scholarly journals Biological Evaluation of Azetidine-2-One Derivatives of Ferulic Acid as Promising Anti-Inflammatory Agents

Processes ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 1401
Author(s):  
Maria Drăgan ◽  
Cătălina Daniela Stan ◽  
Andreea Teodora Iacob ◽  
Oana Maria Dragostin ◽  
Mihaela Boancă ◽  
...  
Keyword(s):  
Ferulic Acid ◽  
Chronic Inflammation ◽  
Acute Inflammation ◽  
Liver Enzymes ◽  
Biological Evaluation ◽  
Control Group ◽  
Inflammation Model ◽  
Anti Inflammatory ◽  
Derivatives Of

The purpose of this study was to evaluate the in vivo biological potential of new azetidine-2-one derivatives of ferulic acid (6a–f). First, the in vivo acute toxicity of azetidine-2-one derivatives of ferulic acid on Swiss white mice was investigated and, based on the obtained results, it can be stated that the studied derivatives belong to compounds with moderate toxicity. The in vivo anti-inflammatory potential of these derivatives was determined in a model of acute inflammation induced by carrageenan in rats and in a chronic inflammation model induced in rats using the granuloma test. In the acute inflammation model, all the studied compounds had a maximum anti-inflammatory effect 24 h after administration, which suggests that these compounds may be classified, from a pharmacokinetic point of view, in the category of long-acting compounds. The most active compound in the series was found to be compound 6b. In the case of the chronic inflammation model, it was observed that the studied compounds (6a–f) reduced the formation of granulation tissue compared to the control group, having an intense effect of inhibiting the proliferative component. The most important inhibitory effect of inhibiting the proliferative component was recorded for compound 6b. Additionally, the investigation of liver function was performed by determining the serum levels of liver enzymes aspartate transaminase (AST), alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and bilirubin (total and direct). The results showed that, in the series of azetidin-2-one derivatives, the liver enzymes concentration values were close to those recorded for the reference anti-inflammatories (diclofenac sodium and indomethacin) and slightly higher compared to the values for the healthy control group. At the end of the experiment, the animals were euthanized and fragments of liver, lung, and kidney tissue were taken from all groups in the study. These were processed for histopathological examination, and we noticed no major changes in the groups treated with the azetidine 2-one derivatives of ferulic acid compared to the healthy groups.

scholarly journals SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW NAPROXEN ANALOGUES HAVING 1, 2, 4-TRIAZOLE-3-THIOL

2017 ◽  
Vol 9 (7) ◽  
pp. 66
Author(s):  
Monther F. Mahdi ◽  
Noor H. Naser ◽  
Nethal H. Hammud
Keyword(s):  
Aromatic Aldehydes ◽  
Heterocyclic Ring ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Dose Equivalent ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: The objective of this search was to synthesize a new naproxen analogues having a 1,2,4-triazole-3-thiol heterocyclic ring, and preliminary pharmacological assessment of the anti-inflammatory activity of the synthesized compounds. Methods: The synthesis of naproxen analogues that having 1,2,4-triazole-3-thiol heterocyclic ring occur through esterification of naproxen, and then its reaction with hydrazine hydrate, and carbon disulfide, finally different aromatic aldehydes reacted with triazole derivatives of naproxen containing amino group to produce schiff bases.Results: In vivo acute anti-inflammatory activity of the synthesize compounds (Va-Vd) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (50 mg/kg) of naproxen. All tested compounds were produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Compound Vd produced superior anti-inflammatory activity compared to naproxen.Conclusion: The results obtained in this work give evidence about the valid synthesis of 1,2,4 triazole-3-thiol derivatives of naproxen, which reacted with different aldehydes to yield several schiff bases. The incorporation of benzaldehyde possess para-electron donating group (para-hydroxyl benzaldehyde) will increase the anti-inflammatory activity of naproxen.

scholarly journals Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-Inflammatory and Analgesic Agents. Synthesis and in Vitro and in Vivo Biological Evaluation

2010 ◽  
Vol 53 (2) ◽  
pp. 723-733 ◽  
Author(s):  
Mariangela Biava ◽  
Giulio C. Porretta ◽  
Giovanna Poce ◽  
Claudio Battilocchio ◽  
Fabrizio Manetti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Derivatives Of

ANTI-IFLAMMATORY EFFECTS OF GRANULES OF TIEN LIET THANH GIAI ON EXPERIMENTAL ANIMAL MODELS

2016 ◽  
pp. 81-87
Author(s):  
Thi Phuong Quynh Nguyen ◽  
Thi Ngoc Thanh Vu ◽  
Thi Tan Nguyen
Keyword(s):  
Animal Models ◽  
Key Words ◽  
Chronic Inflammation ◽  
Experimental Animal ◽  
Control Group ◽  
Group Key ◽  
Experimental Animal Models ◽  
Inflammation Model ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Acute and chronic anti-inflammatory effects of granules of Tien liet thanh giai were evaluated. For acute anti-inflammatory effect, granules of Tien liet thanh giai didn’t change the test indicators. In the chronic inflammation model, granules of Tien liet thanh giai remarkably provoked chronic anti-inflammatory effect through significantly decreasing granuloma weight as compared with the control group. key words: granules of Tien liet thanh giai, acute anti-inflammatory effect, chronic anti-inflammatory effect.

scholarly journals In Vivo Evaluation of Anti-inflammatory Activity of 2-[3-Acetyl- 5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanylbutyric Acid

Folia Medica ◽  
2018 ◽  
Vol 60 (2) ◽  
pp. 270-274
Author(s):  
Hristina Zlatanova ◽  
Stanislava Vladimirova ◽  
Ilia Kostadinov ◽  
Atanas T. Bijev
Keyword(s):  
Chronic Inflammation ◽  
Butyric Acid ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
In Vivo Evaluation ◽  
Continuous Administration ◽  
Inflammation Model ◽  
Anti Inflammatory ◽  
Acid Compound

Abstract Background: Persisting inflammatory stimuli cause chronic inflammation recognized as the major factor contributing to the development of a number of diseases. One group of drugs used in the treatment of chronic inflammation is the group of non-steroidal anti-inflammatory drugs and, more specifically, the selective COX-2 inhibitors (coxibs). However, most of the coxibs were withdrawn from the market in view of their safety profile. In the present study, 2-[3-Acetyl-5-(4-chlorophenyl)- 2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e), an Npyrrolylcarboxylic acid derivative structurally related to celecoxib, is evaluated for anti-inflammatory activity after single and multiple (14 days) administration using an animal inflammation model. Aim: To evaluate the anti-inflammatory properties of 2-[3-Acetyl-5-(4-chlorophenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e) after single and multiple (14 days) administration using an animal inflammation model. Materials and methods: Forty Wistar rats were allocated into 5 groups (n=8) treated with saline (controls), diclofenac (25 mg/kg b.w.), compound 3e (10, 20 and 40 mg/kg b.w.) intraperitoneally. The volume of the right hind paw of the animals of all groups is measured prior to treatment and two, three and four hours after administration of carrageenan using a plethysmometer (Ugo Basile, Italy). The percentage of paw edema is calculated using the Trinus formula. Results: In a single administration, compound 3e in doses of 10 and 20 mg/kg b.w. did not inhibit paw edema, while a dose of 40 mg/kg b.w. significantly inhibited carrageenan-induced paw edema at 2 hours in comparison with the control group. After continuous administration, compound 3e in doses of 10, 20 and 40 mg/kg b.w. significantly reduced paw edema at 2, 3, and 4 hours compared to animals treated with saline. Conclusions: Compound 3e shows anti-inflammatory properties similar to those of diclofenac after continuous administration.

scholarly journals Spearmint (Mentha spicata L.) essential oil from tipaza (Algeria): in vivo anti-inflammatory and analgesic activities in experimental animal models

2020 ◽  
Vol 90 (1) ◽  
pp. 15-26
Author(s):  
Sarah Kehili ◽  
Mohamed Amine Boukhatem ◽  
Asma Belkadi ◽  
Faiza Boulaghmen ◽  
Mohamed Amine Ferhat ◽  
...  
Keyword(s):  
Essential Oil ◽  
Acute Inflammation ◽  
Kidney Injury ◽  
Topical Administration ◽  
Positive Control ◽  
Control Group ◽  
Mentha Spicata ◽  
Ear Edema ◽  
Anti Inflammatory

Introduction Although analgesic and nonsteroidal anti-inflammatory drugs (NSAIDs) are usually used to treat a diversity of illnesses, their administration is linked with acute kidney injury and gastrointestinal side effects. The research of new biomolecules and natural products is still needed such as medicinal plants. Aims The present research was aimed to investigate, for the first time, the anti-inflammatory and anti-nociceptive effects of spearmint essential oil (SEO) in mouse models of acute inflammation and pain. Materials and Method Chemical analysis of SEO was done by gas chromatography. The anti-inflammatory activity was tested using two models of acute inflammation namely carrageenan-induced paw edema and xylene-induced ear edema. Histological examination of both non-inflamed and inflamed tissues was evaluated. The anti-nociceptive activity was tested using the pain model induced by acetic acid. Results The main constituent of the SEO was found to be carvone (52.60%). The SEO exhibited a promising anti-inflammatory effect as demonstrated by statistically significant (p<0.05) inhibition of paw volume by 77.24% at the dose of 20 µL/kg and 65.87% at the dose of 200 µL/kg. Furthermore, topical administration of the SEO inhibited xylene-induced ear edema in comparison with the control group (p<0.05). The higher dose (200 µL /kg) significantly (p<0.001) reduced xylene-induced ear edema which was similar to that observed with positive control (ketoprofen). The pathological analysis of the paws and ears revealed that SEO was capable of reducing cellular infiltration and subcutaneous edema. Else, the SEO produced significant anti-nociceptive activity (p<0.001) at higher dose by inhibiting spontaneous nociception. Conclusion These results support the use of SEO in the development of pharmaceuticals for the management of inflammation and pain.

Jobelyn® exhibited anti-inflammatory, antioxidant, and membrane-stabilizing activities in experimental models

2015 ◽  
Vol 26 (5) ◽  
Author(s):  
Solomon Umukoro ◽  
Oluwafemi Gabriel Oluwole ◽  
Anthony T. Eduviere ◽  
Omogbiya Itievere Adrian ◽  
Abayomi M. Ajayi
Keyword(s):  
Chronic Inflammation ◽  
Acute Inflammation ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Experimental Models ◽  
Hypotonic Medium ◽  
Air Pouch ◽  
Anti Inflammatory ◽  
Air Pouch Model

AbstractJobelynAcute inflammation was induced with intraplanter injection of carrageenan and increase in rat paw volume was measured using plethysmometer. The volume of fluid exudates, number of leukocytes, concentrations of malondialdehyde (MDA), and glutathione (GSH) in the fluid were measured on day 5 after induction of chronic inflammation with carrageenan in the granuloma air pouch model. RBC lysis induced by hypotonic medium as determined by release of hemoglobin was measured spectrophotometerically.JB (50–200 mg/kg) given orally produced a significant inhibition of acute inflammation induced by carrageenan in rats. It reduced the volume and number of leukocytes in inflammatory fluid in the granuloma air pouch model of chronic inflammation. It further decreased the levels of MDA in the fluid suggesting antioxidant property. JB elevated the concentrations of GSH in inflammatory exudates indicating free radical scavenging activity. It also significantly inhibited RBC lysis caused by hypotonic medium, suggesting membrane-stabilizing property.JB has in vivo anti-inflammatory activity, which may be related to its antioxidant and membrane-stabilizing properties, supporting its use for the treatment of arthritic disorder.

scholarly journals Farnesol-Loaded Liposomes Protect the Epidermis and Dermis from PM2.5-Induced Cutaneous Injury

2021 ◽  
Vol 22 (11) ◽  
pp. 6076
Author(s):  
Yu-Chiuan Wu ◽  
Wei-Yun Chen ◽  
Chun-Yin Chen ◽  
Sheng I. Lee ◽  
Yu-Wen Wang ◽  
...  
Keyword(s):  
Chronic Inflammation ◽  
Water Solubility ◽  
Antibacterial Properties ◽  
Hair Follicles ◽  
Protective Effects ◽  
Cutaneous Injury ◽  
Anti Inflammatory ◽  
High Concentrations ◽  
Acute And Chronic Inflammation

Particulate matter with aerodynamic diameter ≤2.5 μm (PM2.5) increases oxidative stress through free radical generation and incomplete volatilization. In addition to affecting the respiratory system, PM2.5 causes aging- and inflammation-related damage to skin. Farnesol (Farn), a natural benzyl semiterpene, possesses anti-inflammatory, antioxidative, and antibacterial properties. However, because of its poor water solubility and cytotoxicity at high concentrations, the biomedical applications of Farn have been limited. This study examined the deleterious effects of PM2.5 on the epidermis and dermis. In addition, Farn-encapsulated liposomes (Lipo-Farn) and gelatin/HA/xanthan gel containing Lipo-Farn were prepared and applied in vivo to repair and alleviate PM2.5-induced damage and inflammation in skin. The prepared Lipo-Farn was 342 ± 90 nm in diameter with an encapsulation rate of 69%; the encapsulation significantly reduced the cytotoxicity of Farn. Lipo-Farn exhibited a slow-release rate of 35% after 192 h of incubation. The half-maximal inhibitory concentration of PM2.5 was approximately 850 μg/mL, and ≥400 μg/mL PM2.5 significantly increased IL-6 production in skin fibroblasts. Severe impairment in the epidermis and hair follicles and moderate impairment in the dermis were found in the groups treated with post-PM2.5 and continuous subcutaneous injection of PM2.5. Acute and chronic inflammation was observed in the skin in both experimental categories in vivo. Treatment with 4 mM Lipo-Farn largely repaired PM2.5-induced injury in the epidermis and dermis, restored injured hair follicles, and alleviated acute and chronic inflammation induced by PM2.5 in rat skin. In addition, treatment with 4 mM pure Farn and 2 mM Lipo-Farn exerted moderate reparative and anti-inflammatory effects on impaired skin. The findings of the current study indicate the therapeutic and protective effects of Lipo-Farn against various injuries caused by PM2.5 in the pilosebaceous units, epidermis, and dermis of skin.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

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