• Journal of the Korean Orthopaedic Association
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• v.55 no.1
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• pp.9-28
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• 2020

Non-steroidal anti-inflammatory drugs (NSAIDs) are the most commonly used drugs worldwide for chronic pain, such as arthritis, and there are many different types depending on their composition and mechanism. After long-term use, various side effects can occur, such as gastrointestinal and cardiovascular complications. With a similar analgesic effect to that of traditional non-selective NSAIDs, cyclooxygenase-2-selective NSAIDs have been highly anticipated, because they could complement gastrointestinal tolerance. On the other hand, because of concerns about cardiovascular safety in 2004 and 2005, and the license withdrawals of rofecoxib and valdecoxib, the interest in the side effects of NSAIDs is increasing. Therefore, it is important to use the necessary drugs at a minimum, considering the side effects and interactions of each drug. This study examined the side effects and characteristics of each NSAID that may occur and reviewed the recent research and guidelines related to the use of non-selective NSAIDs and cyclooxygenase-2-selective NSAIDs.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.29-38
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• 2023

Recent studies have highlighted the link between diseases and inflammation across our lifespan. Our sedentary lifestyle, high-calorie diet, chronic stress, chronic infections, and exposure to pollutants and xenobiotics, collectively intensify the course and recurrence of infections and inflammation in our bodies, promoting the prevalence of chronic diseases and aging. Given such phenomena and considering additional factors such as the frequency of prescription, and easy access to over-the-counter drugs, the need for anti-inflammatory therapeutics is ever-increasing. However, the readily available anti-inflammatory treatment option comes with a greater risk of side effects or high cost (biologics). Therefore in this growing competition of discovering and developing new potent anti-inflammatory drugs, we focused on utilizing the established knowledge of traditional medicine to find lead compounds. Since lead optimization is an indispensable step toward drug development, we applied this concept for the production of potent anti-inflammatory compounds achieved by structural modification of flavonoids. The derivative obtained through acetylation of myricetin, 3,3',4',5,5',7-hexaacetate myricetin, showed a greater inhibitory effect in the production of pro-inflammatory mediators such as nitric oxide, Prostaglandin E₂, and pro-inflammatory cytokines like interleukin-6, interleukin1β, in lipopolysaccharide-stimulated RAW264.7 mouse macrophage cells compared to myricetin. The increased potency of inhibition was in conjunction with an increased inhibitory effect on inducible nitric oxide synthase and cyclooxygenase-2 proteins. Through such measures, this study supports lead optimization for well-established lead compounds from traditional medicine using a simpler and greener chemistry approach for the purpose of designing and developing potent anti-inflammatory therapeutics with possibly fewer side effects and increased bioavailability.

• Preventive Nutrition and Food Science
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• v.14 no.3
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• pp.179-187
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• 2009

Five kinds of coumarin compounds were successfully purified from Angelica gigas Nakai by using recyclingpreparative HPLC and identified as decursin (1), decursinol angelate (2), 7-demethylsuberosine (3), marmesin (4), and decursinol (5) by NMR analyses. None of the purified compounds in ethanol showed DPPH radical scavenging activity, while the A. gigas extract (AGNEX) displayed a significant level of activity. Interestingly, compounds 3 in phosphate buffered saline (PBS) showed good $ABTS^+$ radical scavenging activity ($IC_{50}=8.1{\mu}g$/mL) as did compounds 4 and 5. The anti-inflammatory activities of the purified compounds were evaluated and compared using the NO concentration assay and western blot analysis on LPS-stimulated RAW 264.7 cells. NO production was significantly suppressed by all the compounds in a dose-dependent manner among which compounds 1, 2, and 3 showed very good activities with $IC_{50}$ values of 7.4, 6.5, and $7.6{\mu}g$/mL, respectively. Treatment with compounds 1-5 effectively suppressed the expression levels of iNOS, IL-1$\beta$, and COX-2, which are responsible for promoting the inflammatory process. Thus, the ethanol extract and coumarin compounds of A. gigas Nakai hold promise for use as potential anti-inflammatory agents.

• Journal of Yeungnam Medical Science
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• v.17 no.1
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• pp.1-11
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• 2000

Inhibition of cyclooxygenase(COX), and thus prevention of the formation of prostaglandins, provided a unifying explanation of the therapeutic and toxic actions of nonsteroidal anti-inflammatory drugs (NSAIDs). Recently, the discovery of the two isoforms of COX was made by molecular biologists studying neoplastic transformation in chick embryo cells. The constitutive enzyme, COX-1, is obviously responsible for the production of prostaglandins involved in housekeeping functions such as maintenance of integrity of the gastric mucosa, renal blood flow and platelet aggregation. The inducible form of COX (COX-2) is responsible for the formation of prostaglandins that pathologically affects inflammation, pain and fever. Clearly, all the experimental and clinical data support the hypothesis that the beneficial effects of NSAIDs are due to inhibition of the COX-2 enzyme, whereas the gastrotoxicity is due to inhibition of COX-1. The cox-2/COX-1 ratios of the NSAIDs in common use have been measured and compared with epidemiological data on their side effects. There is little evidence to suggest that one NSAID is clearly more effective than another, But substantial individual variability is present with respect to the pharmacology and pharmacokinetics of these drugs: therefore it is essential to adjust the dosage and choose specific drug to the patient's response.

• Biomolecules & Therapeutics
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• v.8 no.4
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• pp.349-353
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• 2000

Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.

• Journal of Powder Materials
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• v.25 no.6
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• pp.459-465
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• 2018

Most commercially available detonation nanodiamonds (DNDs) require further processing to qualify for use in biomedical applications, as they often contain many impurities and exhibit poor dispersibility in aqueous media. In this work, DNDs are modified to improve purity and impart a high colloidal stability to the particles. The dispersive and adsorption properties of modified DNDs are evaluated in terms of the suitability of DNDs as carriers for non-steroidal anti-inflammatory drugs (NSAIDs) in transdermal delivery. The study of adsorption on strongly positively and strongly negatively charged DNDs showed their high loading capacity for NSAIDs, and a pronounced relationship between the drugs and the particles' charges. Experiments on long-term desorption carried out with DND/NSAID complexes indicate that the nanoparticles exert a sustained effect on the drug release process.

• Korean Journal of Pharmacognosy
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• v.16 no.1
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• pp.18-25
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• 1985

Experimental studies were conducted to investigate for the effect of Tongkyu-tang on analgesic, antipyretic, sedative, anti-inflammatory, isolated ileum and anti-histamine actions. Tongkyu-Tang was composed of sixteen crude drugs including Astragali Radix, which has been used for the treatment of common cold, headache, rhinitis, nasal obstruction, rhincospasm, etc. The following results have been obtained; analgesic and antipyretic actions were obtained. Prolonged action against the hypnotic duration of pentobarbital were significantly noted in mice. Anti-inflammatory effects in the paw edema induced by 1% carrageenin and 1% dextran were significantly shown in rats. Spontaneous motilities of isolated ileum of mice were strongly suppressed, and contractions of isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Antihistamine actions were noted. Considering the above experimental results, it is suggested that effects of Tongkyu-tang based on the Oriental Medical References were similarly consistent with the actual experimental results.

• YAKHAK HOEJI
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• v.25 no.1
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• pp.9-14
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• 1981

Anti-infammatory, analgesic and ulcerogenic activities of fentiazac were investigated in comparison with those of acetylsalicylic acid, fenbufen, naproxen and phenylbutazone. On the anti-inflammatory activity in carrageenin-induced rat paw edema and the analgesic activity on writhing syndrome induced with acetic acid in mice, fentiazac displayed more potent effect than acetylsalicylic acid, fenbufen and pbenylbutazone. But the ulcerogenic action of fentiazac on gastrointestinal tract in fasting rats was less than that of reference drugs. From these investigation, fentiazac seemed to indicate a poor correlation between the extent of anti-inflammatory activity and ulcerogenic action.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.11-18
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• 1996

We have established an air pouch-type allergic inflammation model in rats [1,2] and a peritoneal eosinophilia model in rats [3]. Employing the two models, chemical mediators and cytokines responsible for the development of inflammation induced by at allergic mechanisms are investigated to clarify the usefulness of the two models for the screening of anti-allergic inflammatory drugs.

• Bulletin of the Korean Chemical Society
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• v.30 no.11
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• pp.2827-2829
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• 2009