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Potential Antitumor ${\alpha}$-methylene-${\gamma}$-butyrolactone-bearing nucleic acid bases. 2. synthesis of $5^I-Methyl-5^I$-[2-(5-substituted uracil-1-yl)ethyl]-$2^I-oxo-3^I$-methylenetetrahydrofurans

  • Kim, Jack-C.;Kim, Ji-A;Park, Jin-Il;Kim, Si-Hwan;Kim, Seon-Hee;Choi, Soon-Kyu;Park, Won-Woo
    • Archives of Pharmacal Research
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    • v.20 no.3
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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 $(IC_50:0.4~2.8 {\mu}g/ml)$.

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Synthesis and Antitumor Evaluation of cis-(1,2-Diaminoethane) dichloroplatinum (II) Complexes Linked to 5- and 6-Methyleneuracil and -uridine Analogues

  • Kim, Jack-C.;Lee, Min-Hwa;Choi, Soon-Kyu
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.465-469
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    • 1998
  • The search for platinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diaminedichloroplatinum (II) complexes linked to uracil and uridine. Six heretofore unreported uracil and uridine-platinum (II) complexes are; [N-(uracil-5-yl-methyl)ethane-1,2-di-amine]dichloroplatinum (II) (3a), [N-(uracil-6-yl-methyl)ethane-1,2-diaminel dichloroplatinum (II) (3b), t[N-($2^1$, $3^1$,$5^1$-tri-O-acetyl)uridine-5-yl-methyl] ethane-1,2-diamineldichloroplatinum (II) (6a), {[N-($2^1$,$3^1$, $5^1$-tri-O-acetyl) uridine-6-yl-methyl]ethane-1,2-diamine)dichloroplatinum (II) (6b),[N-(uridine- 5-yl-methyl)ethane-1,2-diamine]dichloroplatinum (II) (7a), [N-(uridine-6-yl- methyl)ethane-1,2-diamine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-chloromethyluracil (1a) and 6-chloromethyluracil (1b) which were reacted with ethylenediamine to afford the respective 5-[(2-aminoethyl)aminol methyluracil (2a) and 6-[(2-aminoethyl)amino]methyluracil (2b). The cis-platin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b with potassium tetrachloroplatinate (II). The heterocyclic nucleic acid bases 1a and 1b were efficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannic chloride under anhydrous acetonitrile to yield the stereospecific .betha.-anomeric 5-chloromethyl- $2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4a) and 6-chloromethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (4b), respectively. The nucleosides 4a and 4b were coupled with ethylenediamine to provide the respective 5-[(amino-ethyl)aminolmethyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5a) and 6-[(aminoethyl)amino] methyl-$2^1$,$3^1$,$5^1$-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b, respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH$_{3}$ONa. The cytotoxic activities were evaluated against three cell lines (FM-3A, P-388 and J-82) and none of the synthesized compounds showed any significant activity.

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Distribution and Diversity of Saprophytic, Mycorrhizal and Parasitic Higher Fungi in Kwangnung Experimental Forest in Korea (광릉시험림(光陵試驗林)의 부생성(腐生性), 균근성(菌根性) 및 기생성(寄生性) 고등균류(高等菌類)의 분포(分布)와 다양성(多樣性)에 관(關)한 연구(硏究))

  • Lee, Kyung Joon;Miller, Orson K. Jr.;Kim, Yang Sup
    • Journal of Korean Society of Forest Science
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    • v.76 no.4
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    • pp.376-389
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    • 1987
  • Higher fungi (Basidiomycetes) were collected from forest stands of Kwangnung Experimental Forest, Kwangnung, Kyonggido, during the summer and fall seasons of 1976, 1984, 1985 and 1986. A total of 257 species and varieties in 104 genera were identified. Saprophytic fungi accounted for 135 species in 75 genera while mycorrhizal fungi accounted for 120 species in 28 genera. Two parasitic species were collected and they were root parasites. Among the mycorrhizal species Amanita, Russula, Lactarius, and species in the Boletaceae were the dominant taxa. The mycorrhizal fungi appear to be an important component in the essential elements needed for forest management in Korea. A reevaluation of the higher fungi previously described in Korea was made and we report 77 higher fungi previously undescribed from Korea. This is from a single experimental forest and suggests that there are many unreported higher fungi which play an important role in Korean forests.

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A Preliminary Study on Micro-earthquakes Occurred from 2010 to 2017 in Busan, Korea (2010-2017년 부산지역의 미소 지진 예비 탐색)

  • Yoon, Soheon;Han, Jongwon;Won, Deokhee;Kang, Su Young;Ryoo, Yong Gyu;Kim, Kwang-Hee
    • Journal of the Korean earth science society
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    • v.40 no.3
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    • pp.272-282
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    • 2019
  • Although the knowledge of current seismicity is a critical information for making and implementing effective earthquake-related policy, the detailed seismicity information of the metropolitan areas with high-population density has been largely underestimated due to the high-level of cultural noise and small earthquake magnitude. This study presents 12 earthquakes including 2 earthquakes previously known and 10 additional earthquakes occurred from 2010 to 2017 in Busan, but they were unreported by the Korea Meteorological Administration. Matched filter technique is used to detect micro-earthquakes. Although the epicenters of micro-earthquakes though present a distinguished linearity, a correlation with faults in the area is unknown. A repeated micro-seismicity suggests that there are subsurface structures responsible for observed events. If large earthquakes occur along the fault in Busan, they may cause catastrophic natural disasters. Given the fact that the recent earthquakes did not accompany any surface signatures, it is highly recommended that the current micro-seismicity be investigated, and updated seismicity information be incorporated into establishing active fault maps in Korea.

Optical Properties of the Eu2+ Doped Li2SrSiO4-αNα (Li2SrSiO4-αNα에 첨가된 Eu2+의 광학적 특성)

  • Namkhai, Purevdulam;Kim, Taeyoung;Woo, Hyun-Joo;Jang, Kiwan;Jeong, Jung Hyun
    • New Physics: Sae Mulli
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    • v.68 no.11
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    • pp.1196-1202
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    • 2018
  • $Li_2Sr_{1-x}Eu_xSiO_{4-{\alpha}}N_{\alpha}$ ($Li_2SrSiO_{4-{\alpha}}N_{\alpha}:Eu^{2+}$) phosphors were synthesized by using a solid state reaction (SSR) method with submicron $Si_3N_4$ and nano $Si_3N_4$ powders as the sources of Si and N, and the optical properties of those phosphors were studied. The studied phosphors showed efficient excitation characteristics over the broad range from 230 to 530 nm. Also, They showed broad emission spectra covering a range from 500 to 700 nm, with a peak at 568 nm, which was shifted longer wavelength by 18 nm as compared with that of commercial $YAG:Ce^{3+}$. Combined with a 450 nm blue LED chip, the results support the application of the $Li_2SrSiO_{4-{\alpha}}N_{\alpha}:Eu^{2+}$ phosphor as a luminescent material for a white-light source thaat is warmer than the commercial $YAG:Ce^{3+}$ white-light source. In addition, the $Li_2SrSiO_{4-{\alpha}}N_{\alpha}$ phosphors prepared from a submicron $Si_3N_4$ powder was found to emit a previously unreported self-activated luminescence in $Li_2SrSiO_{4-{\alpha}}N_{\alpha}$.

Identification and functional prediction of long noncoding RNAs related to intramuscular fat content in Laiwu pigs

  • Wang, Lixue;Xie, Yuhuai;Chen, Wei;Zhang, Yu;Zeng, Yongqing
    • Animal Bioscience
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    • v.35 no.1
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    • pp.115-125
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    • 2022
  • Objective: Intramuscular fat (IMF) is a critical economic indicator of pork quality. Studies on IMF among different pig breeds have been performed via high-throughput sequencing, but comparisons within the same pig breed remain unreported. Methods: This study was performed to explore the gene profile and identify candidate long noncoding RNA (lncRNAs) and mRNAs associated with IMF deposition among Laiwu pigs with different IMF contents. Based on the longissimus dorsi muscle IMF content, eight pigs from the same breed and management were selected and divided into two groups: a high IMF (>12%, H) and low IMF group (<5%, L). Whole-transcriptome sequencing was performed to explore the differentially expressed (DE) genes between these two groups. Results: The IMF content varied greatly among Laiwu pig individuals (2.17% to 13.93%). Seventeen DE lncRNAs (11 upregulated and 6 downregulated) and 180 mRNAs (112 upregulated and 68 downregulated) were found. Gene Ontology analysis indicated that the following biological processes played an important role in IMF deposition: fatty acid and lipid biosynthetic processes; the extracellular signal-regulated kinase cascade; and white fat cell differentiation. In addition, the peroxisome proliferator-activated receptor, phosphatidylinositol-3-kinase-protein kinase B, and mammalian target of rapamycin pathways were enriched in the pathway analysis. Intersection analysis of the target genes of DE lncRNAs and mRNAs revealed seven candidate genes associated with IMF accumulation. Five DE lncRNAs and 20 DE mRNAs based on the pig quantitative trait locus database were identified and shown to be related to fat deposition. The expression of five DE lncRNAs and mRNAs was verified by quantitative real time polymerase chain reaction (qRT-PCR). The results of qRT-PCR and RNA-sequencing were consistent. Conclusion: These results demonstrated that the different IMF contents among pig individuals may be due to the DE lncRNAs and mRNAs associated with lipid droplets and fat deposition.

Legal Transformation of Advisory Procedure of the ITLOS into an Alternative Dispute Settlement Mechanism - From the Evaluation of Request for an Advisory Opinion Submitted by the Sub-Regional Fisheries Commission (Case No. 21), ITLOS (분쟁해결을 위한 대체적 수단으로서 ITLOS 권고적 의견 절차 활용 - SRFC 권고적 의견 사건(사건번호 21)을 중심으로 -)

  • Choi, Jee-hyun
    • Ocean and Polar Research
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    • v.44 no.2
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    • pp.147-160
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    • 2022
  • SRFC (Sub-Regional Fisheries Commission) requested to the ITLOS (International Tribunal for the Law of the Sea) an advisory opinion relating to the IUU (Illegl, Unreported, and Unregulated) fishing (Case No-21 of the ITLOS). Since, in the UNCLOS, there is no article authorizing the jurisdiction of the ITLOS full court's Advisory opinion, so various scholarly opinion wad divided. But ITLOS delivered its Advisory opinion confirming its jurisdictional competence over the Advisory proceedings with its legal opinion about the IUU issues. It opens new possibility of the alternative dispute settlement mechanism of the ITLOS through the advisory procedures. In reality, there has been a view that ICJ (International Court of Justice) could take the part of a kind of dispute settlement through its Advisory procedures. But the advisory procedures of the ITLOS, with no definite clause in UNCLOS about the advisory procedures, which provides more allowances for the function of advisory opinion as the alternative dispute settlement mechanism. ITLOS accepted the requests of the advisory opinion by the State parties through international organization or themselves directly. And the advisory opinion of the ITLOS aims the interpretation and application into the special issues-specially IUU fishing in Case No. 21 of the ITLOS-. Those factors could enable more enhanced role of the ITLOS as an alternative dispute settlement mechanism. But those possibility has contain risk of excessive and unlimited advisory role of the ITLOS. So it is important to focus on the restriction on the role of the State parties in the request of the advisory opinion to the ITLOS. In this regard it is meaningful that the ITLOS has suggested a kind of legal standing in the advisory procedures in that only coastal States could request the Advisory opinion about the IUU in their EEZ. Furthermore the discretionary power of the ITLOS in the Article 138 of the Rules of the Tribunal could curtail the abuse of the Advisory opinion initiated by the States parties of the UNCLOS. Under this framework, Advisory opinion could broaden more alternative option to the disputes between State parties of the UNCLOS in that after being delivered detailed interpretation of the UNCLOS about the specific issues, States parties could devote themselves to searching for flexible solution for the disputes between State parties. It could obtain legal explanation about the dispute under the Article 297 and Article 298 by detouring the jurisdiction limits through advisory procedures.

Estimation of Consumer Value on Import Management of Seafood Obtained from IUU Fishing: Using Choice Experiment Method

  • Ji-Eun An;Se-Hyun Park;Heon-Dong Lee
    • Journal of Korea Trade
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    • v.27 no.2
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    • pp.115-129
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    • 2023
  • Purpose - This study empirically analyzes the consumer value of risk management associated with illegal, unreported, and unregulated (IUU) fishing of fishery products imported to Korea. The global regulatory paradigm for IUU fishing has shifted from production-centered to market-centered. As a result, changes in the international fisheries trade environment emphasizing "transparency" and "legality" of the production process are accelerating. Therefore, changes in the management systems of fishery products entering the country are also needed. Accordingly, this study estimated the consumer value for risk management of IUU fishing, targeting major fish species imported to Korea, and derived the feasibility of introducing related policies. Design/methodology - This study used the choice experiment as an analysis model to estimate consumers' willingness to pay for the "possibility to check for IUU fishing." The choice experiment assumes that the value of a good or service is composed of separable attributes and that the sum of the part-worth of these individual attributes becomes the total value. In this study, respondents were presented with profiles comprising three attributes (country of origin, price, and possibility of checking IUU fishing) and the levels of frozen poulp squid, the subject of the analysis. The participants were asked to select their preferred profile. The marginal willingness to pay for each attribute was derived from the results of the respondents' choices using conditional logit model estimates. Findings - There is a marked difference in utility based on the preference of the country of origin of fishery products among consumers. In addition, the utility of fishery products that have undergone IUU fishing verification was observed to be higher, with the utility marked to be higher for lower prices. Originality/value - Estimating the policy value of the risk management in IUU fishing of imported fisheries products in this study is a novel attempt that has never been conducted before. Several studies have been conducted to assess the risk of IUU fishing associated with the import of fishery products internationally. However, such studies are yet to be conducted in Korea. Instead, policies and studies have focused on issues related to complying with trading partners' legal and transparent standards for exporting fishery products. This study should be the beginning of more in-depth empirical and theoretical explorations to establish order in the domestic seafood market and respond to changes in international regulations on IUU fishing.

A Study on the Establishment of Management Methods about Occupational Dermatoses (직업성 피부질환에 대한 현황 파악 및 관리 대책 수립을 위한 연구)

  • Lim, Hyun-Sul;Cheong, Hae-Kwan;Choi, Byung-Soon;Kim, Ji-Yong;Sung, Yeol-Oh;Kim, Yang-Ho
    • Journal of Preventive Medicine and Public Health
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    • v.29 no.3 s.54
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    • pp.617-637
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    • 1996
  • Occupational dermatosis is one of the most prevalent occupational disorders. However, the extent of the occupational dermatoses including incidences and prevalencies of each disease entity, and etiologic materials are not yet welt stated in Korea. Authors reviewed the literatures on the statistic data and reports on the occupational dermatoses, and surveyed on the occupational dermatoses in two factories, and surveyed the physicians responsible to the occupational dermatoses with formed questionnaire. The results are as follows; 1. Among medical journals published since 1964, there were 31 articles on the occupational dermatoses. Of 31 articles, 18 were case reports and all others were review articles. Of 18 case reports, 9 were epidemiologic survey. The Workers' Periodic Health Examinations revealed that prevalence of the occupational dermatoses was highest(4.36 per 10,000 workers) in 1974, but number of the cases reported were decreased sharply since 1978 with some tendency to increase since 1981. There were 2,240 reported cases of occupational dermatoses between 1966 and 1992, which is 1.90% of all the reported occupational diseases. Skin infection and injuries due to chemicals were most frequent and there were 6 cases of skin cancer. 2. In an epidemiological survey on the dermatoses among 995 workers in a metal product manufacturing factory and 225 workers in a coal chemical factory, there were 794 with dermatomycosis, 296 workers with acne, 130 workers with scar, 123 workers with deformity of toe nails. Scars, photosensitivity dermatitis, deformity of finger and toe nails, and acne were more prevalent in the metal product manufacturing factory(p<0.05). In the metal prouct manufacturing factory, workers treating organic solvents and oils had more dermatoses than those without treating the materials(p<0.05). On the skin patch performed on 16 workers in the metal product manufacturing factory, there were 8 cases of irritation dermatitis and 5 cases of contact dermatitis. Prevalence of contact dermatitis in the metal product manufacturing factory was 1.3%. 3. On the questionnaire survey, 34 dermatologists, 29 doctors of preventive medicine, and 22 family physician replied. The proportion of occupational etiology among all dermatoses assumed by the physicians were below 9%, and the most important occupational dermatosis in Korea was contact dermatitis. Main etiologic materials related to the occupational dermatosis were organic solvent, acid and alkali, and metals. The reason for the scarcity of report of occupational dermatoses were difficulty in diagnosis and physician's ignorance of the occupational etiology. They replied that to prevent the occupational dermatoses in the workplace, the use of protective devices was most important, and development of diagnostic criteria on the occupational dermatoses is urgent. Above results shows us that there is many workers with occupational dermatoses, but they are mostly unreported. Measures to prevent and manage the occupational dermatoses are not satisfactory at present. Hence, authors suggest measures for the precise diagnosis, report and prevention of the occupational dermatoses. a. Dermatologist, preventive physician, and industrial hygienist should work as a team to examine the high risk group and establish the preventive measures. b. Disease entities, diagnostic criteria of occupational dermatoses should be listed, criteria for the compensation and job fitting at recruitment should be established, and manual for the proper treatment and effective prevention of each occupational dermatosis should be developed. c. Patch test antigens against each occupational category should be developed and it should be available to any physicians responsible. d. To facilitate the diagnosis of occupational dermatoses by the doctors responsible for the Workersr Periodic Health Examination, development of standardized questionnaire, education on the techniques of the patch test, and cooperation with the dermatologist in diagnosis of occupational dermatoses is essential.

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Cause-Specific Mortality at the Provincial Level (시도의 사망원인별 사망력)

  • Park Kyung Ae
    • Korea journal of population studies
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    • v.26 no.2
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    • pp.1-32
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    • 2003
  • An analysis on cause-specific mortality at the provincial level provides essential information for policy formulation and makes it possible to draw hypotheses regarding various diseases and causes of death. Although the mortality level and causes of death at the provincial level are determined by the multiple effects of socioeconomic, cultural, medical and ecological factors, this study primarily intends to examine similarities and differences of cause-specific mortality at the provincial level. Utilizing the registered death and the registered population as of 1998, the delayed death registration and unreported infant deaths were supplemented at the provincial level and age-standardized death rates and life tables were calculated. Regarding the mortality level due to all causes, major findings were as follow: (1) For both sexes as a whole, Seoul showed the lowest mortality level, and Jeonnam showed the highest mortality level; and (2) The differences of the mortality level among provinces were greater for males than females and for those less than 65 years than those 65 years and over. Regarding the cause-specific mortality level revealed in all indicators (cause-specific age-standardized mortality rates and the probability of dying at birth due to a specific cause for males, females, and both sexes combined respectively), the major findings were as follow: (1) The mortality level due to heart diseases was the highest in Busan and the lowest in Gangweon; (2) The mortality level due to liver diseases was the highest in Chonnam; and (3) The mortality level due to traffic accidents was the highest in Chungnam and the lowest in Inchon. As the mortality differentials at the provincial level are related to various factors, exploratory statistical analysis is attempted for the 25 explanatory variables including socioeconomic variables and 90 mortality variables. Mortality due to all causes are related to socioeconomic variables. Among cause-specific mortality, mortality due to liver diseases and traffic accidents is related to socioeconomic variables. Finally, the need to improve the quality of death certificate is discussed.