• Title/Summary/Keyword: Anti-inflammatory drugs

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Inhibition of Human Leukocyte Cathepsin G by NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) (NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)에 의한 사람 중성구 Cathepsin G의 활성도 억제)

  • Bae, Sung-Jun;Ghim, Sa-Youl;Kang, Koo-Il
    • 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.

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Anti-inflammatory Effect of Leaves Extracts from Aralia cordata through Inhibition of NF-κB and MAPKs Signaling in LPS-stimulated RAW264.7 Cells

  • Ji, Eo Hyun;Kim, Da Som;Sim, Su Jin;Park, Gwang Hun;Song, Jeong Ho;Jeong, Jin Boo;Kim, Nahyun
    • Korean Journal of Plant Resources
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    • v.31 no.6
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    • pp.634-640
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    • 2018
  • Aralia cordata (A. cordata), which belongs to Araliaceae, is a perennial herb widely distributed in East Asia. We evaluated the anti-inflammatory effect of stems (AC-S), roots (AC-R) and leaves (AC-L) extracted with 100% methanol of A. cordata and elucidated the potential signaling pathway in LPS-stimulated RAW264.7 cells. The AC-L showed a strong anti-inflammatory activity through inhibition of NO production. AC-L dose-dependently inhibited NO production by suppressing iNOS, COX-2 and $IL-{\beta}$ expression in LPS-stimulated RAW264.7 cells. AC-L inhibited the degradation and phosphorylation of $I{\kappa}B-{\alpha}$, which donated to the inhibition of p65 nuclear accumulation and $NF-{\kappa}B$ activation. Furthermore, AC-L suppressed the phosphorylation of ERK1/2 and p38. These results suggested that AC-L may utilize anti-inflammatory activity by blocking $NF-{\kappa}B$ and MAPK signaling pathway and indicated that the AC-L can be used as a natural anti-inflammatory drugs.

MOLECULAR TARGETS IN SIGNALING PATHWAYS MEDIATING ANTI-TUMOR EFFECTS OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (NSAIDs)

  • Hwang, Daniel
    • 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)

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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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Quantum Chemical Analysis of Structure-Activity Relationships in Salicylic Acids as Anti-inflammatory Drugs (소염제로서의 살리씰산유도체의 구조-활성 상관관계에 관한 양자화학적 해석)

  • Rhee, Jong-Dal;Koo, Bon-Ki
    • YAKHAK HOEJI
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    • v.33 no.2
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    • pp.87-100
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    • 1989
  • Salicylic acids as anti-inflammatory agents were analyzed by ab initio, quantum chemical methods to study the possible modes of binding to the receptor. As the result of multiple regression analysis of reactivity indices and interpretation of normalized frontier orbital charges of drugs, potency seems to be related to energy of HOMO and LUMO at the 5 position of benzene ring, and in the 5-phenyl substituted case, the para position of substituting ring is important. The binding occurs first at the positive site of its receptor. The charge density exhibited by the frontier orbitals suggests that charge moves from receptor site to carboxyl group. The electrostatic orientation effect makes an important contribution to the binding of the active molecules to their receptors. Also the electrostatic potential model may be able to rationalize the source of activity or inactivity of the drugs under investigation.

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Flavonoid and Skin Inflammation

  • Kim, Hyun-Pyo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2007.11a
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    • pp.67-73
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    • 2007
  • There have been various inflammatory skin disorders in humans including atopic dermatitis, eczema and psoriasis. Although some drugs have been used for these disorders, there is an urgent need for safer and more effective topical anti-inflammatory agents. Plant flavonoids possess anti-inflammatory activity and some of them have multiple pharmacological mechanisms, inhibition of eicosanoid metabolizing enzymes, histamine release and/or down-regulation of pro inflammatory gene expression. These properties of flavonoids may be suitable for treating chronic skin inflammatory disorders. Especially, wogonin, some prenylated flavonoids and biflavonoids have a strong potential as new anti-inflammatory agents by topical application.

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Recent Advances in Anti-inflammatory Synthetic Flavonoids as Potential Drugs

  • Kim, Hyun-Pyo;Park, Hae-Il
    • Natural Product Sciences
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    • v.16 no.2
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    • pp.59-67
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    • 2010
  • Flavonoids are well-known anti-inflammatory agents that exert their effects via a variety of mechanisms including antioxidative action, inhibition of eicosanoid metabolizing enzymes and regulation of theexpression of proinflammatory molecules. In this review, synthetic approaches to obtain more useful flavonoid derivatives are summarized. Human clinical trials of flavonoid therapy are discussed. Through continual investigation to identify more potent and comparable flavonoids, new anti-inflammatory flavonoid therapy will be successfully launched, especially for the treatment of chronic inflammatory disorders.

All about pain pharmacology: what pain physicians should know

  • Kim, Kyung-Hoon;Seo, Hyo-Jung;Abdi, Salahadin;Huh, Billy
    • The Korean Journal of Pain
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    • v.33 no.2
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    • pp.108-120
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    • 2020
  • From the perspective of the definition of pain, pain can be divided into emotional and sensory components, which originate from potential and actual tissue damage, respectively. The pharmacologic treatment of the emotional pain component includes antianxiety drugs, antidepressants, and antipsychotics. The anti-anxiety drugs have anti-anxious, sedative, and somnolent effects. The antipsychotics are effective in patients with positive symptoms of psychosis. On the other hand, the sensory pain component can be divided into nociceptive and neuropathic pain. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioids are usually applied for somatic and visceral nociceptive pain, respectively; anticonvulsants and antidepressants are administered for the treatment of neuropathic pain with positive and negative symptoms, respectively. The NSAIDs, which inhibit the cyclo-oxygenase pathway, exhibit anti-inflammatory, antipyretic, and analgesic effects; however, they have a therapeutic ceiling. The adverse reactions (ADRs) of the NSAIDs include gastrointestinal problems, generalized edema, and increased bleeding tendency. The opioids, which bind to the opioid receptors, present an analgesic effect only, without anti-inflammatory, antipyretic, or ceiling effects. The ADRs of the opioids start from itching and nausea/vomiting to cardiovascular and respiratory depression, as well as constipation. The anticonvulsants include carbamazepine, related to sodium channel blockade, and gabapentin and pregabalin, related to calcium blockade. The antidepressants show their analgesic actions mainly through inhibiting the reuptake of serotonin or norepinephrine. Most drugs, except NSAIDs, need an updose titration period. The principle of polypharmacy for analgesia in case of mixed components of pain is increasing therapeutic effects while reducing ADRs, based on the origin of the pain.

Machine learning Anti-inflammatory Peptides Role in Recent Drug Discovery

  • Subathra Selvam
    • Journal of Integrative Natural Science
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    • v.17 no.1
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    • pp.21-30
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    • 2024
  • Several anti-inflammatory small molecules have been found in the process of the inflammatory response, and these small molecules have been used to treat some inflammatory and autoimmune diseases. Numerous tools for predicting anti-inflammatory peptides (AIPs) have emerged in recent years. However, conducting experimental validations in the lab is both resource-intensive and time-consuming. Current therapies for inflammatory and autoimmune disorders often involve nonspecific anti-inflammatory drugs and immunosuppressants, often with potential side effects. AIPs have been used in treating inflammatory illnesses like Alzheimer's disease and can limit the expression of inflammatory promoters. Recent advances in adverse incident predictions (AIPs) have been made, but it is crucial to acknowledge limitations and imperfections in existing methodologies.

Effect of Lower Abdomen Warmer on Primary Dysmenorrhea Patients Taking Nonsteroidal Anti-Inflammatory Drugs (비스테로이드성 소염진통제를 복용하는 원발성 월경곤란증 환자에 대한 하복부 온열찜질기의 효과)

  • Kim, Hyeong-Jun;Lee, Dong-Nyung;Ahn, Ha-Young
    • The Journal of Korean Obstetrics and Gynecology
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    • v.32 no.3
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    • pp.128-141
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    • 2019
  • Objectives: This study was performed to investigate the pain relief effect of lower abdomen warmer on primary dysmenorrhea patients taking nonsteroidal anti-inflammatory drugs and whether the using of warmer can supplement or replace the drugs. Methods: 30 women with primary dysmenorrhea were assigned to treatment group (n=15) and control group (n=15). At 1st visit, the treatment group was provided with a wirless multiuse warmer and trained to use at least three times per menstrual cycle. The control group was not provided with the warmer, and both groups were provided with a menstrual diary and instructed to record their pain intensity and dose of analgesic every menstrual period. Visual Analogue Scale (VAS) were used to assess the intensity of overall pain and the most severe pain during the menstrual period. And the total number of analgesic taken during menstruation and the average number of analgesic taken during a single dose were measured. Results: There was significant pain relief in the treatment group compared to before baseline, and there was a significant difference from the control group. In addition, there was no significant difference in the frequency of taking analgesic during the menstrual period between the treatment group and the control group, but the dose of analgesic was significantly lower in the treatment group than in the control group. Conclusions: This clinical trial showed that lower abdomen warmer would helpful in relieving primary dysmenorrhea and could help reduce the use of nonsteroidal anti-inflammatory drugs.