• Title/Summary/Keyword: Yield potential

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Novel Isoquinolinamine and Isoindoloquinazolinone Compounds Exhibit Antiproliferative Activity in Acute Lymphoblastic Leukemia Cells

  • Roolf, Catrin;Saleweski, Jan-Niklas;Stein, Arno;Richter, Anna;Maletzki, Claudia;Sekora, Anett;Escobar, Hugo Murua;Wu, Xiao-Feng;Beller, Matthias;Junghanss, Christian
    • Biomolecules & Therapeutics
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    • v.27 no.5
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    • pp.492-501
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    • 2019
  • Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.

Evaluation of biological activity for Dangyuja (Citrus grandis) leaves and investigation of optimal concentrations extracted by alternative ethanol concentrations (에탄올 농도별 당유자 잎의 최적추출조건 및 생리활성 평가)

  • Nakamura, Masaya;Ra, Jong-Hwan;Kim, Ju-Sung
    • Journal of Plant Biotechnology
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    • v.46 no.1
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    • pp.45-55
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    • 2019
  • TheCitrus grandis Osbeck is a special product in the Jeju island. The product has been as a remedy for liver damage and hang over. This study demonstrates how to investigate and compare the antioxidant, phenol content, tyrosinase and ${\alpha}$-glucosidase inhibitory activity, antimicrobial, and alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) activity with the C. grandis leaves extracted in different ethanol concentrations. From the yield, a 20% ethanol extract demonstrated the highest results among the other extracts. The distilled water extract showed the most abundant in a total phenol content and highest ABTS radical scavenging activity and reducing power assay. In the DPPH radical scavenging activity, ${\alpha}$-glucosidase and tyrosinase inhibitory assay (used ${\text\tiny{L}}$-tyrosine as substrate), the 80% ethanol extract exhibited a higher value than other extracts. The 60% ethanol extract showed prominent activities in the tyrosinase inhibitory (used ${\text\tiny{L}}$-dopa as substrate), ADH and ALDH activity assay. In the minimum inhibitory concentration (MIC) assay, 60% and 80% ethanol extracts inhibited the bacterial growth almost similarly. Moreover, the gram-positive bacteria was more restrained than the gram-negative bacteria. The resultsrevealed that the distilled water and 80% ethanol extract showed a relatively higher antioxidant activity compared to other extracts. The 60 ~ 80% ethanol extracts demonstrated potential tyrosinase, ${\alpha}$-glucosidase inhibitory, antimicrobial, ADH and ALDH activities. Therefore, the C. grandis is suggested to be considered as a functional material for various proposes.

Evaluation of Oxidation Inhibition and Nitrogen Oxide Scavenging Activity from Curcuma longa L. Extracts (울금(Curcuma longa L.) 추출물의 산화억제 및 질소산화물 소거활성)

  • Oh, Da-Young;Kim, Han-Soo
    • Journal of the Korean Applied Science and Technology
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    • v.36 no.1
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    • pp.13-22
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    • 2019
  • The aim of the present investigation was to assess the oxidation inhibition by nitrogen oxide scavenging activity and physiological activities. Bioactive compound of proanthocyanidin $69.000{\pm}2.737mg$ catechin equivalents (CE)/g dry weight. Antioxidant effects (nitric oxide radical scavenging activity, nitrite scavenging activity, ${\beta}$-carotene bleaching assay and lipid peroxidation inhibition activity) of distilled water (DW), 70% ethanol and n-butanol extract of turmeric (Curcuma longa L.). Turmeric extracts yield were DW 17.11%, 70% ethanol 15.26% and n-butanol 4.12%, respectively. Oxidation inhibition activity of the samples exhibited a dose-dependent increase. However, in the current study, none of the samples evaluated showed activity as strong as the BHA and trolox. Total flavonoid content was the highest in the n-butanol extract, followed by 70% ethanol and DW extract. Further, nitrite scavenging activity was the highest for the n-butanol extract. As a result of this experiment, the turmeric can be utilized as a valuable and potential natural oxidation inhibition for the functional food industry.

Improvement of Salt Accumulated Soil and Crop Growth using Coal Ash (석탄회를 이용한 염류집적 토양 개선과 작물 생육 증진)

  • Lee, Jong Cheol;Oh, Se Jin;Kang, Min Woo;Kim, Young Hyun;Kim, Dong Jin;Lee, Sang Soo
    • Korean Journal of Environmental Agriculture
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    • v.40 no.2
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    • pp.83-91
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    • 2021
  • BACKGROUND: Cultivation area using agricultural plastic film facilities in Korea is rapidly increasing every year; however, it accelerates the salt accumulation in soils due to repeated cultivation and excessive use of chemical fertilizers. Coal ash contains various trace elements and has high potential to be used in agricultural purposes. This research was aimed to improve the quality of salts-accumulated soils and crop growth grown in the plastic film facilities using the soil amendment derived from coal ash and zero-valent iron powder. METHODS AND RESULTS: Soil amendment used in the study was manufactured using coal ash with iron powder and subjected to a typical upland soil for soil quality enhancement and two salts-accumulated soils for crop growth. After one month incubation of the salts-accumulated soils treated with the soil amendment, soil pH increased significantly and soil EC decreased by approximately 50%, compared to the control or the treatment without the soil amendment. Since the soil salts' concentration is proportional to EC, the subjected soil amendment can be proposed as an effective way to overcome soil salts accumulation in agricultural plastic film facilities. For crop growth, the length of roots and stems increased by approximately 10% and the dry weight also increased by a maximum of 75%, compared to the control. CONCLUSION: The soil amendment made from waste resources such as coal ash and zero-valent iron was found to not only be effective in improving salt-accumulated soils and crop yield but also be safe against harmful heavy metals.

Biosynthesis of Compound K, a biologically active saponin of ginseng(Panax ginseng) by bioconversion (인삼(Panax ginseng)으로부터 생물전환을 이용한 생리활성물질인 Compound K의 생합성)

  • Kim, MooSung;Kim, Ja-i;Jung, Kyung-Hwan;Yu, Kwang-Won;Moon, Gi-Seong;Lee, Hyang-Yeol
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.5
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    • pp.1335-1344
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    • 2021
  • Ginsenoside Compound K is a triterpene saponin found in the leafs, stems and roots of Panax ginseng. This study aimed to prepare a valuable ginsenoside Compound K using ginseng extracts with the enzyme(Plantase). Plantase showed very efficient activity to produce Compound K from ginseng extracts. Plantase exhibited the highest activity at pH 5 and 50 ℃, as a result of investigating the yield of Compound K by changing the temperature and pH, while fixing the enzyme concentration to 10% or 15% over 48 hours of reaction time. Under optimium conditions, Plantase produced and accumulated Compound K over 35 wt% of whole ginseng extracts. Antimicrobial activitiy of bioconvertied ginseng extracts showed selectivity against Cutibacterium acnes KCTC 3314. Minimal inhibitory concentration (MIC) of bioconverted ginseng extract (35% of Compound K enriched extract) against Cutibacterium acnes KCTC 3314 strain is 31.25ug/mL. These results suggest that the Compound K enriched extract is potential materials for cosmetic products and Plantase is a very useful enzyme for Compound K production.

The Antioxidant and Skin-whitening Effects of Saccharomyces cerevisiae FT4-4 Isolated from Berries Grown in Sunchang (화장품 소재로서 순창 베리류 유래 Sacchromyces cerevisiae FT4-4의 항산화 활성 및 미백 효과)

  • Seo, Ji won;Ryu, Myeong Seon;Yang, Hee-Jong;Jeong, Su-Ji;Jeong, Do-Youn
    • Journal of Life Science
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    • v.31 no.2
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    • pp.175-182
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    • 2021
  • Saccharomyces lysate has the well-known function of soothing the skin in various ways: it is an anti-irritant and can treat skin care conditions, such as skin whitening and antioxidative activity. However, data on the safety for use of Saccharomyces lysate in cosmetics and skin care products are still limited. To design a new cosmetic material with antioxidant and skin-whitening effects, 80 yeast strains were isolated from berries grown in Sunchang. Among the isolates, the FT4-4 strain, which exhibited superior biological activities, was selected for further experiments. The FT4-4 strain was identified as Saccharomyces cerevisiae by 18S rRNA gene sequencing analysis. S. cerevisiae FT4-4 showed higher DPPH radical-scavenging (51.41%), superoxide dismutase (62.23%), and tyrosinase inhibition (64.75%) activities. The highest yield of biomass (3.16 g/l) and maximum growth rate of S. cerevisiae FT4-4 were observed within 16 h. Furthermore, the cytotoxicity potential of S. cerevisiae FT4-4 on B16F10 melanoma cells was measured by an MTT assay, and the results indicated that S. cerevisiae FT4-4 had a capacity to inhibit melanin up to 72.02% at an initial 10 mg/ml concentration. These results suggest that S. cerevisiae FT4-4 could be a promising candidate as a multi-functional material for application in the cosmetic industry, especially because of its antioxidant and skin-whitening effects.

Complementary measures for Environmental Performance Evaluation Index of External Space of Green Standard for Energy and Environmental Design for Apartment Complex - Focused on the Respect of Response to Climate Change - (공동주택 녹색건축인증기준의 외부공간 환경성능 평가지표 보완방안 - 기후변화 대응 측면을 중심으로 -)

  • Ye, Tae-Gon;Kim, Kwang-Hyun;Kwon, Young-Sang
    • Journal of the Architectural Institute of Korea Planning & Design
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    • v.34 no.1
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    • pp.3-14
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    • 2018
  • An apartment complex is a building use with great potential to contribute to solving problems related to urban ecological environment and climate change. The first goal of this study is to grasp the current situation of application and limitations of the ecological area rate, which is a representative evaluation index used to evaluate the environmental performance of the external space of an apartment complex in Green Standard for Energy and Environmental Design (G-SEED). The second goal is to propose a prototype of the evaluation index for evaluating greenhouse gas (GHG) reduction performance in order to supplement the evaluation index for the environmental performance of the external space in terms of response to climate change. We analyzed 43 cases of apartment complexes certified according to G-SEED, which was enforced since July 1, 2010, and found application characteristics of each space type and the limitations of ecological area rate. We analyzed overseas green building certification systems such as LEED and BREEAM that derived implications for supplementing the limitations of ecological area rate, which is focused on the evaluation of soil and water circulation function, and set up a development direction of complementary measures. Through analysis of previous studies, relevant regulations and standards, and technical documents of the manufacturer, the heat island mitigation performance of the pavement and roof surfaces of the apartment complex and the carbon uptake performance of the trees in the apartment complex was selected as parameters to yield the GHG reduction performance of the external space of the apartment complex. Finally, a quantitative evaluation method for each parameter and a prototype of the evaluation index for the GHG reduction performance were proposed. As a result of applying the prototype to an apartment complex case, the possibility of adoption and applicability as an evaluation index of G-SEED were proved.

Study on Reinforcing Skin Barrier and Anti-aging of Exosome-like Nanovesicles Isolated from Malus domestica Fruit Callus (사과 캘러스로부터 분리된 엑소좀-유사 Nanovesicles 의 피부 장벽 및 피부 노화 방지 개선 연구)

  • Seo, Yu-Ri;Lee, Kwang-Soo;Kang, Yong-Won
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.2
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    • pp.139-145
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    • 2021
  • Plant-derived exosome-like nanovesicles (PELNs) are known to include various biological activities and possess high biocompatibility. Because PELNs can influence immune responses, cell differentiation, and proliferation regulation, they can be applied in multiple industries. However, the studies on the skin physiological of exosome-like nanovesicles derived from plant callus are insignificant compared to nanovesicles derived from mammalian cells. In this study, callus was induced from apple fruit (Malus domestica), and exosome-like nanovesicles (ACELNs) were isolated for improving skin barrier and anti-aging. The yield of ACELNs was 6.42 × 109 particles/mL, and the particle size was ranged from 100 to 200 nm. HDF cells and HaCaT cells were concentration-dependent, increased in cell, and decreased in cytotoxicity. The cornified envelope formation was significantly increased compared to the control group. The COL1A1 expression and the FBN1 expression in HDF cells were increased. In addition, the ACELNs promoted collagen biosynthesis in UVA-irradiated HDF cells. These results might be considered as potential materials that could improve skin barrier and prevent skin aging.

Effects of Aucklandia lappa Decne. Extract on Hair Growth in Depilated CL57BL/6 Mice (CL57BL/6 마우스의 발모에 미치는 목향 추출물의 영향)

  • Kim, Joung-Hee;Lee, Syng-Ook;Beik, Gyoung Yeun;Kim, Keuk-Jun
    • Korean Journal of Clinical Laboratory Science
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    • v.53 no.1
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    • pp.88-95
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    • 2021
  • Aucklandia lappa Decne., a traditional herbal medicine, has been used to treat various diseases, including asthma, coughs, rheumatism, and diarrhea. In the present study, the effects of the oral administration of Aucklandia lappa Decne. extract on hair growth was investigated in hair-removed mice. A 70% ethanol extract of Aucklandia lappa Decne. (ALD) was prepared, and the extraction yield and total polyphenol content of ALD were measured as 27.30±0.01 and 28.39 mg gallic acid equivalent (GAE)/g, respectively. The oral administration of ALD to hair-removed CL57BL/6 mice for six weeks had no significant effects on food intake and body weight changes. Biochemical and histological examinations also showed that the oral administration of ALD for six weeks had no significant effect on the liver and kidney functions. On the other hand, hair growth was significantly higher in the ALD group than the control group and the Pancidil group (positive control). In addition, the number of hair follicles and the degree of collagen production in the dermis were significantly higher in the ALD group than in the control and pancidil groups. These results suggest that ALD is a potential source of nutricosmetics with hair growth-promoting effects.

Effects of rice straw fermented with spent Pleurotus sajor-caju mushroom substrates on milking performance in Alpine dairy goats

  • Fan, Geng-Jen;Chen, Mei-Hsing;Lee, Churng-Faung;Yu, Bi;Lee, Tzu-Tai
    • Animal Bioscience
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    • v.35 no.7
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    • pp.999-1009
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    • 2022
  • Objective: To improve the feeding value of rice straw (RS), this study evaluated the potential of rice straw fermented with Pleurotus sajor-caju (FRS) as dairy goat feed. Methods: Spent Pleurotus sajor-caju mushroom substrate was used as fungi inoculum to break the lignocellulose linkage of rice straw, which was solid-fermented at 25℃ to 30℃ for 8 weeks. The ruminal degradation of pangolagrass hay (PG), FRS, and RS were measured in situ for 96 hours in three dry Holstein cows, respectively. Effect of fungi fermented RS on milking performance was studied in feeding trials. A total of 21 Alpine goats a trial were divided into 3 groups: a control group in which PG accounted for 15% of the diet dry matter, and FRS or RS was used to replace the PG in the control group. Goats were fed twice a day under two 28-day trial in individual pens. Meanwhile, a 3×3 Latin square trial (14 days/period) was conducted to study the rumen digestion of three diets by using three fistulated dry goats. Rumen contents were collected for metabolite analyses every one to three hours on the last two days. Results: In situ study showed that fermentation could elevate the rumen degradable fraction and effective degradability of RS (p<0.05). Effective degradability of FRS dry matter was significantly increased from 29.5% of RS to 41.7%. Lactating trial results showed that dry matter intake and milk yield in the PG group and FRS group were similar and higher than those in RS group (p<0.05). The concentration of propionic acid and total volatile fatty acid in the RS group tended to be lower than those in PG group (p<0.10). There were no differences in rumen pH value and ammonia nitrogen level among the groups tested. Conclusion: Fermentation of rice straw by spent Pleurotus sajor-caju mushroom substrate could substantially enhance its feeding value to be equivalent to PG as an effective fiber source for dairy goat. The fermented rice straw is recommended to account for 15% in diet dry matter.