• 약학회지
• /
• 제47권3호
• /
• pp.125-129
• /
• 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.

• Journal of Plant Biotechnology
• /
• 제34권3호
• /
• pp.243-251
• /
• 2007

BRs의 생합성 경로는 $C_{28}-BRs$ 생합성 경로 외에 $C_{27}-BRs$ 생합성 경로가 존재함이 확인되었고, 최근 $C_{29}-BRs$의 생합성 경로가 존재함이 보고되어 BRs의 생합성 과정이 복잡하게 연결되어 있을 가능성이 예상되었다. 이에 $C_{29}-BRs$인 28-homoTE와 28-homoTY 등이 동정된 벼의 유식물을 대상으로 하여 $C_{29}-BR$인 25-homoCS의 대사 과정을 조사하였다. 그 결과 in vitro 효소변환 연구를 통해 28-homoCS은 CS와 26-nor-28-homoCS으로 전환됨을 확인 할 수 있었으며, 그 역반응인 CS에서 28-homoCS로 또는 26-nor-28-homoCS에서 28-homoCS로의 전환은 일어나지 않음을 알 수 있었다. 이는 $C_{29}-BRs$인 28-homoCS은 C-28위치의 demethylation에 의해 보다 강한 활성의 $C_{28}-BRs$인 CS로 생합성 되는 과정과 C-26 위치의 demethylation에 의해 26-nor-28-homoCS으로 생분해 되는 과정이 존재함을 최초로 확인하였다. 한편, $C_{28}-BRs$인 CS에서 BL로의 전환과 동일한 반응이 $C_{29}-BRs$에서도 일어나는지 확인하고자 하였으나 벼 유식물에서는 28-homoCS에서 28-homoBL로 전환되지 않음을 확인 할 수 있었다. 이는 $C_{29}-BRs$와 $C_{28}-BRs$의 생합성과정의 연결이 28-homoCS에서 CS를 통하고 있음을 알 수 있었다. 따라서 28-homoCS에서 CS로 전환되는 과정을 통하여 $C_{29}-BRs$ 또한 $C_{28}-BRs$ 와 동일한 과정을 거쳐 활성형의 CS로 전환됨을 확인 할 수 있었으며, BRs의 생합성은 $C_{27}-BRs$과 $C_{28}-BRs$의 생합성과정이 연결된 것처럼 $C_{29}-BRs$ 또한 $C_{28}-BRs$ 생합성 과정과 연결되어 있음을 확인 할 수 있었다. 즉, 활성형 BR인 CS은 $C_{27}-BRs$, $C_{28}-BRs$의 생합성 과정뿐만 아니라 $C_{29}-BRs$의 생합성 과정을 통하여 생성되는 과정이 식물체내에 존재함을 확인 할 수 있었다.

• Journal of Plant Biotechnology
• /
• 제32권1호
• /
• pp.63-71
• /
• 2005

강낭콩 현탁 배양세포로부터 얻어진 효소원을 이용한 효소 변환 실험을 통하여 동 세포내에 cholesterol$\to$cholestanol과 6-deoxo-28-norteasterone$\leftrightarrow$ 6-deoxo-28-nor-3-dehydroteasterone $\leftrightarrow$ 6-deoxo-28-nortyphasterol$\to$6-deoxo-28-norcastasterone$\to$28-norcastasterone의 생합성과정이 존재함을 확인하였다. 이 결과는 비록 cholestanol에서 6-deoxo-28-norcathasterone을 경유하여 6-deoxo-28-norteasterone로의 변환은 확인하지 못하였지만 동 세포에는 cholesterol에서부터 6-deoxo-28-nor형 brassinosteroids를 경유하여 28-norcastasterone을 생합성하는 모든 효소들이 포함되어 있음을 시사하는 것으로서, 동 세포에는 상기의 생합성과정, 즉 $C_{27}$ brassinosteroids의 the late C-6 oxidation 과정이 작용하고 있음을 나타내는 결과라 하겠다. 또한 얻어진 효소원은 5-adenosyl-methionine과 NADPH의 존재 하에 28-norcastasterone을 castasterone으로 변환시켜, 강낭콩세포내의 $C_{28}$ 활성형 brassinosteroid인 castasterone의 생합성에 $C_{27}$ brassinosteroids 생합성과정이 중요한 경로중 하나임을 알 수 있었다. 이러한 결과들은 이미 본 연구실에서 밝힌 토마토에 있어 $C_{27}$ brassinosteroids 생합성과정이 토마토의 활성형 brassinosteroid인 castasterone의 함량조절에 관여한다는 결과와 함께 토마토 이외의 식물들에 있어서도 $C_{27}$ brassinosteroids 생합성에 의한 활성형 $C_{28}$ brassino-steroid(s)의 함량조절에 일어나고 있음을 처음으로 밝힌 중요한 결과라 하겠다.

• 대한치과기공학회지
• /
• 제10권1호
• /
• pp.55-66
• /
• 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%.

• 생약학회지
• /
• 제17권4호
• /
• pp.292-301
• /
• 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.

• Asian Pacific Journal of Cancer Prevention
• /
• 제16권7호
• /
• pp.3067-3072
• /
• 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.

• 천문학회지
• /
• 제46권3호
• /
• pp.133-140
• /
• 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.

• 대한화학회지
• /
• 제52권1호
• /
• pp.23-29
• /
• 2008

간단한 Keggin형의 텅스텐과 몰리브덴의 헤테로 다중산인, H3PW12O40과 H3PMo12O40는 표준식수에서 34% 과산화 수소와 함께 알코올의 산화를 위한 수분-관용적인 촉매로 사용되어졌다. 우리의 실험결과에 따르면 H3PW12O40는 좋은 수율로 표준식수에서 치환을 위한 간단하고, 효과적이고, 값싼 촉매로 사용되어질 수 있다. 반응 과정 중 25-80 oC에서 다른 용매 효과와 촉매의 농도변화와 기질 또한 연구하였다.

• 대한핵의학회지
• /
• 제33권3호
• /
• pp.298-305
• /
• 1999

목적: PET을 이용하여 도파민운반체를 영상화하는데 유용한 [$^{18}F$]FP-CIT는 그 동안 여러 연구팀들에 의하여 합성이 시도되어졌으나 합성의 난이성 때문에 문제가 되어왔다. 이 연구에서는 새로운 방법에 의하여 유효비방사능이 높은 [$^{18}F$]FP-CIT를 높은 수율로 합성하고자 하였다. 대상 및 방법: [$^{18}F$]Fluoropropyl기를 도입하기 위하여 사용된 3-bromo-1-[$^{18}F$]Fluoropropane은 THF 용매 하에서 3-bromo-propyl-1-triflate $5{\mu}L$와 $nBu_4N^{18}F$를 $80^{\circ}C$에서 2분 동안 가열하여 얻어졌으며 정제하지 않고 직접 알킬화반응에 사용하였다. 이렇게 생성된 3-bromo-1-[$^{18}F$]fluoropropane에 nor-${\beta}$-CIT를 넣고 DMF $5{\sim}6$방울이 함유된 아세토니트릴을 반응용매, $Et_3N$을 생성된 산의 중화제로 사용하여 140f에서 20분동안가열하였다. 생성된 [$^{18}F$]FP-CIT는 HPLC에 의해 정제되고 13% 에탄올이 함유된 생리식염수를 사용하여 제제화하였다. 정도관리는 HPLC 및 방사능 박층크로마토그라피에 의한 분석, pH, 발열성 검사로 이루어졌다. 결과· 3-Bromo-1-[$^{18}F$]Fluoropropane은 3-bromopropyl-1-triflate의 triflate기를 $^{18}F$으로 치환하여 $77{\sim}80%$의 높은 방사화학적 수율로 얻어졌으며 같은 반응용기에 nor-${\beta}$-CIT를 넣고 $140^{\circ}C$의 반응온도에서 아세토니트릴과 최소량의 DMF를 사용하여 알킬화반응을 실행하였다. 이때 DMF의 높은 극성과 비점 때문에 HPLC로 정제할 때 문제가 되었으므로 초기에 0.8% $Et_3N$을 포함한 물만을 사용하는 정제방법을 개발하였다. [$^{18}F$]FP-CIT의 동정은 비방사성 동일물질인 FP-CIT와 동시에 HPLC에 주입하여 확인되었다. [$^{18}F$]FP-CIT의 정도관리를 실행한 결과, 방사화학적 순도는 99% 이상, 유효비방사능은 $37GBq/{\mu}mol$ 이상으로 우수하였으며 총 감쇠보정된 방사화학적 수율도 $5{\sim}10%$로 높았다. 최종생성물의 pH는 약 7.0이었으며 발열물질은 없었다. 결론: 이 연구에서는 [$^{18}F$]fluorination 반응의 전구물질로서 3-bromopropyl-1-triflate를 사용하였고 HPLC 정제 조건을 새롭게 개발함으로써 유효비방사능이 높고 비교적 수율도 높은 [$^{18}F$]FP-CIT를 합성하는 새로운 방법을 확립하였다. 이 [$^{18}F$]FP-CIT는 뇌 도파민운반체의 체내 연구에 유용하게 사용될 것으로 사료된다.

• The Korean Journal of Physiology and Pharmacology
• /
• 제24권4호
• /
• pp.339-348
• /
• 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 (T3_1d) and 3 (T3_3d) 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 T3_1d and T3_3d rats were unmodified. T3_3d, but not T3_1d, 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 T3_3d rats. In endothelium-denuded aortas of T3_3d 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, T3_3d-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.