Local Anti-inflammatory Activity and Systemic Side Effects of NM-135, a New Prodrug Glucocorticoid, in an Experimental Inflammatory Rat Model

The incidence and prevalence of inflammatory bowel disorders (IBD) are increasing around the world due to bacterial infection, abnormal immune response, etc. The conventional medicines for IBD treatment possess serious side effects. Periplaneta americana (P. americana), a traditional Chinese medicine, has been used to treat arthritis, fever, aches, inflammation, and other diseases. This study aimed to evaluate the anti-inflammatory effects of oligosaccharides from P. Americana (OPA) and its possible mechanisms in vivo. OPA were purified and biochemical characterization was analyzed by HPGPC, HPLC, FT-IR, and GC–MS. Acute colitis mice model was established, the acute toxicity and anti-inflammatory activity were tested in vivo. The results showed OPA with molecular mass of 1.0 kDa were composed of 83% glucose, 6% galactose, 11% xylose, and the backbone was (1→4)-Glcp. OPA had potent antioxidant activities in vitro and significantly alleviated the clinical symptoms of colitis, relieved colon damage without toxic side effects in vivo. OPA exhibited anti-inflammatory activity by regulating Th1/Th2, reducing oxidative stress, preserving intestinal barrier integrity, and inhibiting TLR4/MAPK/NF-κB pathway. Moreover, OPA protected gut by increasing microbial diversity and beneficial bacteria, and reducing pathogenic bacteria in feces. OPA might be the candidate of complementary and alternative medicines of IBD with low-cost and high safety.

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VSL#3 probiotics exerts the anti-inflammatory activity via PI3k/Akt and NF-κB pathway in rat model of DSS-induced colitis

Molecular and Cellular Biochemistry ◽

10.1007/s11010-012-1488-3 ◽

2012 ◽

Vol 374 (1-2) ◽

pp. 1-11 ◽

Cited By ~ 78

Author(s):

Cong Dai ◽

Chang-Qing Zheng ◽

Fan-ji Meng ◽

Zheng Zhou ◽

Li-xuan Sang ◽

...

Keyword(s):

Rat Model ◽

Inflammatory Activity ◽

Anti Inflammatory

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Design, Synthesis and Anti-inflammatory Activity of Structurally Simple Anthranilic Acid Congeners Devoid of Ulcerogenic Side Effects

Chemical and Pharmaceutical Bulletin ◽

10.1248/cpb.c12-00516 ◽

2012 ◽

Vol 60 (10) ◽

pp. 1290-1300 ◽

Cited By ~ 6

Author(s):

Amal Abdel Haleem Mohamed Eissa ◽

Gamal Abd El-Hakeem Soliman ◽

Moayad Hussein Khataibeh

Keyword(s):

Side Effects ◽

Anthranilic Acid ◽

Inflammatory Activity ◽

Design Synthesis ◽

Anti Inflammatory

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Preliminary Analysis of the Anti-Inflammatory Activity of Essential Oils of Zingiber zerumbet

Biological Research For Nursing ◽

10.1177/1099800410386590 ◽

2010 ◽

Vol 13 (4) ◽

pp. 425-432 ◽

Cited By ~ 9

Author(s):

Z. A. Zakaria ◽

A. S. Mohamad ◽

M. S. Ahmad ◽

A. F. Mokhtar ◽

D. A. Israf ◽

...

Keyword(s):

Side Effects ◽

Essential Oil ◽

Preliminary Analysis ◽

Formalin Test ◽

Inflammatory Activity ◽

Paw Edema ◽

Zingiber Zerumbet ◽

Cotton Pellet ◽

Inflammatory Drugs ◽

Anti Inflammatory

Nonsteroidal anti-inflammatory drugs (NSAIDs) have been widely used for the treatment of inflammation. However, despite their effectiveness, most NSAIDs cause various side effects that negatively affect the management of inflammation and, in part, pain. Thus, there is a need to search for new anti-inflammatory agents with few, or no, side effects. Natural products of plant, animal, or microorganism origin have been good sources of new bioactive compounds. The present study was carried out to evaluate the acute and chronic anti-inflammatory activities of the essential oil of the rhizomes of Zingiber zerumbet (Zingiberaceae) using the carrageenan-induced paw edema and cotton pellet-induced granuloma tests, respectively. The effect of the essential oil on inflammatory- and noninflammatory-mediated pain was also assessed using the formalin test. Essential oil of Z. zerumbet, at doses of 30, 100, and 300 mg/kg, was administered intraperitoneally to rats. The substance exhibited significant anti-inflammatory activity both in acute and chronic animal models. The essential oil also inhibited inflammatory- and noninflammatory-mediated pain when assessed using the formalin test. In conclusion, the essential oil of Z. zerumbet possessed anti-inflammatory activity, in addition to its antinociceptive activity, which may explain its traditional uses to treat inflammatory-related ailments.

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Synthesis, Anti-Inflammatory Activity and Molecular Docking Studies of 1,4,5,6-Tetrahydropyrimidine-2-Carboxamides

Pharmaceutical Sciences ◽

10.34172/ps.2020.100 ◽

2020 ◽

Vol 27 (3) ◽

pp. 353-365

Author(s):

Volodymyr Ya. Horishny ◽

Pavlo V. Zadorozhnii ◽

Ivanna V. Horishnia ◽

Vasyl S. Matiychuk

Keyword(s):

Molecular Docking ◽

Side Effects ◽

Docking Studies ◽

Inflammatory Activity ◽

Cox Inhibitors ◽

White Rats ◽

Urgent Task ◽

Inflammatory Drugs ◽

Anti Inflammatory

Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in the world. The widespread use of NSAIDs is associated with a number of serious side effects and complications observed for both selective and non-selective COX inhibitors. Therefore, the search for new COX inhibitors, which along with their effectiveness will have minimal side effects, is a very important and urgent task. Methods: This work studied the synthesis of new 1,4,5,6-tetrahydropyrimidine-2-carboxamides based on the reaction of 2-morpholin-4-yl-N-(het)aryl-2-thioxoacetamides with 1,3-diaminopropane. All obtained compounds were tested for anti-inflammatory activity in vitro and in silico conditions. All synthesized 1,4,5,6-tetrahydropyrimidine-2-carboxamides were tested for influence on the course of the exudative phase of the inflammatory process based on the carrageenan model of paw edema of laboratory nonlinear heterosexual white rats weighing 220-250 g, using Diclofenac as a reference. Optimization of the geometry of the studied structures and molecular docking was carried out using the ArgusLab 4.0.1 software package. Results: The target products were obtained with yields of 71-98% and easily isolated from the reaction mixture. The best anti-inflammatory activity was found in N-(4-chlorophenyl)-1,4,5,6-tetrahydropyrimidine-2-carboxamide and in N-[4-chloro-3-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydropyrimidine-2-carboxamide, suppression of the inflammatory response was 46.7 and 46.4%, respectively. The results of molecular docking with COX-1 and COX-2 enzymes were in good agreement with the experimental data, R2 ˃ 0.92 and R2 ˃ 0.83, respectively. Conclusion: The compounds under study were shown to be promising as potential anti-inflammatory agents.

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Topical capsaicin versus topical ibuprofen in acute musculoskeletal injuries: A randomized, double-blind trial

Hong Kong Journal of Emergency Medicine ◽

10.1177/1024907920975368 ◽

2020 ◽

pp. 102490792097536

Author(s):

Sultan Tuna Akgol Gur ◽

Sinem Dogruyol ◽

Abdullah Osman Kocak ◽

Tugba Sanalp Menekse ◽

Ilker Akbas ◽

...

Keyword(s):

Emergency Department ◽

Side Effects ◽

Confidence Interval ◽

Visual Analog Scale ◽

Musculoskeletal Injuries ◽

Analog Scale ◽

Scale Scores ◽

Systemic Side Effects ◽

Anti Inflammatory ◽

Topical Capsaicin

Background: Acute musculoskeletal pain is one of the common causes of emergency admissions. Topical analgesics are an easily tolerated option in the treatment of these pains. Objective: This study aimed to compare the efficacy of topical capsaicin and topical non-steroidal anti-inflammatory drugs in acute musculoskeletal injuries. Methods: In this prospective, randomized, controlled, double-blinded study, patients were allocated to two groups—the topical non-steroidal anti-inflammatory drug (n = 60) and topical capsaicin (n = 59). For both groups, the first dose treatment was applied as a thin layer in the emergency department to a maximum area of 5 × 5 cm. The remaining doses were administered at home by the patients for 72 h. The initial visual analog scale scores were compared with the 60th and 120th minute as well as the 24th and 72nd hour values. Differences between the visual analog scale scores, clinical response to the treatment, and side effects were evaluated. Results: The proportional reduction in visual analog scale scores for topical capsaicin was significantly higher, especially at 36 and 72 h. These rates were 0.75 (95% confidence interval: 0.77–1.42; p = 0.029) and 9.08 (95% confidence interval: 1.02–17.14; p = 0.028) at 36 h, respectively. At 72 h, they were 1.27 (95% confidence interval: 0.48–2.05; p = 0.002) and 17.07 (95% confidence interval: 8.39–25.76; p < 0.001), respectively. In the topical capsaicin group, the clinical response to treatment was significantly higher (p = 0.001). Treatment-related systemic side effects were experienced only in the topical non-steroidal anti-inflammatory drug group (1.7%). Conclusion: Topical capsaicin can be used safely in patients presenting to the emergency department with acute pain with its high analgesic efficacy and absence of systemic side effects.

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