• Title/Summary/Keyword: NOR-3

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Topoisomerase I Inhibition of 2-Substituted 5-Nitrobenzimidazoles (2 위치가 치환된 5-니트로 Benzimidazole 유도체들의 Topoisomerase I 억제 활성)

  • ;Edmond J. LaVoie
    • YAKHAK HOEJI
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    • v.47 no.3
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    • pp.125-129
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    • 2003
  • A series of 2-phenyl-5-nitrobenzimidazoles substituted at the para positon of the 2-phenyl moiety was synthesized & evaluated for their activity to inhibit topoisomerase I. The structure-activity relationship study revealed that neither the electronic nor lipophilic parameters were related to the topoisomerase I inhibition. A strict spatial requirement seems to be present for retention of topoisomerase I inhibition activity.

Metabolic Study on C29-Brassinosteroids in Young Rice Plants (벼 유식물을 이용한 C29-Brassinosteroids의 대사)

  • Won, So-Yun;Joo, Se-Hwan;Kim, Seong-Ki
    • Journal of Plant Biotechnology
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    • v.34 no.3
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    • pp.243-251
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    • 2007
  • It has been recently demonstrated the presence of not only $C_{28}-BRs$ biosysnthesis, but also $C_{27}-$ and $C_{29}-BRs$ biosynthesis in plants, suggesting that BRs biosynthesis are complicatedly connected to produce biologically active BR (s). This prompted us to investigation of metabolism of a $C_{29}-BR$, 28-homoCS in seedlings of rice from which $C_{29}-BRs$ such as 28-homoTE and 28-homoTY have been identified. In vitro enzyme conversion study using a crude enzyme solution prepared from rice seedlings revealed that 28-homoCS is converted into both CS and 26-nor-28-homoCS, but their reversed reaction did not occur. This indicated that 28-homoCS is biosynthetically converted into more biologically active $C_{28}-BR$, CS by C-28 demethylation and biodegraded into 26-nor-28-homoCS by C-26 demethylation. Next, bio-conversion of 28-homoCS to 28-homoBL was examined by the same enzyme solution. No 28-homoBL as a metabolite of 28-homoCS was detected, meaning that biosynthetic reaction for 28-homoCS to 28-homoBL is not contained, and main connection of $C_{28}-BRs$ and $C_{29}-BRs$ biosynthesis is between CS and 28-homoCS in the rice seedling. This study is the first demonstrated that $C_{29}-BRs$ and $C_{28}-BRs$ bionsynthetic pathways are connected, and that $C_{29}-BRs$ biosynthetic pathway is an alternative biosynthetic pathway to produce more biologically active $C_{28}-BR$, CS in plant.

Ability for Biosynthesis of C27 Brassinosteroids by an Enzyme Pool Prepared from Cultured Cells of Phaseolus vulgaris (강낭콩 현탁배양세포에서 추출된 Enzyme Pool의 C27 Brassinosteroids 합성 능력)

  • Kim Tae-Wuk;Joo Se-Hwan;Kim Seong-Ki
    • Journal of Plant Biotechnology
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    • v.32 no.1
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    • pp.63-71
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    • 2005
  • A cell-free enzyme solution prepared from suspension cultured cells of Phaseolus vulgaris successfully mediated conversions of cholesterol $\to$ cholestanol and 6-deoxo-28-norteasterone $\leftrightarrow$ 6-deoxo-28-nor-3-dehydroteasterone $\leftrightarrow$ 6-deoxo-28-nortyphasterol $\to$ 6-deoxo-28-norcastasterone $\to$ 28-norcastasterone. Al-though conversion of cholestanol to 6-deoxo-28-norteasterone intermediated by 6-deoxo-28-norcathasterone was not demonstrated, this strongly suggests that a complete set of biosynthetic enzymes catalyzing reactions from cholesterol to 28-norcastasterone via 6-deoxo-28-nor type brassinosteroids is endogenously present in the cells, which demonstrates that a $C_{27}$ brassinosteroids biosynthetic pathway, namely the late C-6 oxidation for $C_{27}$ brassinosteroids, is operative in the cells. Additionally, the enzyme solution mediated conversion of 28-norcastasterone to castasterone in the presence of S-adenosyl-methionine and NADPH, providing that the $C_{27}$ brassinosteroids biosynthesis is an important route to generate castasterone in the cells. Together with our previous finding that castasterone can be biosynthesized by the same biosynthetic pathway in tomato, this study demonstrates that the $C_{27}$ brassinosteroids biosynthesis is a common alternative process to maintain endo-genous level of castasterone, an active $C_{28}$ brassinosteroid, in plants.

A Study on Satisfactory degree of Dental Laboratory Heads about Dental Technician Who Graduated from Junior College in Pusan (부산지역(釜山地域) 치과기공소운영자(齒科技工所運營子)의 전문대학(專門大學) 치과기공과출신(齒科技工科出身) 치과기공사(齒科技工士)에 관(關)한 만족도(滿足度) 조사(調査))

  • Lee, Myung-Kon
    • Journal of Technologic Dentistry
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    • v.10 no.1
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    • pp.55-66
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    • 1988
  • The great sudden change of circle of dental laboratory technology brought many discord between the new growing environmental group and the old group. In order to know the satisfactory degree of Dental Laboratory Heads about all and woman dental technicians who graduated from junior college, this study was conducted for 41 dental laboratory heads in Pusan area during Aug. to Sep. 1986 by means of a questionaire. The results are obtained as follows : 1. By born place, the dental laboratory heads’ satisfactory degree mean of items about all dental technician who graduated from junior college were Pusan group 3.55, Kyungnam group 2.94. The difference among the groups was significant enough(P<0.05). The satisfactory degree about woman dental technician graduated from junior college were Pusan group 3.45, Kyungnam group 2.72. 2. By age, The degree of satisfaction of items about all graduate dental technician were 30$\sim$34 age group 3.13, 40$\sim$44 age group 2.71. The degree of satisfaction about woman graduate dental technician were 30$\sim$34 age group 3.13, 40$\sim$44 age group 2.71. The degree of satisfaction about woman graduate dental technician were as follow : 35$\sim$39 age group 3.50, 45$\sim$49 age group 3.16, 30$\sim$34 age group 2.86, 40$\sim$44 age group 2.43. 3. By job career, the highest degree item out of satisfaction about all graduate dental technician was 6$\sim$10 years group 3.58, the other items were 1$\sim$15 years group 2.90, 16$\sim$20 years group 2.71. The satisfactory degree item about woman graduate dental technician was 6$\sim$10 years group 3.43, 16$\sim$20 years group 3.15, 11$\sim$15 years group 2.82 respectively. 4. By managing term of respondents’ dental laboratory, the satisfactory degree of items about all graduate dental technician were below 2 years group 3.25, 3$\sim$6 years group 3.14, 7$\sim$10 years group 2.93 in order. The satisfactory degree items about woman graduate dental technician were 11$\sim$14 years group 3.25, 3$\sim$6 years group 3.14 7$\sim$10 years group 2.80 in order. 5. By acquired qualification of licence test, the satisfactory degree of dental laboratory heads about all graduate dental technician were job career group 3.07, graduated from Dept. of Dental Technology group 3.00. The satisfactory degree about woman graduate dental technician were job career group 3.03 and graduated from Dept. of Dental Technology group 2.57. 6. By dental technician numbers of respondents’ dental laboratory. the satisfactory degree of items was as follow: 10$\sim$13 persons group is 2.86, 6$\sim$9 persons group 3.25, below 5 persons group 3.11. There was significant enough.(P<0.01). The satisfactory degree items about woman graduate dental technician were below 5 persons group is 3.00, 10$\sim$13 persons group 2.79, 6$\sim$9 persons group 2.67. 7. by the outlook of occupation, the satisfactory degree of dental laboratory heads about all dental technicians who graduated from junior college were neither good norbad group 3.20 bad group 2.59, good group 3.13. The difference among the groups was significant enough(P<0.01). The satisfactory degree about woman dental technicains graduated from junior college were good group 3.25, neither good nor bad group 2.80, bad group 2.75. The difference among the groups was significant enough.(P<0.01) 8. By occupational satisfaction, The satisfactory degree of items about all graduate dental technician were neither satisfied nor dissatisfied group 3.08, satisfied group 3.17, dissatisfied group 2.89. The satisfactional degree of items about woman graduate dental technician were satisfied group and neither satisfied mor dissatisfied group each 3.00 9. By the outlook of employment, the satisfactory degree of items about all graduate dental techician were bad group and neither good nor bad group 3.00. There was significant enough.(p<0.02) About woman graduate dental technician were good group 3.80, neither good nor bad group 3.00, bad group 2.84. The difference among the groups was significant enough.(P<0.01) 10. By cognition of the number of graduate dental technician, the satisfactory degree of dental laboratory heads about all graduate dantal technician were too many group 2.86, many group 3.32. There was significant enough.(P<0.05) About woman graduate dental techician were too many group 2.60, many group 3.20 The difference among the groups was significant enough.(P<0.01) 11. As compared with the items ut of satisfaction and improvement about all dental technician who graduated from junior college, the rate of satisfaction item was for as follow : dental technological theory is 5.21%, ability of adaptation and sincerity each 17.1%. The rate of improvement items was as follow : sincerity is 39%, ability of work and ability of basical work each 24.4%. 12. As compared with the items out of satisfaction and improvement about woman dental laboratory technician who graduated from junior college, the rate of satisfaction item was as follow : atmosphere of the office is 56.1%, sincerity 22%. The rate of improvement items was as follow : ability of adaptation is 36.6%, ability of work 31.7%.

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Pharmacological Actions of the Combined Preparations, 'Sahyangsohap-won' and 'Woohwangporyong-hwan' (사향소합원 및 우황포룡환의 약효 연구)

  • Lee, Eun-Bang;Han, Yong-Nam
    • Korean Journal of Pharmacognosy
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    • v.17 no.4
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    • pp.292-301
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    • 1986
  • The combined preparations of the traditional Korean prescriptions, Sahyangsohap-won (A1) and Woohwangporyong-hwan (B1) were evaluated on pharmacological actions in rats and mice, in parallel with the preparations of their modified prescriptions (A2 and B2). The acute toxicities of the four preparations were very low of which $LD_{50}$ values were more than 4g/kg, p.o. and no systematic symptoms were found at the doses. All the preparations showed sedative action by prolongation of sleeping time induced with hexobarbital sodium. The action was more potent in the modified preparations than in the original ones. All the preparations had no anticonvulsant action both in chemoshock seizures induced by pentetrazole and strychnine and in electroshock seizure. In rat fundus preparation, A1 and A2 elicited strong contraction at the concentration of $1{\times}10^{-3}\;g/ml$ in bath, whereas B1 and B2 did neither contraction nor relaxation at the same concentration. The four preparations had no inhibitory effect against acetylcholine induced spasm. In rat intestinal preparation, the four preparations exhibited neither contraction nor relaxation. However, A1 and A2 had antagonistic effect against spasm at the concentration of $1{\times}10^{-3}\;g/ml$. Single administration of each preparation at the dose of 0.24g/kg, p.o. stimulated the secretion of pepsin in rat stomach without inciting the secretion of gastric juice. Their stimulating actions were more marked in B1 and B2 than in A1 and A2, and were more promptly exhibited in the modified preparations (A2 and B2). Accelerating action of bile secretion by single administration of each preparation was found at the dose of 0.24g/kg, p.o. in rats. All the preparations except A2 also stimulated the secretion of bile acid.

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Survival Rates of Cervical Cancer Patients in Malaysia

  • Muhamad, Nor Asiah;Kamaluddin, Muhammad Amir;Adon, Mohd Yusoff;Noh, Mohamed Asyraf;Bakhtiar, Mohammed Faizal;Tamim, Nor Saleha Ibrahim;Mahmud, Siti Haniza;Aris, Tahir
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.7
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    • pp.3067-3072
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    • 2015
  • Cervical cancer is the most common malignant cancer of the female reproductive organs worldwide. Currently, cervical cancer can be prevented by vaccination and detected at an early stage via various screening methods. Malaysia, as a developing country faces a heavy disease burden of cervical cancer as it is the second most common cancer among Malaysian women. This population based study was carried out to fulfil the primary aim of determining the survival rates of Malaysian women with cervical cancer and associated factors. Data were obtained from two different sources namely, the Malaysian National Cancer Registry (MNCR) and National Health Informatics Centre (NHIC) from 1st January 2000 to 31st December 2005. Kaplan Meier analyses were conducted to identify the overall survival rates and median survival time. Differences in survival among different ethnic and age group were compared using the log-rank test. A total of 5,859 patients were included. The median survival time for cervical cancer in this study was 65.8 months and the 5-year survival rate was 71.1%. The overall observed survival rates at 1, 3 and 5 years were 94.1%, 79.3% and 71.1% respectively. The log-rank test finding also showed that there were significant differences in the 5-year survival rate among different ethnic groups. Malays had the lowest survival rate of 59.2% followed by Indians (69.5%) and Chinese (73.8%). The overall 5-year survival rate among patients with cervical cancer in Malaysia is relatively good. Age and ethnic groups remain as significant determining factors for cervical cancer survival rate.

CAN MASSIVE GRAVITY EXPLAIN THE MASS DISCREPANCY-ACCELERATION RELATION OF DISK GALAXIES?

  • Trippe, Sascha
    • Journal of The Korean Astronomical Society
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    • v.46 no.3
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    • pp.133-140
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    • 2013
  • The empirical mass discrepancy-acceleration (MDA) relation of disk galaxies provides a key test for models of galactic dynamics. In terms of modified laws of gravity and/or inertia, the MDA relation quantifies the transition from Newtonian to modified dynamics at low centripetal accelerations $a_c{\lesssim}10^{-10}ms^{-2}$. As yet, neither dynamical models based on dark matter nor proposed modifications of the laws of gravity/inertia have predicted the functional form of the MDA relation. In this work, I revisit the MDA data and compare them to four different theoretical scaling laws. Three of these scaling laws are entirely empirical; the fourth one - the "simple ${\mu}$" function of Modified Newtonian Dynamics - derives from a toy model of gravity based on massive gravitons (the "graviton picture"). All theoretical MDA relations comprise one free parameter of the dimension of an acceleration, Milgrom's constant aM. I find that the "simple ${\mu}$" function provides a good fit to the data free of notable systematic residuals and provides the best fit among the four scaling laws tested. The best-fit value of Milgrom's constant is $a_M=(1.06{\pm}0.05){\times}10^{-10}ms^{-2}$. Given the successful prediction of the functional form of the MDA relation, plus an overall agreement with the observed kinematics of stellar systems spanning eight orders of magnitude in size and 14 orders of magnitude in mass, I conclude that the "graviton picture" is sufficient (albeit probably not a necessary nor unique approach) to describe galactic dynamics on all scales well beyond the scale of the solar system. This suggests that, at least on galactic scales, gravity behaves as if it was mediated by massive particles.

Simple Heteropoly Acids as Water-Tolerant Catalysts in the Oxidation of Alcohols with 34% Hydrogen Peroxide, A Mechanistic Approach (34% 과산화 수소와 함께 알코올의 산화에서 수분-관용적인 촉매로서의 간단한 헤테로 다중산)

  • Tayebee, Reza
    • Journal of the Korean Chemical Society
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    • v.52 no.1
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    • pp.23-29
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    • 2008
  • Simple Keggin type tungsten and molybdenum heteropoly acids, H3PW12O40 and H3PMo12O40, were usedas water-tolerant catalysts for the oxidation of alcohols with 34% hydrogen peroxide in normal drinking water. Accordingto our findings, H3PW12O40 may be used as a simple, effective, and cheap catalyst for this type of transformation in nor-mal drinking water with excelent yields. Efects of diferent solvents at 25-80oC and changing concentration of catalystand substrate on the reaction progress were also studied.

Synthesis of a Dopamine Transporter Imaging Agent, N-(3-[$^{18}F$]fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane (도파민운반체 방사성추적자 N-(3-[$^{18}F$Fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane의 합성)

  • Choe, Yearn-Seong;Oh, Seung-Jun;Chi, Dae-Yoon;Kim, Sang-Eun;Choi, Yong;Lee, Kyung-Han;Kim, Byung-Tae
    • The Korean Journal of Nuclear Medicine
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    • v.33 no.3
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    • pp.298-305
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    • 1999
  • Purpose: N-(3-[$^{18}F$]Fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane [$^{18}F$]FP-CIT) has been shown to be very useful for imaging the dopamine transporter. However, synthesis of this radiotracer is somewhat troublesome. In this study, we used a new method for the preparation of [$^{18}F$]FP-CIT to increase radiochemical yield and effective specific activity. Materials and Methods: [$^{18}F$]FP-CIT was prepared by N-alkylation of nor-${\beta}$-CIT (2 mg) with 3-bromo-1-[$^{18}F$]fluoropropane in the presence of $Et_3N$ (5-6 drops of $DMF/CH_3CN$, $140^{\circ}C$, 20 min). 3-Bromo-1-[$^{18}F$]fluoropropane was synthesized from $5{\mu}L$ of 3-bromo-1-trifluoromethanesulfonyloxypropane (3-bromopropyl-1-triflate) and $nBu_4N^{18}F$ at $80^{\circ}C$. The final compound was purified by reverse phase HPLC and formulated in 13% ethanol in saline. Results: 3-Bromo-1-[$^{18}F$]fluoropropane was obtained from 3-bromopropyl-1-triflate and $nBu_4N^{18}F$ in 77-80% yield. N-Alkylation of nor-${\beta}$-CIT with 3-bromo-1-[$^{18}F$]fluoropropane was carried out at $140^{\circ}C$ using acetonitrile containing a small volume of DMF as the solvents. The overall yield of [$^{18}F$]FP-CIT was 5-10% (decay-corrected) with a radiochemical purity higher than 99% and effective specific activity higher than the one reported in the literature based on their HPLC data. The final [$^{18}F$]FP-CIT solution had the optimal pH (7.0) and it was pyrogen-free. Conclusion: In this study, 3-bromopropyl-1-triflate was used as the precursor for the [$^{18}F$]fluorination reaction and new conditions were developed for purification of [$^{18}F$]FP-CIT by HPLC. We established this new method for the preparation of [$^{18}F$]FP-CIT, which gave high effective specific activity and relatively good yield.

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Comparative study of acute in vitro and short-term in vivo triiodothyronine treatments on the contractile activity of isolated rat thoracic aortas

  • Lopez, Ruth Mery;Lopez, Jorge Skiold;Lozano, Jair;Flores, Hector;Carranza, Rosa Angelica;Franco, Antonio;Castillo, Enrique Fernando
    • The Korean Journal of Physiology and Pharmacology
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    • v.24 no.4
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    • pp.339-348
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    • 2020
  • We aimed to characterize the participation of rapid non-genomic and delayed non-genomic/genomic or genomic mechanisms in vasoactive effects to triiodothyronine (T3), emphasizing functional analysis of the involvement of these mechanisms in the genesis of nitric oxide (NO) of endothelial or muscular origin. Influences of in vitro and in vivo T3 treatments on contractile and relaxant responsiveness of isolated rat aortas were studied. In vivo T3-treatment was 500 ㎍·kg-1·d-1, subcutaneous injection, for 1 (T31d) and 3 (T33d) days. In experiments with endothelium-intact aortic rings contracted with phenylephrine, increasing concentrations of T3 did not alter contractility. Likewise, in vitro T3 did not modify relaxant responses induced by acetylcholine or sodium nitroprusside (SNP) nor contractile responses elicited by phenylephrine or angiotensin II in endothelium-intact aortas. Concentration-response curves (CRCs) to acetylcholine and SNP in endothelium-intact aortic rings from T31d and T33d rats were unmodified. T33d, but not T31d, treatment diminished CRCs to phenylephrine in endothelium-intact aortic rings. CRCs to phenylephrine remained significantly depressed in both endothelium-denuded and endothelium-intact, nitric oxide synthase inhibitor-treated, aortas of T33d rats. In endothelium-denuded aortas of T33d rats, CRCs to angiotensin II, and high K+ contractures, were decreased. Thus, in vitro T3 neither modified phenylephrine-induced active tonus nor CRCs to relaxant and contractile agonists in endothelium-intact aortas, discarding rapid non-genomic actions of this hormone in smooth muscle and endothelial cells. Otherwise, T33d-treatment inhibited aortic smooth muscle capacity to contract, but not to relax, in an endothelium- and NO-independent manner. This effect may be mediated by delayed non-genomic/genomic or genomic mechanisms.