• Natural Product Sciences
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• v.19 no.4
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• pp.286-289
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• 2013

Phytochemical constituents were isolated from bitter melon (the fruits of Momordica charantia) through open column chromatography. Their structures were identified as ${\beta}$-sitosterol (1), (23E)-$5{\beta}$,19-epoxycucurbita-6,23-diene-$3{\beta}$,25-diol (2), daucosterol (3), uracil (4), and allantoin (5) by interpretation of spectroscopic analysis including MS and $^1H$- & $^{13}C$-NMR. Among them, allantoin (5) was isolated from this plant for the first time.

• Journal of Applied Biological Chemistry
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• v.59 no.2
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• pp.107-112
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• 2016

Pectolinarin was isolated from the ethyl acetate fraction of Cirsium setidens using open column chromatography and was analyzed using spectrometry. Pectolinarin content in Cirsium spp. was determined using HPLC/UV. Pectolinarin content in the aerial part of Cirsium spp. was higher than that in the root and pappus. Pectolinarin content was highest in the aerial part of C. chlorolepis (110.65mg/g extract). Consequently, the aerial part of C. chlorolepis has potential for use in new natural medicinal products, health supplements, and beverages.

• Genomics & Informatics
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• v.16 no.4
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• pp.36.1-36.3
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• 2018

Next generation sequencing (NGS), a high-throughput DNA sequencing technology, is widely used for molecular biological studies. In NGS, RNA-sequencing (RNA-Seq), which is a short-read massively parallel sequencing, is a major quantitative transcriptome tool for different transcriptome studies. To utilize the RNA-Seq data, various quantification and analysis methods have been developed to solve specific research goals, including identification of differentially expressed genes and detection of novel transcripts. Because of the accumulation of RNA-Seq data in the public databases, there is a demand for integrative analysis. However, the available RNA-Seq data are stored in different formats such as read count, transcripts per million, and fragments per kilobase million. This hinders the integrative analysis of the RNA-Seq data. To solve this problem, we have developed a web-based application using Shiny, COEX-seq (Convert a Variety of Measurements of Gene Expression in RNA-Seq) that easily converts data in a variety of measurement formats of gene expression used in most bioinformatic tools for RNA-Seq. It provides a workflow that includes loading data set, selecting measurement formats of gene expression, and identifying gene names. COEX-seq is freely available for academic purposes and can be run on Windows, Mac OS, and Linux operating systems. Source code, sample data sets, and supplementary documentation are available as well.

• Natural Product Sciences
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• v.17 no.4
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• pp.367-371
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• 2011

Effects of the extract and fractions from Parasenecio pseudotaimingasa on rat lens aldose reductase (AR) inhibition have been investigated. Among them, the n-BuOH fraction was exhibited good inhibitory potencies ($IC_{50}$ value 1.42 ${\mu}g/ml$). Phytochemical constituents were isolated from the n-BuOH fraction by open column chromatography. Their structures were elucidated as luteolin-7-O-rutinoside (1) and luteolin-7-Oglucoside (2) on the basis of spectroscopic analysis. Compounds 1 and 2 exhibited strong AR inhibitory activity, with $IC_{50}$ values of 2.37 and 1.05 ${\mu}M$, respectively. This is the first report on the isolation of compounds 1 and 2 from P. pseudotaimingasa. These results suggest that P. pseudotaimingasa could be a useful material in the development of a novel AR inhibitory agent against diabetic complications.

• Journal of Microbiology and Biotechnology
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• v.29 no.6
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• pp.839-844
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• 2019

Anthranilate derivatives have been used as flavoring and fragrant agents for a long time. Recently, these compounds are gaining attention due to new biological functions including antinociceptive and analgesic activities. Three anthranilate derivatives, N-methylanthranilate, methyl anthranilate, and methyl N-methylanthranilate were synthesized using metabolically engineered stains of Escherichia coli. NMT encoding N-methyltransferase from Ruta graveolens, AMAT encoding anthraniloyl-coenzyme A (CoA):methanol acyltransferase from Vitis labrusca, and pqsA encoding anthranilate coenzyme A ligase from Pseudomonas aeruginosa were cloned and E. coli strains harboring these genes were used to synthesize the three desired compounds. E. coli mutants (metJ, trpD, tyrR mutants), which provide more anthranilate and/or S-adenosyl methionine, were used to increase the production of the synthesized compounds. MS/MS analysis was used to determine the structure of the products. Approximately, $185.3{\mu}M$ N-methylanthranilate and $95.2{\mu}M$ methyl N-methylanthranilate were synthesized. This is the first report about the synthesis of anthranilate derivatives in E. coli.

• Journal of Ginseng Research
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• v.47 no.5
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• pp.662-671
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• 2023

Background: 20(S)-protopanaxadiol (PPD), a ginsenoside metabolite, has prominent benefits for the central nervous system, especially in improving learning and memory. However, its transcriptional targets in brain tissue remain unknown. Methods: In this study, we first used mass spectrometry-based drug affinity responsive target stability (DARTS) to identify the potential proteins of ginsenosides and intersected them with the transcription factor library. Second, the transcription factor PURA was confirmed as a target of PPD by biolayer interferometry (BLI) and molecular docking. Next, the effect of PPD on the transcriptional levels of target genes of PURA in brain tissues was determined by qRT-PCR. Finally, bioinformatics analysis was used to analyze the potential biological features of these target proteins. Results: The results showed three overlapping transcription factors between the proteomics of DARTS and transcription factor library. BLI analysis further showed that PPD had a higher direct interaction with PURA than parent ginsenosides. Subsequently, BLI kinetic analysis, molecular docking, and mutations in key amino acids of PURA indicated that PPD specifically bound to PURA. The results of qRT-PCR showed that PPD could increase the transcription levels of PURA target genes in brain. Finally, bioinformatics analysis showed that these target proteins were involved in learning and memory function. Conclusion: The above-mentioned findings indicate that PURA is a transcription target of PPD in brain, and PPD upregulate the transcription levels of target genes related to cognitive dysfunction by binding PURA, which could provide a chemical and biological basis for the study of treating cognitive impairment by targeting PURA.

• Journal of Ginseng Research
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• v.45 no.4
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• pp.465-472
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• 2021

Background: Ginseng can help regulate brain excitability, promote learning and memory, and resist cerebral ischemia in the central nervous system. Ginsenosides are the major effective compounds of Ginseng, but their protein targets in the brain have not been determined. Methods: We screened proteins that interact with the main components of ginseng (ginsenosides) by affinity chromatography and identified the 14-3-3 ζ protein as a potential target of ginsenosides in brain tissues. Results: Biolayer interferometry (BLI) analysis showed that 20(S)-protopanaxadiol (PPD), a ginseng saponin metabolite, exhibited the highest direct interaction to the 14-3-3 ζ protein. Subsequently, BLI kinetics analysis and isothermal titration calorimetry (ITC) assay showed that PPD specifically bound to the 14-3-3 ζ protein. The cocrystal structure of the 14-3-3 ζ protein-PPD complex showed that the main interactions occurred between the residues R56, R127, and Y128 of the 14-3-3 ζ protein and a portion of PPD. Moreover, mutating any of the above residues resulted in a significant decrease of affinity between PPD and the 14-3-3 ζ protein. Conclusion: Our results indicate the 14-3-3 ζ protein is the target of PPD, a ginsenoside metabolite. Crystallographic and mutagenesis studies suggest a direct interaction between PPD and the 14-3-3 ζ protein. This finding can help in the development of small-molecular compounds that bind to the 14-3-3 ζ protein on the basis of the structure of dammarane-type triterpenoid.

• Journal of Ginseng Research
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• v.43 no.1
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• pp.154-160
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• 2019

Background: Compound K (CK) is an active metabolite of ginseng saponin, ginsenoside Rb1, that has been shown to have ameliorative properties in various diseases. However, its role in inflammation and the underlying mechanisms are poorly understood. In this report, the antiinflammatory role of CK was investigated in macrophage-like cells. Methods: The CK-mediated antiinflammatory mechanism was explored in RAW264.7 and HEK293 cells that were activated by lipopolysaccharide (LPS) or exhibited overexpression of known activation proteins. The mRNA levels of inflammatory genes and the activation levels of target proteins were identified by quantitative and semiquantitative reverse transcription polymerase chain reaction and Western blot analysis. Results: CK significantly inhibited the mRNA expression of inducible nitric oxide synthase and tumor necrosis factor-${\alpha}$ and morphological changes in LPS-activated RAW264.7 cells under noncytotoxic concentrations. CK downregulated the phosphorylation of AKT1, but not AKT2, in LPS-activated RAW264.7 cells. Similarly, CK reduced the AKT1 overexpression-induced expression of aldehyde oxidase 1, interleukin-$1{\beta}$, interferon-${\beta}$, and tumor necrosis factor-${\alpha}$ in a dose-dependent manner. Conclusion: Our results suggest that CK plays an antiinflammatory role during macrophage-mediated inflammatory actions by specifically targeting the AKT1-mediated signaling pathway.

• The Journal of Korean Medicine
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• v.43 no.3
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• pp.16-26
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• 2022

Objectives: Traditional Korean medicine (TKM) has been supplied as part of a national health care system in South Korea under a dual medical system, however it has been difficult to mix western medicine and TKM medical practices in existing hospitals. For the objective of innovative integration between them, Comprehensive and Integrative Medicine Hospital were founded in Daegu, South Korea. Here, we discussed the clinical outcomes of cancer patients who received integrative cancer treatment (ICT). Methods: A total of 678 patients previously diagnosed with cancer were retrospectively checked in our institution for 2 years. After applying inclusion/exclusion criteria, 573 patients were eligible for the final analysis. The overall survival (OS) of these patients in the aftercare period were determined. We looked at how clinical factors and treatments including chemotherapy, complementary and alternative medicine (CAM), and TKM affected the OS. Results: At the first visit, 212 subjects had no evidence of disease after tumor resection and 355 ones with advanced cancer, who receiving ICT including chemotherapy, CAM, and TKM showed better OS compared to the CAM including TKM or the best supportive care (median OS = 216, 78, and 46 days, respectively). The median OS was not reached in TKM only, even though the sample size was small (N=12). Even after adjusting for clinical factors associated to liver, renal, and hematologic manifestation, ICT still remained significant. Conclusions: We demonstrated that ICT might be beneficial for advanced cancer regardless of the performance status, liver and renal function, since it positively affected the OS.

• Biomolecules & Therapeutics
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• v.29 no.2
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• pp.227-233
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• 2021

Benzo[a]pyrene (B[a]P) is a polycyclic aromatic hydrocarbon and ubiquitous environmental toxin with known harmful effects to human health. Abnormal phenotypes of keratinocytes are closely associated with their exposure to B[a]P. Resorcinol is a component of argan oil with reported anticancer activities, but its mechanism of action and potential effect on B[a]P damage to the skin is unknown. In this study, we investigated the effects of resorcinol on B[a]P-induced abnormal keratinocyte biology and its mechanisms of action in human epidermal keratinocyte cell line HaCaT. Resorcinol suppressed aryl hydrocarbon receptor (AhR) activity as evidenced by the inhibition of B[a]P-induced xenobiotic response element (XRE)-reporter activation and cytochrome P450 1A1 (CYP1A1) expression. In addition, resorcinol attenuated B[a]P-induced nuclear translocation of AhR, and production of ROS and pro-inflammatory cytokines. We also found that resorcinol increased nuclear factor (erythroid-derived 2)-like 2 (Nrf2) activity. Antioxidant response element (ARE)-reporter activity and expression of ARE-dependent genes NAD(P)H dehydrogenase [quinone] 1 (NQO1), heme oxygenase-1 (HO-1) were increased by resorcinol. Consistently, resorcinol treatment induced nuclear localization of Nrf2 as seen by Western analysis. Knockdown of Nrf2 attenuated the resorcinol effects on ARE signaling, but knockdown of AhR did not affect resorcinol activation of Nrf2. This suggests that activation of antioxidant activity by resorcinol is not mediated by AhR. These results indicate that resorcinol is protective against effects of B[a]P exposure. The mechanism of action of resorcinol is inhibition of AhR and activation of Nrf2-mediated antioxidant signaling. Our findings suggest that resorcinol may have potential as a protective agent against B[a]P-containing pollutants.