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Potential Antitumor $\alpha$-Methylene-$\gamma$-butyrolactone-Bearing Nucleic Acid Base. 3. Synthesis of $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans

  • Kim, Jack-C.;Kim, Si-Hwan;Kim, Ji-A;Choi, Soon-Kyu;Park, Won-Woo
    • Archives of Pharmacal Research
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    • v.21 no.4
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    • pp.458-464
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    • 1998
  • Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

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Behaviors of Arsenic in Paddy Soils and Effects of Absorbed Arsenic on Physiological and Ecological Characteristics of Rice Plant lll. Effect of Water Management on As Uptake and the Growth of Rice Plant at As Added Soil (토양중(土壤中) 비소(砒素)의 행동(行動)과 수도(水稻)의 비소흡수(砒素吸收)에 의(依)한 피해생리(被害生理) 생태(生態)에 관(關)한 연구(硏究);Ⅲ.물관리(管理)가 수도의 비소흡수(砒素吸收) 및 생육(生育)에 미치는 영향(影響))

  • Lee, Min-Hyo;Lim, Soo-Kill-H
    • Korean Journal of Environmental Agriculture
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    • v.6 no.1
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    • pp.1-6
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    • 1987
  • A pot experiment was conducted to find out the effect of water management on the growth and uptake of arsenic and inorganic nutrients of rice plant at As added soil. The arsenic were added to soil at the levels of As 0, 10, 50, 100 and 150 ppm, respectively. Water management was done with two ways: intermittent irrigation from ten days after transplanting, and continuous submersion until harvest. Higher soil As levels increased As content in plant but reduced growth rate. Aresenic content in plant was considerably reduced with intermittent irrigation compared to continuous submersion. Rice growth showed also same trend. With increasing As levels in soil, N content in plant was increased but P, K, Ca, Mg, $SiO_2$, Fe and Mn content in plant were tend to be decreased. These inorganic nutrients in plant were also much absorbed in continuous submersion compared to intermittent irrigation. Soil pH was slightly increased with increasing As levels in soil while soil Eh has no relationship with soil As levels. On the other hand, soil pH was higher in the treatment of continuous submersion than that of intermittent irrigation but soil Eh showed reverse trend. With increasing As levels in soil, water soluble-As and Ca-As fractions in soil tend to be increased with continuous submersion, but these fractions has no tendency with intermittant irrigation.

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Effect of COY (Cooking Oil and Yolk mixture) and ACF (Air-circulation Fan) on Control of Powdery Mildew and Production of Organic Lettuce (난황유와 공기순환팬의 상추 흰가루병 방제효과 및 생산에 미치는 영향)

  • Jee, Hyeong-Jin;Ryu, Kyung-Yul;Park, Jong-Ho;Choi, Du-Hoe;Ryu, Gab-Hee;Ryu, Jae-Gee;Shen, Shun-Shan
    • Research in Plant Disease
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    • v.14 no.1
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    • pp.51-56
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    • 2008
  • Powdery mildew of lettuce that is a newly reported disease became a threat to organic cultivation of lettuce in Korea since the disease caused by Podosphaera fusca resulted in a half of yield loss in heavily infected fields. To improve micro-environmental conditions around lettuce, ACF (air-circulation fan) was installed on inside roof of plastic house at 6 m intervals. The ACF increased 57% of lettuce yield and reduced 71.4% of lettuce seedling death. COY (cooking oil and yolk mixture) consisted of cooking oil 0.3% and egg yolk 0.08% reduced lettuce seedling death from 89.3% to 92.9% under the greenhouse. Seven-day interval spray of COY resulted in high control values of powdery mildew of lettuce ranging from 89.6% to 96.3%, which was comparable to a fungicide, Azoxystrobin. Lettuce yield was increased about two times compared to a non-treated conventional cultivation. Qualities of lettuce such as hardness and chlorophyll content were also improved by COY and ACF combination. Effect of COY on control of the disease was improved when $CaCO_3$ or $SiO_2$ 1,000 ppm was supplemented. Results indicated that the COY made of cooking oil such as canola emulsified with yolk was highly effective on control of powdery mildew of lettuce and suitable for organic agriculture, especially when combined with ACF.

Feasibility of Phytoremediation for Metal-Contaminated Abandoned Mining Area (광산 인근 토양의 중금속 오염에 따른 식물정화기술의 적용성 탐색)

  • Ok, Yong-Sik;Kim, Si-Hyun;Kim, Dae-Yeon;Lee, Han-na;Lim, Soo-Kil;Kim, Jeong-Gyu
    • Korean Journal of Soil Science and Fertilizer
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    • v.36 no.5
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    • pp.323-332
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    • 2003
  • This study was carried out to provide information for the present status of soil pollution near abandoned old-zinc mining area through analysis of bound form and 0.1 N-HCl extractable concentrations of heavy metals in soils and plants. Feasibility of endemic plants for phytoremediation was evaluated by the investigation of vegetation in soils. Cd contents of the selected samples near old-zinc mining soils ranged from 0.2 to $42mg\;kg^{-1}$. Nonagricultural soils near the mining area contained great amounts of Zn, Pb, Cd, and Cu than the paddy and upland soils. Some Korean wild plants, Artemisia princeps, Artemisia montana, Erigeron canadensis, and Pueraria thunbergiana, were found to grow vigorously in the studied area. Among them, Artemisia princeps was selected as a possible phytoremediator for cleaning heavy metal contaminated soils. Artemisia princeps contained about 43 and $52mg\;kg^{-1}$ of Cd in their root and shoot as dry weight, respectively. Average contents of Cd in the rhizosphere soil, $15.68mg\;kg^{-1}$, was slightly higher than the soil-root interface soils, $14.1mg\;kg^{-1}$. Sequential extraction of Cd contaminated soils showed that average $2.4mg\;kg^{-1}$ (about 7%) of cadmium existed as exchangeable form and the average amounts increased as follows : adsorbed < organically bound < exchangeable << oxide carbonate << sulfide residual fractions. Amendment of organic by-product fertilizer in metal-contaminated soils promoted the growth of roots significantly as compared with the other treatments containing chemical fertilizer.

Method for Supplementing Lecithin to Ginseng Extract (레시틴이 강화된 인삼 추출물 제조 방법)

  • Park, Soon-Hye;Kim, Il-Woong;Kim, Dong-Man;Kim, Si-Kwan
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.35 no.9
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    • pp.1245-1250
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    • 2006
  • This study was carried out to develop the method of preparing lecithin-fortified ginseng extract. Firstly, soybean lecithin was mixed with soybean oil (LCS) in varying ratio (2.5%, 5%, 10% and 20%). Then, one part volume of LCS was mixed with three parts volume of ginseng extract with 10% solid matter content and the mixture was vortexed vigorously. Finally, the mixture was spinned at the speed of 3,000 rpm for 30 minutes to separate oil and aqueous ginseng extract layer (AG). AG was then subjected to qualitative and quantitative analysis of phospholipids and ginsenosides. Fatty acid composition and crude fat content before and after LCS was determined. Stability of lecithin in ginseng extract was determined by analyzing phospholipid content in the one third upper and lower layer of the concentrated AG in Falcon tubes while storing the LCS treated concentrated AG in 4, 25 and 40oC for 6 months. Ratio of lecithin transferred to AG increased with the increase in lecithin content of soybean oil. There was no significant change in fatty acid composition and crude fat content, and ginsenoside content in the ginseng extract before and after LCS treatment. TLC and HPLC pattern of saponin fraction before and after treating the ginseng extract with LCS demonstrated no observable difference. There was no change in lecithin content in the upper and lower one third layer of ginseng extract in the tubes after storing the concentrated AG in 4, 25 and $40^{\circ}C$ for 6 months. Ginsenosides HPLC pattern was not changed when stored the LCS-treated ginseng extract in those conditions for six months, indicating satisfiable stability of the LCS-treated concentrated ginseng extract. From these results, it can be concluded that treatment of the ginseng extract with lecithin containing soybean oil is a labor effective method with satisfiable stability to fortify lecithins to ginseng extract.

The Relationship Between High School Teachers Health Perception and Health Promotion Behavior (고등학교 교사의 건강지각과 건강증진행위의 관계)

  • Kim, Dong-Hwan;Park, Young-Soo
    • The Journal of Korean Society for School & Community Health Education
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    • v.4
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    • pp.21-41
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    • 2003
  • The purposes of this study were to ; first, investigate High School Teachers health promotion behavior types; second, explore the effects High School Teachers perceived benefits and perceived barriers have on their health promotion behavior ; third, suggest a desirable course that will increase teachers health. To this end, this researcher conducted a survey on health promotion behavior, perceived benefits, and perceived barriers to 329 High School teachers working in Goyang-si, Gyonggi-do. The results of the survey are as follows: Health Promotion Behavior A closer look at high school teachers health promotion behavior shows that male teachers, compared with female teachers, more actively promote their health. However, female teachers are more aware of their personal hygiene and disease risks. Older teachers, rather than younger teachers, are more willing to promote their health through better eating habits and more frequent exercise. A comparison between married and single teachers revealed that married teachers promote their health through better eating habits, and single teachers receive less stress and are better at managing their stress. Teachers working in technical high schools are better at managing their stress and personal hygiene than academic high schools teachers. Teachers working after 8 o'clock show better health promotion behavior through proper eating habits, stress management, regular exercise, disease prevention: however, teachers working before 7:30 are poor at managing their stress. Teachers not teaching supplementary lessons and not supervising night self-study are better at managing their stress, exercise schedule, and disease prevention than teachers who are. Perceived Benefits, Perceived Barriers, and Health Promotion Behavior A Comparison between male and female teachers shows that female teachers firmly believe improved eating habits and regular exercises would greatly enhance their health. However, female teachers felt more discomfort in their working environment and in utilizing medical institutes. Teachers in the 20s and 40s perceived health benefits through regular lifestyle and exercise. Teachers with less experience feel more pressure from their work environment. Teachers below their 30s feel more dissatisfaction towards using medical facilities. Teachers working in Technical High Schools are more aware of promoting their health through regular health checkups, exercise, and lifestyle ; however, teachers from Academic High Schools feel more pressure from their work environment. Teachers not performing supplementary lessons and supervising night self-study sessions are more willing to go through regular health checkups than those performing them. Also, teachers with supplementary lessons and night self-study supervisions claimed lack of leisure time, pressure from work environment, and inconvenience in using medical facilities a deterrent to promoting their health behavior. The Relationship between Health Promotion Behavior, Perceived Benefits, and Perceived Barriers The correlation ratio between Health Promotion Behavior and Perceived Benefits shows a positive relationship. The results show that High School teachers believed regular health checkups are necessary in maintaining their health. This research shows that teachers consider the following factors important in the order shown ; regular lifestyle and exercise, prevention of geriatric diseases, improving ones eating habits. In short, teachers who are more aware of the importance of regular health checkups are also more aware of the importance of promoting their health. The correlation ratio between Health Promotion Behavior and Perceived Barriers shows negative relationship. High School Teachers believe that lack of leisure activity, pressure from work environment, familys financial burden, fear of diseases, inconvenience in using medical facilities are a deterrent in promoting their health behavior. In other words, teachers with less leisure time and negative pressures from their work environment were less active in promoting their health behavior. This study shows that High School teachers will be able to promote their health behavior by maintaining regular health checkups, lifestyle, exercise, and preventing geriatric diseases. However, teachers believed that insufficient leisure time and negative pressure from their work environment acted as a deterrent to maintaining their health behavior. Most High School teachers believe they are at present healthy, and they were actively engaged in Preventative Health Promotion. The result of this study demonstrates that External factors have a large impact on teachers, which in turn acts negatively on their Health Promotion Behavior. In order to guarantee teachers health promotion behavior, systematic health checkups and increased leisure time, improvement in their work environment are necessary. Teachers also need to take a more active interest in their health.

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Impact of Compost Application on Improvement of Rice Productivity and Quality in Reclaimed Soil (간척지 토양에서 퇴비처리가 벼의 생산 및 품질개선에 미치는 영향)

  • Moon, Young-Hun;Kwon, Young-Rip;Ahn, Byung-Koo;Kim, Dae-Hyang;Han, Seong-Soo
    • Korean Journal of Soil Science and Fertilizer
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    • v.44 no.5
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    • pp.808-813
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    • 2011
  • This study was conducted to reduce the dependability of farmers on chemical fertilizers for rice cultivation. Soil chemical and biological properties were monitored before experiment and at the time of harvesting. The results showed that EC, available $SiO_2$, and exchangeable $Ca^{2+}$ were decreased at the time of harvesting while pH, OM, and exchangeable $K^+$ and $Mg^{2+}$ were remain unchanged, compared with soil before experiment. Population of aerobic bacteria, Bacillus sp., and fungi were also increased at the time of harvesting in the paddy field, compared with before fertilization, in the treatment of 50% soil-testing fertilizer+ 50% compost. Concentrations of N, P, and K in rice leaves increased with the fertilizers application, maximum increase was recorded in 50% soil-testing fertilizer+ 50% compost. Non-significant difference was observed in the morphological parameters of rice among the treatments. The chlorophyll contents of rice leaf increased in a similar fashion up to 60 days, thereafter, sharp decrease was observed in all the treatments. Maximum yield (per 10a) was recorded in the field treated with 50% soil-testing fertilizer+ 50% compost followed by standard applied fertilizer, 70% soil-testing fertilizer+ 30% compost, soil-testing fertilizer and unfertilized plot. Amylose content showed non-significant difference within the treatments. Protein content increased with the use of fertilizers and best protein content was recorded in the treatment of 50% soil-testing fertilizer+ 50% compost. It was concluded that the amount of the chemical fertilizer used was directly proportional to the protein content of rice grain. However, the palatability of rice grown in unfertilized field was better than the treatments but minimum yield was obtained. Hence, the treatment of 50% soil-testing fertilizer+ 50% compost, was the best among the fertilizer combinations for rice cultivation as supported by the yield, protein and palatability index.

Design of Cloud-Based Data Analysis System for Culture Medium Management in Smart Greenhouses (스마트온실 배양액 관리를 위한 클라우드 기반 데이터 분석시스템 설계)

  • Heo, Jeong-Wook;Park, Kyeong-Hun;Lee, Jae-Su;Hong, Seung-Gil;Lee, Gong-In;Baek, Jeong-Hyun
    • Korean Journal of Environmental Agriculture
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    • v.37 no.4
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    • pp.251-259
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    • 2018
  • BACKGROUND: Various culture media have been used for hydroponic cultures of horticultural plants under the smart greenhouses with natural and artificial light types. Management of the culture medium for the control of medium amounts and/or necessary components absorbed by plants during the cultivation period is performed with ICT (Information and Communication Technology) and/or IoT (Internet of Things) in a smart farm system. This study was conducted to develop the cloud-based data analysis system for effective management of culture medium applying to hydroponic culture and plant growth in smart greenhouses. METHODS AND RESULTS: Conventional inorganic Yamazaki and organic media derived from agricultural byproducts such as a immature fruit, leaf, or stem were used for hydroponic culture media. Component changes of the solutions according to the growth stage were monitored and plant growth was observed. Red and green lettuce seedlings (Lactuca sativa L.) which developed 2~3 true leaves were considered as plant materials. The seedlings were hydroponically grown in the smart greenhouse with fluorescent and light-emitting diodes (LEDs) lights of $150{\mu}mol/m^2/s$ light intensity for 35 days. Growth data of the seedlings were classified and stored to develop the relational database in the virtual machine which was generated from an open stack cloud system on the base of growth parameter. Relation of the plant growth and nutrient absorption pattern of 9 inorganic components inside the media during the cultivation period was investigated. The stored data associated with component changes and growth parameters were visualized on the web through the web framework and Node JS. CONCLUSION: Time-series changes of inorganic components in the culture media were observed. The increases of the unfolded leaves or fresh weight of the seedlings were mainly dependent on the macroelements such as a $NO_3-N$, and affected by the different inorganic and organic media. Though the data analysis system was developed, actual measurement data were offered by using the user smart device, and analysis and comparison of the data were visualized graphically in time series based on the cloud database. Agricultural management in data visualization and/or plant growth can be implemented by the data analysis system under whole agricultural sites regardless of various culture environmental changes.

Pressure-load Calibration of Multi-anvil Press at Ambient Temperature through Structural Change in Cold Compressed Amorphous Pyrope (비정질 파이로프의 저온 압축에 따른 구조 변화를 이용한 멀티 앤빌 프레스의 상온 압력-부하 보정)

  • Lhee, Juho;Kim, Yong-Hyun;Lee, A Chim;Kim, Eun Jeong;Lee, Seoyoung;Lee, Sung Keun
    • Korean Journal of Mineralogy and Petrology
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    • v.35 no.1
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    • pp.65-73
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    • 2022
  • The proper estimation of physical and chemical properties of Earth materials and their structures at high pressure and high temperature conditions is key to the full understanding of diverse geological processes in Earth and planetary interiors. Multi-anvil press - high-pressure generating device - provides unique information of Earth materials under compression, mainly relevant to Earth's upper mantle. The quantitative estimation of the relationship between the oil load within press and the actual pressure conditions within the sample needs to be established to infer the planetary processes. Such pressure-load calibration has often been based on the phase transitions of crystalline earth materials with known pressure conditions; however, unlike at high temperature conditions, phase transitions at low (or room) temperatures can be sluggish, making the calibration at such conditions challenging. In this study, we explored the changes in Al coordination environments of permanently densified pyrope glasses upon the cold compression using the high-resolution 27Al MAS and 3QMAS NMR. The fractions of highly coordinated Al in the cold compressed pyrope glasses increase with increasing oil load and thus, the peak pressure condition. Based on known relationship between the peak pressure and the Al coordination environment in the compressed pyrope glasses at room temperature, we established a room temperature pressure-load calibration of the 14/8 HT assembly in 1,100-ton multi-anvil press. The current results highlight the first pressure-load calibration of any high pressure device using high-resolution NMR. Irreversible structural densification upon cold compression observed for the pyrope glasses provides insights into the deformation and densification mechanisms of amorphous earth materials at low temperature and high pressure conditions within the subducting slabs.

Studies on agronomic characters of rice and soil textures in Akiochi paddy field (추락도(秋落稻)의 형태적(形態的) 특성(特性) 및 추락답토양(秋落畓土壤)에 관(關)한 연구(硏究))

  • Cho, Baik-Hyun;Lee, C.Y.;Lee, E.W.
    • Applied Biological Chemistry
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    • v.6
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    • pp.61-77
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    • 1965
  • In this experiment, Akiochi was studied especially on plant growth on the degraded soils. Besides, such soils were carefully examined on its character and plant body was analysed to know the difference in various mineral contents. For this purpose, paddy cultivation was done with the variety Pal Dal at Suwon, Sosa and Pyungtak. Three plots were chosen at each location as the normal and 2 levels of akiochi, a-the stronger and b-the weaker. Harvests from these 9 plots were measured agronomically and also chemically analysised. As for soil, after an observation on vertical section of soil, samples from each layer were also studied both physically and chemically. The results are summarized as follows. 1. Outer changes in rice plant and changes in yield components. 1) Rice from Akiochi soil showed remarkably shortened culm length, head length, protrusoion length, blade length of boot leaf, and coleoptile length, compared with that from the normal paddy field. 2) There was a tendency for Akiochi rice to have more heads per plant. 3) Akiochi rice showed poorer intercalary growth of upper 3 internodes. The ratio of this upper internode length to total culm length was also smaller in this case. Consquently the ratio of lower internode length to total culm length became larger than that from normal peddy field. 4) Akiochi rice showed significantly fewer first spikelets and attached grains of head at main stem. 5) Maturing rate of both this main seem of whole plant body was remarkably lower than that of normal rice. 6) Akiochi rice showed lower head weight of main stem, total hulled rice weight, total grain yield, 1000-grain weight, straw weight and straw-hulled rice ratio. 2. Physical and chemical study on soil. 1) Akiochi soil showed thinner upper layer and total thickness of upper and lower parts was smaller than that of normal. 2) Akiochi soil of Suwon was mainly composed of sand, while that of Sosa and Pyungtak was composed of heavy clay. 3) Chemical analysis indicated that content of $SiO_2$ in upper layer is always lower than that of normal. But no other common tendencies were found. 4) This analysis further lillustrates lower content of Fe, & Mn at Suwon ; of Mn at Sosa and higher content of Fe at Sosa and organic matters at Pyungtak. 5) Some differences in the content of N in each plot could be marked though irregular. 3. Chemical Composition of plant body. 1) Chemical analysis on grain, boot leaf and straw did not suggest any remarkable differences between normal and Akiochi rice, except that the latter contains less Si in boot leaf and less Mn in straw. 2) Contents of each chemical element were measured in grain and straw to calculate the percentage of element content in grain to that of whole plant body including both grain and straw. Here, Akiochi rice always showed lower value in N, K and Mn. 4. Relationship between chemical composition of plant body and that of soil. Akiochi soil at Sosa marked lower content of Mn. This caused another lower content of this element in grain, boot leaf and straw. But except that, no remarkable relationship could be found in this study.

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