• Archives of Pharmacal Research
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• 제20권3호
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• pp.253-258
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• 1997

Ten, heretofore unreported, $ 5^I-methyl-5^I-[2-(5-substituted uracil-1-yl)ethyl)]-2^I-oxo-3^I$-methylenetetrahydrofurans (H, F, Cl, Br, I, $ CH_3$,$CF_3$,$CH_2CH_3$,$ CH=CH2$, SePh) (7a-j) were synthesized and evaluated against four cell lines (K-562, FM-3A, P-388 and U-937). For the preparation of ${\alpha}$-methylene-${\gamma}$-butyrolactone-linked to 5-substituted uracils (7a-j), the convenient Reformasky type reaction was employed which involves the treatment of ethyl ${\alpha}$-(bromomethyl)acrylate and zinc with the respective 1-(5-substituted uracil-1-yl)-3-butanone (6a-j). The 5-substituted uracil ketones (6a-j) were directly obtained by the respective Michael type reaction of vinyl methyl ketone with the $K_2CO_3$(or NaH)-treated 5-substituted uracils (5a-j) in the presence of acetic acid in the DMF solvent. The .alpha.-methylene-.gamma.-butyrolactone compounds showing the most significant antitumor activity are 7e, 7f, 7h and 7j (inhibitory concentration $(IC_50)$ ranging from 0.69 to $2.9 {\mu}g/ml$), while 7b, 7g and 7i have shown moderate to significant activity. The compounds 7a, 7c and 7d were found to be inactive. The synthetic intermediate compounds 6a-j were also screened and found marginal to moderate activity where compounds 6b and 6g showed significant activity $(IC_50:0.4~2.8 {\mu}g/ml)$.

• 자원환경지질
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• 제31권2호
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• pp.111-125
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• 1998

Dispersion, migration and enrichment of environmental toxic elements from the Samkwang Au-Ag mine area were investigated based upon major, minor and rare earth element geochemistry. The Samkwang mine area composed mainly of Precambrian granitic gneiss. The mine had been mined for gold and silver, but closed in 1996. According to the X-ray powder diffraction, mineral composition of stream sediments and soils were partly variable mineralogy, which are composed of quartz, orthoclase, plagioclase, amphibole, muscovite, biotite and chlorite, respectively. Major element variations of the host granitic gneiss, stream sediments and soils of mining and non-mining drainage, indicate that those compositions are decrese $Al_2O_3$, $Fe_2O_3$, MgO, $TiO_2$, $P_2O_5$ and LOI with increasing $SiO_2$ respectively. Average compositional ranges (ppm) of minor and/or environmental toxic elements within those samples are revealed as As=<2-4500, Cd=<1-24, Cu=6-117, Sb=1-29, Pb=17-1377 and Zn=32-938, which are extremely high concentrations of sediments from the mining drainage (As=2006, Cd=l1, Cu=71, Pb=587 and Zn=481 ppm, respectively) than concentrations of the other samples and host granitic gneiss. Major elements (average enrichment index=6.53) in all samples are mostly enriched, excepting $SiO_2$, $Na_2O$ and $K_2O$, normalized by composition of host granitic gneiss. Rare earth element (average enrichment index=2.34) are enriched with the sediments from the mining drainage. Minor and/or environmental toxic elements within all samples on the basis of host rock were strongly enriched of all elements (especially As, Br, Cu, Pb and Zn), excepting Ba, Cr, Rb and Sr. Average enrichment index of trace elements in all samples is 15.55 (sediments of mining drainage=37.33). Potentially toxic elements (As, Cd, Cr, Cu, Ni, Pb, and Zn) of the samples revealed that average enrichment index is 46.10 (sediments of mining drainage=80.20, sediments of nonmining drainage=5.35, sediments of confluent drainage=20.22, subsurface soils of mining drainage=7.97 and subsurface soils of non-mining drainage=4.15). Sediments and soils of highly concentrated toxic elements are contained some pyrite, arsenopyrite, sphalerite, galena and goethite.

• 한국지하수토양환경학회지:지하수토양환경
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• 제7권1호
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• pp.63-77
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• 2002

Salinization is an important environmental problem encountered in coastal aquifers. In order to evaluate the salinization problem in the western coastal area of Korea, we have performed a regional hydrochemical study on shallow well groundwaters (N=229) collected within 10 km away from the coastline. The concentrations of analyzed solutes are very wide in range, suggesting that the hydrochemistry is controlled by several processes such as water-rock interaction, seawater mixing, and anthropogenic contamination. Based on the graphical interpretation of cumulative frequency curves for some hydrochemical parameters (esp., $Cl^{-}$ and ${NO_3}^-$), the collected water samples were grouped into two major populations (1) a background population whose chemistry is predominantly affected by water-rock interaction, and (2) an anomalous population which records the potential influences by either seawater mixing or anthropogenic pollution. The threshold values obtained are 34.7 mg/l for $Cl^{-}$ and 37.2 mg/l for ${NO_3}^-$, Using these two constituents, groundwaters were further grouped into four water types as follows (the numbers in parenthesis indicate the percentage of each type water) : (1) type 1 waters (38%) that are relatively poor in $Cl^{-}$ and ${NO_3}^-$, which may represent their relatively little contamination due to seawater mixing and anthropogenic pollution; (2) type 2 waters (21%) which are enriched in $Cl^{-}$, Indicating the considerable influence by seawater mixing; (3) ${NO_3}^-$-rich, type 3 waters (11%) which record significant anthropogenic pollution; and (4) type 4 waters (30%) enriched in both $Cl^{-}$ and ${NO_3}^-$, reflecting the effects of both seawater mixing and anthropogenic contamination. The results of the water type classification correspond well with the grouping on a Piper's diagram. On a Br x $10^4$versus Cl molar ratio diagram, most of type 2 waters are also plotted along or near the seawater mixing line. The discriminant analysis of hydrochemical data also shows that the classification of waters into four types are so realistic to adequately reflect the major process(es) proposed for the hydrochemical evolution of each water type. As a tool for evaluating the degree of seawater mixing, we propose a parameter called 'Seawater Mixing Index (S.M.I.)’ which is based on the concentrations of Na, Mg, Cl, and $SO_4$. All the type 1 and 3 waters have the S.M.I. values smaller than one, while type 2 and type 4 waters mostly have the values greater than 1. In the western coastal area of Korea, more than 21% of shallow groundwaters appear to be more or less affected by salinization process.

• 대한본초학회지
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• 제33권5호
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• pp.105-110
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• 2018

Objectives : We tried to observe the fluorescence anisotropy and intensity of ethidium ion in the intercalating binding interaction between DNA and ethidium ions in the presence of berberine, and then tried to explain the effect of berberine on the intercalating interaction of ethidium ion with DNA. Methods : DNA(calf thymus DNA), berberine and ethidium bromide(EtBr) were purchased from Sigma-Aldrich Co. Proper amount of each compound was dissolved in 20 mM sodium phosphate buffer(pH 7.0) containing 100 mM of NaCl to prepare stock solutions. Collections of the fluorescence anisotropy and intensity data were performed on JASCO FP-8300 spectrofluorometer equipped with a polarizer and a Peltier temperature controller. The excitation of ethidium ion was done at 550 nm and the emission data were collected at 600 nm. For Stern-Volmer plot, the fluorescence data were collected at $18^{\circ}C$ and $30^{\circ}C$. Results : According to the results of this research, the weak competitive binding pattern between ethidium ion and berberine appeared in binding with DNA at low ratio of DNA to ethidium ion. But at high ratio of DNA to ethidium ion, this weak competition disappeared. Instead, berberine might bind to DNA by intercalating way. In other words, berberine could de-intercalate ethidium ion from DNA at low concentration of DNA relative to ethidium ion, but could not at high concentration of DNA relative to ethidium ion. In addition, the mechanism of fluorescence quenching of ethidium ion could also proceed differently, depending on the ratio of the amount of DNA to that of ethidium ion. Conclusions : The effect of berberine on the DNA-ethidium ion intercalating interaction could work differently, depending on the relative ratio of the amount of DNA to that of ethidium ion. This study also showed that fluorescence anisotropy analysis is very useful method to obtain detailed information for investigation of the complex binding interactions. In order to fully understand the mechanism of action of the pharmacological effect by berberine, studies on the effect of berberine on the action of proteins such as various enzymes closely related to berberine-induced medicinal effects should be continued.

• 동국한의학연구소논문집
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• 제10권
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• pp.119-145
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• 2008

Through a simple study of the medical classics in the '$\bar{A}yurveda$', we have summarized them as follows. 1) Traditional Indian medicine started in the Ganges river area at about 1500 B. C. E. and traces of medical science can be found in the "Rigveda" and "Atharvaveda". 2) The "Charaka(閣羅迦集)" and "$Su\acute{s}hruta$(妙聞集)", ancient texts from India, are not the work of one person, but the result of the work and errors of different doctors and philosophers. Due to the lack of historical records, the time of Charaka(閣羅迦) or $Su\acute{s}hruta$(妙聞)s' lives are not exactly known. So the completion of the "Charaka" is estimated at 1st$\sim$2nd century C. E. in northwestern India, and the "$Su\acute{s}hruta$" is estimated to have been completed in 3rd$\sim$4th century C. E. in central India. Also, the "Charaka" contains details on internal medicine, while the "$Su\acute{s}hruta$" contains more details on surgery by comparison. 3) '$V\bar{a}gbhata$', one of the revered Vriddha Trayi(triad of the ancients, 三醫聖) of the '$\bar{A}yurveda$', lived and worked in about the 7th century and wrote the "$Ast\bar{a}nga$ $Ast\bar{a}nga$ hrdaya $samhit\bar{a}$ $samhit\bar{a}$(八支集) and "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$(八心集)", where he tried to compromise and unify the "Charaka" and "$Su\acute{s}hruta$". The "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$" was translated into Tibetan and Arabic at about the 8th$\sim$9th century, and if we generalize the medicinal plants recorded in each the "Charaka", "$Su\acute{s}hruta$" and the "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$", there are 240, 370, 240 types each. 4) The 'Madhava' focused on one of the subjects of Indian medicine, '$Nid\bar{a}na$' ie meaning "the cause of diseases(病因論)", and in one of the copies found by Bower in 4th century C. E. we can see that it uses prescriptions from the "BuHaLaJi(布唅拉集)", "Charaka", "$Su\acute{s}hruta$". 5) According to the "Charaka", there were 8 branches of ancient medicine in India : treatment of the body(kayacikitsa), special surgery(salakya), removal of alien substances(salyapahartka), treatment of poison or mis-combined medicines(visagaravairodhikaprasamana), the study of ghosts(bhutavidya), pediatrics(kaumarabhrtya), perennial youth and long life(rasayana), and the strengthening of the essence of the body(vajikarana). 6) The '$\bar{A}yurveda$', which originated from ancient experience, was recorded in Sanskrit, which was a theorization of knowledge, and also was written in verses to make memorizing easy, and made medicine the exclusive possession of the Brahmin. The first annotations were 1060 for the "Charaka", 1200 for the "$Su\acute{s}hruta$", 1150 for the "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$", and 1100 for the "$Nid\bar{a}na$". The use of various mineral medicines in the "Charaka" or the use of mercury as internal medicine in the "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$", and the palpation of the pulse for diagnosing in the '$\bar{A}yurveda$' and 'XiZhang(西藏)' medicine are similar to TCM's pulse diagnostics. The coexistence with Arabian 'Unani' medicine, compromise with western medicine and the reactionism trend restored the '$\bar{A}yurveda$' today. 7) The "Charaka" is a book inclined to internal medicine that investigates the origin of human disease which used the dualism of the 'Samkhya', the natural philosophy of the 'Vaisesika' and the logic of the 'Nyaya' in medical theories, and its structure has 16 syllables per line, 2 lines per poem and is recorded in poetry and prose. Also, the "Charaka" can be summarized into the introduction, cause, judgement, body, sensory organs, treatment, pharmaceuticals, and end, and can be seen as a work that strongly reflects the moral code of Brahmin and Aryans. 8) In extracting bloody pus, the "Charaka" introduces a 'sharp tool' bloodletting treatment, while the "$Su\acute{s}hruta$" introduces many surgical methods such as the use of gourd dippers, horns, sucking the blood with leeches. Also the "$Su\acute{s}hruta$" has 19 chapters specializing in ophthalmology, and shows 76 types of eye diseases and their treatments. 9) Since anatomy did not develop in Indian medicine, the inner structure of the human body was not well known. The only exception is 'GuXiangXue(骨相學)' which developed from 'Atharvaveda' times and the "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$". In the "$Ast\bar{a}nga$ Sangraha $samhit\bar{a}$"'s 'ShenTiLun(身體論)' there is a thorough listing of the development of a child from pregnancy to birth. The '$\bar{A}yurveda$' is not just an ancient traditional medical system but is being called alternative medicine in the west because of its ability to supplement western medicine and, as its effects are being proved scientifically it is gaining attention worldwide. We would like to say that what we have researched is just a small fragment and a limited view, and would like to correct and supplement any insufficient parts through more research of new records.

• 한국광물학회지
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• 제5권2호
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• pp.109-121
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• 1992

본 연구는 토파즈의 인공착색 처리 방법을 설정하기 위하여 브라질, 중국, 인도, 나이지리아, 스리랑카 등 5개국에서 산출된 토파즈를 대상으로, 전자현미분석(EPMA), 중성자활성분석(NAA), X선 회절분석, 라만 분광분석, 주사현미경(SEM), 부식시험, 굴절률측정, 비중측정, 유체 포유물 관찰 등의 실험을 실시하여 광물학적, 화학적 특성에 관한 연구를 수행하였다. 연구 결과 토파즈는 산지에 따라 화학적, 구조적 및 물리적 특성의 차이를 나타내었으며 특히, F와 OH 고용체 함량의 차이는 물리적, 구조적 특성과 밀접한 관련성이 있음이 확인되었다. F에 대한 OH로 치환정도가 가장 높은 인도산 토파즈는 굴절률, 단위포상수 b, 단위포 체적 및 ${\Delta}021$값이 가장 크고, 비중값은 가장 작으며 스리랑카산, 중국산, 브라질산, 나이지리아산순으로 F에 대한 OH로 치환 정도가 낮다. F에 대한 OH로 치환정도가 가장 낮은 나이지리아산 토파즈는 굴절률, 단위포상수 b, 단위포 체적 및 ${\Delta}021$값이 가장 작고, 비중값은 가장 크다. 토파즈내에 함유되는 미량원소종은 Na, Fe, Br, Co, Ce, La, Sm, Th, Au, Sc, Cr 등이며 이러한 미량원소의 정성정량적 특성은 물리적 특성에는 거의 영향을 미치지 않았다. 라만 분광분석 결과 토파즈의 피크는 산지에 따라 강도의 차이를 나타내었으며 브라질산과 인도산은 455∼458($cm^{-1}$)근처의 피크, 중국산은 282∼284($cm^{-1}$) 근처의 피크가 나타나지 않았다. 산지에 따른 결정구조결함 특성은 주로 point-bottom pit의 negative crystal defect(인도산, 나이지리아산)와 curl-bottom pit의 net work defect(브라질산, 중국산)로 구분되며, 결정내에 발달하는 미세한 균열을 따라 형성된 선결함 양상(linear defect)을 보여준다. 유체 포유물의 특징은 브라질산이 액상 $CO_2$를 가지는 III형이고, 중국산에는 유체 포유물이 거의 관찰되지 않으며 단지 $10{\mu}m$이하의 매우 작은 크기인 초생포유물의 극소량 존재한다. 인도산은 기체가 풍부한 II형이고, 나이지리아산은 암염, 실바이트 등의 고체 포유물을 함유하는 IV형이며 스리랑카산은 거의 대부분의 유체 포유물이 2차 생성의 I형이 주로 형성되어 있다. 본 연구의 결과는 광물학적 특성의 차이를 갖는 산지별 토파즈의 인공착색을 위한 처리 방법을 설정하는 유용한 기초 자료로 이용될 수 있을 것이다.