scholarly journals Evaluation of Anti-Inflammatory Activity of Pseudananas macrodontes (Morr.) Harms (Bromeliaceae) Fruit Extract in Rats

2013 ◽  
Vol 68 (11-12) ◽  
pp. 445-452 ◽  
Author(s):  
María E. Errasti ◽  
Néstor O. Caffini ◽  
Lilian E. Pelzer ◽  
Alejandra E. Rotelli
Keyword(s):  
Proteolytic Activity ◽  
Inflammatory Responses ◽  
Complementary Therapy ◽  
Ananas Comosus ◽  
Inflammatory Models ◽  
Rat Paw Edema ◽  
Cysteine Endopeptidases ◽  
Anti Inflammatory ◽  
Main Components ◽  
Inflammatory Action

Several species of the family Bromeliaceae are characterized by the production of proteases in unusual amounts, especially in fruits. Bromelain, an extract rich in cysteine endopeptidases obtained from Ananas comosus L., and a few other proteases have been used as anti-inflammatory agents for some years, but bromelain is still mainly being used as alternative and/or complementary therapy to the treatment with glucocorticoids, nonsteroidal antirheumatics, and immunomodulators. In this study, the anti-inflammatory action of a partially purified extract from Pseudananas macrodontes (Morr.) Harms fruits (PPEPm) is presented, whose main components are cysteine endopeptidases. The effect of PPEPm was assessed in carrageenan-induced and serotonin-induced rat paw edema, as well as in the cotton pellet granuloma model. Doses with equal proteolytic activity of PPEPm and bromelain produced significantly similar anti-inflammatory responses in the acute inflammatory models assayed, supporting the hypothesis that proteolytic activity could be responsible for the anti-inflammatory action. On the contrary, comparable anti-inflammatory effects of PPEPm and bromelain in the chronic inflammatory assay required a much lower proteolytic activity content of PPEPm, which could be due to a differential affinity for the protein target involved in this process.

In vitro and in vivo delivery of atorvastatin: A comparative study of anti-inflammatory activity of atorvastatin loaded copolymeric micelles

2017 ◽  
Vol 32 (8) ◽  
pp. 1127-1138 ◽  
Author(s):  
Sina Andalib ◽  
Pezhman Molhemazar ◽  
Hossein Danafar
Keyword(s):  
Inflammatory Responses ◽  
Inflammatory Activity ◽  
Lipid Lowering ◽  
Precipitation Method ◽  
Paw Edema ◽  
Scanning Calorimetry ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Statins have been shown to exert ‘pleiotropic effects’ independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)–poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles. The resulting micelles were characterized further by various techniques such as dynamic light scattering and atomic force microscopy. In this study the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles on acute models of inflammation are analyzed, to compare the effect of indometacin in rats. Carrageenan induces rat paw edema; six animals of each group (10 groups) received indometacin, atorvastatin, and atorvastatin/mPEG-PCL micelles orally 1, 6, 12 and 24 h before carrageenan injection in paw. The paw edema thickness measured at 1, 2, 3 and 4 h after injection and percentage inhibition of edema in various groups were calculated. The results showed that the zeta potential of micelles was about −16.6 mV and the average size was 81.7 nm. Atorvastatin was encapsulated into mPEG-PCL micelles with loading capacity of 14.60 ± 0.96% and encapsulation efficiency of 62.50 ± 0.84%. Atorvastatin and atorvastatin/mPEG-PCL micelles showed significant anti-inflammatory activity in the present study. The anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles was significant in comparison with indometacin. Atorvastatin/mPEG-PCL micelles showed more anti-inflammatory activity than atorvastatin. This study revealed the anti-inflammatory activity of atorvastatin and atorvastatin/mPEG-PCL micelles and suggested the statins have a potential inflammatory activity along with its lipid lowering properties. Contrary to anti-inflammatory effects, the pro-inflammatory responses are independent of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibition and can be mediated directly by atorvastatin.

scholarly journals Synthesis, Molecular Docking and Biological Properties of Novel Thiazolo[4,5-b]pyridine Derivatives

2020 ◽  
Vol 67 (4) ◽  
pp. 1035-1043
Author(s):  
Taras I. Chaban ◽  
Yulia E. Matiichuk ◽  
Olga Ya. Shyyka ◽  
Ihor G. Chaban ◽  
Volodymyr V. Ogurtsov ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Pharmacological Profile ◽  
Scavenging Effect ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Action

The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3H-thiazolo[4,5-b]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5-b]pyridin-2-ones were synthesized and modified at the N3, C5 and C6 positions of the main core in order to obtain the compounds with a satisfactory pharmacological profile. The synthesized compounds were preselected via molecular docking for further testing of their anti-inflammatory activity in vitro. Evaluation of novel compounds over the carageenin induced rat paw edema revealed strong anti-inflammatory action of some compounds including (thiazolo[4,5-b]pyridin-3(2H)-yl) propanenitrile (5) and thiazolo[4,5-b]pyridin-3(2H)-yl) propanoic acid (6) even exceeding the standard – Ibuprofen. The antioxidant activity of the synthesized compounds was measured in vitro by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals.

Anti-Inflammatory Activity of the Aqueous Extract of Ficus Deltoidea

2011 ◽  
Vol 14 (1) ◽  
pp. 90-97 ◽  
Author(s):  
Z. A. Zakaria ◽  
M. K. Hussain ◽  
A. S. Mohamad ◽  
F. C. Abdullah ◽  
M. R. Sulaiman
Keyword(s):  
Aqueous Extract ◽  
Formalin Test ◽  
Inflammatory Responses ◽  
Inflammatory Activity ◽  
Second Phase ◽  
Paw Edema ◽  
Ficus Deltoidea ◽  
Inflammatory Models ◽  
Study Results ◽  
Anti Inflammatory

Ficus deltoidea (Family Moraceae) leaves have been used traditionally by the Malays to treat ailments such as wounds, sores, and rheumatism. The aim of the present study was to determine the anti-inflammatory activity of the aqueous extract of F. deltoidea leaf (FDA) using acute and chronic inflammatory models. FDA, in the doses of 30, 100, and 300 mg/kg, was administered intraperitoneally in rats ( n = 6) before the animals were subjected to the carrageenan-induced paw edema test, cotton pellet-induced granuloma test, and formalin test. The first two tests represent acute and chronic models of inflammation, respectively. The first and second phases of the formalin test represent neurogenic pain and inflammatory-mediated pain, respectively; thus, only the second phase was measured in the present study. Results showed that FDA exerted significant ( p < .05) anti-inflammatory activity in all assays, with dose–response effects seen in the paw edema and formalin tests. In conclusion, the leaf of F. deltoidea possesses anti-inflammatory activity against acute and chronic inflammatory responses and against pain-associated inflammatory response. These findings justify the traditional uses of F. deltoidea leaves for treatment of inflammatory-mediated ailments.

scholarly journals ANTI-INFLAMMATORY PROFILING OF SEED AND RIND EXTRACTS OF AMOMUM SUBULATUM

2020 ◽  
pp. 204-208
Author(s):  
SUPRIYA AGNIHOTRI
Keyword(s):  
Inflammatory Activity ◽  
In Vivo Studies ◽  
Inflammatory Models ◽  
Rat Paw Edema ◽  
Soxhlet Apparatus ◽  
Anti Inflammatory ◽  
Amomum Subulatum ◽  
Rat Paw

Objective: The study aimed to evaluate the anti-inflammatory activity of Amomum subulatum (greater cardamom) seed and rind extracts in Wistar rats. Methods: The seed and rind of A. subulatum were air-dried in the shade, powdered, and subjected to 80% hydroalcoholic extraction in the Soxhlet apparatus. The anti-inflammatory activity of the seed and rind extracts of A. subulatum was evaluated by in vivo and in vitro methods. Results and Discussion: In vivo studies, namely, carrageenan-induced rat paw edema, cotton pellet granuloma, and formaldehyde-induced arthritis model confirmed the anti-inflammatory potential of seed and rind extracts of A. subulatum. It was found that rind extract exhibited better inhibition of inflammation as compared to seed extract. A. subulatum rind extract at the dose of 500 μg/ml exhibited best results for in vitro studies, namely, inhibition of albumin denaturation (73% inhibition), antiproteinase action (58% inhibition), membrane stabilization, heat-induced hemolysis, hypotonicity-induced hemolysis (54% inhibition), anti-lipoxygenase activity. Conclusions: The results of the study showed that the rind extract of A. subulatum (greater cardamom) possesses significant anti-inflammatory potential in various in vivo and in vitro anti-inflammatory models in the experimental animals.

scholarly journals Hoveniae Semen Seu Fructus Ethanol Extract Exhibits Anti-Inflammatory Activity via MAPK, AP-1, and STAT Signaling Pathways in LPS-Stimulated RAW 264.7 and Mouse Peritoneal Macrophages

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Yun Hee Jeong ◽  
You-Chang Oh ◽  
Won-Kyung Cho ◽  
Nam-Hui Yim ◽  
Jin Yeul Ma
Keyword(s):  
Signaling Pathways ◽  
Proinflammatory Cytokines ◽  
Inflammatory Responses ◽  
Peritoneal Macrophages ◽  
Inflammatory Activity ◽  
Raw 264.7 ◽  
Dependent Manner ◽  
Anti Inflammatory ◽  
Main Components ◽  
Mouse Peritoneal Macrophages

Hoveniae semen seu fructus (HSF, fruit and seed of Hovenia dulcis Thunb) is an important traditional herbal medicine and food supplement in East Asia for the treatment of liver diseases, alcohol poisoning, obesity, allergy, and cancer. HSF has also been reported to have anti-inflammatory activity, but the cellular mechanism of action is not fully understood. We assessed the anti-inflammatory properties of an HSF ethanol (HSFE) extract and explored its precise mechanism. The ability of HSFE to suppress inflammatory responses was investigated in a murine macrophage cell line, RAW 264.7, and mouse primary macrophages. Secretions of NO, proinflammatory cytokines, inflammatory factors, and related proteins were measured using the Griess assay, ELISA, Western blot analysis, and real-time PCR, respectively. In addition, the main components of HSFE were analyzed by HPLC, and their anti-inflammatory activity was confirmed. Our results showed that pretreatment of HSFE markedly reduced the expression of NO and iNOS without causing cytotoxicity and significantly attenuated secretion of proinflammatory cytokines, including TNF-α, IL-6, and IL-1β. In addition, HSFE strongly suppressed phosphorylation of MAPK and decreased the activation of AP-1, JAK2/STAT, and NF-κB in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner. Furthermore, HSFE strongly suppressed the inflammatory cytokine levels in mouse peritoneal macrophages. Also, as a result of HPLC analysis, three main components, ampelopsin, taxifolin, and myricetin, were identified in the HSFE extract, and each compound effectively inhibited the secretion of inflammatory mediators induced by LPS. These findings show that HSFE exerts anti-inflammatory effects by suppressing the activation of MAPK, AP-1, JAK2/STAT, and NF-κB signaling pathways in LPS-stimulated macrophages. In addition, the anti-inflammatory efficacy of HSFE appears to be closely related to the action of the three main components. Therefore, HSFE appears to be a promising candidate for the treatment of inflammatory diseases.

scholarly journals Molecular Targets Implicated in the Antiparasitic and Anti-Inflammatory Activity of the Phytochemical Curcumin in Trichomoniasis

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5321
Author(s):  
Natalia Mallo ◽  
Jesús Lamas ◽  
Rosa Ana Sueiro ◽  
José Manuel Leiro
Keyword(s):  
Proteolytic Activity ◽  
Inflammatory Mediators ◽  
Trichomonas Vaginalis ◽  
Inflammatory Responses ◽  
Transmitted Disease ◽  
No Production ◽  
Phagocytic Cells ◽  
Sexually Transmitted ◽  
Recommended Treatment ◽  
Anti Inflammatory

Trichomoniasis, is the most prevalent non-viral sexually transmitted disease worldwide. Although metronidazole (MDZ) is the recommended treatment, several strains of the parasite are resistant to MDZ, and new treatments are required. Curcumin (CUR) is a polyphenol with anti-inflammatory, antioxidant and antiparasitic properties. In this study, we evaluated the effects of CUR on two biochemical targets: on proteolytic activity and hydrogenosomal metabolism in Trichomonas vaginalis. We also investigated the role of CUR on pro-inflammatory responses induced in RAW 264.7 phagocytic cells by parasite proteinases on pro-inflammatory mediators such as the nitric oxide (NO), tumor necrosis factor α (TNFα), interleukin-1beta (IL-1β), chaperone heat shock protein 70 (Hsp70) and glucocorticoid receptor (mGR). CUR inhibited the growth of T. vaginalis trophozoites, with an IC50 value between 117 ± 7 μM and 173 ± 15 μM, depending on the culture phase. CUR increased pyruvate:ferredoxin oxidoreductase (PfoD), hydrogenosomal enzyme expression and inhibited the proteolytic activity of parasite proteinases. CUR also inhibited NO production and decreased the expression of pro-inflammatory mediators in macrophages. The findings demonstrate the potential usefulness of CUR as an antiparasitic and anti-inflammatory treatment for trichomoniasis. It could be used to control the disease and mitigate the associated immunopathogenic effects.

scholarly journals Antiplatelet Aggregation, Cardiotonic, Anti-Inflammatory, Antioxidant, and Calcium Channel Antagonistic Potentials of Nepeta ruderalis Buch

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Ambreen Aleem ◽  
Khalid Hussain Janbaz ◽  
Imran Imran ◽  
Muqeet Wahid ◽  
Sumbal Bibi ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Inflammatory Responses ◽  
Radical Scavenging ◽  
Paw Edema ◽  
Traditional System ◽  
Antiplatelet Aggregation ◽  
Rat Paw Edema ◽  
Rabbit Jejunum ◽  
Anti Inflammatory ◽  
Rat Paw

The objective of this study was to authenticate the ethnobotanical claims of the Nepeta ruderalis Buch.-Ham. (N. ruderalis) extract in the traditional system of medicine. Crude extract was prepared via a simple maceration process. DPPH free radical scavenging and carrageenan-induced rat paw edema models were used to monitor antioxidant and anti-inflammatory responses of the N. ruderalis extract. Furthermore, it was tested for antiplatelet aggregation, cardioprotective, and calcium channel antagonistic activities via standard documented protocols. The N. ruderalis extract exhibited 80.82% antioxidant activity (IC50=207.51±4.36 μg) while the anti-inflammatory response was significant (p<0.05 to p<0.01) at 50 mg/kg (45.58%) and 100 mg/kg (60.90%) doses. Moreover, it was found to inhibit platelet aggregation (IC50=1.06 and 0.91 mg/mL) and, in addition, to increase the force of contraction at the concentration of 3.0-10 mg/mL with a decrease in the heart rate on isolated paired atria (EC50=11.78 mg/mL). Relaxant activity was observed on the isolated rabbit jejunum (EC50=0.96 mg/mL) and trachea (EC50=0.89 mg/mL). However, in a cumulative way, an 80-millimolar potassium-induced contraction was evaluated (EC50=1.31 mg/mL). The N. ruderalis extract exhibited antioxidant, anti-inflammatory, platelet aggregating, cardiotonic, and calcium channel antagonistic activities, therefore proving scientifically its effectiveness in the traditional system of medicine.

scholarly journals Anti-inflammatory properties of some novel thiazolo[4,5-b]pyridin-2-ones

Pharmacia ◽  
2020 ◽  
Vol 67 (3) ◽  
pp. 121-127
Author(s):  
Taras Chaban ◽  
Vasyl Matiychuk ◽  
Olexandra Komarytsya ◽  
Iryna Myrko ◽  
Ihor Chaban ◽  
...  
Keyword(s):  
Nmr Spectroscopy ◽  
Elemental Analysis ◽  
Paw Edema ◽  
H Nmr ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Alkylation Reactions ◽  
Rat Paw ◽  
Inflammatory Action

Synthesis of novel N3 and C5 substituted thiazolo[4,5-b]pyridin-2-ones was carried out on the basis of [3+3]-cyclocodensation, acylation and alkylation reactions. The structures of the obtained compounds were confirmed by 1H NMR spectroscopy, and elemental analysis. The anti-inflammatory action of novel thiazolo[4,5-b]pyridine-2-one derivatives was evaluated in vivo employing the carrageenan-induced rat paw edema method. When compared with Ibuprofen, some our compounds were found to be more potent. Graphical abstract

scholarly journals ANTI-INFLAMMATORY EFFECTS OF PROPOXAZEPAM ON DIFFERENT MODELS OF INFLAMMATION

2020 ◽  
Vol 5 (2) ◽  
pp. 105-112 ◽  
Author(s):  
N. Ya. Golovenko ◽  
T. A. Kabanova ◽  
S. A. Andronati ◽  
O. I. Halimova ◽  
V. B. Larionov ◽  
...  
Keyword(s):  
Acute Inflammation ◽  
Experimental Models ◽  
Paw Edema ◽  
Preclinical Trial ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
First Time ◽  
Inflammatory Action

Background. Propoxazepam, 7-bromo-5-(2-chlorophenyl)-3-propoxy-1H-benzo[e][1,4]diazepin-2(3H)-one, is a promising analgesic and anticonvulsant and is on preclinical trial. Objective. The aim of the research was to study the anti-inflammatory and analgesic action of Propoxazepam. Methods. The anti-inflammatory action was evaluated by carrageenan induced rat paw edema, formalin-induced paw licking response in mice and bradykinin-induced pain response in rat models. Results. It was established for the first time that the administration of Propoxazepam caused a significant anti-inflammatory activity when tested in different in vivo chemical experimental models of induced inflammation, i.e. carrageenan-, bradykinin- and formalin-induced inflammation tests. Conclusions. Propoxazepam significantly reduced acute and sub-acute inflammation and proved its efficacy and similar to anti-inflammatory action.

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