• Applied Biological Chemistry
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• v.39 no.2
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• pp.147-152
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• 1996

To screen inhibitors on complement system from natural resources, micro-screening method was established by using hemolytic complement assay. Complement fixation reaction was carried out in the microplate system. For standard hemolysis (50% hemolysis) of the classical pathway (CP), hemolysin and complement serum were diluted to $1/75{\sim}1/100\;and\;1/80{\sim}1/120$, respectively, when sheep erythrocytes were $5.0{\times}10^8\;cells/ml$. In case of the alternative pathway (AP), complement serum was diluted to 1/5 and EGTA and $Mg^{2+}$ were added 4 mM, $4{\sim}8\;mM$, respectively, when rabbit erythrocytes were $4.0{\times}10^8\;cells/ml$. Dimethyl sulfoxide was used for the assay of non-aquous soluble compounds or extracts and its final concentration was not more than 1%. Three phenylpropanoids showed anticomplementary activities in proportion to the concentration for both pathways and rosmarinic acid exihibited the highest inhibitory activities: $5.4{\pm}3.6%(0.063\;mM){\sim}95.8{\pm}0.2%(0.5\;mM)\;and\;35.1{\pm}0.9%(0.063\;mM){\sim}95.6{\pm}1.1%(1\;mM)$ on the CP and the AP, respectively.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.182.2-182.2
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• 2000

• Korean Journal of Food Science and Technology
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• v.49 no.3
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• pp.331-337
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• 2017

To evaluate the antioxidant activity of hexane, ethyl acetate, and butanol fractions obtained from Agastache rugosa extract, we measured the total polyphenol levels, DPPH radical scavenging activity, and reducing power. The ethyl acetate fraction of A. rugosa (AREA) displayed high phenolic levels, potent DPPH radical scavenging effect, and powerful reducing power. In addition, we examined the ability of AREA to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 microglia. AREA suppressed NO production and inducible nitric oxide synthase (iNOS) expression and downregulated interleukin-6 (IL-6) mRNA level in LPS-stimulated BV-2 microglia. Furthermore, we detected rosmarinic acid in AREA by HPLC, which suggested that rosmarinic acid could be one of the bioactive materials responsible for the antioxidant and anti-inflammatory activities of AREA. These results suggested that AREA may be a good source of functional foods with antioxidant and anti-inflammatory activities.

• Nutrition Research and Practice
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• v.10 no.3
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• pp.274-281
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• 2016

BACKGROUND/OBJECTIVES: The accumulation of amyloid-${\beta}$ ($A{\beta}$) in the brain is a hallmark of Alzheimer's disease (AD) and plays a key role in cognitive dysfunction. Perilla frutescens var. japonica extract (PFE) and its major compound, rosmarinic acid (RA), have shown antioxidant and anti-inflammatory activities. We investigated whether administration of PFE and RA contributes to cognitive improvement in an $A{\beta}_{25-35}$-injected mouse model. MATERIALS/METHODS: Male ICR mice were intracerebroventricularly injected with aggregated $A{\beta}_{25-35}$ to induce AD. $A{\beta}_{25-35}$-injected mice were fed PFE (50 mg/kg/day) or RA (0.25 mg/kg/day) for 14 days and examined for learning and memory ability through the T-maze, object recognition, and Morris water maze test. RESULTS: Our present study demonstrated that PFE and RA administration significantly enhanced cognition function and object discrimination, which were impaired by $A{\beta}_{25-35}$, in the T-maze and object recognition tests, respectively. In addition, oral administration of PFE and RA decreased the time to reach the platform and increased the number of crossings over the removed platform when compared with the $A{\beta}_{25-35}$-induced control group in the Morris water maze test. Furthermore, PFE and RA significantly decreased the levels of nitric oxide (NO) and malondialdehyde (MDA) in the brain, kidney, and liver. In particular, PFE markedly attenuated oxidative stress by inhibiting production of NO and MDA in the $A{\beta}_{25-35}$-injected mouse brain. CONCLUSIONS: These results suggest that PFE and its active compound RA have beneficial effects on cognitive improvement and may help prevent AD induced by $A{\beta}$.

• Korean Journal of Environmental Agriculture
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• v.41 no.1
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• pp.50-54
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• 2022

BACKGROUND: Phyllospadix japonica Makino is a perennial plant belonging to the family Zosteraceae. This species is native to the eastern coast of the Korean Peninsula, and it is found attached to rocks on the seashore. As with all seagrass species, P. japonica is also known to play a major role in protecting the marine environment, and studies on its physiological activities suggestive of its antioxidant, antibacterial and anti-inflammatory potentials have been reported. In this study, purification and structural analysis were performed to identify the polyphenol substances derived from P. japonica. METHODS AND RESULTS: An polyphenol substance MP-1 was purified from the 70% aqueous methanol extract of P. japonica using Diaion® HP-20 column chromatography, ODS column chromatography, and medium-pressure liquid chromatography (MPLC). The purified MP-1 was identified as rosmarinic acid having a molecular weight of 360 and a molecular formula of C18H16O8 through electrospray ionization (ESI)-mass and nuclear magnetic resonance (NMR) spectroscopic analysis. CONCLUSION(S): This study highlights the processes used for the identification of the polyphenol substance derived from P. japonica. Rosmarinic acid, the polyphenol derived from P. japonica identified by this study, is a kind of bioactive substance mainly present in plants. These findings provide an important starting point and are valuable for future studies on bioactive substances in seagrass.

• Korean Journal of Organic Agriculture
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• v.21 no.2
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• pp.219-232
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• 2013

The relevant main constituents of rosemary are compound of a vast number of polyphenolics, including carnosic acid, carnosol, rosmarinic acid, and ursolic acid. Recently, phenolic compounds of plant origin have attracted considerable attention due to their beneficial functional and nutritional effects including antioxidant and antibacterial activity. This study was carried out to investigated effect of carnosic acid on pH, thiobarbituric acid reactive substance (TBARS), volatile basic nitrogen (VBN), 2,2-diphenyl-1-picryhydrazyl (DPPH) radical scavenging activity, and total bacteria counts in white sausage during the storage at room temperature. Addition of carnosic acid was decreased of pH, TBARS, VBN, and enhanced antioxidant and antibacterial activity in white sausage. These activities increased with increasing concentrations of carnosic acid. Furthermore, the potent antibacterial activities of carnosic acid against pathogenic bacteria (Escherichia coli KCCM 11234 and Salmonella enteritidis KCCM 12021) were measured. Carnosic acid showed noticeable inhibitory effects on E. coli and S. enteritidis. In conclusion, carnosic acid might be used as a natural preservative in white sausage.

• Journal of Adhesion and Interface
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• v.13 no.1
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• pp.17-23
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• 2012

A fragrant microcapsule was prepared for use by students to reduce the stress of taking examinations. Rosmarinic acid was used as a fragrant oil which had the effect of relaxing stress, polycaprolactone (PCL) was used as a capsule wall material, and poly(vinyl alcohol) (PVA) as a stabilizer. The solvent evaporation method was used to form the microcapsule. The microcapsules were prepared by changing the stirring rate, the concentration of the stabilizer, and the molecular weight of PCL. The shape of the microcapsule was characterized by scanning electron microscopy (SEM). The size of the microcapsule was reduced by increasing the stirring speed. The release rate of rosmarinic acid was decreased when the higher molecular weight PCL was used. When the prepared microcapsule was tested in an aromatherapy class, the microencapsulated fragrant oil had a longer release time than the original fragrant oil. The study data showed that this fragrant oil was effective for increasing concentration ability, reducing stress, increasing digestive power, and increasing memory for the students.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.1
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• pp.47-55
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• 2009

In this study, the antioxidative effects, inhibitory effects on tyrosinase, and component analysis of fermented Melissa officinalis extracts were investigated. The ethyl acetate fraction of fermented extract ($8.38{\mu}g/mL$) showed the most prominent the free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities ($FSC_{50}$) of extract/fractions of M. officinalis. Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of some M. officinalis extracts on ROS generated in $Fe^{3+}$-EDTA/$H_{2}O_{2}$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction of fermented extract ($0.63{\mu}g/mL$) showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of M. officinalis on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The M. officinalis extracts suppressed photohemolysis in a concentration dependent manner ($5\;{\sim}\;75{\mu}g/mL$). The inhibitory effect of M. officinalis extracts on tyrosinase was investigated to assess their whitening efficacy. Inhibitory effects ($IC_{50}$) on tyrosinase of some M. officinalis extracts was 50 % ethanol extract ($365{\mu}g/mL$) < ethyl acetate fraction of fermented extract ($122.43{\mu}g/mL$) < ethylacetate fraction ($94.8{\mu}g/mL$). Fractions of ethyl acetate both from ordinary and fermented M. officinalis extracts showed 2 band in TLC and 2 peak in HPLC (330 nm). In HPLC chromatogram of ethyl acetate fraction, peak 1 (51.64 %) and peak 2 (48.36 %) were identified as caffeic acid and rosmarinic acid in the order of elution time. Also, in HPLC chromatogram of ethyl acetate fraction of fermented extract, peak 1 (4.13 %) and peak 2 (95.87 %) were identified as caffeic acid and rosmarinic acid in the order of elution time. These results indicate that the component and content of ordinary and fermented extracts of M. officinalis are different. And the extract of M. officinalis can be used as an antioxidant.

• Genomics & Informatics
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• v.21 no.1
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• pp.9.1-9.13
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• 2023

Matrix metalloproteinase-9 (MMP-9) is a zinc and calcium-dependent proteolytic enzyme involved in extracellular matrix degradation. Overexpression of MMP-9 has been confirmed in several disorders, including cancers, Alzheimer's disease, autoimmune diseases, cardiovascular diseases, and dental caries. Therefore, MMP-9 inhibition is recommended as a therapeutic strategy for combating various diseases. Cinnamic acid derivatives have shown therapeutic effects in different cancers, Alzheimer's disease, cardiovascular diseases, and dental caries. A computational drug discovery approach was performed to evaluate the binding affinity of selected cinnamic acid derivatives to the MMP-9 active site. The stability of docked poses for top-ranked compounds was also examined. Twelve herbal cinnamic acid derivatives were tested for possible MMP-9 inhibition using the AutoDock 4.0 tool. The stability of the docked poses for the most potent MMP-9 inhibitors was assessed by molecular dynamics (MD) in 10 nanosecond simulations. Interactions between the best MMP-9 inhibitors in this study and residues incorporated in the MMP-9 active site were studied before and after MD simulations. Cynarin, chlorogenic acid, and rosmarinic acid revealed a considerable binding affinity to the MMP-9 catalytic domain (ΔG_binding < -10 kcal/ mol). The inhibition constant value for cynarin and chlorogenic acid were calculated at the picomolar scale and assigned as the most potent MMP-9 inhibitor from the cinnamic acid derivatives. The root-mean-square deviations for cynarin and chlorogenic acid were below 2 Å in the 10 ns simulation. Cynarin, chlorogenic acid, and rosmarinic acid might be considered drug candidates for MMP-9 inhibition.

• Biomolecules & Therapeutics
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• v.22 no.1
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• pp.62-67
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• 2014

This study was designed to find some potential natural products and/or constituents inhibiting proinflammatory cytokine generation in lung inflammation, since cytokines such as tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) and interleukin-6 (IL-6) are pivotal for provoking airway inflammation. In our preliminary screening procedure, the 70% ethanol extract of the leaves of Perilla frutescens (PFE) was found to clearly inhibit TNF-${\alpha}$ production in the lung at 100 mg/kg, after intranasal lipopolysaccharide treatment of mice. Based on this result, ten constituents including phenylpropanoids (allyltetramethoxybenzene, caffeic acid, dillapiole, elemicin, myristicin, nothoapiole, rosmarinic acid methyl ester, rosmarinic acid) and monoterpenes (perilla aldehyde and perilla ketone) were successfully isolated from the extract. Among them, elemicin and myristicin were found for the first time to concentration-dependently inhibit IL-$1{\beta}$-treated IL-6 production from lung alveolar epithelial cells (A549) at concentrations of $10-100{\mu}M$. These findings suggest that the phenylpropanoids including elemicin and myristicin have the potential to be new inhibitory agents against lung inflammation and they may contribute, at least in part, to the inhibitory activity of PFE on the lung inflammatory response.