• Biomolecules & Therapeutics
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• v.3 no.1
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• pp.34-37
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• 1995

Non-steroidal anti-inflammatory drugs (NSAIDs) have been known as inhibitors of the folate-requiring enzymes. In the present work, we have expanded on these observations and have investigated the inhibitory effects of NSAIDs on Lactobacillus casei thymidylate synthase expressed in E. coli. NSAIDs including sulphasalizine, salicylic acid, indomethacin and mefenamic acid were found to be competitive inhibitors with respect to folate of Lactobacillus casei thymidylate synthase. In contrast, aspirin and the antipyretic-analgesic drugs acetaminophen and antipyrine were weak inhibitors of the enzyme. Structure-activity correlation suggests that an aromatic ring with a side chain containing a carboxylic acid is a requirement for competitive inhibition of the thymidylate synthase. The results are consistent with the hypothesis that the antifolate activity of NSAIDs, and hence cytostatic consequences, are important factors in producing anti-inflammatory activity and aspirin exerts its anti-inflammatory effects after its conversion into salicylic acid, which possesses greater antifolate activity than its parent compound.

• Proceedings of the Korean Society of Toxicology Conference
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• 2001.05a
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• pp.14-21
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• 2001

Many epidemiological studies have revealed that the use of aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs) can reduce the risk of colon cancer. Since the well-documented pharmacological action of aspirin and other NSAIDs is the inhibition of cyclooxygenase [COX, the rate-limiting enzyme in prostaglandin (PG) biosynthesis], it has been inferred that the beneficial effect of NSAIDs may be mediated through the inhibition of PG biosynthesis.(omitted)

• 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.

• The Korean Journal of Pharmacology
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• v.26 no.1
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• pp.51-54
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• 1990

Human leukocyte cathepsin-Gs are active participant in the active phase of inflammations like rheumatoid arthritis, emphysema and glomerular injury. Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for treatment of these inflammatory diseases. Mechanism of action of NSAIDs for treatment of inflammatory diseases, especially like rheumatoid arthritis, are known as the inhibitors of prostaglandin synthesis. Inhibitions of the activities of human leukocyte cathepsin-Gs by non-steroidal anti-inflammatory drugs, however, were not same as the known pharmacological effects (inhibition of cyclooxygenase) of these drugs. Among them, especially, sulindac, salicylate, phenylbutazone, oxyphenbutazone, and salicyluric acid inhibited human leukocyte cathepsin-Gs effectively. $IC_{50}s$ of each drug were 4.3mM, 14.3mM, 6.5mM, 11mM and 15mM respectively. The drugs which have same chemical structure and same degree of inhibition effect on cyclooxygenase showed different degree or no effect on inhibition of cathepsin G. These inhibition effect might be, beside of inhibition of cyclooxygenase in the prostaglandin synthesis pathway, another benefitial antiinflammatory effect of NSAIDs by direct protection against tissue destruction in inflammatory diseases.

• 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

• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.4
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• pp.810-814
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• 2008

Most inflammatory disorders are usually treated using anti-inflammatory drugs including non-steroidal anti-inflammatory drugs (NSAID) and steroidal anti-inflammatory drugs (SAID). Prolonged uses of NSAIDs and SAIDs may frequently cause adverse side-effects such as nausea, vomiting, diarrhea, constipation, decreased appetite, kidney and liver failure, ulcers, and prolonged bleeding after an injury or surgery. Thus, it is necessarily required to develop a new anti-inflammatory drug with little side-effects. Dandelion (Taraxacum officinale) possesses the therapeutic abilities to eliminate body heat and toxins and to remove swelling and inflammation. In order to verify the anti-inflammatory activity of dandelion, TPA(12-O-tetra decanoylphorbol-acetate)-induced or croton oil-induced acute edema was developed in the mouse ears, and dandelion extract dissolved in acetone was applied to both sides of inflamed ears. It was found that dandelion could significantly reduce the ear swelling, compared to that of non-treated control. In the case of $20{\mu}{\ell}$ application of $100mg/m{\ell}$ dandelion solution (DA-100), its anti-inflammatory effect was comparable to that of indomethacin, a non - steroidal anti-anflammatory drug. Taken together, it could be concluded that topically applied dandelion extract exhibited its potentials as a new drug candidate with an effective anti-inflammatory activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.4
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• pp.977-981
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• 2005

Most inflammatory disorders are usually treated using anti-inflammatory drugs including non-steroidal anti-inflammatory drugs (NSAID) and steroidal anti-inflammatory drugs (SAID). In a prolonged use, however, they may frequently produce adverse side-effects. Thus, it is necessarily required to develop a new anti-inflammatory drug with little side-effects. Nephrite has been widely used by traditional oriental medicine to cure the various chronic diseases. In order to verify the anti-inflammatory activity of nephrite, the TPA (12-O-tetradecanoylphorbol-acetate) or the croton oil-induced edema was developed in the mouse ears and the nephrite powder suspension or the nephrite water was directly applied to the ear edema. It was found that nephrite could significantly reduce the ear swelling implying its strong potential as an active anti-inflammatory agent when comparing to indomethacin, a non-steroidal anti-inflammatory drug.

• Analytical Science and Technology
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• v.12 no.6
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• pp.571-576
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• 1999

Screening method for NSAIDs (Hon-Steroidal Anti-Inflammatory Drugs) in urine was developed using GC/NCI-MS. Derivatized six fenamates with pentafluoropropionic anhydride showed high sensitivity in NCI-MS. The conditions of the derivatization reaction and chromatographic conditions were established for screening with a trace analysis. Limit of detection was in the range of 4-25 pg/mL. This method may be used to the equine doping analysis for NSAIDs and forensic analysis.

• Journal of Digestive Cancer Reports
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• v.8 no.2
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• pp.77-80
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• 2020

Gastric cancer is one of the leading causes of cancer-related deaths worldwide. The increased expression of cyclooxygenase (COX)-2 has been implicated in the development and progression of gastric cancers. A number of recent studies have been published evaluating the chemopreventive effect of aspirin and non steroidal anti inflammatory drungs (NSAIDs) against gastric cancer. Aspirin and NSAIDs use may reduce the risk of gastric cancer incidence and death, whereas other studies have reported contradictory results. Therefore, further study should be needed to clarify the role of aspirin and NSAIDs in the chemoprevention of gastric cancer.

• CELLMED
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• v.4 no.2
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• pp.10.1-10.8
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• 2014

Affecting more than half of menstruating women, dysmenorrhea is a cramp which causes abdominal or lower back pain just before or during a menstruation. In western medicine, non-steroidal anti-inflammatory drugs (NSAIDs) are normally used to treat primary dysmenorrheal symptoms. Despite their rapidity in relieving pain, NSAIDs have many serious side effects on the liver, kidney, and gastrointestinal tract. Thai traditional medicines comprise many preparations for treating dysmenorrhea, especially Prasaplai preparation which has been listed in the Thai traditional common household drug list since 2006. The use of Prasaplai was originated about 100 years ago and is still being used in the present time to treat dysmenorrhea. This review focuses on the history of the preparation, active ingredients, and biological activities especially on cyclooxygenase inhibitor, artifacts occurred in the preparation, quantitative analysis, and clinical trial of Prasaplai formulation.