• Journal of Life Science
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• v.21 no.5
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• pp.656-663
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• 2011

Licochalcone, a major phenolic constituent of the licorice species Glycyrrhiza inflata, a constituent of licorice, exhibits various biological properties, including chemopreventive-, antibacterial-, and anti-spasmodic activities. Recently, Licochalcone E (LicE) was isolated from the roots of Glycyrrhiza inflate, however its biological functions have not been fully examined. In the present study, we investigated the ability of LicE to regulate inflammation reactions in macrophages. Our in vitro experiments using murine macrophages, RAW264.7 cells, showed that LicE suppressed not only nitric oxide (NO) and prostaglandin $E_2$ generation, but also the expression of inducible NO synthase and cyclooxygenase-2 induced by lipopolysaccharide (LPS). Similarly, LicE inhibited the release of proinflammatory cytokines induced by LPS in RAW264.7 cells, including tumor necrosis factor-${\alpha}$ and interleukin-6. The underlying mechanism of LicE on anti-inflammatory action correlated with down-regulation of the nuclear factor-${\kappa}$B. Our data collectively indicate that LicE inhibited the production of several inflammatory mediators and might be used in the treatment of various inflammatory diseases.

• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.417-422
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• 2005

This study was aimed to design and formulate the moisture-activated patches containing ofloxacin and lidocaine for antibacterial and local anesthetic action. The solubility of lidocaine at $32^{\circ}C$ in various vehicles decreased in the rank order of PG $759.5{\pm}44.5\;mg/mL$ > PGL > IPM > PEG 300 > PEG 400 > Ethanol > PGMC > DGME > PGML > OA > $Captex^{\circledR}\;300$ > $Captex^{\circledR}\;200$ > water $(4.0{\pm}0.1\;mg/mL)$. Ofloxacin revealed very low solubility, which the highest solubility was obtained from PEG 400 $(18.7{\pm}6.3\;mg/mL)$ among the vehicles used. The addition of lactic acid increased the solubility of ofloxacin dramatically; the solubility at 5% lactic acid was $133.7{\pm}9.7\;mg/mL$. As $2-hydroxypropyl-{\beta}-cyclodextrin$ was added at the concentrations of 40, 80, 120, 160 and 200 mM, the solubilities of lidocaine and ofloxacin were enhanced up to three and two times, respectively, with concentration-dependent pattern. Gel intermediates for filmtype patches were prepared with mucoadhesive polymer, viscosity builders, lidocaine or ofloxacin at pH values from 5 to 7. Gels were cast onto a release liner and dried at room temperature. Dried patch was attached onto an adhesive backing layer, thus forming a patch system. Patches containing a single drug component were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane. The release study was carried out at $37^{\circ}C$ using a Franz-type cell. Receptor solutions were isotonic phosphate buffers (pH 7.4). Samples $(100\;{\mu}L)$ were taken over 24 hours and quantitated by a verified HPLC method. The releases from all tested were proportional to the square root of time. The release rates were 0.9, 157.3 and $281.7\;{\mu}g/cm^{2}/min^{1/2}$ for the lidocaine patches and 19.8,37.2 and $50.7\;{\mu}g/cm^{2}/min^{1/2}$ for the ofloxacin patches at the concentrations of 0.3, 0.5 and 1 %, respectively. The release rates were dose dependent in both drug patches $(R^{2}\;=\;0.9077\;for\;lidocaine;\;R^{2}\;=\;0.9949\;for\;ofloxacin)$ and those were also thickness-dependent $(R^{2}\;=\;0.9246\;for\;lidocaine;\;R^{2}\;=\;0.9512\;for\;ofloxacin)$.

• Journal of Periodontal and Implant Science
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• v.42 no.6
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• pp.185-195
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• 2012

Purpose: (-)-epigallocatechin-3-gallate (EGCG) has been reported to exert anti-inflammatory and antibacterial effects in periodontitis. However, its exact mechanism of action has yet to be determined. The present in vitro study evaluated the anti-in-flammatory effects of EGCG on human periodontal ligament fibroblasts (hPDLFs) and human periodontal ligament stem cells (hPDLSCs) affected by bacterial lipopolysaccharide (LPS) extracted from Porphyromonas gingivalis. Methods: hPDLFs and hPDLSCs were extracted from healthy young adults and were treated with EGCG and/or P. gingivalis LPS. After 1, 3, 5, and 7 days from treatment, cytotoxic and proliferative effects were evaluated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and bromodeoxyuridine assay, respectively. And then, the gene expressions of hPDLFs and hPDLSCs were observed for interleukin (IL)-$1{\beta}$, IL-6, tumor necrosis factor (TNF)-${\alpha}$, osteoprotegerin (OPG), receptor activator of nuclear factor kappa-B ligand (RANKL), and RANKL/OPG using real-time polymerase chain reaction (PCR) at 0, 6, 24, and 48 hours after treatment. The experiments were performed with the following groups for hPDLFs and hPDLSCs; 1) No treat, 2) EGCG alone, 3) P. gingivalis LPS alone, 4) EGCG+P. gingivalis LPS. Results: The 20 ${\mu}M$ of EGCG and 20 ${\mu}g/mL$ of P. gingivalis LPS had the lowest cytotoxic effects, so those concentrations were used for further experiments. The proliferations of hPDLFs and hPDLSCs increased in all groups, though the 'EGCG alone' showed less increase. In real-time PCR, the hPDLFs and hPDLSCs of 'EGCG alone' showed similar gene expressions to those cells of 'no treat'. The gene expressions of 'P. gingivalis LPS alone' in both hPDLFs and hPDLSCs were highly increased at 6 hours for IL-$1{\beta}$, IL-6, TNF-${\alpha}$, RANKL, and RANKL/OPG, except the RANKL/OPG in hPDLSCs. However, those increased gene expressions were down-regulated in 'EGCG+P. gingivalis LPS' by the additional treatment of EGCG. Conclusions: Our results demonstrate that EGCG could exert an anti-inflammatory effect in hPDLFs and hPDLSCs against a major pathogen of periodontitis, P. gingivalis LPS.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.122-127
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• 2023

Cardiovascular disease (CVD) is increasingly increasing as the main cause of death worldwide, and activation of platelet in vascular damage is one of the important causes of CVD. In recent, there is a growing interest in anti-thrombotic materials through platelet suppression, and efforts are being made to reduce side effects by using natural bioactive compounds. Known as one of the Flavonoids, hydroxygenkwanin (HGK) is a purified substance in Daphne Genkwa, which is known to have antibacterial, anti-inflammatory and anti-cancer effects, and has been reported to serve as an inhibitor of tissue factor that prevents thrombosis, but its anti-platelet effects and the action mechanisms is not known. In this study, we confirmed that the effects of HGK on the collagen-induced human platelets activation. HGK suppressed phosphorylation of PI3K/AKT and mitogen-activated protein kinases during platelet signaling, and reduced granule secretion in platelets such as ATP and serotonin. In addition, HGK inhibited the phosphorylation of cPLA₂ and strongly undermined the production of TXA₂, which is a powerful aggregation amplifier. As a result, the platelet aggregation derived by Collagen, a cohesive induced substance, was strongly suppressed by HGK to an IC₅₀ of 86.36 µM. Therefore, HGK might be worth the antithrombotic substance that inhibits the activation and aggregation of human platelets that occur through blood vessel damage.

• Journal of East-West Nursing Research
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• v.1 no.1
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• pp.50-71
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• 1997

The intention of this study is to apprehend the con. tents and methods of herb remedies that are commonly conducted when there are health-problem cases of ENT, eyes, teeth and skin. Methods of this study are divided into two stages : 1) For a period of six months from December 1994 to June 1995, some 40 persons who are believed to be well versed with herb remedies have been randomly chosen, and we made a survey on herb remedies by symptoms: and 2) we have endeavored to make their grounds evident through the studies on literatures with the focus on the basic data collected. Their results are as follows: 1) When one feels a pain in ears, such herb remedies are employed as pouring the vapor into ears, which is made by steaming Alaska pollack, or as applying or wiping with the juices of radish or the ginkgo, or' alum. Applying the radish juice is effective for sterilization and fever removal: and applying the ginkgo juice is effective for cleanliness. But, plastering alum, sesame oil or castor oil, or pouring the vapor of Alaska pollack into ears are perhaps effective but do not have any pharmacologic grounds. 2) When one bleeds at the nose, such kinds of herb remedies are applied as stimulating nose or head with cold water, pressing nose or ridge of nose, or filling up nares with mashed mugworts. In addition, they have utilized garlic or leeks. Such methods as stimulating with cold water or just pressing nose and ridge of nose is based on reasonable grounds, i.e. vasoconstriction and vascular compression ; and applying mashed garlic on the sole of foot is good for the circulation of Qui ; and the use of mugworts and leeks is based upon the pharmacological function of hemostasis. 3) When one feels a sore throat such kinds of herb remedies are employed as gargling or rinsing throat with brine, drinking hot gruel or water, or drinking the juice of mugwort, radish, ginger or Chinese quince. Gargling with brine or drinking the juice of mugwort, radish or ginger is based upon the pharmacological function of pain alleviation, fever removal, and detoxication. 4) When a boil is formed in mouth, such herb remedies are applied as spreading honey, brine or alum water, and taking gall nut, Chinese matrimony vine, lotus root, etc, for drugs. Spreading honey, brine or water that is made by infusing gallnut, Chinese matrimony vine, lotus root is based upon such functions as hematosis, astriction, antibacterial, and antiphlogistic, Alum, eggplant and licorice are said to be effective, but their pharmacological effects have no grounds. 5) When one has conjunctivitis such herb remedies are commonly applied as irrigation with brine and dropping breast milk in eyes. Moreover, such other drugs are used as plantain. shepherd's purse, and purslane, etc. The use of brine, breast milk, plantain, shepherd's purse and purslane is based upon such functions as sterilization, antiphlogistic, disinfection and pain relieving. Eriocaulon sieboldianum, bean stem, bean pod and narcissus leaves are said to be effective, but their pharmacological action have no basis. When one has a stye, such herb remedies are applied as extracting eyelashes, stimulating by a massage of middle finger, third finger or big toe, as well as sear ing with a heated bamboo comb that is fine-toothed. Other than these, plantain and nightshade's nuts are used as drugs for it. Extracting eyelashes corresponds with exclusing suppurative node and draining the stye of pus ; and the use of plantain is based upon disinfection: and nightshade's nuts are said to be effective, however, their pharmacological action has no grounds. 6) For a treatment of toothache, such herb remedies are commonly employed as rinsing mouth with brine and holding cold water or gasoline in the mouth ; and as the drugs that are believed to be effective have been Welsh onion, ginger and castor-oil, plant, etc. The use of Welsh onion is based upon pain killing, antiinflammatory actions, and the use of ginger is based upon detoxication and disinfection ; and seeds of castor-oil plants are said to be effective, but they have no pharmacological basis. 7) When one has hives, such herb remedies are commonly applied as rubbing burned straw in affected parts, exposing to its smoke, rubbing with salt, sweeping down with a broom, and spreading and drinking boiled water of trifoliate orange. The use of cassia tora seeds, walnut, aloe and radish is said to be effective. The use of cassia tor a seeds has the functions of intestinal order, anti-paralysis, etc. The use of walnut has resulted in an increase of blood by invigorating spirits ; and the use of aloe is based upon disinfection, antibiotic, anti-salt, antihistamine and detoxication action. But, the effects of radish juice and straw's smoke have no pharmacological grounds. 8) When one gets a boil, such herb remedies are commonly used as applying a plaster, paste of flour mixed with yolk, soy sauce or honey, as well as spreading pounded elm tree. Other remedies that have been said to be effective are ; heating with mugwort, brine, wild rocambole, aloe, onion, squid's bone, etc. The use of mugwort is based upon pain killing, astringent antiinflammatory and tranquility. Wild rocambole is based upon the generation and maintenance functions of cell-joining textures ; elm tree upon antiphlogistic ; aloe upon fever removal and antiphlogistic ; onion on pain killing, fever removal, antiphlogistic and tranquility ; squid's bone on astriction: and brine or vinegar on sterilization. Pine resin and gardenia seed are said to be effective, but they have no pharmacological basis. 9) When one cuts his skin, such herb remedies are commonly employed as spreading mugwort's juice or squid's bone powder, or pressing the wounds. In addition, kalopanax, onion and fine soil are employed. The use of mugwort, kalopanax and squid's bone is based upon such functions as hemostasis, sedation, pain killing, antibacterial ; and fine soil is said to be effective, but it has no pharmacological basis. 10) When one suffers from whitlow, such herb remedies are commonly utilized as heating with boiled soy sauce, spreading soybean paste, or dipping into eggs, etc. Other drugs that have been employed are onion root, brine, eggplant, potato, loach, etc. The use of onion is based upon pain killing and antiphlogistic functions ; and that of brine upon antiphlogistic function. The use of soy sauce or soybean paste, fomentation, eggplant, potato and loach is said to be effective, but it has no pharmacblogic ground. 11) For the treatment of frostbite, such herb remedies are commonly used as dipping the affected part into frozen soybean sack, using boiled water of eggplant stem, garlic caulis, onion, hot pepper, caulis. Onion is based upon antiphlogistic and tranquility actions garlic upon disintection, metabolic exacerbation, tonic and aphrodisiac actions and the use of eggplant and hot pepper is based upon help blood circulation, dissolution and excretion of waste matters in vein. 12) For the treatment of burn, such herb remedies or drugs are commonly used as cleansing with Korean gin, spreading eggs, cleansing with cold water and soap water ; and as brine, cactus, moss, soybean paste, oil, etc. The cleansing with Korean gin, cold water, soap water, brine, vinegar is based upon cleaning and sterilizing functions ; and the use of cucumber is based upon nu. trition provision, and strengthening of resisting power by adjustment of metabolism. The use of potato, cactus, moss, oil and eggs is said to be effective, but their phamacological functions are not clarified. In view of the above results, we can realize that the drugs that have been employed in herb remedies are quite diverse. However, in regard to majority of herb remedies that have been employed by symptoms, the pharmacological functions of their drugs have not been clarified, and they are merely known as effective. Furthermore, they have not been recorded in the literature as yet ; and we confirm that there have been many herb remedies that were executed without the proper knowlege of their effects. It is now our view that the results of this survey may be utilized for consulting data in regard to the use of herb remedies.

• The Journal of Korean Medicine
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• v.26 no.2 s.62
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• pp.95-104
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• 2005

Objectives: This was a double blinded, randomized, placebo-controlled clinical study for evaluation of safety and effective dose finding of Cardiotonic Pills$^{(R)}$ in patients with chest pain and discomfort. Cardiotonic Pills$^{(R)}$ are composed of Salviae Miltiorrhizae Radix (丹蔘), Notoginseng Radix (三七根) and Borneolum (龍腦). Major effects of Salviae Miltiorrhizae Radix and Notoginseng Radix are vasodilatation, sedation and analgesic action. Borneolum has an antibacterial effect, and can stimulate the central nervous system. All of these substances are oriental herbs that have been used for a long time in east Asia. Cardiotonic Pills fi received Investigational New Drug (IND) approval from the Food and Drug Administration (FDA) in the USA and 40 million people in the world take this pill. We performed a phase IV clinical study to confirm its efficacy and safety in patients who have probable cardiogenic or psychogenic chest pain or chest stifling. Methods: This study was planned for a multi-center clinical trial including four university hospitals of oriental medicine in Korea. This was the first time to evaluate the 'planning treatment according to diagnosis (辨證施治)' of chest pain or chest discomfort according to oriental medical guidelines. The patients who were included in this trial were adult volunteers from 20 to 70 years old who had chest pain or chest discomfort more than twice during a recent month, and we received written consent to participate in this study from all of them. After administration of Cardiotonic Pills$^{(R)}$ for 8 weeks, number of occurrences, duration, appearance and degree of chest pain or chest discomfort was observed and degree of symptoms (severity of illness, global improvement) were measured using a patient's global assessment composite scale. Results: In the patient's global assessment scale, the severity of illness of the Cardiotonic Pills$^{(R)}$ group (n=25) was 14/25=0.56 but of the placebo group (n=25) was 7/25=0.28 (p-value=0.0449). This result indicates Cardiotonic Pills$^{(R)}$have a positive effect on the symptoms of chest pain and discomfort. However, the global improvement of the Cardiotonic Pills$^{(R)}$group was 23/25=0.92, and of the placebo group was 22/25=0.88 (p-value=0.6374). The total symptom score of the Cardiotonic Pills$^{(R)}$ group was $1.68\pm20.06$, and of the placebo group was $16.76\pm72.l4$(p-value=0.2285). The number of symptom events of the Cardiotonic Pills$^{(R)}$ group was $72\pm29.78$, and of the placebo group (n=25) was $10.80\pm38.42$ (p­value=0.3660). We could not find any effects on the other factors examined besides the severity of illness, beyond the difference of standard deviations. Conclusions: Cardiotonic Pills$^{(R)}$ significantly reduced chest pain and chest discomfort in patients. Therefore, we expect that Cardiotonic Pills$^{(R)}$ will be helpful for patients with chest pain and chest discomfort not only caused by heart disease but also by other diseases.

• Microbiology and Biotechnology Letters
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• v.38 no.2
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• pp.190-197
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• 2010

To develop the safe and natural antimicrobial agents, the 68 ethanol extracts from the 61 different kinds of oriental herbal medicine were prepared and their antimicrobial activities were evaluated. The herbal medicine used were from China (46 kinds), South Korea (14 kinds), North Korea (5 kinds) and Vietnam (3 kinds), respectively, and the root (27 species) was popular part in this study. The average water content and extraction ratio for ethanol were 7.10% and 6.75%, respectively. Determination of antimicrobial activity by disc-diffusion assay at 0.5 mg/disc concentration showed that the extract of Angelica tenuissima Nakai (china), Illicium verum, Junci medulla, Rhus javanica L., Salvia miltiorrhiza Bunge and Syzygium aromaticum has strong antimicrobial activities against different food spoilage and pathogenic bacteria and fungi. Determination of MIC and MBC/MFC further showed that the extract of Syzygium aromaticum has MIC of 1.25 mg/mL and MBC/MFC of 1.25~5.00 mg/mL against Listeria monocytogenes, Bacillus subtilis, Staphylococcus epidermidis, Staphylococcus aureus, Salmonella typhimurium, Proteus vulgaris, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Saccharomyces cerevisiae. And, the extract of Junci medulla, Rhus javanica L. and Salvia miltiorrhiza Bunge showed strong antibacterial activities with MIC of 0.08~0.63 mg/mL and MBC/MFC of 0.08~2.50 mg/mL against the tested bacteria except E. coli and P. aeruginosa. In a while, the results of hemolytic activity of 68 different herbal extracts against human red blood cells showed that the extract of Angelica tenuissima Nakai has hemolytic activity at 0.5 mg/mL concentration. Therefore, Illicium verum, Junci medulla, Rhus javanica L., Salvia miltiorrhiza Bunge and Syzygium aromaticum were finally selected for natural antimicrobial resources. Further research on active substances and the mode of action of the selected herbal medicine is necessary.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.2
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• pp.481-489
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• 2005

Lonicerae Flos has antibacterial effects against Staphylococcus aureus, streptococci, pneumococci, Bacillus dysenterii, Salmonella typhi, and paratyphoid. It is an antiviral agent. The herb has a cytoprotective effect against $CCl_{4}-induced$ hepatic injury. It has antilipemic action, interfering with lipid absorption from the gut. Nowadays this herb is used mainly in the treatment of upper respiratory infections, such as tonsillitis and acute laryngitis. It is also used in the treatment of skin suppurations, such as carbuncles, and to treat viral conjunctivitis, influenza, pneumonia, and mastitis. Lonicerae Flos is dried flower buds of Lonicera japonica, L. hypoglauca, L. confusa, or L. dasystyla. But, for the most part, we use whole plant of Lonicera japonica, as a flower bud of it. And, little is known of the original copy of effects of whole plant, except for the 'Bon-Cho-Gang-Mok', which is written the effects of flower of Lonicera japonica are equal to effects of leaves and branch of it. The present study was conducted to evaluate the effect of flower and whole plant of Lonicera japonica on the regulatory mechanism of cytokines, inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2) for the immunological activities in Raw 264.7 cells. In Raw 264.7 cells stimulated with lipopolysaccharide (LPS) to mimic inflammation, flower and whole plant of Lonicera japonica water extracts inhibited nitric oxide production in a dose-dependent manner and abrogated iNOS and COX-2. Flower and whole plant of Lonicera japonica water extract did not affect on cell viability. To investigate the mechanism by which flower and whole plant of Lonicera japonica water extract inhibits iNOS and COX-2 gene expression, we examined the on phosphorylation of inhibitor ${\kappa}B{\alpha}$ and assessed production of $TNF-{\alpha}$, $interleukin-1{\beta}$ $(IL-1{\beta})$ and interleukin-6 (IL-6). Results provided evidence that flower and whole plant of Lonicera japonica inhibited the production of $IL-1{\beta}$, IL-6 and activated the phosphorylation of inhibitor ${\kappa}B{\alpha}$ in Raw 264.7 cells activated with LPS. These findings suggest that flower and whole plant of Lonicera japonica can produce anti-inflammatory effect, which may play a role in adjunctive therapy in Gram-negative bacterial infections, respectively.