• Title/Summary/Keyword: Nonsteroidal antiinflammatory drugs

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Studies on the Antiinflammatory Effects and the Change of Copper Content after Administration of Nonsteroidal Antiinflammatory Drugs in Rats (쥐에서 비스테로이드성 항염증제의 투여후 항염효과와 혈청 및 조직내 구리함량변화에 관한 연구)

  • 허인회;임철빈
    • YAKHAK HOEJI
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    • v.26 no.2
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    • pp.97-103
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    • 1982
  • This paper presents anti-inflammatory effects of nonsteroidal anti-inflammatory drugs and their copper complexes, and the change of content of copper in serum, liver, brain and edema foot induced by 1% carrageenan in rats, and also investigation of stomach hemorrhage. The results were as follows. 1. The content of copper decreased in liver and brain, however, the concentration of copper significantly increased in serum and edema site after carrageenan injection in rats. 2. The content of copper in serum and edema site was decreased after administration of anti-inflammatory drugs. 3. Edema inhibition rate of aspirin was, higher than that of copper (II) aspirinate, but edema inhibition rate of copper complex of naproxen was markedly higher than that of naproxen. 4. Hemorrhage of stomach of copper salicylate was higher than that of sodium salicylate, but hemorrhage of stomach of sodium naproxen was higher than that of copper naproxen.

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Inhibition of Heat-induced Denaturation of Albumin by Nonsteroidal Antiinflammatory Drugs (NSAIDs): Pharmacological Implications

  • Luciano-Saso;Giovanni-Valentini;Casini, Maria-Luisa;Eleonora-Grippa;Gatto, Maria-Teresa;Leone, Maria-Grazia;Bruno-Silvestrini
    • Archives of Pharmacal Research
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    • v.24 no.2
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    • pp.150-158
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    • 2001
  • The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could also act by protecting endogenous proteins against denaturation, we evaluated their effect on heat-induced denaturation human serum albumin (HSA) in comparison with several fatty acids which are known to be potent stabilizers of this protein. By the Mizushimas assay and a recently developed HPLC assays we observed that NSAIDs were slightly less active [$EC_{50}~10^{-5}-10^{-4}$ M] than FA and that the HPLC method was less sensitive but more selective than the turbidimetric assay, i.e. it was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates. In conclusion, this survey could be useful for the development of more effective agents in protein condensation diseases like rheumatic disorders, cataract and Alzheimers disease.

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Protective Effect of DA-9601, an Extract of Artemisiae Herba, against Naproxen-induced Gastric Damage in Arthritic Rats

  • Oh, Tae-Young;Ryu, Byong-Kweon;Ko, Jun-Il;Ahn, Byoung-Ok;Kim, Soon-Hoe;Kim, Won-Bae;Lee, Eun-Bang;Jin, Joo-Hyun;Hahm, Ki-Baik
    • Archives of Pharmacal Research
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    • v.20 no.5
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    • pp.414-419
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    • 1997
  • Gastrointestinal irritation is the most frequent adverse effect in patients chronically taking nonsteroidal antiinflammatory drugs (NSAIDs) for the treatment of arthritic conditions. Gastroprotective effect of DA-9601, a new antiulcer agent from Artemisiae Herba extract, against NSAID was evaluated in a rat model of arthritis that is similar in many aspects to human rheumatoid arthritis. Daily oral dosing of naproxen (30 mg/kg), one of the most commonly used NSAID, induced apparent gastric lesions as well as a significant decrease in mucosal prostagiandin $E_2;(PGE_2)$ and prostagiandin F_${1{\alpha}}$$(PGF_{1{\alpha}})$ levels. Coadministration of DA-9601 prevents naproxen-induced mucosal injury and depletion of prostaglandins, in a dose-related manner. DA-9601 did not alter the antiinflammatory or analgesic effect of naproxen. The present results suggest that DA-9601 may be useful as a mucoprotectant against NSAIDs in clinical practice.

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Antiinflammatory Activity of Ketoprofen Gel (케토프로펜 겔의 함염증작용)

  • Tan, Hyun-Kwang;Chi, Sang-Cheul;Jun, H.Won
    • Journal of Pharmaceutical Investigation
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    • v.24 no.1
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    • pp.17-24
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    • 1994
  • The antiinflammatory and antirheumatic activities of a 3% ketoprofen gel (ID-GEL) were evaluated using carrageenan-induced paw edema method and adjuvant-induced arthritis method, respectively, after its transdermal administration of 50 mg on rat paws in reference to existing transdermal preparations containing 3% ketoprofen and other nonsteroidal antiinflammatory drugs (NSAIDs). The % inhibition of carrageenan-induced edema by ID-GEL was 56.2-65.0%, close to the maximum inhibition obtainable with this model, while the % inhibition by existing 3% ketoprofen gels and other NSAID transdermal preparations were 33.8-47.7% and 18.7-29.2%, respectively. ID-GEL had a pronounced antirheumatic activity in both preventive and curative studies with adjuvant-induced arthritis in rats in respect with the inhibition of edema, arthritis score and weight gain, in reference to existing 3% ketoprofen gel.

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Flavonoids: Potential Antiinflammatory Agents

  • Kim, Hyun-Pyo;Son, Kun-Ho;Chang, Hyun-Wook;Kang, Sam-Sik
    • Natural Product Sciences
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    • v.2 no.1
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    • pp.1-8
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    • 1996
  • Flavonoids are widely distributed polyphenol compounds in plant kingdom and known to possess varieties of biological/pharmacological activities in vitro and in vivo. A search for antiinflammatory/immunoregulatory flavonoids as potential therapeutic agents has been continued, since serious side effects of currently used nonsteroidal and steroidal antiinflammatory drugs limit their long term uses for the inflammatory disorders. In this reserch, various flavonids were isolated and tested for their in vivo antiinflammatory activity and in vitro inhibitory activity of lymphocyte proliferation. Using a mouse ear edema assay, it was found that certain flavones/flavonols possess mild antiinflammatory activity and a C-2,3-double bond might be essential. Isoflavones were less active. These flavonoids inhibited in vitro lymphocyte proliferation, relatively specific for T-cell proliferation $(IC_{50}=1-10\;{\mu}M)$ and the inhibition was reversible. We have also tested several biflavonoid derivatives, since we recently found that biflavones were phospholipase $A_2$ inhibitors. It was demonstrated that biflavones such as ochnaflavone and ginkgetin inhibited lymphocyte proliferation induced by both concanavaline A and lipopolysaccharide. The inhibition was irreversible in contrast to that of flavones/flavonols. And antiinflammatory activity of biflavonoids are discussed.

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Synthesis of 1,2-Benzothiazine Derivatives as Oxicam Family (옥시캄 계열의 1,2-벤조티아진 유도체의 합성)

  • Park, Myung-Sook
    • YAKHAK HOEJI
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    • v.44 no.6
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    • pp.494-498
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    • 2000
  • Noble 7,7'-substituted (or unsubstituted) 4-oxo-1,1',2,2'-dibenzothiazine-3,3'-dicarboxylic acid methyl ester 1,1,1',1'-tetraoxide 3,4'-yl ethers 2a-h were synthesized through the dehydration of 7-substituted (or unsubstituted) 4-hydroxy-1,2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxides 1a-h using silver(I) oxide for the development of new nonsteroidal antiinflammatory drugs (NSAIDs). Optimal reaction was proceeded through stirring of distilled acetone using 100 mol% of silver(I) oxide at room temperature for 24-68 hrs.

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SAR of COX-2 Inhibitors (COX-2 억제제의 구조-활성)

  • 권순경
    • Biomolecules & Therapeutics
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    • v.9 no.2
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    • pp.69-78
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    • 2001
  • Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachi-donic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet aggregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDS) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAms. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.

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Effect of Auricular Acupuncture on Nonsteroidal Antiinflammatory Drug Dose in Primary Dysmenorrhea : A Randomized Controlled Trials (비스테로이드성 소염진통제를 복용하는 원발성 월경곤란증 환자에 대한 이침치료의 무작위대조군임상시험)

  • Hur, Da-Hee;Kang, So-Hyeon;Kwon, Han-Seul;Ahn, Ha-Young;Baek, Hyung-Chan;Kim, Hyeong-Jun
    • The Journal of Korean Obstetrics and Gynecology
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    • v.35 no.4
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    • pp.161-173
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    • 2022
  • Objectives: This study was conducted to evaluate the effectiveness of acupuncture in patients with primary menstrual difficulties taking NSAIDs. Methods: 30 women with primary menstrual difficulties with NSAIDs were assigned to treatment groups (n=15) and control groups (n=15). On their first visit, both groups were provided with a menstrual diary and were required to record the intensity of pain and the dosage of painkillers during each menstrual cycle. The treatment group received two acupuncture treatments per cycle during two cycles, and the control group did not receive acupuncture. Pain strength during menstruation was evaluated using Visual Analogue Scale (VAS), and the total number of painkillers taken during menstruation and the average number of painkillers taken during a single dose was measured. Results: The treatment group had significant pain relief compared to the pre-test group and significant differences from the control group. In addition, there was a significant difference between the treatment group and the control group in the frequency of taking painkillers during the menstrual period and the dose in the test group was significantly lower than before treatment. Conclusions: This clinical trial showed that this acupuncture can help alleviate primary menstruation and reduce the use of nonsteroidal anti-inflammatory drugs.