• Journal of Microbiology and Biotechnology
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• v.18 no.6
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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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• v.35 no.4
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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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• v.20 no.2
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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.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.6
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• pp.1147-1151
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• 2001

We investigated stabilities of blue pigment extracted from Gardenia jasminoides at various conditions to check its applicability for beverages. Gardenia blue pigment with maximum absorption at 587 nm was obtained from the reaction of glycine and genipin (aglycone of geniposide). The blue pigment was found to be relatively unstable at acidic pH but very stable at alkaline conditions with half-life values of 102 days and 126 days at PH 9.0 and PH 11.0, respectively. The pigment also showed high thermal stability with half-life value of 55, 18, and 2 days at 50, 70, and 9$0^{\circ}C$, respectively. The addition of inorganic ions, sugars, and amino acids to model beverage containing this blue pigment increased retention rate at room temperature while addition of vitamin C decreased the stability. The sensory evaluation of the model beverage showed that inorganic ions and amino acids increased overall acceptability, indicating that the blue pigments of Gardenia jasminoides can be used as a natural colorant for leverage.

• Journal of People, Plants, and Environment
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• v.23 no.4
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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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• v.18 no.4
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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.

• Proceedings of the PSK Conference
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• 2003.10b
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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)

• Journal of dental hygiene science
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• v.10 no.2
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• pp.79-83
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• 2010

This study manufactured hydrogel, which was contained NSAIDs(non-steroidal anti-inflammatory drugs) Ketorolac tromethamine and hydrolyzed products of gardeniae fructus extract, and experimented viscosity, surface tension, tensile strength and bio-adhesiveness by using hairless mouse. Thus, it was performed in expectation for being probably able to develop as effective auxiliary agent of periodontal disease after non-surgical or surgical periodontal treatment. As a result, the following conclusions were obtained. 1. Out of KGE and KGH gel materials, the content of ketorolac tromethamine was 1.02~0.97%. The content of geniposide was 0.34% in KGE gel A and C. However, it got lower to 0.11% in KGH gel B and D. The content of genipin wasn't shown in KGE gel A and C, but was shown with 0.13% in KGH gel B and D. 2. As for viscosity according to temperature in gel material, the gel, which used independently Carbopol 940 as gel inoculant, maintained the higher viscosity than the gel, which added Poloxamer 407. The surface tension in each material showed 34.77~40.58 dyne/cm at 37. As for tensile strength in material, KGH gel B was shown the higher tensile strength in about 3.5 times compared to the control group. 3. As for bio-adhesiveness, the back-skin upper part(epidermis) and abdomen skin were shown to be 50.62 N in KGH gel B, thereby having indicated higher value in about 5 times compared to control group. The back-skin lower part(dermis) and abdomen skin were shown to be 35.93 N in KGH gel B, thereby having indicated higher value in about 3.5 times compared to control group.

• Journal of dental hygiene science
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• v.5 no.3
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• pp.113-117
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• 2005

After producing 4 kinds of hydrogel materials by mixing the composite preparation in Gardeniae Fructus extracts with ketorolac tromethamine, which is NSAIDs (nonsteroidal anti-inflammatory drugs), through the experiment of measurement in the tensile strength, in the skin permeation, and in the periodontal-pocket reduction rate, the following conclusions were obtained. 1. The tensile strength of a drug indicated the tensile strength 3.5-fold higher compared to the control group, in KGH gel B. 2. The skin-permeation volume in ketorolac tromethamine was highest with $105.62{\mu}m/cm^2$ in KGH gel B for 8 hours, and the permeation volume in geniposide was relatively high with $73.8{\mu}m/cm^2$ in KGE gel A, but the permeation volume in genipin, which is the hydrolysis, represented the highest permeation amount with $50.17{\mu}m/cm^2$ in KGH gel B. 3. In terms of the periodontal-pocket reduction rate, after 4 weeks, KGE gel A showed the falling rate of 23.85% compared to the control group, but did not indicate the significant difference, and KGH gel B represented the reduction rate of 29.46% compared to the control group, thus it indicated the significantly treatment effect.

• YAKHAK HOEJI
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• v.57 no.4
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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.