• Journal of Pharmaceutical Investigation
• /
• 제13권2호
• /
• pp.66-72
• /
• 1983

Ketoprofen, 2-(3-benzoyl phenyl) propionic acid, has many advantages over the other antiinflammatory drugs, such as salicylates, phenytbutazone, and indomethacin. According to the reports, ketoprofen is well tolerated by patients and has very low incidence of side effects and toxic reactions. Although ketoprofen is widely used as an antiinflammatory agent, it shows poor solubility in water. In order to enhance water solubility, ketoprofen was made as lysine salt, such as acetylsalicylate lysine salt, ibuprofen lysine salt and amino acid salt of phenylbuatzone. The purpose of this study was to compare with ketoprofen lysinate in aspect of binding to human serum albumin (HSA) were made, and the association constant and the number of binding site were obtained using difference spectrophotometry. The number of binding site of HSA for ketoprofen and ketoprofen lysinate appears to be 3.3,3.2 respectively and association constants were found as follow; HSA-ketoprofen $2.23{\times}10^4\;M^{-1}$, HSA-ketoprofen lysinate $1.02{\times}10^4\;M^{-1}$.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
• /
• pp.33-33
• /
• 1993

Among the Glycosaminoglycans (GAGs), Heparin and its fractions or fragments, obtained by several different processes, are of considerable interest .In these last few years, the goal of the researchers in this field has been finding molecular species having selective action, like for instance species having only antithrombotic activity disjointed from any anticoagulant effect, and assessing the effects of these GAGs and of other GAGs, like dermatan sulphate, not only in the field of venous or arterial thrombosis but also on cell factors like smooth muscle cell proliferation and even on aspects of antiinflammatory activity.

• 한국자원식물학회:학술대회논문집
• /
• 한국자원식물학회 2005년도 International Symposium & conference of the Plant Resources Society of Korea
• /
• pp.185-185
• /
• 2005

• Journal of Pharmaceutical Investigation
• /
• 제17권4호
• /
• pp.197-204
• /
• 1987

Novel pranoprofen algininate and lysinate salts were manufactured and their salt formation was confirmed by melting point, infrared spectroscopy, nuclear magnetic resornance spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. The physical properties of pranoprofen lysinate and argininate salts were compared with those of pranoprofen through in vitro and in vivo tests. Solubility, $pK_a$ and lipid-water partition coefficient were measured through in vitro experiments, while antiinflammatory efficacy, analgesic effect, acute toxicity and in situ absorption were tested through in vivo experiments. The results obtained were as follows: 1) The solubilities of pranoprofen argininate and lysinate salts were increased markedly in pH 6.8 and pH 7.5 phosphate buffer solutions, comparing with that of pranoprofen itself. 2) $pK_a$ values of pranoprofen, pranoprofen argininate and lysinate salts were 6.34, 7.99 and 7.56 in carbon tetrachloride, and 5.86, 6.69 and 7.92 in chloroform, respectively by liquid-liquid partition method. 3) The lipid-water partition coefficients of pranoprofen argininate and lysinate salts were increased more than that of pranoprofen in carbon tetrachloride, chloroform, or benzene-pH 6.8 buffer system, but were nearly identical using pH 1.2 buffer as water phase. 4) Antiinflammatory effects of pranoprofen argininate and lysinate salts were remarkably increased and analgesic effects of the salts were as same as that of pranoprofen. 5) Pranoprofen argininate and lysinate salts were safer than pranoprofen itself in acute toxicity, and the in situ absorption rates of pranoprofen, pranoprofen argininate and lysinate salts were 0.392, 0.960 and $0.762\;hr^{-1}$, respectively according to the rat intestine recirculation experiment.

• Natural Product Sciences
• /
• 제14권4호
• /
• pp.274-280
• /
• 2008

Platycosides are the saponins in Platycodi Radix and they have several beneficial effects such as antiinflammatory and anti-obesity activities. This study was designed to determine the changes in the saponin composition in Platycodi Radix (platycosides) after being processed under steam and pressure and to investigate the anti-inflammatory effects of their extracts. The change of the platycoside compositions was investigated after 1, 2, 3, 6 and 9h heat processing of Platycodi Radices by using HPLC coupled with an evaporative light scattering detection (ELSD) system. After heat treatment ($125^{\circ}C$, 1, 2, 3, 6 and 9 h), the contents of several platycosides such as platycoside E, platycodin $D_3$, platycodin D, polygalacin D, and platycodin A decreased as the processing time was longer. While the total contents of the saponins decreased, the contents of deapi-forms of deapiplatycoside E, deapi-platycodin $D_3$, and deapi-platycodin D increased relatively. These results indicate that the linkage between apiose and xylose located at C-28 is labile to heat and pressure. The LPS-induced iNOS inhibitory activities of the samples treated for 1 and 2 hours were enhanced and after then, the activities were reduced. These results suggested that heat treatment of the samples affect the content of the total saponins and the saponin content may be the important criteria representing the anti-inflammatory activity.

• Journal of Ginseng Research
• /
• 제45권5호
• /
• pp.610-616
• /
• 2021

Background: Thymic stromal lymphopoietin (TSLP) acts as a master switch for inflammatory responses. Ginsenoside Rg3 (Rg3) which is an active ingredient of Panax ginseng Meyer (Araliaceae) is known to possess various therapeutic effects. However, a modulatory effect of Rg3 on TSLP expression in the inflammatory responses remains poorly understood. Methods: We investigated antiinflammatory effects of Rg3 on an in vitro model using HMC-1 cells stimulated by PMA plus calcium ionophore (PMACI), as well as an in vivo model using PMA-induced mouse ear edema. TSLP and vascular endothelial growth factor (VEGF) levels were detected using enzyme-linked immunosorbent assay or real-time PCR analysis. Murine double minute 2 (MDM2) and hypoxia-inducible factor 1α (HIF1α) expression levels were detected using Western blot analysis. Results: Rg3 treatment restrained the production and mRNA expression levels of TSLP and VEGF in activated HMC-1 cells. Rg3 down-regulated the MDM2 expression level increased by PMACI stimulation. The HIF1α expression level was also reduced by Rg3 in activated HMC-1 cells. In addition, Rg3-administered mice showed the decreased redness and ear thickness in PMA-irritated ear edema. Rg3 inhibited the TSLP and VEGF levels in the serum and ear tissue homogenate. Moreover, the MDM2 and HIF1α expression levels in the ear tissue homogenate were suppressed by Rg3. Conclusion: Taken together, the current study identifies new mechanistic evidence about MDM2/HIF1α pathway in the antiinflammatory effect of Rg3, providing a new effective therapeutic strategy for the treatment of skin inflammatory diseases.

• Journal of Ginseng Research
• /
• 제43권2호
• /
• pp.319-325
• /
• 2019

Background: Ginsenoside Rf is a ginseng saponin found only in Panax ginseng that affects lipid metabolism. It also has neuroprotective and antiinflammatory properties. We previously showed that Korean Red Ginseng (KRG) inhibited the expression of cyclooxygenase-2 (COX-2) by hypoxia via peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$). The aim of the current study was to evaluate the possibility of ginsenoside Rf as an active ingredient of KRG in the inhibition of hypoxia-induced COX-2 via $PPAR{\gamma}$. Methods: The effects of ginsenoside Rf on the upregulation of COX-2 by hypoxia and its antimigration effects were evaluated in A549 cells. Docking of ginsenoside Rf was performed with the $PPAR{\gamma}$ structure using Surflex-Dock in Sybyl-X 2.1.1. Results: $PPAR{\gamma}$ protein levels and peroxisome proliferator response element promoter activities were promoted by ginsenoside Rf. Inhibition of COX-2 expression by ginsenoside Rf was blocked by the $PPAR{\gamma}-specific$ inhibitor, T0070907. The $PPAR{\gamma}$ inhibitor also blocked the ability of ginsenoside Rf to suppress cell migration under hypoxia. The docking simulation results indicate that ginsenoside Rf binds to the active site of $PPAR{\gamma}$. Conclusions: Our results demonstrate that ginsenoside Rf inhibits hypoxia induced-COX-2 expression and cellular migration, which are dependent on $PPAR{\gamma}$ activation. These results suggest that ginsenoside Rf has an antiinflammatory effect under hypoxic conditions. Moreover, docking analysis of ginsenoside Rf into the active site of $PPAR{\gamma}$ suggests that the compound binds to $PPAR{\gamma}$ in a position similar to that of known agonists.

• 한국식품영양학회지
• /
• 제23권4호
• /
• pp.542-548
• /
• 2010

This study was conducted to investigate the effects of Acanthopanax senticosus extracts(ASE) on alcohol administered mice. The administration of Acanthopanax senticosus extracts(60 mg/kg) had beneficial actions toward alcohol degradation in acute alcohol treated mice. In the acute alcohol degradation experiment, serum alcohol concentration were lower 3 and 6 hours after taking ethanol(5 g/kg) in ASE treated mice. The oral administration of ASE showed decreased gastric mucous membrane damage produced in ethanol treated mice. In addition, intraperitoneal(i.p.) administration of ASE showed antiinflammatory effects in inhibition tests of vascular permeability produced by acetic acid. ASE also reduced concentrations of nitric oxide(NO), tumor necrosis alpha(TNF)-${\alpha}$ and interleukin(IL)-6 in macrophages that were activated by LPS. These results demonstrate that Acanthopanax senticosus extracts possesses the potential to stimulate alcohol degradation and inhibit inflammatory effects in mice.

• 한방안이비인후피부과학회지
• /
• 제20권3호
• /
• pp.43-50
• /
• 2007

Background and Objectives : The aim of this study was to investigate the anti-oxidant and anti-inflammatory effects of the Taglisodog-eum(TSE) extract on the RAW264.7 cell Methods : The RAW264.7 cell was cultured using Dulbecco's modified Eagle's medium(DMEM, USA), including the 10% fetal-bovine serum(FBS; Sigma, USA) in a $37^{\circ}C$, 5% CO2 incubator. Results : The anti-oxidant ability of TSE were dose-dependantly increased. The LPS-induced IKK, iNOS and COX-2 mRNA expression were dose-dependantly decreased in the RAW264.7 cells treated with TSE. $NF-kB$ activation was suppressed. Conclusion : The findings in this study show that TSE has anti-oxidant and anti-inflammatory effects, such as the inhibition of $NF-kB$ activity.

• 생약학회지
• /
• 제17권3호
• /
• pp.206-214
• /
• 1986

These studies were conducted an attempt to investigate effects of 'Paeryungtang' and 'Kamipaeryungtang' water extracts on diuretic, antipyretic, antiinflammatory and analgesic actions. The results of these studies were summarized as follows; Increase in urinary volume, urinary $Na^+$ excretions were significantly recognized in normal rat. Increase in urinary volume, urinary $Na^+\;and\;Cl^-$ excretions were significantly shown in rat with 2mg/kg $HgCl_2$-induced acute renal failure. Antipyretic, anti-inflammatory and analgesic effects of 'Paeryungtang' and 'Kamipaeryungtang' were recognized in mice, rats and rabbits.