• Journal of Microbiology and Biotechnology
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• 제18권6호
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• pp.1109-1114
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• 2008

To understand the role of intestinal microflora in the biological effect of functional herbs, which have been used in Korea, Japan, and China as traditional medicines, and suggest new bioactive compounds transformed from herbal constituents, the metabolic activities of the functional herb components (ginsenoside Rb1, crocin, amygdalin, geniposide, puerarin, ginsenoside Re, poncirin, hesperidin, glycyrrhizin, and baicalin) toward their bioactive compounds (compound K, crocetin, benzaldehyde, genipin, daidzein, ginsenoside Rh1, ponciretin, hesperetin, 18b-glycyrrhetic acid, and baicalein) were measured in fecal specimens. The metabolic activities of these components were $882.7{\pm}814.5$, $3,938.1{\pm}2,700.8$, $2,375.5{\pm}913.7$, $1,179.4{\pm}795.7$, $24.6{\pm}10.5$, $11.4{\pm}10.8$, $578.8{\pm}206.1$, $1,150.0{\pm}266.1$, $47.3{\pm}58.6$, and $12,253.0{\pm}6,527.6\;{\mu}mol/h/g$, respectively. No differences were found in the metabolic activities of the tested components between males and females, although these metabolic activities between individuals are extensively different. The metabolites of functional herb components showed more potent cytotoxicity against tumor cells than nonmetabolites. These findings suggest that intestinal microflora may activate the pharmacological effect of herbal food and medicines and must be the biocatalytic converter for the transformation of herbal components to bioactive compounds.

• Journal of Pharmaceutical Investigation
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• 제35권4호
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• pp.255-263
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• 2005

Research was undertaken to compare the pharmacological activity of Lithospermi radix (LR) reported as an oriental medicine for classical uses. LR contains naphthoquinone pigments : shikonin, acetylshikonin, isobutylshikonin, etc. LR is used for the treatment of excision wound, burn, eczema, blister, scarlatina and septicemia as antifebrile, antidotic and antiphlogistic. Gardeniae fructus (GF) has been used for the treatment to jaundice, hepatic disease, anti-inflammatory and analgesic effects, and it contains crocin, geniposide and its derivatives. The therapeutic effects of burn and excision wound healing from LR & GF hydrogel with $Nano-ATP^{\circledR}$ (GLN) were investigated. To evaluate the therapeutic value of various hydrogels, thermal burn model and excision wound mouse model were used. The burn and wound reduction rate and therapeutic period were measured to calculate the healing extent after 5 experiments. The 2nd degree burn was prepared on hairless mouse back skin and dressing with collagen. The burn and wound reduction rate of GLN hydrogel treated group decreased more rapidly than that of other gel group in animal model. Furthermore therapeutic periods of GLN hydrogel treated group was shorter than that of other gel group. In anti-inflammatory test, GLN hydrogel treated group decreased edema rapidly than that of other gel group. These results suggest that the GLN hydrogel treatment has an therapeutic effect on burn and excision wound healing.

• Biomolecules & Therapeutics
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• 제20권2호
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• pp.214-219
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• 2012

This research was designed to determine what components of Gardenia jasminoides play a major role in inhibiting the enzymes related antidepressant activity of this plant. In our previous research, the ethyl acetate fraction of G. jasminosides fruits inhibited the activities of both monoamine oxidase-A (MAO-A) and monoamine oxidase-B (MAO-B), and oral administration of the ethanolic extract slightly increased serotonin concentrations in the brain tissues of rats and decreased MAO-B activity. In addition, we found through in vitro screening test that the ethyl acetate fraction showed modest inhibitory activity on dopamine-${\beta}$ hydroxylase (DBH). The bioassay-guided fractionation led to the isolation of five bio-active compounds, protocatechuic acid (1), geniposide (2), 6'-O-trans-p-coumaroylgeniposide (3), 3,5-dihydroxy-1,7-bis(4-hydroxyphenyl) heptanes (4), and ursolic acid (5), from the ethyl acetate fraction of G. jasminoides fruits. The isolated compounds showed different inhibitory potentials against MAO-A, -B, and DBH. Protocatechuic acid showed potent inhibition against MAO-B ($IC_{50}$ $300{\mu}mol/L$) and DBH ($334{\mu}mol/L$), exhibiting weak MAO-A inhibition (2.41 mmol/L). Two iridoid glycosides, geniposide ($223{\mu}mol/L$) and 6'-O-trans-p-coumaroylgeniposide ($127{\mu}mol/L$), were selective MAO-B inhibitor. Especially, 6'-O-trans-p-coumaroylgeniposide exhibited more selective MAO-B inhibition than deprenyl, well-known MAO-B inhibitor for the treatment of early-stage Parkinson's disease. The inhibitory activity of 3,5-dihydroxy-1,7-bis (4-hydroxyphenyl) heptane was strong for MAO-B ($196{\mu}mol/L$), modest for MAO-A ($400{\mu}mol/L$), and weak for DBH ($941{\mu}mol/L$). Ursolic acid exhibited significant inhibition of DBH ($214{\mu}mol/L$), weak inhibition of MAO-B ($780{\mu}mol/L$), and no inhibition against MAO-A. Consequently, G. jasminoides fruits are considerable for development of biofunctional food materials for the combination treatment of depression and neurodegenerative disorders.

• 한국식품영양과학회지
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• 제30권6호
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• pp.1147-1151
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• 2001

치자열매에서 geniposide를 추출하여 glycine과 반응시켜 얻은 치자 청색소를 식품에 활용하기 위하여 pH, 온도 및 첨가물에 대한 안정성과 음료 모델의 관능적 특성을 조사하였다. 치자 청색소는 산성에서 불안정하였으며 중성이나 알칼리성 조건에서는 매우 안정하였다. 상온에서 청색소는 매우 안정하여 약 93일의 반감기를 나타내었고, 온도가 증가할수록 분해속도가 증가하여 9$0^{\circ}C$에서는 약 2일의 반감기를 나타내었다. 혼합 이온용액($Na^{+}$, $K^{+}$, $Mg^{2+}$, $Ca^{2+}$) 0.01 M을 첨가한 경우 45일 저장 후 대조군에 비해 색소 잔존율이 높았다. 당의 종류는 색소의 안정성에 큰 영향을 미치지 않는 것으로 나타났고, 아미노산을 첨가할 경우에는 색소를 약간 안정화시켰으나, 비타민 C를 첨가할 경우 청색소의 안정성을 크게 떨어뜨리는 것으로 나타났다. 치자 청색소를 첨가한 모델음료의 관능평가 결과 대조군에 비해 당류나 무기이온, 아미노산을 첨가한 시료에 대해 높은 선호도를 나타내었다.

• 인간식물환경학회지
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• 제23권4호
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• pp.455-464
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• 2020

Background and objective: This study was conducted to examine changes in the composition and physiological activity of Gardenia Fructus after being roasted. Methods: The antioxidant, anti-inflammatory and antibacterial activity of Gardenia Fructus was evaluated using the Gardenia Fructus (GF) and roasted Gardenia Fructus (RGF) ethanol extracts, and their components were analyzed through HPLC. Results: As a result, it was confirmed that the content of gardenoside and geniposide decreased and the content of genipin increased when GF was roasted. The total content of polyphenols was 54.5 ± 2.18 mg gallic acid equivalents (GAE) per gram of the GF extract and 69.6 ± 0.36 mg GAE per gram of the RGF extract. As a result of evaluating 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, both the GF and RGF extracts showed the similar activity to ascorbic acid at the concentrations of 1 mg/mL or higher. In RAW 264.7 macrophages stimulated by lipopolysaccharides (LPS), the RGF extract showed a higher effect of reducing NO production, and significantly reduced the expression of an inflammatory cytokine, IL-6. As a result of evaluating the antimicrobial activity, the RGF extract showed higher antimicrobial activity against Escherichia coli and Bacillus subtilis. In the dextran sulfate sodium salt (DSS) induced inflammatory bowel disease mouse model, the RGF extract reduced the weight of the spleen, and both the GF and RGF extracts reduced the number of bacteria in the colon. Conclusion: Therefore, it has been confirmed through this study that roasting at a high temperature changes the main components of the GF extract and increases its biological activity. The RGF extract is expected to be used as a natural material with antioxidant, anti-inflammatory and antibacterial effects.

• Food Science and Biotechnology
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• 제18권4호
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• pp.867-871
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• 2009

Response surface methodology (RSM) was used for the optimization of antioxidant capacity in gardenia extracts. The antioxidant capacities of gardenia fruit extracts were investigated by ferric reducing ability (FRA) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity (RSA) assays. The optimum extraction parameters for the strongest antioxidant capacity were the ethanol concentration (EtOH) of 48.9%, extraction temperature of $72.9^{\circ}C$, and extraction time of 29.9 min. Analysis of variance (ANOVA) showed that the quadratics of EtOH and extraction temperature had highly significant effect on the antioxidant capacity (p<0.001). The antioxidant capacity was correlated with contents of bioactive components [crocin, geniposide, and total phenolic (TP) compounds] in gardenia extracts and mainly attributed to the content of the TP compounds.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.190.1-190.1
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• 2003

A bioassay-guided fractionation of the stem bark extract of Eucommia ulmoides Oliver (Eucommiaceae) led to the isolation of three iridoid constituents, genipin (1), geniposide (3), geniposidic acid (4) as well as (${\pm}$)-guaiacylglycerol (2) and fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted)

• 치위생과학회지
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• 제10권2호
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• pp.79-83
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• 2010

소염진통제인 Ketorolac tromethamine에 치자엑스 복합제제를 혼합하여 4종의 하이드로겔을 제조한 다음 주성분의 확인, 점도, 표면장력, 인장강도 및 생체부착성 실험을 통해 다음과 같은 결론을 얻었다. 1. KGE 및 KGH gel 제제 중 Ketorolac tromethamine의 함량은 1.02~0.97%이었고, Geniposide의 함량은 KGE gel A와 C에서 0.34%이었으나, KGH gel B와 D에서 0.11%로 낮아졌고, Genipin의 함량은 KGE gel A와 C에서는 나타나지 않았으나, KGH gel B와 D에서 0.13%로 나타났다. 2. Gel 제제의 온도에 따른 점도는 gel 화제로 Carbopol 940을 단독으로 사용한 gel이 Poloxamer 407을 추가한 gel보다 더 높은 점도를 유지하였으며, 각 제제에서의 표면장력은 $37^{\circ}C$에서 34.77~40.58 dyne/cm를 나타냈다. 제제의 인장강도는 KGH gel B에서 대조군에 비하여 3.5배 정도 높은 인장강도를 나타냈다. 3. 생체부착성은 등피부 상부(표피층)와 배피부의 경우 KGH gel B 에서 50.62 N으로 나타나 대조군에 비해 5배 정도 높은 수치를 나타내었고, 등피부 하부(진피층)와 배피부의 경우 KGH gel B의 에서 35.93 N으로 나타나 대조군에 비해 3.5배 정도 높은 수치를 나타냈다.

• 치위생과학회지
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• 제5권3호
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• pp.113-117
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• 2005

소염진통제인 케토롤락트로메타민에 치자엑스 복합제제를 혼합하여 4종의 하이드로겔 제제를 제조한 후 인장강도측정, 피부투과 및 치주낭 감소율측정 실험을 통해 다음과 같은 결론을 얻었다. 1. 제제의 인장강도는 KGH gel B에서 대조군에 비하여 3.5배 정도 높은 인장강도를 나타내었다. 2. 케토롤락트로메타민의 피부투과량은 8시간 동안 KGH gel B에서 $105.62{\mu}m/cm^2$로 가장 높았고, geniposide 투과량은 KGE gel A에서 $73.8{\mu}m/cm^2$ 비교적 높았으나 가수분해물인 genipin의 투과량은 KGH gel B에서$50.17{\mu}m/cm^2$ 가장 높은 투과량을 나타내었다. 3. 치주낭 감소율은 4주 후 KGE gel A는 대조군에 비하여 23.85%의 감소율을 나타내었으나 유의성 있는 차이는 나타내지 못하였으며, KGH gel B는 대조군에 비하여 29.46%의 감소율을 보여 유의성 있는 치료효과를 나타내었다.

• 약학회지
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• 제57권4호
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• pp.293-298
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• 2013

Hwangryunhaedok-tang (HRT) is a traditional herbal medicine, which has been known as a useful prescription for anti-biotic, anti-inflammatory, anti-oxidative and immunosuppressive activity. In this study, the variation in the amount of eight bioactive components of Hwangryunhaedok-tang (HRT) and its fermentation HRT with Lactobacillus casei KFRI 127, Lactobacillus curvatus KFRI 166 and Lactobacillus confuses KFRI 227 was investigated via high-performance liquid chromatography coupled with diode array detection (HPLC-DAD). Simultaneous qualitative and quantitative analysis of eight bioactive components; geniposide, genipin, baicalin, wogonoside, palmatine, berberine, baicalein and wogonin was achieved by comparing their retention times ($t_R$) and UV spectra with those of the standard components. All calibration curve of standard components showed good linearity ($r^2$ >0.979). As a result, the geniposide amount was $15.52{\pm}0.19{\mu}/mg$ that as a main components in HRT. The wogonoside was decreased by 29.28~58.35% with Lactobacillus casei KFRI 127 and L. confuses KFRI 227 ($3.17{\pm}0.31{\mu}g/mg$ and $3.55{\pm}0.13{\mu}g/mg$) compared with the original HRT ($5.02{\pm}0.14{\mu}g/mg$). Otherwise wogonin was increased by 16.28~41.86% with Lactobacillus casei KFRI 127 and L. confuses KFRI 227 ($0.61{\pm}0.01{\mu}g/mg$ and $0.50{\pm}0.02{\mu}g/mg$) compared with the original HRT($0.43{\pm}0.00{\mu}g/mg$). HRT fermented with L. casei KFRI 127 and L. confuses KFRI 227 were evaluated as creating the changes in wogonoside to that aglycon wogonine. In the fermented HRT using Lactobacillus acidophilus KFRI 166, the genipin was only detected, among 3 species of fermentation strains. Thus, these results considered that the strains 166 were exhibited the remarkable changes in genipin.