• 동아시아식생활학회지
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• 제26권3호
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• pp.215-222
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• 2016

This study was carried out to investigate the antimicrobial and anti-inflammatory activities of ethanol extract from Glycyrrhizae radix (GR) and ethanol extract from Glycyrrhizae radix cultured with Paecilomyces japonica mycelium (GRPM). Antimicrobial activity was measured by paper disc diffusion assay and minimum inhibitory concentration (MIC). Anti-inflammatory activity was evaluated by measurement of NO production in LPS-stimulated RAW264.7 cells. For the results of the paper disc diffusion assay, GRPM showed high antimicrobial activities against Bacillus cereus, Listeria monocytogenes, and Staphylococcus aureus. In addition, the MIC of GRPM (100 ppm) was lower than that of GR (200 ppm) against L. monocytogenes. When the morphology of L. monocytogenes treated with GRPM was observed using a FE-SEM, the surface of cells treated with GRPM were damaged, and some parts of the cell wall were destroyed. The inhibitory effect on NO production in LPS-stimulated RAW264.7 cells was significantly increased by GRPM treatment. In conclusion, GRPM is superior to GR in terms of antimicrobial and anti-inflammatory activities.

• 약학회지
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• 제56권5호
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• pp.309-313
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• 2012

Antiobesity, hypotriglyceridemic and antihypertensive activities of isoflavone-free peptide mixture (black soybean peptide, BSP) were reported in our previous experiments. In the present study, angiotensin converting enzyme inhibitory (ACEi) activity was decreased in the aorta tissues of spontaneously hypertensive rats (SHRs) treated with BSP (1% in drink water) for 4 weeks, but not in serum. BSP administration significantly decreased ACE activity by 17.5% (from $33.2{\pm}4.5$ to $27.4{\pm}1.96$ mUnit/mg, p=0.0013) in aorta tissue hydrolysate. BSP treatment also decreased significantly mean blood pressure (BP) (from $213.0{\pm}16.96$ to $184.0{\pm}6.53$ mmHg, p<0.0001) as expected. These results indicate that BSP has antihypertensive activity as well as ACEi activity.

• 약학회지
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• 제26권1호
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• pp.1-8
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• 1982

Derivation of triterpenoids and then the screening for corticomimetics among them is our primary interest. $C_{11}$-oxo-triterprenoids except glycyrrhetinic acid are rarely found in the plant kingdom. Based on the facts that $C_{3}$ and $C_{11}$-Oxo-group are essential for the corticoid-like-activity through its competitive inhibition on the corticoid-5.betha.-reductase, it was attempted to produce artificial inhibitor on the enzyme by introducing $C_{11}$-oxo group to the triterpenoids of oleanene series such as oleanolic acid and hederagenin. We could obtain the $C_{11}$-oxo-oleanolic acid m.p. $264-6^{\circ}$, uv ${\lambda}max$ 249 and $C_{11}$-oxo-hederagenin amorp. uv ${\lambda}max$ 251 by acetylation, $CrO_{3}$-oxid., and deacetylation. Glycyrrhetinic acid, a natural 11-oxo-compound and the other 11-oxo-derivatives of oleanolic acid and hederagenin were compared in their inhibitory activity on the corticoid-5.betha.-reductase. The inhibitory activity of those compound were decreased in the order of $C_{11}$-oxo-oleanolic acid, $C_{11}$-oxo- hederagenin, glycyrrhetinic acid. This suggests more strong corticomimetic activity of those artificially derived $C_{11}$-oxo-oleanolic acid and $C_{11}$-oxa-hederagenin. Their Ki value were $4.6{\times}10^{-4}M$ and $5.8{\times}10^{-4}M$ respectively.

• Journal of Acupuncture Research
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• 제22권2호
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• pp.133-139
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• 2005

Cobrotoxin, a venom of Vipera lebetina turanica, is a group of basic peptidescomposed of 233 amino acids with six disulfide bonds formed by twelve cysteins. NF-kB is activated by subsequent release of inhibitory IkB and translocation of p50. Since sulfhydryl group is present in kinase domain of p50 subunit of NF-kB, cobrotoxin could modify NF-kB activity by protein-protein interaction. We therefore examined effect of cobrotoxin on NF-kB activities in lipopolysaccharide (LPS) and sodium nitroprusside (SNP)-stimulated Raw 264.7 mouse macrophages. Cobrotoxin suppressed the LPS and SNP-induced release of IkB and p50 translocation resulted in inhibition of DNA binding activity of NF-kB. Inhibition of NF-kB resulted in reduction of the LPS and SNP-induced production of inflammatory mediators NO and PGE2 generation. The inhibitory effect of cobrotoxin on the NF-kB activity were blocked by addition of reducing agents dithiothreitol and glutathione. These results demonstrate that cobrotoxin inhibits activation of NF-kB, and suggest that pico to nanomolar range of cobrotoxin could inhibit the expression of genes in the NF-kB signal pathway.

• Natural Product Sciences
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• 제13권4호
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• pp.289-294
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• 2007

Ethanolic extract (50% v/v) and alkaloid fraction of Tylophora indica leaves were examined for lysosomal enzyme inhibitory activity in adjuvant-induced arthritic rats. The alkaloid fraction showed statistically significant inhibition of arthritic lesions (p < 0.05) from day 18, (p < 0.025) from day 20 and (p < 0.001) from day 21 onwards in the adjuvant-induced arthritis, which was comparable to the response of standard drug Indomethacin. The ethanolic extract was less significant than the alkaloidal fraction in inhibition of arthritis. Alkaloid fraction showed significant (p < 0.001) inhibitory effect on the lysosomal enzyme activities in adjuvantinduced arthritic rats. It also significantly prevented decrease in collagen levels and synovial damage observed during arthritis and also inhibited increase in urinary excretion levels of collagen degradation products like hydroxyproline, hexosamine, hexuronic acid, etc. Both ethanolic extract as well as the alkaloid fraction, however, did not show any significant activity in normal nonarthritic rats. The ethanolic extract and the alkaloid fraction may thus be able to inhibit the progress of inflammation and inhibit the destructive activity of lysosomal enzymes on structural macromolecules like collagen etc. in the synovial capsule in joints during arthritic states. They may thus prevent synovial damage observed during arthritis.

• 통합자연과학논문집
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• 제7권1호
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• pp.45-49
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• 2014

The (c-Jun N-terminal kinase 3) JNK3 is a potential therapeutic target for various neurological disorders. Here, a three dimensional quantitative structure-activity relationship (3D-QSAR) study on phenoxypyridine as JNK3 inhibitors was performed to rationalize the structural requirements responsible for the inhibitory activity of these compounds. The comparative molecular field analysis (CoMFA) using different partial atomic charges, was employed to understand the structural factors affecting JNK3 inhibitory potency. The Gasteiger-Marsili yielded a CoMFA model with cross-validated correlation coefficient ($q^2$) of 0.54 and non-cross-validated correlation coefficient ($r^2$) of 0.93 with five components. Furthermore, contour maps suggested that bulky substitution with oxygen atom in $R^3$ position could enhance the activity considerably. The work suggests that further chemical modifications of the compounds could lead to enhanced activity and could assist in the design of novel JNK3 inhibitors.

• Fisheries and Aquatic Sciences
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• 제21권12호
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• pp.38.1-38.9
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• 2018

Alzheimer's disease (AD) is a disturbing and advanced neurodegenerative disease and is characterized pathologically by the accumulation of amyloid beta ($A{\beta}$) and the hyperphosphorylation of tau proteins in the brain. The deposition of $A{\beta}$ aggregates triggers synaptic dysfunction, and neurodegeneration, which lead to cognitive disorders. Here, we found that FF isolated from an eatable perennial brown seaweed E.bicyclis protect against $A{\beta}$-induced neurotoxicity in neuroblastoma cells stably transfected with two amyloid precursor protein (APP) constructs: the APP695 cDNA (SH-SY5Y-APP695swe). The FF demonstrated strong inhibitory activity for ${\beta}$-secretase ($IC_{50}$ $16.1{\mu}M$) and its inhibition pattern was investigated using Lineweaver-Burk and Dixon plots, and found to be non-competitive. Then, we tested whether FF could inhibit production of $A{\beta}$ in SH-SY5Y-APP695swe. FF inhibited the production of $A{\beta}$ and soluble-APP, residue of APP from cleaved APP by ${\beta}$-secretase. Our data show that FF can inhibit the production of $A{\beta}$ and soluble-$APP{\beta}$ via inhibition of ${\beta}$-secretase activity. Taken together these results suggest that FF may be worthy of future study as an anti-AD treatment.

• 대한의생명과학회지
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• 제26권4호
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• pp.383-388
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• 2020

Ingestion of food contaminated with microorganism, if not always, could lead to severe health problem. Preservatives has been added to food to prevent food from being contaminated with microorganism. But, these have potential to threaten the health. Therefore, much effort has been taken to find the safe materials showing the anti-microbial activity. In this study, we investigated the anti-bacterial activity of Oenothera lamarckiana aerial part extract against eight bacteria strain. In paper disc assay, extract inhibited the growth of Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus cereus and Shigella dysenteriae at 200 μg/disc, but not against Escherichia coli, E. coli O157:H7, Salmonella Typhi and S. enteritidis. Minimum inhibitory concentration (MIC) against Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus cereus and Shigella dysenteriae is 250, 250, 500 and 500 μg/mL, respectively. Compared with reported MIC of other plant resources, O. lamarckiana aerial part extract showed the relatively high anti-bacterial activity. O. lamarckiana aerial part could be suitable for the preservative development. But, it still remains to be studied to evaluate safety and so on.

• Biomolecules & Therapeutics
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• 제29권5호
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• pp.562-570
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• 2021

Topoisomerase IIα has been a representative anti-cancer target for decades thanks to its functional necessity in highly proliferative cancer cells. As type of topoisomerase IIα targeting drugs, topoisomerase II poisons are frequently in clinical usage. However, topoisomerase II poisons result in crucial consequences resulted from mechanistically induced DNA toxicity. For this reason, it is needed to develop catalytic inhibitors of topoisomerase IIα through the alternative mechanism of enzymatic regulation. As a catalytic inhibitor of topoisomerase IIα, AK-I-191 was previously reported for its enzyme inhibitory activity. In this study, we clarified the mechanism of AK-I-191 and conducted various types of spectroscopic and biological evaluations for deeper understanding of its mechanism of action. Conclusively, AK-I-191 represented potent topoisomerase IIα inhibitory activity through binding to minor groove of DNA double helix and showed synergistic effects with tamoxifen in antiproliferative activity.

• Journal of Microbiology and Biotechnology
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• 제32권5호
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• pp.594-601
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• 2022

This study evaluated the biological properties of lemongrass (Cymbopogon citratus) extracts. The EtOAc extract of lemongrass had DPPH, TEAC, and nitric oxide-scavenging activity assay results of 58.06, 44.14, and 41.08% at the concentration of 50, 10, and 50 ㎍/ml, respectively. The EtOAc extract had higher elastase and collagenase inhibitory activities than the 80% MeOH, n-hexane, BuOH, and water extracts and comparable whitening activity toward monophenolase or diphenolase. Also, the EtOAc fraction had higher lipase inhibitory and antimicrobial activities against Cutibacterium acnes among extracts which is known to an important contributor to the progression of inflammatory acne vulgaris, and an opportunistic pathogen present in human skin. Total phenolic and flavonoid concentrations in the EtOAc extract were 132.31 mg CAE/g extract and 104.50 mg NE/g extract, respectively. Biologically active compounds in lemongrass extracts were analyzed by LC-MS. This study confirms that lemongrass extracts have potential use as cosmetic skincare ingredients. Thus, lemongrass can be considered a promising natural source of readily available, low-cost extracts rich in antioxidant, skincare, and antimicrobial compounds that might be suitable for replacing synthetic compounds in the cosmeceutical industry.