• Bulletin of the Korean Chemical Society
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• 제6권4호
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• pp.222-224
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• 1985

The crystal structure of sulindac, $C_{20}H_{17}Fo_3S$, one of the nonsteroid antiinflammatory agents, has been determined by the X-ray diffraction techniques using diffractometer data obtained by the $\varpi-2{\theta}$ scan technique with Cu $$K_{\alpha}$$ radiation from a crystal with space group symmetry Pbca and unit cell parameters a = 8.166(1), b = 18.291(8), c = 23.245(10) ${\AA}.$ The structure was solved by direct methods and refined by full-matrix least-squares to a final R = 0.11 for the 1153 observed reflections. The carboxyl group is nearly perpendicular to the indenyl ring as observed in indomethacin. The dihedral angle between the indenyl and phenyl rings is $35^{\circ}while$ the corresponding angle in indomethacin is $67^{\circ}.$ Crystal packing consists of a hydrogen bond and partial ring stacking between the indenyl rings.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.282.2-283
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• 2003

The carboxylated acidic non-steroidal antiinflammatory drugs (NSAIDs) constitute the principal class of agents for controlling the pain and inflammation of the rheumatic diseases. It is mostly administered as a racemic mixture like most other drugs with asymmetric carbon atoms. However enantiomers of many racemic drug substances have been shown to posses different pharmacological toxicological properties. (omitted)

• Journal of Ginseng Research
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• 제43권3호
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• pp.335-341
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• 2019

Background: Inflammation is a host-defensive innate immune response to protect the body from pathogenic agents and danger signals induced by cellular changes. Although inflammation is a host-defense mechanism, chronic inflammation is considered a major risk factor for the development of a variety of inflammatory autoimmune diseases, such as rheumatic diseases. Rheumatic diseases are systemic inflammatory and degenerative diseases that primarily affect connective tissues and are characterized by severe chronic inflammation and degeneration of connective tissues. Ginseng and its bioactive ingredients, genocides, have been demonstrated to have antiinflammatory activity and pharmacological effects on various rheumatic diseases by inhibiting the expression and production of inflammatory mediators. Methods: Literature in this review was searched in a PubMed site of National Center for Biotechnology Information. Results: The studies reporting the preventive and therapeutic effects of ginseng and ginsenosides on the pathogenesis of rheumatic diseases were discussed and summarized. Conclusion: Ginseng and ginsenosides play an ameliorative role on rheumatic diseases, and this review provides new insights into ginseng and ginsenosides as promising agents to prevent and treat rheumatic diseases.

• Archives of Pharmacal Research
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• 제16권1호
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• pp.18-24
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• 1993

In this inverstigation, the various flavonoid aglycones were evaluated for their inhibitory activities against croton-oil or arachidonic acid induced mouse ear edema by oral or topical administration. The compounds tested were thirteen derivatives of flavan-3-ol(catechin and epicatechin), flavanone (flavanone and naringenin), flavone (flavone, chrysin and apigenin), flavonol(favonol, galangin, quercetin and morin) and isoflavone (biochanin A and 2-carbethoxy-5,7-dihydroxy-4'-methoxyisoflavone), along with hydrocortisone, indomethacin, 4-bormophenacyl bromide, nordihydroguaiaretic acid and phenidone as positive controls. A(isoflavone) were found to show broad inhibitoty activities (14-52%) against croton-oil or arachidonic acid induced ear edema by oral or topical application at the dose of 2 mg/mouse, although they showed less activity than hydrocortisone (26-88%) or indomethacin (36-80%). Flavonoid agtlycones tested showed higher activity when aplied topically than by the oral administration. It was also found that they inhibited arachidonic acid induced edema more profoundly than croton-oil induced edema by topical application. In arachidonic acid induced edema when applied topically, flavone derivatives such as flavone, chrysin and apigenin were revealed to be the good inhibitory agents in addition to flavonols and isoflavones. When quercetin and biochanin. A were selected for evaluating in carrageenan induced rat pleurisy and biochanin both flavonoids showed antiinflammatory activity at the dose of 70 mg/kg by the oral adminis-tration. All of these results revealed that flavonoid aglycones, especially 5,7-dihydroxy-flavonols having hydroxyl group(s) in B-ring and biochanin A (isoflavone) possessed in vivo antiinflammatory activity.

• Environmental Analysis Health and Toxicology
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• 제14권3호
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• pp.95-101
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• 1999

The scavenging effects of two hyaroxycinnamic acids such as caffeic acid and chlorogenic acid on paraquat induced pulmonary toxicity were investigated. The results are summerized as follows: 1. In the 5-lipoxygenase assay, caffeic acid and chlorogenic acid inhibited the enzyme activities whose inhibition concentration (IC$\_$50/) were 4.1 and 9.6 ${\mu}$M respectively. 2. To evaluate the antiinflammatory effects on mediator related to the mechanism of inflammation, ADP-induced platelet aggregation assay and histamine degranulation assay were used. Caffeic acid and chlorogenic acid inhibited on ADP-induced platelet aggregation and histamine release at a concentration dependent manners. 3. Arachidonic acid-induced ear edema were inhibited by administration of caffeic acid and chlorogenic acid. 4. Cytologicad analysis of branchoalveolar lavage fluid (BALF) which was the useful tool for detection of an inflammatory response in the lungs of animals intoxicated with chemicals were used. Alveolar macrophages and neutrophils in BALF, as well as the protein content and the LDH activity in BALF supernatant increased by intoxication of paraquat, but decreased by administration of caffeic acid and chlorogenic acid. Therefore, two hydroxyeinnamic acids tested were the useful candidates for scavenger and antiinflammatory agents on paraquat induced pulmonary toxicity.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.165-171
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• 1997

Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/$2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ inclusion compound on release of suppository was investigated. Complex formation was confirmed by $^{1}H-\;and\;^{13}C-NMR$ spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with $HP{\beta}CD$. The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/$HP{\beta}CD$ complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.

• Archives of Pharmacal Research
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• 제28권1호
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• pp.1-15
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• 2005

Cancer is still a major global health concern even after an everlasting strive in conquering this dread disease. Emphasis is now given to chemoprevention to reduce the risk of cancer and also to improve the quality of life among cancer afflicted individuals. Recent progress in molecular biology of cancer has identified key components of the cellular signaling network, whose functional abnormality results in undesired alterations in cellular homeostasis, creating a cellular microenvironment that favors premalignant and malignant transformation. Multiple lines of evidence suggest an elevated expression of cyclooxygenase-2 (COX-2) is causally linked to cancer. In response to oxidative/pro-inflammatory stimuli, turning on unusual signaling arrays mediated through diverse classes of kinases and transcription factors results in aberrant expression of COX-2. Population-based as well as laboratory studies have explored a broad spectrum of chemopreventive agents including selective COX-2 inhibitors and a wide variety of anti-inflammatory phytochemicals, which have been shown to target cellular signaling molecules as underlying mechanisms of chemoprevention. Thus, unraveling signaling pathways regulating aberrant COX-2 expression and targeted blocking of one or more components of those signal cascades may be exploited in searching chemopreventive agents in the future.

• 생약학회지
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• 제2권3호
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• pp.121-123
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• 1971

In series of the the development of domestic natural products, the studies were conducted to evaluate the pharmacologically active substances of the roots of Pursatilla koreana, which is a specific plant, widely distributed in this country and known to be effective as antiinflammatory, hemostatic and antidysentric agents in oriental remedies. From the hydrolysis of methanol extract of the root, a triterpenic substance was isolated. It was identified as $hederagenin\;C_{30}H_{48}O_4,\; m.p.\;333^{\circ}{\sim}334^{\circ}$, by the m.m.p. with authentic sample, elemental analysis, IR, mass spectra and the other physico-chemical experimentations.

• 생약학회지
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• 제8권2호
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• pp.61-68
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• 1977

The content of micro inorganic compounds in the 145 kinds of crude drugs on market was determined with Model 207 Atomic Absorption Spectrophotometer and Model 306 Flameless A.A. Content of Fe, Cu, Ni, Mn, Cd, Cr, Sn, and Pb was examined and the results revealed that the crude drugs which are using as a hematics and emmenagogues contained high content of iron, and those which are using as a antiinflammatory and emmenagogues contained high content of copper. Aromatic stomachics contain manganese and zinc, and diuretics and antiinaflammatory agents do tin. High content of Ni was found in tonics, but chronium and cadmium were not detected in crude drugs. There were no differences of content of trace metals in the various site of plants used.

• 생약학회지
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• 제38권1호
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• pp.22-26
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• 2007

Leaves and stem of Viburnum sargentii for. sterile(Caprifoliaceae) has been used as therapeutic agents as a pain of the joints, skin disease as styptics, analgesics for traditional folk medicines. The present study describes the preliminary evaluation of biological activities-analgesic, anti-inflammatory, hepatoprotective activities, of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in inflammation and writhing test.