• Title/Summary/Keyword: active compound

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Comparison of network pharmacology based analysis results according to changes in principal herb in Sagunja-tang (사군자탕(四君子湯)에서 군약(君藥)의 변화에 따른 네트워크 약리학적 분석 결과 비교)

  • Lee, Byoungho;Cho, Suin
    • Herbal Formula Science
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    • v.27 no.3
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    • pp.189-197
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    • 2019
  • Objectives : The purpose of this study was to confirm whether Codonopsis Radix(CR) could be used in the same way for expected indications or diseases of adaptation instead of Ginseng Radix(GR), which acts as a principal herb in Sagunja-tang. Methods : The Traditional Chinese Medicine Systems pharmacology(TCMSP), a database for the study of systems biology related to Chinese medicine, screened potential active compounds in each quartet. By searching for all the proteins that each compound provides, the target of Sagunja-tang with GR(GRST) and the target of Sagunja-tang with CR(CRST) were compared using the network analysis method, and the top ranked target of each serving was selected. Results : Through TCMSP, a Chinese medicine database, the potential effective ingredients of GRST or CRST screened, and the target proteins related to these substances were found to be the most affected by Glycyrrhizae Radix et Rhizome, an herbal medicine mixed in Sagunja-tang, and the target diseases were the same. And the same were found for the target protein, gene and target diseases of GRST and CRST. Conclusions : The prescription with similar composition is likely to have similar network pharmacology analysis results, and the analysis result may be controlled by the herbal medicines which are assumed to be the main function. Therefore, rich and reproducible basic studies is more important because network pharmacological studies can be dominated by data that has been done a lot of previous studies.

The inflammatory activity of purified-ferulic acid from Tetragonia tetragonioides

  • Kim, Na-Hyeon;Park, Hye-Jin;Lee, Eun-Ho;Cho, Eun-Bi;Kang, In-Kyu;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.62 no.3
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    • pp.239-246
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    • 2019
  • In this study, an evaluation of the anti-inflammatory effect of ferulic acid isolated from Tetragonia tetragonioides in lipopolysaccharide (LPS) simulated RAW 264.7 cells was made. The chemical structure of the active compound was elucidated by $^1H$-NMR, $^{13}C$-NMR, and FAB-MS, and was confirmed to be ferulic acid. Ferulic acid was purified via open column chromatography with Sephadex LH-20 and MCI gel CHP-20. To test the anti-inflammatory effect of ferulic acid, LPS-stimulated RAW 264.7 cells were treated in subsequent experiments with different concentrations of ferulic acid (5, 10, and $25{\mu}g/mL$) and the levels of inflammatory cytokines and enzymes were also measured by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Cell viability was above 95% at acid concentrations ranging from $5-25{\mu}g/mL$. The results showed that 30% of the production of nitric oxide and 66% of prostaglandin $E_2$ were inhibited by $25{\mu}g/mL$ of ferulic acid, it also inhibited the protein expression of both inducible nitric oxide synthase and cyclooxygenase-2 by 70%. Additionally, it inhibited the production of the pro-inflammatory cytokines, tumor necrosis factor-${\alpha}$, interleukin-6, and interleukin-$1{\beta}$ by 40, 75, and 77%, respectively. According to these results, the anti-inflammatory activity of ferulic acid was demonstrated via his implication in the inhibition of the expression and secretion of inflammatory substances in LPS-stimulated RAW 264.7 cells. Therefore, we concluded that ferulic acid can be used as a functional additive having anti-inflammatory activity.

Rice bran fermentation by lactic acid bacteria to enhance antioxidant activities and increase the ferulic acid, ρ-coumaric acid, and γ-oryzanol content

  • Le, Bao;Anh, Pham Thi Ngoc;Kim, Jung-Eun;Cheng, Jinhua;Yang, Seung Hwan
    • Journal of Applied Biological Chemistry
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    • v.62 no.3
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    • pp.257-264
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    • 2019
  • Rice bran is considered a natural source of antioxidants. In this study, rice bran was fermented with lactic acid bacteria to increase its antioxidant activity. Four strains isolated from fermented food, Lactobacillus plantarum MJM60383, Lactococcus lactis subsp. lactis MJM60392, Lactobacillus fermentum MJM60393, and Lactobacillus paracasei MJM60396, were confirmed as safe through stability tests such as safety assessment for biogenic amine production, hemolytic activity, and mucin degradation, and showed high reducing capacity. The antioxidant activity of rice bran fermentation altered by these strains was evaluated using several methods including measurement of $Fe^{2+}$ chelating activity and scavenging activity by 1,1-diphenyl-2-picryl-hydrazil (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and nitric oxide assays. In this study, the total phenolic content and ${\gamma}$-oryzanol were evaluated by high-performance liquid chromatography. Compared to non-fermented rice bran and a commercial product, rice bran fermented with Lactococcus lactis subsp. lactis MJM60392 showed the highest phenolic content (844.13 mg GAE/g). Moreover, the content of ferulic acids, ${\rho}$-coumaric acid, and ${\gamma}$-oryzanol in rice bran increased after fermentation with L. lactis subsp. lactis MJM60392 and L. fermentum MJM60393 compared to other samples. Indeed, the DPPH radical scavenging activity and NO scavenging activity were also found to be high in these fermented rice brans. These results indicated that fermentation with lactic acid bacteria increases the active compound levels and the potent antioxidant activities of rice bran.

Microorganisms Involved in Natural Fermentation of Asparagus cochinchinensis Roots and Changes in Efficacies after Fermentation (천문동 뿌리의 자연발효에 관여하는 미생물 및 발효 후 효능 변화)

  • Kim, Min-Jee;Shin, Na Rae;Lee, Myeong-Jong;Kim, Hojun
    • Journal of Korean Medicine for Obesity Research
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    • v.18 no.2
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    • pp.96-105
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    • 2018
  • Objectives: The aim of this study was to examine the effect of Asparagus cochinchinensis (AC) and fermented AC (fAC) on microorganisms and efficacies. Methods: AC was fermented for four weeks without using any bacterial strains. Then we investigated fermentation characteristics including potential of hydrogen (pH), total sugar, microbial profiling and antioxidant compound contents such as total polyphenol and total flavonoid. The anti-obesity effects of AC and fAC were evaluated by using Oil Red O staining in 3T3-L1 adipocyte. Also anti-diabetic effects of them were evaluated by using 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-d-glucose (2-NBDG) uptake in C2C12 skeletal muscle cell. Results: Both pH and total sugar of fAC were decreased significantly compared to unfermented AC. And the abundance of total bacteria and lactic acid bacteria increased during fermentation, especially Lactobacillus plantarum. Also fermentation of AC increased the content of total polyphenol. On the metabolic aspects, we found that AC and fAC suppressed fat accumulation. Conclusions: After four weeks of fermentation, AC increased concentrations of active compounds, altered microbial composition, and inhibited fat accumulation such as triglyceride. These results indicate that fermentation of AC might be a beneficial therapeutic approach for obesity.

Effect of Inorganic Nanocomposite Based Liners on Deodorization of Kimchi

  • Chung, Kwon;Park, Hyun Jin;Shin, Yang Jai
    • KOREAN JOURNAL OF PACKAGING SCIENCE & TECHNOLOGY
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    • v.27 no.2
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    • pp.55-62
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    • 2021
  • This study aims to reduce the rancid odor generated during the fermentation process of kimchi by inserting zinc oxide (ZnO) into an inorganic porous material with a high surface area to decompose or adsorb the fermentation odor. ZnO activated by the presence of moisture exhibits decomposition of rancid odors. Mixed with Titanium dioxide (TiO2), a photocatalyst. To manufacture the packaging liner used in this study, NaOH, ZnCl2, and TiO2 powder were placed in a tank with diatomite and water. The sludge obtained via a hydrothermal ultrasonication synthesis was sintered in an oven. After being pin-milled and melt-blended, the powders were mixed with linear low-density polyethylene (L-LDPE) to make a masterbatch (M/B), which was further used to manufacture liners. A gas detector (GasTiger 2000) was used to investigate the total amount of sulfur compounds during fermentation and determine the reduction rate of the odor-causing compounds. The packaging liner cross-section and surface were investigated using a scanning electron microscope-energy dispersive X-ray spectrometer (SEM-EDS) to observe the adsorption of sulfur compounds. A variety of sulfur compounds associated with the perceived unpleasant odor of kimchi were analyzed using gas chromatography-mass spectrometry (GC-MS). For the analyses, kimchi was homogenized at room temperature and divided into several sample dishes. The performance of the liner was evaluated by comparing the total area of the GC-MS signals of major off-flavor sulfur compounds during the five days of fermentation at 20℃. As a result, Nano-grade inorganic compound liners reduced the sulfur content by 67 % on average, compared to ordinary polyethylene (PE) foam liners. Afterwards SEM-EDS was used to analyze the sulfur content adsorbed by the liners. The findings of this study strongly suggest that decomposition and adsorption of the odor-generating compounds occur more effectively in the newly-developed inorganic nanocomposite liners.

Inhibition of Jurkat T Cell Proliferation by Active Components of Rumex japonicus Roots Via Induced Mitochondrial Damage and Apoptosis Promotion

  • Qiu, Yinda;Li, Aoding;Lee, Jina;Lee, Jeong Eun;Lee, Eun-Woo;Cho, Namki;Yoo, Hee Min
    • Journal of Microbiology and Biotechnology
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    • v.30 no.12
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    • pp.1885-1895
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    • 2020
  • Rumex japonicus Houtt (RJH) is a valuable plant used in traditional medicine to treat several diseases, such as scabies and jaundice. In this study, Jurkat cell growth inhibitory extracts of R. japonicus roots were subjected to bioassay-guided fractionation, resulting in the isolation of three naphthalene derivatives (3-5) along with one anthraquinone (6) and two phenolic compounds (1 and 2). Among these compounds, 2-methoxystypandrone (5) exhibited potent anti-proliferative effects on Jurkat cells. Analysis by flow cytometry confirmed that 2-methoxystypandrone (5) could significantly reduce mitochondrial membrane potential and promote increased levels of mitochondrial reactive oxygen species (ROS), suggesting a strong mitochondrial depolarization effect. Real-time quantitative polymerase chain reaction (qPCR) analysis was also performed, and the results revealed that the accumulation of ROS was caused by reduced mRNA expression levels of heme oxygenase (HO-1), catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD). In addition, 2-methoxystypandrone (5) triggered strong apoptosis that was mediated by the arrest of the G0/G1 phase of the cell cycle. Furthermore, 2-methoxystypandrone (5) downregulated p-IκB-α, p-NF-κB p65, Bcl2, and Bcl-xl and upregulated BAX proteins. Taken together, these findings revealed that 2-methoxystypandrone (5) isolated from RJH could potentially serve as an early lead compound for leukemia treatment involving intracellular signaling by increasing mitochondrial ROS and exerting anti-proliferative effects.

Syntheses, X-ray Structures and Second Harmonic Generation Efficiencies of MAP (Methyl (2,4-dinitrophenyl)-aminopropanoate) Analogues

  • Lee Joo-Hee;Kim Kimoon;Kim Jong-Hyun;Kim Jong-Jean
    • Bulletin of the Korean Chemical Society
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    • v.13 no.3
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    • pp.268-274
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    • 1992
  • An attempt to improve the second harmonic generation (SHG) efficiency of MAP (methyl (2,4-dinitrophenyl)aminopropanoate) by modifying the substituents on the amino group of MAP is described. Several MAP analogues have been prepared using optically active amino acids alanine, phenylalanine and serine, and their SHG efficiencies measured. None of the MAP analogues exhibited SHG efficiencies as high as that of MAP. X-ray crystal structures of three MAP analogues have been determined. In the crystal structures of two of them, which were the derivatives of phenylalanine, two crystallographically-independent molecules existing in the asymmetric unit are aligned almost antiparallel. These structures are consistent with the very low SHG efficiencies of these compounds. On the other hand, the crystal structure of a serine derivative reveals substantial alignment of the dinitroaniline chromophore along the polar axis. However, the angle of 86.2° between the molecular charge tranfer axis and the polar axis of the crystal is still far away from the optimum value of 54.74° for the phase-matchable SHG. The structure is consistent with the SHG efficiency of this compound which is much higher than those of the phenylalanine derivatives but still lower than that of MAP. This study demonstrates the importance of the orientation of molecules in the crystal lattice in determining secod-order nonlinear optical properties of crystalline materials.

Liquid Chromatography-Tandem Mass Spectrometric Analysis of Nannozinone A and Its Application to Pharmacokinetic Study in Mice

  • Lee, Chul Haeng;Kim, Soobin;Lee, Jaehyeok;Jeon, Ji-Hyeon;Song, Im-Sook;Han, Young Taek;Choi, Min-Koo
    • Mass Spectrometry Letters
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    • v.12 no.1
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    • pp.21-25
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    • 2021
  • We aimed to develop and validate a sensitive analytical method of nannozinone A, active metabolite of Nannochelins A extracted from the Myxobacterium Nannocytis pusilla, in mouse plasma using a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Mouse plasma samples containing nannozinone A and 13C-caffeine (internal standard) were extracted using a liquid-liquid extraction (LLE) method with methyl tert-butyl ether. Standard calibration curves were linear in the concentration range of 1 - 1000 ng/mL (r2 > 0.998) with the inter- and intra-day accuracy and precision results less than 15%. LLE method gave results in the high and reproducible extraction recovery in the range of 78.00-81.08% with limited matrix effect in the range of 70.56-96.49%. The pharmacokinetics of nannozinone A after intravenous injection (5 mg/kg) and oral administration (30 mg/kg) of nannozinone A were investigated using the validated LC-MS/MS analysis of nannozinone A. The absolute oral bioavailability of nannozinone A was 8.82%. Plasma concentration of nannozinone A after the intravenous injection sharply decreased for 4 h but plasma concentration of orally administered nannozinone A showed fast distribution and slow elimination for 24 h. In conclusion, we successfully applied this newly developed sensitive LC-MS/MS analytical method of nannozinone A to the pharmacokinetic evaluation of this compound. This method can be useful for further studies on the pharmacokinetic optimization and evaluating the druggability of nannozinone A including its efficacy and toxicity.

Enhanced Large-Scale Production of Hahella chejuensis-Derived Prodigiosin and Evaluation of Its Bioactivity

  • Jeong, Yu-jin;Kim, Hyun Ju;Kim, Suran;Park, Seo-Young;Kim, HyeRan;Jeong, Sekyoo;Lee, Sang Jun;Lee, Moo-Seung
    • Journal of Microbiology and Biotechnology
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    • v.31 no.12
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    • pp.1624-1631
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    • 2021
  • Prodigiosin as a high-valued compound, which is a microbial secondary metabolite, has the potential for antioxidant and anticancer effects. However, the large-scale production of functionally active Hahella chejuensis-derived prodigiosin by fermentation in a cost-effective manner has yet to be achieved. In the present study, we established carbon source-optimized medium conditions, as well as a procedure for producing prodigiosin by fermentation by culturing H. chejuensis using 10 L and 200 L bioreactors. Our results showed that prodigiosin productivity using 250 ml flasks was higher in the presence of glucose than other carbon sources, including mannose, sucrose, galactose, and fructose, and could be scaled up to 10 L and 200 L batches. Productivity in the glucose (2.5 g/l) culture while maintaining the medium at pH 6.89 during 10 days of cultivation in the 200 L bioreactor was measured and increased more than productivity in the basal culture medium in the absence of glucose. Prodigiosin production from 10 L and 200 L fermentation cultures of H. chejuensis was confirmed by high-performance liquid chromatography (HPLC) and liquid chromatography-mass spectrometry (LC-MS) analyses for more accurate identification. Finally, the anticancer activity of crude extracted prodigiosin against human cancerous leukemia THP-1 cells was evaluated and confirmed at various concentrations. Conclusively, we demonstrate that culture conditions for H. chejuensis using a bioreactor with various parameters and ethanol-based extraction procedures were optimized to mass-produce the marine bacterium-derived high purity prodigiosin associated with anti-cancer activity.

Evaluation of Acute Toxicity of Pomace Schisandra chinensis Extracts Using SD-rats (SD-rats를 이용한 오미자박 추출물의 급성경구독성 평가)

  • Seokho, Kim;Bo Ra, Yoo;Young-Suk, Kim;Jong-Min, Lim;Bon-Hwa, Ku;Kyeong Tae, Kwak;Byeong Yeob, Jeon
    • Herbal Formula Science
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    • v.30 no.4
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    • pp.281-291
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    • 2022
  • Objectives : In this study, acute oral toxicity test of pomace Schisandra chinensis extracts was conducted in order to up-cycling to a high value-added industry using by-products discarded in the production process of Schisandra chinensis products and active ingredients such as dibenzocyclooctadiene lignans in Schisandra chinensis. Methods : Pomace Schisandra chinensis extracts were orally administered to SD-rats(female, n=3) without a control group according to the 'OECD guidelines'. After, mortality and clinical signs were observed, and the deceased animals were subjected to an autopsy. In addition, acute oral toxicity test was sequentially performed in step I (300 mg/kg), step II(300 mg/kg), step III(2,000 mg/kg), and step IV(2,000 mg/kg) according to the mortality. Results : There were no abnormalities caused by pomace Schisandra chinensis extracts in step I and step II. However, one animal each died in step III and step IV. In addition, clinical signs(salivation, decrease in food intake, prone position, decrease of locomotor activity, loss of locomotor activity, convulsion, hypothermia, lacrimation, staining around mouth, soiled perineal region, reddish urine, chromaturia, decrease of fecal volume, lying on side, blackish stool, no stool, compound-colored stool, refusal to feed, excitement, hypersensitivity, rigidity, dorsal position, etc.) were observed. But, no clinical signs were observed from 5th day, and experiment animals recovered completely. Conclusions : As a result of this study, pomace Schisandra chinensis extracts may exhibit acute toxicity at concentrations of 2,000 to 5,000 mg/kg, and the GHS classification was designated as 'Category 5'.