• The Korea Journal of Herbology
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• v.37 no.6
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• pp.1-8
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• 2022

Objectives : This research aimed to investigate chondro-protective and anti-inflammatory effects of Caraganae Sinicae Flos 50% ethanol extract and its compound, tilianin. Methods : Caraganae Sinicae Flos was extracted with 50% ethanol. Tilianin in Caraganae Sinicae Flos 50% ethanol extract was quantified by HPLC analysis method. To investigate chondro-protective effects of Caraganae Sinicae Flos 50% ethanol extract, ATDC5 chondrogenic cells were co-treated with Caraganae Sinicae Flos 50% ethanol extract (or tilianin) and tumor necrosis factor-𝛼 (TNF𝛼) for 24 hours. After treatement for 24 hours, media supernatant was used for quantifying protein level of matrix metalloproteinase-3 (MMP3) by ELISA and harvested cells were used for analyzing mRNA expression level of matrix metalloproteinase-13 (MMP13) by reverse transcription PCR. To identify anti-inflammatory effects of Caraganae Sinicae Flos 50% ethanol extract, RAW 264.7 macrophage cells were co-treated with Caraganae Sinicae Flos 50% ethanol extract (or tilianin) and lipopolysaccharide (LPS) for 24 hours. media was used for quantifying the level of prostaglandin E2 (PGE2), interleukin-6 (IL6) by ELISA and nitric oxide by Griess reagent asssay. Results : Caraganae Sinicae Flos 50% ethanol extract and tilianin attenuated protein level of MMP3 and mRNA expression level of MMP13 in TNF𝛼-activated ATDC5 cells. Caraganae Sinicae Flos 50% ethanol extract inhibited the level of PGE2, IL6 and NO in LPS-activated RAW 264.7 cells in dose dependent manner, though tilianin inhibited PGE2 only. Conclusions : These results presented that Caraganae Sinicae Flos 50% ethanol extract could be used as natural medicines for osteoarthritis.

• Proceedings of the Korean Society of Toxicology Conference
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• 2003.10b
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• pp.192-193
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• 2003

In previous study, we demonstrated tilianin inhibits tumor necrotic factor-${\alpha}$ (TNF-${\alpha}$) induced vascular cell adhesion molecule-1 (VCAM-1) expression in human umbilical vein endothelial cells (HUVEC). In this study, we demonstrate inhibition of the production of atherogenic cytokines and the anti-atherogenic effects of tilianin in Ldlr-/- mice.(omitted)

• Journal of Microbiology and Biotechnology
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• v.27 no.1
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• pp.49-56
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• 2017

In the human airway, mucus exists to protect the respiratory system as a primary barrier of the innate immune system. However, hyperexpressed mucus limits airflow, resulting in a decrease of lung function. Among more than 20 mucin family members, MUC5AC and MUC5B are major glycoproteins in human airway mucus. The epidermal growth factor receptor (EGFR) signaling pathway is one of the mechanisms of these mucins expression and specificity protein-1 (Sp1) transcription factor is the downstream signal of this pathway, playing pivotal roles in mucin expression. Even though there are some drugs for treating mucus hypersecretion, no drug has proven effects on humans. We found that the flavonoid tilianin regulated MUC5AC expression and also inhibited Sp1 phosphorylation. In this study, we investigated how tilianin would modulate EGFR signaling and regulate mucin production. In conclusion, tilianin inhibited MUC5AC expression mediated via modulating the EGFR-MEK-ERK-Sp1 signaling pathway in NCI-H292 human airway epithelial cells. This study may provide the basis for the novel treatment of mucus hypersecretion.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.10a
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• pp.128-129
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• 2001

Tilianin, purified from acrial part of Agastache rugosa Kuntze, reduces progression and may induce some regression of aortic foam cell formation in low density lipoprotein receptor deficient mice (LDLR -/- mice). We investigated whether tilianin can prevent high fat diet-induced atherosclerosis. Twenty-six male mice were divided into three groups.(omitted)

• Proceedings of the PSK Conference
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• 2003.10a
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• pp.64-65
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• 2003

Investigation of immunomodulating activities of the Agastache rugosa (Bae-cho-hyang) extract and its components was preformed through screening in vitro assays and evaluating anti-inflammatory activity and anti-atherosclerotic activity of the extract and tilianin in vivo. The extract showed strong anti-inflammatory activity in carrageenan-induced acute edema mouse model and anti-atherogenic activity in LDLR (low density lipoprotein receptor) deficient mouse model. (omitted)

• Journal of Bio-Environment Control
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• v.31 no.4
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• pp.319-324
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• 2022

The objective of this study was to determine the proper night interruption of photoperiods and dark periods for accumulating bioactive compounds of Agastache rugosa without decreasing plant growth. Five-week-old seedlings were transplanted in a DFT system with white LEDs. A. rugosa was treated with night interruption time treatments of 18:1:2:3, 18:2:2:2, 18:3:2:1 (light:dark:light:dark), and 20:4 (control) for 4 weeks. There were no significant differences except for leaf length, leaf width, and the number of flowers. The content of antioxidants in the shoot of A. rugosa was high in tilianin and acacetin, and the content of rosmarinic acid (RA) was significantly higher in the underground part. The RA content per dry weight of A. rugosa was 47.92 and 51.46% higher than that of the control in 18:1:2:3 and 18:2:2:2, and tilianin and acactin per dry weight were significantly higher in 18:3:2:1. There was no significant difference in growth due to the same day light integral, but 18:2:2:2 showed high total polyphenol contents. Therefore, it is thought that the effect of increasing secondary metabolites of A. rugosa without degradation of growth can be expected through night interruption treatment in plant factory cultivation systems using artificial light.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2003.10a
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• pp.192-193
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• 2003

• Proceedings of the Korean Society of Crop Science Conference
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• 2002.05a
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• pp.77-81
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• 2002

The scope of the research is investigation of immune-modulating activities of A. rugosa (Baechohyang) extract was preformed through the screening active constituents using in vitro assays and evaluating anti-inflammatory activity and anti-atherosclerotic activity of the extract and active compound (tilianin) in vivo. In addition, various functional foods using the extract and whole plant was developed. The extract showed strong anti-inflammatory activity in carrageenan-induced acute edema mouse model and anti-atherogenic lesion activity in LDLR (low density lipoprotein receptor) deficient mouse model. These activities were thought to be resulted from modulation activity of several pathways of inflammation process. Among the main constituents of Baechohyang, polyunsaturated fatty acids (PUFA), Phytosterols, oleanolic acid and rosmarinic acid showed anticomplement activity, and PUFA, acacetin and tilianin newly showed potent ICAM-1 expression inhibition activity. The processes of extraction, mixing ratio of additives and storage conditions were established for drinks, granule tea, leaf tea, mixed tea and furigake.

• Journal of Bio-Environment Control
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• v.26 no.4
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• pp.249-257
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• 2017

Agastache rugosa, is a perennial medicinal plant commonly used in Chinese herbalism, and may have anti-atherogenic and antibacterial properties. Here in this study, we investigated the growth and variations in antioxidant contents of A. rugosa in response to nutrient solution and photosynthetic photon flux density (PPFD) with artificial lighting for a hydroponics culture. Fluorescent light at 150, and $200{\mu}mol{\cdot}m^{-2}{\cdot}s^{-1}$ PPFD with a 16/8 (light/dark) photoperiod, combined with four different nutrient solutions [developed by Horticulture experiment station in Japan (HES), University of Seoul (UOS), Europe vegetable research center (EVR), Otsuka-house 1A (OTS)], were used in a hydroponics culture system for 6 weeks. The shoot and root dry weights of A. rugosa grown with the OTS were significantly higher than those of other nutrient solutions. The amount of tilianin was the highest grown with the OTS, followed by EVR, HES, and UOS. Total acacetin content was the highest in A. rugosa grown under EVR which was statistically similar with OTS. The A. rugosa grown under $200{\mu}mol{\cdot}m^{-2}{\cdot}s^{-1}$ PPFD produced higher fresh weight and both acacetin and tilianin contents than that grown under $150{\mu}mol{\cdot}m^{-2}{\cdot}s^{-1}$ PPFD. The present results suggested that OTS along with $200{\mu}mol{\cdot}m^{-2}{\cdot}s^{-1}$ PPFD could be an optimum growing condition for better growth and higher accumulation of tilianin and acacetin contents in A. rugosa with hydroponic culture systems in a plant factory.

• Journal of Bio-Environment Control
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• v.27 no.3
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• pp.260-268
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• 2018

The aim of this study was to evaluate the effect of light quality using either monochromatic or combined LEDs on the growth and antioxidant accumulation of Agastache rugosa cultivated under hydroponics for 4 weeks. This experiment was performed in a controlled-environment room at $22{\pm}1^{\circ}C$ and $18{\pm}1^{\circ}C$ (day and night temperatures, respectively) and 50-70% relative humidity, with a provided photosynthetic photon flux density (PPFD) of $180{\pm}5{\mu}mol{\cdot}m^{-2}{\cdot}s^{-1}$ and irradiated with either monochromatic (W10 and R10) or mixed LEDs (W2B1G1, R3B1, R2B1G1, and W2B1G1) with a differing ratio of each LED's PPFD and fluorescent lighting (FL: control) with a 16/8 h photoperiod. Fresh and dry weights were highest for plants grown under the W2B1G1 treatment. A. rugosa grown with R10 had the greatest plant height but the lowest SPAD among all treatments. The concentration of rosmarinic acid in plants grown under W2B1G1 was significantly higher than that of plants grown under other treatments. Tilianin content was significantly higher in R3B1 than in the other treatments. However, whole-plant rosmarinic acid and tilianin content was the highest under the W2B1G1 condition. To cultivate A. rugosa in a plant factory, mixed-LED light conditions with W2B1G1 is considered to be more advantageous for the growth and antioxidant accumulation of A. rugosa. It is though that the total whole-plant antioxidant content is more crucial for commercial use; the present study demonstrates the potential to achieve higher content of functional materials in plants through the selection of light quality.