• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.105-112
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• 2003

Selective COX (cyclooxygenase)-2 inhibitors including celecoxib have been shown to induce apoptosis and cell cycle changes in various tumor cells. New inhibitors are recently being developed as chemomodulating agents. We evaluated celecoxib and screened 150 synthetic compounds for anti-proliferative activities in vitro. Effects of celecoxib on COX activity, cell growth, cell cycle distribution, and apoptosis induction were determined in A549 COX-2 overexpressing human non-small cell lung cancer (NSCLC) cells. The COX inhibition of celecoxib increased with concentration up to 82% at $1\;{\mu}M$ after 24 hr exposure. Forty ${\mu}M$ and $50\;{\mu}M$ of ce1ecoxib induced $G_1$ arrest, and TUNEL-positive apoptotic cells, respectively. Among 150 compounds, several compounds were selected for having greater COX-2 inhibitory activity and higher selectivity than celecoxib with growth inhibitory activity. Celecoxib showed concentration-dependent COX inhibitory activity, and ability to induce cell cycle arrest and apoptosis in human NSCLC cells in vitro. Among synthetic analogues screened, several compounds showed promising in vitro activity as COX-2 inhibitory anticancer agents, which warrant further evaluation in vitro and in vivo.

• Korean Journal of Medicinal Crop Science
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• v.25 no.1
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• pp.10-15
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• 2017

Background: We investigated the antioxidative and tyrosinase inhibitory activities of 70% ethanol extract, and its fractions, of the root of Rumex japonicus HOUTT. Methods and Results: The total phenolic compound contents of the 70% ethanol extract and ethyl acetate fraction were 168.99 mg/g and 651.78 mg/g, respectively. The antioxidant activity was compared through the DPPH radical and nitric oxide (NO) scavenging assays. The ethyl acetate fraction showed the highest DPPH radical and NO scavenging abilities, which confirmed the antioxidant activity. Specifically, the ethyl acetate fraction showed a higher DPPH radical scavenging ability than ascorbic acid. These results were related to the total phenolic compound content of the ethyl acetate fraction. Moreover, in the tyrosinase inhibition assay, the ethyl acetate fraction exhibited stronger inhibitory activity than arbutin, which was used as the positive control. The cell viability of L929 cells was analyzed by MTT assay after treatment with 70% ethanol extract and all fractions; no changes in viability were observed, which demonstrated the nontoxic nature of the extract and fractions. Conclusions: These results suggested that the extract from the root of R. japonicus and its ethyl acetate fraction could be a novel resource for the development of a cosmetic with antioxidant and tyrosinase inhibitory activity.

• Korean Journal of Pharmacognosy
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• v.47 no.1
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• pp.29-37
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• 2016

Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and ${\alpha}$-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and ${\alpha}$-glucosidase with $IC_{50}$ value of $96.29{\pm}0.3$ and $264.71{\pm}14.87{\mu}g/mL$, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-${\beta}$-D-glucopyranoside and oleanolic acid-3-O-${\beta}$-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and ${\alpha}$-glucosidase over a range of concentrations ($12.5-50{\mu}M$). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited ${\alpha}$-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

• Korean Journal of Medicinal Crop Science
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• v.19 no.4
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• pp.257-263
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• 2011

This study investigated the changes of antioxidant activity and ${\alpha}$-glucosidase inhibitory effect of Jerusalem artichoke (Helianthus tuberosus) 100% methanol extracts by various heat treatment. The contents of total phenolic and flavonoid compounds in methanol extract tended to increased gradually with the rise of temperature to 180$^{\circ}C$. The maximum yield of gallic acid (51.52 ${\pm}$ 2.17mg/g extract weight) and quercetin (13.39 ${\pm}$ 0.03mg/g extract weight) were obtained with extraction temperature of 180$^{\circ}C$ for 120min. In addition, the improving extraction efficiency resulted in the increased biological activities, such as electronic donation ability (EDA, 90.36${\pm}$ 0.57%), reducing power (Abs 1.14) and ${\alpha}$-glucosidase inhibitory effect (92.14 ${\pm}$ 1.14%). Overall, the results of this study indicate that the optimum conditions for the extraction process were an extraction temperature at 180$^{\circ}C$ for 120 min, and will provide the basis for future research on the improving extraction yield of phenolic and flavonoid compounds.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2019.04a
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• pp.110-110
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• 2019

Beet (Beta vulgaris) is a crop similar to sugar beet, chard and leaf beets, and its origin is the Mediterranean coast of southern Europe and Central Asia. Among the components contained in beet, betalain, the main component of the root, has been reported to prevent lipid peroxidation induced by active oxygen and free radicals due to its high radical scavenging ability. Among these, the betalain, betanin (Betanidin 5-O-${\beta}$-glucoside) contains both phenolic and cyclic amine groups, all of which are highly electron-donating and act as antioxidants and has tyrosinase inhibitory activity. Betanin accounts for about 75-95% of the total pigment found in the beet. EM stands for effective microorganisms and is a collection of beneficial microorganisms. EM includes yeast, lactic acid bacteria, mycelia, photosynthetic bacteria, actinomycetes, etc. Human patch test according to CTFA guidelines was observed to be a safe source of no stimulation when 5% (v/v) of the EM fermentation liquid was applied to the human body. In addition, beneficial microorganisms are synergistic in the process of co-existence and cultivation and it has the effect of increasing antioxidant capacity and inhibiting corruption. This study confirms the difference in tyrosinase inhibitory activity and betanin content of beetroot extracts and EM fermented beetroot extracts. Hence, these results confirm that EM fermented beetroot extracts are highly beneficial for the human body.

• The Journal of the Korea Contents Association
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• v.21 no.11
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• pp.518-527
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• 2021

This study verifies the polyphenol and flavonoid contents of a dried extract, as well as its antioxidant effect and growth inhibitory effect on cancer cells to investigate the potential of yellow cherry tomatoes as a physiologically active food material. The polyphenol and flavonoid contents were determined as 10.96 ± 1.57 and 4.12 ± 0.41 mg/g, respectively. The antioxidant activity was confirmed by measuring DPPH and ABTS radical scavenging ability, and RC50-the concentration that reduces free radicals by 50%-were determined as 490.83 ± 17.35 ㎍/mL and 355.90 ± 0.79 ㎍/mL, respectively. The dried extract showed no cytotoxicity with respect to normal hepatocytes (Chang) and no growth inhibitory activity with respect to A549 lung cancer cells, whereas dried extract showed growth inhibitory activities of 15.2% and 18.4% with respect to human cervical adenocarcinoma (HeLa) and human hepatocellular carcinoma (HepG2) cells, respectively, when treated with a concentration at 100㎍/mL. The results of this study confirm the potential of yellow cherry tomatoes as a physiologically active food material by verifying their antioxidant activity and their growth inhibitory activity with respect to cervical and liver cancer cells.

• Nutrition Research and Practice
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• v.16 no.4
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• pp.419-434
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• 2022

BACKGROUND/OBJECTIVES: Benign prostatic hyperplasia (BPH) is the most common prostate disease and one of the most common chronic diseases caused by aging in men. On the other hand, there has been no research on BPH using Abeliophyllum distichum Nakai (A. distichum). Therefore, this study investigated the effects of A. distichum on BPH. MATERIALS/METHODS: A. distichum leaves were extracted with distilled water, 70% ethanol, and 95% hexane as solvents. Subsequently, the inhibitory effects of each A. distichum extract on androgen receptor (AR) signaling were evaluated in vitro. The testosterone-induced BPH model was then used to confirm the efficacy of A. distichum leaves in 70% ethanol extract (ADLE). RESULTS: ADLE had the strongest inhibitory effect on AR signaling. A comparison of the activity of ADLE by harvest time showed that the leaves of A. distichum harvested in autumn had a superior inhibitory effect on AR signaling to those harvested at other times. In the BPH rat model, the administration of ADLE reduced the prostate size and prostate epithelial cell thickness significantly and inhibited AR signaling. Subsequently, the administration of ADLE also reduced the expression of growth factors, thereby inactivating the PI3K/AKT pathway. CONCLUSIONS: An analysis of the efficacy of ADLE to relieve BPH showed that the ethanol extract grown in autumn exhibited the highest inhibitory ability of the androgen-signaling related factors in vitro. ADLE also inhibited the expression of growth factors by inhibiting the expression of the androgen-signaling related factors in vivo. Overall, ADLE is proposed as a functional food that is effective in preventing BPH.

• The Journal of the Convergence on Culture Technology
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• v.8 no.6
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• pp.615-624
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• 2022

In this study, we assessed anti-oxidant activity, anti-microbial, inhibition of biofilm formation and inflammatory factors(nitric oxide, interleukin-6, interleukin-8) inhibitory effect of Perillae semen hydrothermal extract(PSW) and three kinds of Perillae semen supercritical fluid extract(PSSs) extracted by controlling temperature with no variation of pressure. Compared with PSW, PSSs had significantly lower minimal inhibitory concentrations(MICs) against Staphylococcus aureus(S. aureus) and the ability of PSSs to inhibit formation of biofilm was also superior. PSSs reduce the production of inflammatory mediator and inflammatory cytokines significantly compared to PSW. We suggest, therefore, Perillae semen supercritical fluid 45℃ extract which showed the best anti-microbial, inhibition of biofilm formation, and inhibition of inflammatory factors production among the supercritical fluid extracts could be used for protecting patients with atopic dermatitis from pruritus and transepidermal water loss as a functional ingredient from nature.

• Journal of Pharmacopuncture
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• v.26 no.4
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• pp.307-318
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• 2023

Objectives: Bacterial biofilm is regarded as a significant threat to the production of safe food and the arise of antibiotic-resistant bacteria. The objective of this investigation is to evaluate the quorum sensing inhibitory effect of Nepeta curviflora methanolic extract. Methods: The effectiveness of the leaves at sub-inhibitory concentrations of 2.5, 1.25, and 0.6 mg/mL on the virulence factors and biofilm formation of P. aeruginosa was evaluated. The effect of N. curviflora methanolic extract on the virulence factors of P. aeruginosa, including pyocyanin, rhamnolipid, protease, and chitinase, was evaluated. Other tests including the crystal violet assay, scanning electron microscopy (SEM), swarming motility, aggregation ability, hydrophobicity and exopolysaccharide production were conducted to assess the effect of the extract on the formation of biofilm. Insight into the mode of antiquorum sensing action was evaluated by examining the effect of the extract on the activity of N-Acyl homoserine lactone (AHL) and the expression of pslA and pelA genes. Results: The results showed a significant attenuation in the production of pyocyanin and rhamnolipid and in the activities of protease and chitinase enzymes at 2.5 and 1.25 mg/mL. In addition, N. curviflora methanolic extract significantly inhibited the formation of P. aeruginosa biofilm by decreasing aggregation, hydrophobicity, and swarming motility as well as the production of exopolysaccharide (EPS). A significant reduction in AHL secretion and pslA gene expression was observed, indicating that the extract inhibited quorum sensing by disrupting the quorum-sensing systems. The quorum-sensing inhibitory effect of N. curviflora extract appears to be attributed to the presence of kaempferol, quercetin, salicylic acid, rutin, and rosmarinic acid, as indicated by LCMS analysis. Conclusion: The results of the present study provide insight into the potential of developing anti-quorum sensing agents using the extract and the identified compounds to treat infections resulting from quorum sensing-mediated bacterial pathogenesis.

• Journal of Korean society of Dental Hygiene
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• v.20 no.3
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• pp.387-397
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• 2020

Objectives: This study aimed to evaluate the inhibitory effects of probiotics containing Lactobacillus reuteri on Streptococcus mutans and Aggregatibacter actinomycetemcomitans. In addition, the degree of biofilm formation, initial acidity, buffering ability, and acid production performance were measured to confirm the dental caries-inducing ability. Methods: S. mutans (KCTC3065) and A. actinomycetemcomitans (KCTC2581) were used as experimental strains. The number of viable cells, degree of biofilm formation, initial pH, buffering capacity, and production performance were measured for comparing L. reuteri-containing probiotics and Bulgaris. Results: The viability of S. mutans in the groups was reduced in the following order: Bulgaris, probiotics, control. The degree of biofilm formation was significantly higher at 0% and gradually reduced at different concentrations (p<0.01). At 2.5%, the absorbance of the probiotics and Bulgaris groups differed significantly (p<0.01). The acid formation ability differed significantly based on the performance of S. mutans in each product (p<0.05). The absorbance of the probiotics group was significantly lower than that of the Bulgaris group (p<0.01). Conclusions: This study suggests that the use of L. reuteri-containing probiotics as an adjuvant for the prevention and decreasing of oral diseases may reduce their incidence, which can be considered one of the benefits of using probiotics.