• Biomolecules & Therapeutics
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• 제32권4호
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• pp.442-450
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• 2024

The type-1 cannabinoid receptor (CB₁R) is a potential therapeutic target in several pathological conditions, including neuropsychological disorders and neurodegenerative diseases. Owing to their structural diversity, it is not easy to derive general structure-activity relationships (SARs) for CB₁R ligands. In this study, CB₁R ligands were classified into six structural families, and the corresponding SAR was determined for their affinities for CB₁R. In addition, we determined their functional activities for the activation of extracellular signal-regulated kinases (ERKs). Among derivatives of indol-3-yl-methanone, the highest ligand affinity was observed when a pentyl and a naphthalenyl group were attached to the N1 position of the indole ring and the carbon site of the methanone moiety, respectively. In the case of adamantane indazole-3-carboxamide derivatives, the presence of fluorine in the pentyl group, the substituent at the N1 position of the indazole ring, strongly increased the affinity for CB₁R. For (naphthalen-1-yl) methanone derivatives, the presence of 4-alkoxynaphthalene in the methanone moiety was more beneficial for the affinity to CB₁R than that of a heterocyclic ring. The functional activities of the tested compounds, evaluated through ERK assay, were correlated with their affinity for CB₁R, suggesting their agonistic nature. In conclusion, this study provides valuable insight for designing novel ligands for CB₁R, which can be used to control psychiatric disorders and drug abuse.

• Asian-Australasian Journal of Animal Sciences
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• 제28권7호
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• pp.958-965
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• 2015

Lycopene, a red non-provitamin A carotenoid, mainly presenting in tomato and tomato byproducts, has the highest antioxidant activity among carotenoids because of its high number of conjugated double bonds. The objective of this study was to investigate the effect of lycopene supplementation in the diet on plasma lipid profile, lipid peroxidation and antioxidant defense system in feedlot lamb. Twenty-eight Bamei male lambs (90 days old) were divided into four groups and fed a basal diet (LP0, 40:60 roughage: concentrate) or the basal diet supplemented with 50, 100, and 200 mg/kg lycopene. After 120 days of feeding, all lambs were slaughtered and sampled. Dietary lycopene supplementation significantly reduced the levels of plasma total cholesterol (p<0.05, linearly), total triglycerides (TG, p<0.05) and low-density lipoprotein cholesterol (LDL-C, p<0.05), as well as atherogenic index (p<0.001), whereas no change was observed in high-density lipoprotein cholesterol (p>0.05). The levels of TG (p<0.001) and LDL-C (p<0.001) were decreased with the feeding time extension, and both showed a linear trend (p<0.01). Malondialdehyde level in plasma and liver decreased linearly with the increase of lycopene inclusion levels (p<0.01). Dietary lycopene intake linearly increased the plasma antioxidant vitamin E level (p<0.001), total antioxidant capacity (T-AOC, p<0.05), and activities of catalase (CAT, p<0.01), glutathione peroxidase (GSH-Px, p<0.05) and superoxide dismutase (SOD, p<0.05). The plasma T-AOC and activities of GSH-Px and SOD decreased with the extension of the feeding time. In liver, dietary lycopene inclusion showed similar antioxidant effects with respect to activities of CAT (p<0.05, linearly) and SOD (p<0.001, linearly). Therefore, it was concluded that lycopene supplementation improved the antioxidant status of the lamb and optimized the plasma lipid profile, the dosage of 200 mg lycopene/kg feed might be desirable for growing lambs to prevent environment stress and maintain normal physiological metabolism.

• 대한임상검사과학회지
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• 제53권2호
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• pp.165-173
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• 2021

할미밀망은 국내에서 자생하는 미나리아재비과의 낙엽활엽덩굴식물이다. 어린 잎은 식용으로 사용되며 줄기와 뿌리는 약재로 사용된다. 할미밀망 줄기에 대한 항산화 연구는 보고되었으나 잎에 대한 연구는 현재 수행되지 않았다. 본 연구에서는 할미밀망을 70% 에탄올 추출물로 제조하고 항산화 및 항염증 생리 활성을 비교하였다. 항산화 활성을 측정하기 위해 5가지 분석(총 폴리 페놀 함량, 플라보노이드 함량, 환원력, ABTS 및 DPPH 라디칼 소거 활성)이 사용되었으며 모든 분석에서 농도 의존적 효과를 나타냈다. 항염증 활성을 조사하기 위해 RAW 264.7 세포를 사용했다. 할미밀망은 농도(31.25-250 ㎍/mL)에서 세포 독성을 나타내지 않았다. 할미밀망(250 ㎍/mL)은 LPS에 비해 세포의 수지상적 형태 변화를 억제하였고(34.4%), NO (77.4%), IL-6 (85.5%) 및 TNF-α (41.2%)의 발현을 억제함으로써 염증을 낮추는 효과를 나타내었다. 또한 할미밀망(250 ㎍/mL)은 LPS 단독 처리군에 비해 COX-2 (79.8%), iNOS2 (93.9%), IL-6 (87.6%) 및 TNF-α (77.3%)의 유전자 발현을 억제했다. 이러한 결과는 할미밀망이 우수한 항산화 및 항염증 작용을 가지고 있음을 보여준다. 그러므로 할미밀망은 향후 항산화 및 항염증 효과를 가진 천연 생물 유래 소재로 활용될 수 있을 것이다.

• Journal of Plant Biotechnology
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• 제49권4호
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• pp.339-346
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• 2022

본 연구는 벌나무 에탄올 추출물의 황색포도상구균에 대한 항균 및 항산화 활성을 검증하였다. 총 폴리페놀 및 플라보노이드 함량, DPPH와 ABTS 라디칼 소거효능과 FRAP법을 사용한 환원력을 측정하여 벌나무 에탄올 추출물의 항산화활성을 검증하였고, Paper disc법, MIC 및 MBC법을 통하여 황색포도상구균에 대한 벌나무 에탄올 추출물의 항균 활성을 검증하였다. 총 폴리페놀 및 플라보노이드 함량은 각각 266.66 ㎍ GAE/mg와 6.46 ㎍ QE/mg이었다. DPPH와 ABTS 라디칼 소거능은 농도 의존적 소거능을 보였고, 벌나무 에탄올 추출물의 RC₅₀ 값은 각각 21.49, 12.81 ㎍/mL이었다. 환원력을 평가하기 위해 수행된 FRAP 분석에서 벌나무 추출물은 0.73 ± 0.19 mM FeSO₄ E/mg의 효능을 보여주었다. Paper disc법을 이용한 황색포도상구균에 대한 벌나무 추출물의 항균 활성은 2 mg에서 3 mm의 저해환을 보여주었으며, 최소 저해농도 연구에서는 1 mg/mL 이상의 농도에서 80% 이상의 억제력을 보여주었고, 16 mg/mL 이상의 농도에서 최소저해 농도를 확인할 수 있었다. 또한, 최소살균농도 연구에서는 32 mg/mL에서 최소살균농도를 확인할 수 있었다. 벌나무 추출물을 사용한 항산화 및 황색포도상구균에 대한 항균 활성을 확인한 결과 벌나무 추출물의 아토피피부염에 유효한 물질로서의 가능성을 확인할 수 있었다.

• 축산식품과학과 산업
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• 제7권1호
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• pp.21-23
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• 2018

• 한국동물위생학회지
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• 제34권2호
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• pp.167-178
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• 2011

Garlic (Allium sativum L.) has long history of reputed value and actual use for its medicinal, antimicrobial and pesticidal properties. This study was conducted to find possible developments to natural food preservatives and natural antimicrobials from garlic extracts. The antimicrobial activities of raw garlic extract, heat, pH, temperature against pathogenic bacteria were investigated. E. coli, S. Enteritidis, L. monocytogenes, and S. aureus exhibited antimicrobial activities at 20% garlic extract, but no antimicrobial activity was seen in E. faecium. Raw garlic extract and garlic extract heated for 2 min at $95^{\circ}C$ showed strong antimicrobial activities, but the antimicrobial activity of garlic extract heated for 10 min at $95^{\circ}C$ was much less. The antimicrobial activities of 50% garlic extract adjusted pH 4.0~7.0 showed much the same, but the antimicrobial activities decreased at pH 8.0 or higher. The antimicrobial activities by storage $-18^{\circ}C$ of garlic extract showed much the same. When five strains were cultured for 72 hr at $35^{\circ}C$ in the TSB containing 1~10% garlic extract, viable cell number of five strains were decreased to $10^0{\sim}10^4$ CFU/ml even at 1% or 2.5% (E. faecium) after 24 hr, but later increased to $10^4{\sim}10^9$ CFU/ml after 72 hr. When five strains were cultured for 21 day at $4^{\circ}C$ in the TSB containing 1%, 2.5%, 5%, and 10% garlic extract, viable cell number of E. coli, S. Enteritidis, and S. aureus were decreased to $10^3$, $10^0{\sim}10^2$, $10^1{\sim}10^4$ CFU/ml after 21 day, respectively, but L. monocytogenes and E. faecium increased to $10^8$ and $10^6$ CFU/ml after 21 day.

• 대한의생명과학회지
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• 제12권4호
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• pp.393-398
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• 2006

These studies were carried out to characterize the physiological functionalities of Codonopsis lanceolata, Cornus officinalis, and their mixtures. We investigated the antioxidative, fibrinolytic, and ${\alpha}$-glucosidase inhibitory activities of them. The antioxidative activities of Codonopsis lanceoiata and Cornus officinalis were 87% and 90%, respectively. Addition of salt to Codonopsis lanceolata and Cornus officinalis did not affect its antioxidative activities. In spite of fourfold addition of Codonopsis lanceolata to Cornus officinalis, the antioxidative activity was conserved at 90%. The fibrinolytic activities of Codonopsis lanceolata and Cornus officinalis were 0.78 plasmin unit/ml and 1.74 plasmin unit/ml, respectively. Addition of salt decreased the fibrinolytic activities of both Codonopsis lanceolata and Cornus officinalis. A mixture (3:1) of Codonopsis lanceolata and Cornus officinalis exhibited a 21% increase in activity. The ${\alpha}$-glucosidase inhibitory activities of Codonopsis ianceoiata and 100-fold diluted Cornus officinalis were 25% and 73%, respectively. The addition of salt to Codonopsis lanceolata and Cornus officinalis slightly decreased their ${\alpha}$-glucosidase inhibitory activities. According to the addition of Cornus officinalis to Codonopsis lanceoiata, the ${\alpha}$-glucosidase inhibitory activities of the resulting mixture were highly increased. We anticipate that these results will be used as basic data for the development of new bifunctional foods.

• Asian-Australasian Journal of Animal Sciences
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• 제31권6호
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• pp.873-880
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• 2018

Objective: The objective of this experiment was to compare the effects of adding 130 mg/kg Cu from either copper sulfate (CS) or tribasic copper chloride (TBCC) on growth performance, mineral deposition in tissues, and the excretion in feces of pigs as well as changes in the mineral contents in tissues and feces when the supplemental Cu level was decreased from 130 mg/kg to 10 mg/kg. Methods: A total of 72 pigs ($32.6{\pm}1.2kg$) were randomly assigned to a CS diet or a TBCC diet with 6 pens per treatment. The trial lasted 102 d and included 3 phases (phase 1, 1 to 30 d; phase 2, 31 to 81 d; and phase 3, 82 to 102 d). The supplemental levels of Cu in the 2 treatments were 130 mg/kg in phase 1 and 2 and 10 mg/kg in phase 3. Results: The results showed that pigs fed the CS diet tended to have higher average daily gain than pigs fed the TBCC diet during d 1 to 81 (p<0.10). Compared with CS, TBCC increased the activities of aspartate transaminase (AST), ceruloplasmin, and superoxide dismutase in serum on d 30 (p<0.05). The TBCC decreased the Cu level in the liver on d 81 (p<0.05) and increased the Mn level in the liver on d 102 (p<0.05). The concentration of Cu in feces sharply decreased when the supplemental Cu level in diet changed from 130 mg/kg to 10 mg/kg in both diets (p<0.05). Conclusion: The result suggested that TBCC and CS had no significant difference on growth performance but TBCC had higher activities of AST and antioxidant enzymes and lower liver Cu than CS when pigs fed diets with 130 mg Cu /kg diet.

• Journal of Microbiology and Biotechnology
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• 제30권7호
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• pp.1027-1036
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• 2020

Stipa purpurea is a unique and dominant herbaceous plant species in the alpine steppe and meadows on the Qinghai-Tibet Plateau (QTP). In this work, we analyzed the composition and diversity of the culturable endophytic fungi in S. purpurea according to morphological and molecular identification. Then, we investigated the bioactivities of these fungi against plant pathogenic fungi and 1-aminocyclopropane-1-carboxylate deaminase (ACCD) deaminase activities. A total of 323 fungal isolates were first isolated from S. purpurea, and 33 fungal taxa were identified by internal transcribed spacer primers and grouped into Ascomycota. The diversity of endophytic fungi in S. purpurea was significantly higher in roots as compared to leaves. In addition, more than 40% of the endophytic fungi carried the gene encoding for the ACCD gene. The antibiosis assay demonstrated that 29, 35, 28, 37 and 34 isolates (43.9, 53.1, 42.4, 56.1, and 51.5%) were antagonistic to five plant pathogenic fungi, respectively. Our study provided the first assessment of the diversity of culture-depending endophytic fungi of S. purpurea, demonstrated the potential application of ACCD activity and antifungal activities with potential benefits to the host plant, and contributed to high biomass production and adaptation of S. purpurea to an adverse environment.

• Journal of Ginseng Research
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• 제43권3호
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• pp.377-384
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• 2019

Background: Inflammation is widespread in the clinical pathology and closely associated to the progress of many diseases. Triterpenoid saponins as a key group of active ingredients in Panax notoginseng (Burk.) F.H. Chen were demonstrated to show antiinflammatory effects. However, the chemical structures of saponins in the leaves and stems of Panax notoginseng (PNLS) are still not fully clear. Herein, the isolation, purification and further evaluation of the antiinflammatory activity of dammarane-type triterpenoid saponins from PNLS were conducted. Methods: Silica gel and reversed-phase C8 column chromatography were used. Furthermore, preparative HPLC was used as a final purification technique to obtain minor saponins with high purities. MS, NMR experiments, and chemical methods were used in the structural identifications. The antiinflammatory activities of the isolated saponins were assessed by measuring the nitric oxide production in RAW 264.7 cells stimulated by lipopolysaccharides. Real-time reverse transcription polymerase chain reaction was used to measure the gene expressions of inflammation-related gene. Results: Eight new minor dammarane-type triterpene oligoglycosides, namely notoginsenosides LK1-LK8 (1-8) were obtained from PNLS, along with seven known ones. Among the isolated saponins, gypenoside IX significantly suppressed the nitric oxide production and inflammatory cytokines including tumor necrosis $factor-{\alpha}$, interleukin 10, interferon-inducible protein 10 and $interleukin-1{\beta}$. Conclusion: The eight saponins may enrich and expand the chemical library of saponins in Panax genus. Moreover, it is reported for the first time that gypenoside IX showed moderate antiinflammatory activity.