosine, in concentrations ranging from $0.3{\sim}300\;{\mu}M$, decreased the ACh release in a dose-dependent manner, without affecting the basal rate of release. The adenosine effects were significantly inhibited by $DPCPX\;(2\;{\mu}M)$, a selective $A_1-receptor$ antagonist. The responses to N-ethylmaleimide $(10&30{\mu}M)$, a SH-alkylating agent of G-protein, were characterized by increments of the evoked ACh-release and the basal release, and the adenosine effects were completely abolished by NEM pretreatment. PDB $(1{\sim}10\;{\mu}M)$, a specific protein kinase C (PKC) activator, increased, whereas PMB $(0.03{\sim}1\;mg)$, a PKC inhibitor, decreased the evoked ACh-release, and the adenosine effects were not affected by these agents. Nifedipine $(1\;{\mu}M)$, a $Ca^{2+}\;-channel$ blocker of dihydropyridine analogue, significantly inhibited the adenosine effect, but glibenclamide, a $K^+-channel$ blocker, did not. Finally, 8-bromo cyclic AMP $(100\;&\;300{\mu}M)$, a membrane-permeable analogue of cAMP, did not alter the ACh release, but adenosine effects were inhibited by pretreatment with large dose of 8-br-cAMP $(300\;{\mu}M)$. These results indicate that the decrement of the evoked ACh-release by $A_1-adenosine$ receptor is mediated by the G-protein, and nifedipine-sensitive $Ca^{2+}-channel$ and adenylate cyclase system are coupled partly to this effect, and that protein kinase C and glibenclamide-sensitive $K{^+}-channel$ are not involved in this process.