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Evaluation of External Quality of Brand Soybeans (콩 시판 브랜드 제품의 외관 품질 평가)

  • Jong, Seung-Keun;Woo, Shun-Hee;Kim, Hong-Sig
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.52 no.3
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    • pp.239-248
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    • 2007
  • Although high nutritional values and continuous identification of important functional substances of soybean [Glycine max (L.) Merrill.] promote consumption of soybean products worldwide, informations on quality of brand soybean is not enough for consumers. Total of 100 brand soybeans [32 for soypaste and source, 45 black testa (lage), and 17 black testa (small) or medicinal soybean and beansprout soybean] were collected at supermarkets and several external quality factors were analyzed. Brand soybeans were marked with the environmental friendly and intimating words along with soybean (white or yellow), black soybean (black-, frost-, late frost-, green or inner-green-), medicinal soybean and beansprout soybean. Among 100 brand soybeans 30% was 1 kg package and 59% was 500 g package, difference between printed and actual weights of 70% brand soybeans was ${\pm}1%$ and weights of 2/3 of brand soybeans were higher than printed weight. Range of 100 seed weights of soypaste and source, black testa (large) and black testa (small) and beansprout soybeans were $23.7{\sim}47.8g$, $21.9{\sim}44.5g$ and $9.5{\sim}15.0g$, respectively. Although ranges of 100 seed weights of soypaste and source and black testa (large) soybeans were similar, 63% of soypaste and source were less than 29 g, while 78% of black testa (large) soybeans were higher than 30 g. Although average and highest percentages of seeds separated with 6.7 mm sieve were similar with 87.4% and 99.9% for soypaste and source soybean and 86.5% and 99.5% for black testa (large) soybean, respectively, the lowest percentages were 70.7% for soypaste and source soybean and 14.4% for black testa (large) soybean. When 100 seed weight was greater than 35 g, 90% of seeds were remained on 6.7 mm sieve. On the other hand 100 g weight and percentage of seeds remained on 6.7 mm sieve showed significantly positive correlations [r=0.7488** for soypaste and source soybean and r=0.7874** for black testa (large) soybean when 100 seed weight was $20{\sim}30g$. Based on hilum color and/or appearance, 76% of brand soybeans collected (more than 90% in yellow testa soybeans) were found to be mixed more than 10% with other cultivars or landraces. Foreign materials such as sand, piece of clothe, wood piece, dead insects, other soybeans were found in 20% of brand soybeans. Average test weight of brand soybeans was 762g $L^{-1}$ with a range of $645{\sim}820g\;L^{-1}$. Soybeans from local markets were as good as brand soybeans in 100 seed weight, uniformity of seeds, weight of foreign materials and test weight.

Estimation of Fresh Weight and Leaf Area Index of Soybean (Glycine max) Using Multi-year Spectral Data (다년도 분광 데이터를 이용한 콩의 생체중, 엽면적 지수 추정)

  • Jang, Si-Hyeong;Ryu, Chan-Seok;Kang, Ye-Seong;Park, Jun-Woo;Kim, Tae-Yang;Kang, Kyung-Suk;Park, Min-Jun;Baek, Hyun-Chan;Park, Yu-hyeon;Kang, Dong-woo;Zou, Kunyan;Kim, Min-Cheol;Kwon, Yeon-Ju;Han, Seung-ah;Jun, Tae-Hwan
    • Korean Journal of Agricultural and Forest Meteorology
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    • v.23 no.4
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    • pp.329-339
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    • 2021
  • Soybeans (Glycine max), one of major upland crops, require precise management of environmental conditions, such as temperature, water, and soil, during cultivation since they are sensitive to environmental changes. Application of spectral technologies that measure the physiological state of crops remotely has great potential for improving quality and productivity of the soybean by estimating yields, physiological stresses, and diseases. In this study, we developed and validated a soybean growth prediction model using multispectral imagery. We conducted a linear regression analysis between vegetation indices and soybean growth data (fresh weight and LAI) obtained at Miryang fields. The linear regression model was validated at Goesan fields. It was found that the model based on green ratio vegetation index (GRVI) had the greatest performance in prediction of fresh weight at the calibration stage (R2=0.74, RMSE=246 g/m2, RE=34.2%). In the validation stage, RMSE and RE of the model were 392 g/m2 and 32%, respectively. The errors of the model differed by cropping system, For example, RMSE and RE of model in single crop fields were 315 g/m2 and 26%, respectively. On the other hand, the model had greater values of RMSE (381 g/m2) and RE (31%) in double crop fields. As a result of developing models for predicting a fresh weight into two years (2018+2020) with similar accumulated temperature (AT) in three years and a single year (2019) that was different from that AT, the prediction performance of a single year model was better than a two years model. Consequently, compared with those models divided by AT and a three years model, RMSE of a single crop fields were improved by about 29.1%. However, those of double crop fields decreased by about 19.6%. When environmental factors are used along with, spectral data, the reliability of soybean growth prediction can be achieved various environmental conditions.

The Effects of d-Amphetamine on the Brain 5-HT, 5-HIAA, MAO and the Behavior of Rat (d-Amphetamine이 백서뇌의 5-HT, 5-HIAA, MAO 및 행동에 미치는 영향에 관한 연구)

  • Suh, Yoo-Hun;Woo, Jong-In;Park, Chan-Woong
    • The Korean Journal of Pharmacology
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    • v.17 no.2
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    • pp.47-62
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    • 1981
  • d-amphetamine이 사람에서 paranoid schizophrenia와 아주 유사한 model psychosis를 일으키며 또한 사람과 실험동물에서 실제 정신분열증에서 뚜렷이 관찰되는 behavioral perservation을 일으킬 수 있음이 관찰되었다. 이에 많은 학자들은 이러한 양상의 행동변화가 정신분열증의 원인 추구에 중요한 의미를 주는 뇌변화를 반영할지도 모른다는 생각에 많은 연구를 거듭하여 왔다. 지금까지는 주로 catecholamine기전에 대하여 집중적 연구가 수행되어져 왔으나 최근에는 d-amphetamine의 약리기전의 일부는 5-HT기전이 차지하고 있으며, 여러 행동변화에는 catecholaimin 보다 5-HT 가 더 중요하게 관계하고 있다는 주장이 나오고 있다. 또한 d-amphetamine은 시험관내에서 MAO 특히 신경전달물질 분해요소인 A type를 가역적으로 억제할 수 있음이 보고되어 많은 흥미를 끌어왔으나 생체내에서의 억제여부는 직접적으로 확인이 되고 있지 않다. 그러나 최근에 Braestrup(1977)과 El Hait(1978)등은 간접적인 방법으로 생체내에서도 억제시킬 수 있음을 보고하고 있다. 이에 저자는 d-amphetamine에 의해 야기되는 행동변화와 그 밑바탕을 이루는 생화학적 기전에 5-HT가 차지하는 역할을 알아보기 위해서 다음의 실험을 시행하였다. 첫째, d-amphetamine의 급성, 만성 투여가 5-HT의 5-HIAA 로의 turnover와 MAO활성도에 어떤 영향을 미치며, 더 나아가서 이 양자사이에 어느 정도 상관관계가 있는지를 알아보기 위해서 d-amphetamine을 투여한 후 시간 경과에 따라서 뇌내 5-HT, 5-HIAA, 5-HT turnover rate와 MAO 활성도를 측정하였다. 둘째, d-amphetamine, 5-HT 합성을 증가시키는 약물과 합성을 억제시키는 약물을 투여하고, 위의 생화학적 실험과 행동관찰을 병합 실시하여 비교분석하였다. 그 결과는 다음과 같다. 1) d-amphetamine (6 mg/kg)을 급성투여시, 뇌내 5-HT함량이 투여 1시간 후에 최고로(대조치의 123%, p<0.001) 증가되다가 이후 감소하며, 5-HIAA 함량은 처음 15분부터 감소하기 시작하다가 30분에 최저로 떨어지며(대조치의 78%, p<0.005) 이후 증가하여 24시간째는 약간 대조치 이상으로 회복되었다. 미토콘드리아 MAO활성도는 1시간째에 최저로 떨어지다가(대조치의 89%, p<0.05)이후 회복하기 시작하여 24시간째에 약간 대조치 이상으로 회복되었다. 5-HT의 turnover rate는 MAO활성도 변화와 거의 같은 변화를 보였다. 2) 만성투여시 (하루 2번, 14일간 투여)는 5-HT 함량, 5-HIAA 함량, MAO 활성도 및 5-HT turnover rate 모두가 중등도로 감소되었다. (각각 대조치의 87%, 69%, 80%, 79%). 3) MAO 활성도와 5-HT turnover rate 사이에는 높은 상관관계가 있었다. (r=0.866, p<0.001, N=94). 4) MAO 활성도의 역동학 실험에서는 대조치에 비해 투여군에서 Km 값은 의미가 있는 증가가 있었으나 $V_{max}$값은 큰 변동이 없었다. 5) d-amphetamine을 급성 투여할때는 sleeping과 lying components는 상당한 감소를 보인 반면, locomotor activity 는 1시간까지는 상당한 증가를 보였으며 용량이 적을수록 더 큰 증가가 있었다. 반면 stereotypy는 1시간까지 용량이 증가할수록 더 큰 증가가 나타나서 locomotor activity에서 stereotypy 의 증가로 이행을 나타내었다. 만성 투여시는 locomotor activity는 점차적인 감소를 보였으나 stereotypy는 점차적인 증가가 나타나서 14일쯤에는 평형에 도달하였다. 6) PCPA 단독 투여군(400 mg/kg, 3번)에 있어서는 5-HT와 5-HIAA 함량의 상당한 감소가 나타났으나 MAO 활성도와 행동에는 큰 변화를 나타내지 않았다. PCPA전 처치군에 있어서도 5-HT와 5-HIAA 함량은 마찬가지로 상당한 감소를 나타내었으나 gnawing, sniffing과 locomotor activity는 더 증가를, stereotyped head weaving, forepaw treading과 hindlimb abduction은 상당한 감소를 나타내었다. 7) L-tryptophan(100 mg/kg)단독 투여시는 5-HT 함량은 약간 증가를 나타내었으나 5-HIAA 함량은 상당한 증가를 보였다. MAO활성도나 행동은 큰 변화없었다. L-tryptophan 전처치군에 있어서는 5-HT 함량은 더 큰 증가를 보였으나, 5-HIaa 함량은 MAO 활성도는 별 변화없었으며 stereotypedlateral head waving, forepaw treading 과 hindlimb abduction은 증가를, locomotor activity, gnawing과 sniffing components는 감소를 나타내었다. 8) d-amphetamine 단독투여, 혹은 L-tryptophan 전처치, PCPA 전처치후 측정한 5-HT 함량과 stereotyped head weaving, forepaw treading, hinilimb abduction components 사이에는 높은 상관관계가 있었다(r=0.789, p<0.001). 반면 5-HT 함량과 locomotor activity, stereotyped gnawing과 sniffing components 사이에는 약한 음성의 상관관계가 있었다. (r=0.554, p <0.005). 이상의 결과로 미루어 볼때 5-HT의 5-HIAA 로의 turnover rate 는 주로 MAO 활성도에 의해서 조절되며 5-HT 기전이 d-amphetamine에 의해서 야기된 여러 행동변화 중 상당한 부분에서 중요한 역할을 하리라고 생각된다.

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Biochemical Characterizations of Phenylalanine Ammonia-Lyase and its Mutants to Develop an Enzymatic Therapy for Phenylketonuria (페닐케톤뇨증의 효소치료 개발을 위한 phenylalanine ammonia-lyase 및 유전자 변이형의 생화학적 특성)

  • Kim, Woo-Mi
    • Journal of Life Science
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    • v.19 no.9
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    • pp.1226-1231
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    • 2009
  • Enzyme substitution with recombinant phenylalanine ammonia-lyase (PAL, EC 4.3.1.5) is currently being explored for treatment of phenylketonuria (PKU), an autosomal recessive genetic disorder with mutations of the gene encoding phenylalanine-4-hydroxylase (EC 1.14.16.1). However, oral administration of PAL is limited because of proteolytic digestion in the gastrointestinal tract. The aim of this study was to determine the biochemical properties of PAL and delinate the susceptibility of wild-type PAL to pancreatic proteolysis by exploring several mutants, and to develop therapeutic drugs with PAL for PKU. The specific activity of PAL was assayed and its optimal pH, temperature stability, and intestinal protease susceptibility were investigated. Its $V_{max}$ values for phenylalanine and tyrosine were 1.77 and $0.47{\mu}mol$/ min/mg protein, respectively, and its $K_m$ values were $4.77{\times}10^{-4}$ and $4.37{\times}10^{-4}\;M$, respectively. PAL showed an optimal pH at 8.5, corresponding to the average pH range of the small intestine. It showed no loss of activity at $-80^{\circ}C$ for 5 months and possessed 93.4% of its activity under $4^{\circ}C$ for 4 wks. PAL was susceptible to chymotrypsin digestion and, to a lesser extent, to trypsin, elastase, carboxypeptidase A, and B. The trypsin and chymotrypsin cleaving sites were mutated to investigate protection from pancreatic digestion and the specific activities of these mutants were evaluated. The six mutants displayed low specific activities compared to the wild-type, suggesting that the primary trypsin and chymotrypsin cleaving sites may be essential for catalytic reaction. The PAL mutants could therefore be applied as a pretreatment modality without susceptibility to proteolytic attack, however, additional modification for enhancing enzymatic activity is needed to reduce the Phe levels effectively.

Variations in Nutrients & CO2 Uptake Rates and Photosynthetic Characteristics of Saccharina japonica from the South Coast of Korea (다시마(Saccharina japonica)의 생장에 따른 영양염 및 CO2 흡수율과 광합성 특성 변화)

  • Hwang, Jae-Ran;Shim, Jeong-Hee;Kim, Jeong-Bae;Kim, Sook-Yang;Lee, Yong-Hwa
    • The Sea:JOURNAL OF THE KOREAN SOCIETY OF OCEANOGRAPHY
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    • v.16 no.4
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    • pp.196-205
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    • 2011
  • To investigate the contribution of macroalgae to biogeochemical nutrients and carbon cycles, we measured the uptake rates of nutrients and $CO_2$ and characteristics of fluorescence of Saccharina japonica (Laminaria japonica Areschoug) using an incubation method in an acrylic chamber. From January to May 2011, S.japonica was sampled at Ilkwang, one of well-known macroalgae culture sites around Korea and ranged 46~288 cm long and 4.8~22.0 cm wide of whole thallus. The production rate of dissolved oxygen by S. japonica (n=25) was about $6.9{\pm}5.8{\mu}mol\;g^{-1}$ fresh weight(FW) $h^{-1}$. The uptake rate of total dissolved inorganic carbon ($TCO_2$), calculated by total alkalinity and pH, was $8.9{\pm}7.9{\mu}mol\;g^{-1}\;FW\;h^{-1}$. Mean nutrients uptake were $175.6{\pm}161.1\;nmol\;N\;g^{-1}\;FW\;h^{-1}$ and $12.7{\pm}10.1\;nmol\;P\;g^{-1}\;FW\;h^{-1}$. There were logarithmic relationships between thallus length and uptake rates of nutrients and $CO_2$, which suggested that younger specimens (<100-150 cm) were much more efficient at nutrients and $CO_2$ uptake than old specimens > 150 cm. There was a positive linear correlation ($r^2$=9.4) existed between the dissolved oxygen production rate and the $TCO_2$ uptake rate, suggesting that these two factors may serve as good indicators of S. japonica photosynthesis. There was also positive linear relationship between maximal quantum yield ($F_v/F_m$) and production/uptake rates of dissolved oxygen, $TCO_2$ and phosphate, suggested that $F_v/F_m$ could be used as a good indicator of photosynthetic ability and $TCO_2$ consumption of macroalgae. Maximum relative electron transport rate ($rETR_{max}$) of S. japonica increased as thallus grew and was high in distal part of thallus which may be resulted from the increase of photosynthetic cell density per area. The annual $TCO_2$ uptake by S. japonica in Gijang area was estimated about $1.0\sim1.7{\times}10^3C$ ton, which was about 0.02-0.03% of carbon dioxide emission in Busan City. Thus, more research should be focused on macroalgae-based biogeochemical cycles to evaluate the roles and contributions of macroalgae to the global carbon cycle.

Antioxidant Activities of Stachys sieboldii MIQ Roots (초석잠(Stachys sieboldii MIQ) 뿌리 추출물의 항산화 활성 고찰)

  • 백홍석;나영수;김도한;이창한;류병호;송승구
    • Journal of Life Science
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    • v.14 no.1
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    • pp.1-7
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    • 2004
  • The root of Stnchys Sieboldif MIQ was extracted three times with methanol and extract was found to contain 3.02% of polyphenols and 1.97% of flavonoids. DPPH radical scavenging method, ferric thiocyanate method, and nitrite scavenging ability method were employed to investigate the constituents of the extract and to measure their activity on antioxidation. The fraction extracted by ethylacetate showed higher anti oxidation value than that of $\alpha-tocopherol$, butylated hydroxyanisole (BHA), and butylated hydroxytoluene (BHT) at the same concentration. UV-VIS spectral data of the extract by ethylacetate that was isolated on a silica gel column proved adsorption maxima in the range of 280∼330 nm. The fraction ES-RS that has $\lambda_{max}(nm)$ of band 1, 325nm and band II, 289nm exhibitd the strongest activity on antioxidation. ES-R5 fraction showed similar pattern to flavones by the analysis of UV-VIS spectral data.

Effect of Thermal Treatments on Flavonoid Contents in Domestic Soybeans (국내산 대두(Glycine max. Merr)자원의 플라보노이드 대사체 동정 및 열처리 효과)

  • Shin, Jae-Hyeong;Kim, Heon-Woong;Lee, Min-Ki;Jang, Ga-Hee;Lee, Sung-Hyen;Jang, Hwan-Hee;Hwang, Yu-Jin;Park, Keum-Yong;Song, Beom-Heon;Kim, Jung-Bong
    • Korean Journal of Environmental Agriculture
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    • v.34 no.2
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    • pp.105-110
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    • 2015
  • BACKGROUND: Soy isoflavones, structurally similar to endogenous estrogens, may affect human body through both hormonally mediated and non-hormonally related mechanisms. Heat processing could change chemical compositions. The effects of different thermal processes, boiling and HTHP(high temperature and high pressure) on the composition of isoflavone compounds and total amount of domestic soybeans were investigated in this study. METHOD AND RESULTS: Three different kinds of soybean samples were collected from RDA-Genebank. The samples were extracted using methanol, distilled water, and formic acid based solvent. Also the same solvents were used for mobile phase in UPLC/ToF/MS. All of the isoflavone compounds were analyzed based on the aglycone type of external standard for quantification. The standard calibration curve presented linearity with the correlation coefficient R2 > 0.98, analysed from 1 to 50 ppm concentration. The total isoflavone contents does not change by treatment within the same breed. While "boiling" and "HTHP" processes tend to increase the contents of aglycone and ${beta}$-glucosides, "fresh" soybeans retained the high concentration of malonylglucosides. CONCLUSION: These results have to be considered while developing an effective functional food, from the health while point of view using soybeans.

Effects of Food Combinations of Leguminous Seeds on Nymphal Development, Adult Longevity and Oviposition of Bean Bug, Riptortus clavatus Thunberg (두류품종의 먹이조합에 따른 톱다리개미허리노린재의 약충발육, 성충 수명 및 산란)

  • 배순도;김현주;박정규;정진교;조현제
    • Korean journal of applied entomology
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    • v.43 no.2
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    • pp.123-127
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    • 2004
  • This study was conducted to determine the effect of food combinations of leguminous seeds on the nymphal development and adult fecundity of Riptortus clavatus Thunberg. Nymphal duration ranged from 20 to 28 days depending on food combinations with the shortest on the seed of soybean (Glycine max Linnaeus), soybean + kidney bean (Phaseolus vulgaris Linnaeus) and soybean + peanut (Archis hypogaea Linnaeus) and the longest on the seed of kidney bean. Instar duration was longer with increasing instar from 2.4 to 2.5 days in the 1st instar to 5.3 to 7.3 days in the 5th instar Accordingly, instar duration was significantly different on food combinations exception of 1 st instar Percent emergence varied from 3.5% on peanut to 65.0% on the seed of soybean + peanut. Nymphal mortality was the highest in the 1 st instar regardless of food combinations. Adult longevity was in range of 5.5 days to 11.2 days which was the shortest on the seed of kidney bean+peanut and the longest on soybean + peanut and was about 8.0 days on the other food combinations. Total number of eggs laid by female was most on soybean+peanut and was least on kidney bean + peanut. Accordingly, it can be recommended that food combination of the seed of soybean + peanut was the best and then was soybean only while other food communications of leguminous seeds was hard to use for mass rearing of R. clavatus.

A Benchmark of AI Application based on Open Source for Data Mining Environmental Variables in Smart Farm (스마트 시설환경 환경변수 분석을 위한 Open source 기반 인공지능 활용법 분석)

  • Min, Jae-Ki;Lee, DongHoon
    • Proceedings of the Korean Society for Agricultural Machinery Conference
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    • 2017.04a
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    • pp.159-159
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    • 2017
  • 스마트 시설환경은 대표적으로 원예, 축산 분야 등 여러 형태의 농업현장에 정보 통신 및 데이터 분석 기술을 도입하고 있는 시설화된 생산 환경이라 할 수 있다. 근래에 하드웨어적으로 급증한 스마트 시설환경에서 생산되는 방대한 생육/환경 데이터를 올바르고 적합하게 사용하기 위해서는 일반 산업 현장과는 차별화 된 분석기법이 요구된다고 할 수 있다. 소프트웨어 공학 분야에서 연구된 빅데이터 처리 기술을 기계적으로 농업 분야의 빅데이터에 적용하기에는 한계가 있을 수 있다. 시설환경 내/외부의 다양한 환경 변수는 시계열 데이터의 난해성, 비가역성, 불특정성, 비정형 패턴 등에 기인하여 예측 모델 연구가 매우 난해한 대상이기 때문이라 할 수 있다. 본 연구에서는 근래에 관심이 급증하고 있는 인공신경망 연구 소프트웨어인 Tensorflow (www.tensorflow.org)와 대표적인 Open source인 OpenNN (www.openn.net)을 스마트 시설환경 환경변수 상호간 상관성 분석에 응용하였다. 해당 소프트웨어 라이브러리의 운영환경을 살펴보면 Tensorflow 는 Linux(Ubuntu 16.04.4), Max OS X(EL capitan 10.11), Windows (x86 compatible)에서 활용가능하고, OpenNN은 별도의 운영환경에 대한 바이너리를 제공하지 않고 소스코드 전체를 제공하므로, 해당 운영환경에서 바이너리 컴파일 후 활용이 가능하다. 소프트웨어 개발 언어의 경우 Tensorflow는 python이 기본 언어이며 python(v2.7 or v3.N) 가상 환경 내에서 개발이 수행이 된다. 주의 깊게 살펴볼 부분은 이러한 개발 환경의 제약으로 인하여 Tensorflow의 주요한 장점 중에 하나인 고속 연산 기능 수행이 일부 운영 환경에 국한이 되어 제공이 된다는 점이다. GPU(Graphics Processing Unit)의 제공하는 하드웨어 가속기능은 Linux 운영체제에서 활용이 가능하다. 가상 개발 환경에 운영되는 한계로 인하여 실시간 정보 처리에는 한계가 따르므로 이에 대한 고려가 필요하다. 한편 근래(2017.03)에 공개된 Tensorflow API r1.0의 경우 python, C++, Java언어와 함께 Go라는 언어를 새로 지원하여 개발자의 활용 범위를 매우 높였다. OpenNN의 경우 C++ 언어를 기본으로 제공하며 C++ 컴파일러를 지원하는 임의의 개발 환경에서 모두 활용이 가능하다. 특징은 클러스터링 플랫폼과 연동을 통해 하드웨어 가속 기능의 부재를 일부 극복했다는 점이다. 상기 두 가지 패키지를 이용하여 2016년 2월부터 5월 까지 충북 음성군 소재 딸기 온실 내부에서 취득한 온도, 습도, 조도, CO2에 대하여 Large-scale linear model을 실험적(시간단위, 일단위, 주단위 분할)으로 적용하고, 인접한 세그먼트의 환경변수 예측 모델링을 수행하였다. 동일한 조건의 학습을 수행함에 있어, Tensorflow가 개발 소요 시간과 학습 실행 속도 측면에서 매우 우세하였다. OpenNN을 이용하여 대등한 성능을 보이기 위해선 병렬 클러스터링 기술을 활용해야 할 것이다. 오프라인 일괄(Offline batch)처리 방식의 한계가 있는 인공신경망 모델링 기법과 현장 보급이 불가능한 고성능 하드웨어 연산 장치에 대한 대안 마련을 위한 연구가 필요하다.

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The Promotive Effects of Antioxidative Apigenin on the Bioavailability of Paclitaxel for Oral Delivery in Rats

  • Choi, Sang-Joon;Choi, Jun-Shik
    • Biomolecules & Therapeutics
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    • v.18 no.4
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    • pp.469-476
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    • 2010
  • This study was to investigate the effect of apigenin on the bioavailability of paclitaxel after oral and intravenous administration in rats. The effect of apigenin on P-glycoprotein (P-gp), cytochrome P450 (CYP)3A4 activity was evaluated. The pharmacokinetic parameters of paclitaxel were determined in rats after oral (40 mg/kg) or intravenous (5 mg/kg) administration of paclitaxel with apigenin (0.4, 2 and 8 mg/kg) to rats. Apigenin inhibited CYP3A4 activity with 50% inhibition concentration ($IC_{50}$) of 1.8 ${\mu}M$. In addition, apigenin significantly inhibited P-gp activity. Compared to the control group, apigenin significantly increased the area under the plasma concentration-time curve (AUC, p<0.05 by 2 mg/kg, 59.0% higher; p<0.01 by 8 mg/kg, 87% higher) of oral paclitaxel. Apigenin also significantly (p<0.05 by 2 mg/kg, 37.2% higher; p<0.01 by 8 mg/kg, 59.3% higher) increased the peak plasma concentration ($C_{max}$) of oral paclitaxel. Apigenin significantly increased the terminal half-life ($t_{1/2}$, p<0.05 by 8 mg/kg, 34.5%) of oral paclitaxel. Consequently, the absolute bioavailability (A.B.) of paclitaxel was significantly (p<0.05 by 2 mg/kg, p<0.01 by 8 mg/kg) increased by apigenin compared to that in the control group, and the relative bioavailability (R.B.) of oral paclitaxel was increased by 1.14- to 1.87-fold. The pharmacokinetics of intravenous paclitaxel were not affected by the concurrent use of apigenin in contrast to the oral administration of paclitaxel. Accordingly, the enhanced oral bioavailability by apigenin may be mainly due to increased intestinal absorption caused via P-gp inhibition by apigenin rather than to reduced renal and hepatic elimination of paclitaxel. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the gastrointestinal tract via the inhibition of P-gp and reduced first-pass metabolism of paclitaxel via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by apigenin. It appears that the development of oral paclitaxel preparations as a combination therapy is possible, which will be more convenient than the i.v. dosage form.