Antiinflamm Antiallergy Agents Med Chem [JOURNAL]
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200 papers
New Anti-inflammatory Triterpene Esters and Glycosides from Alstonia scholaris.
Sultana N, Qazi MS, Kamal M
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31339078 · Publisher ↗
BACKGROUND: Phytochemical studies on the ethanolic extract of aerial parts of Alstonia scholaris lead to the isolation of two new triterpenoid of the lanostanetype, lanosta 5ene,24-ethyl-3-O-β-D-glucopyranoside (1), lano...
BACKGROUND: Phytochemical studies on the ethanolic extract of aerial parts of Alstonia scholaris lead to the isolation of two new triterpenoid of the lanostanetype, lanosta 5ene,24-ethyl-3-O-β-D-glucopyranoside (1), lanosta,5ene,24-ethyl-3-O-β-D-glucopyranosideester (2) and new ursane type triterpenoidmethylester, 12-ursene-2,3,18,19-tetrol,28 acetate (nighascholarene) (3), together with seven known triterpenes, betuline, triterpene of the lupane type, alstoprenyol (4), 3β-hydroxy-28-β-acetoxy-5-olea triterpene (5),α-amyrin acetate (6), α-amyrin (7), lupeol acetate (8), 3β-hydroxy-24-nor-urs-4,12,28-triene triterpene (9) and ursolic acid (l0). METHODOLOGY: The triterpenoid structures of these colorless compounds were deduced from the 1H and 13C-NMR data, and in particular from the application of two-dimensional 1H, 13C correlation experiments as well as by comparison with reported literature data. CONCLUSION: This study deals with isolation and structural elucidation of natural new triterpenoidesters and glycosides with anti-inflammatory activity.
Psoralen Derivatives: Recent Advances of Synthetic Strategy and Pharmacological Properties.
Jamalis J, Yusof FSM, Chander S … +5 more , Wahab RA, P Bhagwat D, Sankaranarayanan M, Almalki F, Hadda TB
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31241020 · Full text
Psoralen or furocoumarin is a linear three ring heterocyclic compound. Psoralens are planar, tricyclic compounds, consisting of a furan ring fused to a coumarin moiety. Psoralen has been known for a wide spectrum of biol...
Psoralen or furocoumarin is a linear three ring heterocyclic compound. Psoralens are planar, tricyclic compounds, consisting of a furan ring fused to a coumarin moiety. Psoralen has been known for a wide spectrum of biological activities, spanning from cytotoxic, photosensitizing, insecticidal, antibacterial to antifungal effect. Thus, several structural changes were introduced to explore the role of specific positions with respect to the biological activity. Convenient approaches utilized for the synthesis of psoralen skeleton can be categorized into two parts: (i) the preparation of the tricyclic ring system from resorcinol, (ii) the exocyclic modification of the intact ring system. Furthermore, although psoralens have been used in diverse ways, we mainly focus in this work on their clinical utility for the treatment of psioraisis, vitiligo and skin-related disorder.
Comparative Evaluation of Colon Cancer Specific Antigen-2 Test and Chromocolonoscopy for Early Detection of Egyptian Patients with Colorectal Cancer.
Elhossary M, Hawash N, Badawi R … +7 more , Yousef M, Abd-Elsalam S, Elhendawy M, Wasfy R, Abou-Saif S, ElBendary A, Ismail S
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31241019 · Full text
BACKGROUND: Effective screening of colorectal cancer (CRC) in early stage could reduce the advancement of CRC and therefore mortality. Effective screening is based on either stool dependent tests or colon dependent exami...
BACKGROUND: Effective screening of colorectal cancer (CRC) in early stage could reduce the advancement of CRC and therefore mortality. Effective screening is based on either stool dependent tests or colon dependent examination. AIMS: The aim of the study was a comparative evaluation of chromocolonoscopy and Colon Cancer-Specific Antigen-2 test for early detection of colorectal cancer in Egyptian patients. METHODS: This case control study was carried out on 55 patients classified into 3 groups: Group I consisted of twenty patients with precancerous lesions detected by colonoscopy, Group II consisted of twenty patients diagnosed with colorectal cancer and Group III consisted of fifteen individuals (who underwent colonoscopy for other indications) as a control group. All the subjects were subjected to measure occult blood in the stool, measurement of Colon Cancer-Specific Antigen-2 level in serum and tissue and chromo colonoscopy using Indigo Carmine stain. RESULTS: In group II, there was a statistically significant increase in CCSA2 in serum as compared to the other 2 groups. Cutoff >11.3 CCSA2 in serum showed 65% sensitivity, 85% specificity, 81.2% PPV, 70.8% NPV and 70.3% accuracy in the differentiation of group II with cancer colon from group I with premalignant colonic lesions. A cutoff > 9.1 CCSA2 in serum showed 95% sensitivity, 46.67% specificity, 70.4% PPV, 87.5% NPV and 73.5% accuracy in differentiating group II with cancer colon from normal controls (group III). CONCLUSION: CCSA-2 level in serum was significantly higher in cancer colon. Chromoendoscopy has a role in the detection of polyps, both neoplastic and non-neoplastic.
Omalizumab for the Treatment of Persistent Drug Induced Urticaria Elicited by Thienopyridines: A Case Report.
Calogiuri G, Nettis E, Mandurino-Mirizzi A … +5 more , Di Leo E, Macchia L, Foti C, Vacca A, Kounis NG
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31113348 · Publisher ↗
The anti-IgE Omalizumab may be helpful to treat clopidogrel hypersensitivity without stopping thienopyridine administration in patients requirining continuous antiplatellet therapy after coronary stent placement.
The anti-IgE Omalizumab may be helpful to treat clopidogrel hypersensitivity without stopping thienopyridine administration in patients requirining continuous antiplatellet therapy after coronary stent placement.
Synergistic Effect of Polyalthia longifolia Leaf and Antibiotics against Clinical Isolates of Methicillin-Resistant Staphylococcus aureus (MRSA) by Microscopic Technique.
Kirubakari B, Chen Y, Sasidharan S
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31113347 · Publisher ↗
BACKGROUND: Polyalthia longifolia is a popular medicinal plant and has been widely used as a traditional remedy for centuries in curing of various ailments. The purpose of this study was conducted to determine the in sit...
BACKGROUND: Polyalthia longifolia is a popular medicinal plant and has been widely used as a traditional remedy for centuries in curing of various ailments. The purpose of this study was conducted to determine the in situ antimicrobial synergistic effects between Polyalthia longifolia leaf ethyl acetate fraction (PLEAF) and ampicillin against MRSA local isolate by using modern microscopy technique. METHODS: Hence, the evaluation of the synergistic activity of PLEAF and ampicillin against MRSA local isolate was conducted with scanning electron microscopy (SEM). RESULTS: The combinational effect of PLEAF fraction and ampicillin exhibited significant antibacterial activity against MRSA. Bacterial cells observations showed invagination, impaired cell division, extensive wrinkles, cell shrinkage, the appearance of a rougher cell with fibrous matrix and clustered cells which confirmed the synergistic effect of PLEAF and ampicillin against MRSA local isolate by SEM. CONCLUSION: Conclusively, the in situ SEM observation proved the synergistic antimicrobial activity between PLEAF fraction and ampicillin to destroy the MRSA resistance bacteria which is an important aspect of PLEAF fraction to be used in the future combinational therapy.
Evaluation of the Anti-Inflammatory Activities of Diclofenac Sodium, Prednisolone and Atorvastatin in Combination with Ascorbic Acid.
Ahmed T, Archie SR, Faruk A … +3 more , Chowdhury FA, Al Shoyaib A, Ahsan CR
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 31084596 · Full text
OBJECTIVES: Inflammation is our body's normal defense mechanism, but in some cases, it may be responsible for causing different kinds of disorders. Several antiinflammatory drugs are present for the treatment of these di...
OBJECTIVES: Inflammation is our body's normal defense mechanism, but in some cases, it may be responsible for causing different kinds of disorders. Several antiinflammatory drugs are present for the treatment of these disorders; however, the conventional anti-inflammatory drugs cause side effects when used in the long term and therefore, it is better to use them in a low dose for a shorter duration of time. This study was designed to find out whether there is an augmentation of the therapeutic effectiveness of the antiinflammatory drugs like diclofenac sodium (NSAID), prednisolone (steroid) and atorvastatin (statin) when used in combination with ascorbic acid (antioxidant). METHODS: Wistar Rats (n=144) were selected and divided into 24 groups of 6 rats in each. Carrageenan and formalin were used to induce local inflammation and neuropsychiatric effects, respectively. The inhibitions of such responses were measured after administering a drug alone and in combination with ascorbic acid. RESULTS: In case of carrageenan mediated inflammation, the combination of 5 mg/kg diclofenac and 200 mg/kg ascorbic acid gave the highest inhibition of 74.19% compared to other groups of drugs. The combination of 5 mg/kg diclofenac and 200 mg/kg ascorbic acid gave 97.25% inhibition for formalin-mediated inflammation group. In both cases, combination therapy showed statistically significant anti-inflammatory activities compared to monotherapy (p values <0.05). CONCLUSION: All the data clearly indicate new combinations of drug therapy comprising diclofenac sodium, prednisolone, atorvastatin with ascorbic acid, which may be more effective against both local edema and the neuropsychiatric effect caused due to inflammation.
Analgesic and Anti-inflammatory Effects of Caryocar brasiliense.
Junior AJ, Leitão MM, Bernal LPT … +5 more , Dos Santos E, Kuraoka-Oliveira ÂM, Justi P, Argandoña EJS, Kassuya CAL
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30961515 · Publisher ↗
BACKGROUND: Caryocar brasiliense, popularly known as pequi, is widely distributed in the Amazon rainforest and Brazilian savannah. The fruit obtained from pequi is used in cooking and has folk use as an anti-inflammatory...
BACKGROUND: Caryocar brasiliense, popularly known as pequi, is widely distributed in the Amazon rainforest and Brazilian savannah. The fruit obtained from pequi is used in cooking and has folk use as an anti-inflammatory and for the treatment of respiratory disease. Until now, these two properties had not been scientifically demonstrated for Pequi oil in a carrageenan model. OBJECTIVE: Our group determined the composition and safe use of Pequi oil from the Savannah of Campo Grande, and the anti-inflammatory and anti-nociceptive activities of this pequi oil were investigated in vivo models. MATERIALS AND METHODS: Doses of 300, 700, and 1000 mg/kg of Pequi oil were administered orally (p.o.) to Swiss male mice, and three parameters of inflammation (mechanical hyperalgesia, cold, hyperalgesia, and oedema) were analyzed in a carrageenan model to induce an inflammatory paw state. RESULTS AND DISCUSSION: The effects of Pequi oil were also carrageenan in pleurisy model, formalin, and acetic acid induced nociception. Oral administration of 1,000 mg/kg orally Pequi oil (p.o.) inhibited (*P<0.05), the migration of total leukocytes, but not alter plasma extravasation, in the pleurisy model when compared to control groups. The paw edema was inhibited with doses of 700 (P <0.05) and 1,000 mg (P<0.001) of pequi oil after 1, 2, and 4 hours after carrageenan. Pequi oil (1,000 mg/kg) also blocked the mechanical hyperalgesy and reduced cold allodynia induced by carrageenan in paw (P <0.05). Pequi oil treatment (1,000 mg/kg) almost blocked (P < 0.001) all parameters of nociception observed in formalin and acid acetic test. CONCLUSION: This is the first time that the analgesic and anti-inflammatory effects of Pequi oil have been shown.
Phycocyanin Extracted from Oscillatoria minima Shows Antimicrobial, Algicidal, and Antiradical Activities: In silico and In vitro Analysis.
Venugopal VC, Thakur A, Chennabasappa LK … +4 more , Mishra G, Singh K, Rathee P, Ranjan A
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30950358 · Full text
BACKGROUND: Phycocyanin is an algae-derived protein, which binds to pigment for harvesting light. It has been reported in various different species, including that of red algae, dinoflagellates, and cryptophyta. Importan...
BACKGROUND: Phycocyanin is an algae-derived protein, which binds to pigment for harvesting light. It has been reported in various different species, including that of red algae, dinoflagellates, and cryptophyta. Importantly, phycocyanin has enormous applications, including cosmetic colorant, food additive, biotechnology, diagnostics, fluorescence detection probe, an anticancer agent, anti-inflammatory, immune enhancer, etc. In addition, several different algae were utilized for the isolation of cyano-phycocyanin (C-PC), but most of the purification methods consist of several steps of crude extraction. AIM: To isolate C-PC from a new source of microalgae with better purity level and to evaluate its antimicrobial, algicidal, and antiradical activities. METHODS: Biological activity, permeability, pharmacokinetics, and toxicity profile of C-PC were predicted by in silico studies. C-PC was purified and isolated by using ammonium sulphate precipitation, ion-exchange chromatography and gel-filtration chromatography. C-PC was characterized by SDS-PAGE and elution profile (purity ratio) analysis. Antimicrobial and algicial activities of C-PC were evaluated by the microtitre plate based assays. Antiradical activity of C-PC was evaluated by DPPH- and ABTS*+ radical scavenging assays. CONCLUSION: C-PC was extracted from Oscillatoria minima for the first time, followed by its quantitative as well qualitative evaluation, indicating a new alternative source of this important protein. Furthermore, the antimicrobial, algicidal, and antiradical activities of the isolated C-PC extract have been demonstrated by both in silico as well as in vitro methods.
Amyloid A in Serum and Ascitic Fluid as a Novel Diagnostic Marker of Spontaneous Bacterial Peritonitis.
Badawi R, Asghar MN, Abd-Elsalam S … +11 more , Elshweikh SA, Haydara T, Alnabawy SM, Elkadeem M, ElKhalawany W, Soliman S, Elkhouly R, Soliman S, Watany M, Khalif M, Elfert A
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30931865 · Full text
BACKGROUND: Diagnosis of Spontaneous Bacterial Peritonitis (SBP) depends mainly on ascetic fluid culture which may be negative in spite of the clinical suggestion of SBP and high ascetic fluid neutrophilic count. AIMS: T...
BACKGROUND: Diagnosis of Spontaneous Bacterial Peritonitis (SBP) depends mainly on ascetic fluid culture which may be negative in spite of the clinical suggestion of SBP and high ascetic fluid neutrophilic count. AIMS: This study aimed to evaluate the biological importance of amyloid A biomarker in both serum and ascetic fluid to diagnose SBP as early as possible and to compare it to other markers (C-reactive protein (CRP), and the neutrophil-to-lymphocyte ratio (NLR)). METHODS: This study included 37 patients with hepatic ascites; twenty-two of them had SBP, and 15 patients did not have SBP. Serum and ascetic fluid amyloid A, ascetic fluid neutrophil, C-reactive protein, and neutrophil-to-lymphocyte ratio were measured in all subjects before the start of antimicrobial chemotherapy to the infected ones. RESULTS: Both the serum and ascetic fluid amyloid and also, CRP were significantly higher in patients infected with ascetic fluid than others. The cut-off point of serum amyloid A for early detection of SBP was 9.25ug/ml with the high sensitivity and specificity. For ascetic amyloid A, the sensitivity and specificity were 90.09% and 60% at cut-off point 2.85ug/ml, respectively. CONCLUSION: Amyloid A in serum and ascitic fluid can be considered as a good biomarker for early diagnosis of SBP.
Design, Synthesis and Pharmacological Evaluation of Gastro- Protective Anti-inflammatory Analgesic Agents based on Dual Oxidative Stress / Cyclooxygenase Inhibition.
Gaba M, Singh S, Mohan C … +4 more , Dhingra R, Chauhan M, Rana P, Dhingra N
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30914035 · Publisher ↗
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) derived local generation of reactive oxygen species (ROS) plays a crucial role in the formation of gastric ulceration. OBJECTIVE: Therefore, anti-inflammatory an...
BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) derived local generation of reactive oxygen species (ROS) plays a crucial role in the formation of gastric ulceration. OBJECTIVE: Therefore, anti-inflammatory analgesics with potent antioxidant activity could be a potential therapeutic strategy for the treatment of pain and inflammatory disorders without gastrointestinal (GI) side effects. METHODS: In an effort to develop gastroprotective analgesic and anti-inflammatory agents, a series of 2-methylamino-substituted-1H-benzo[d] imidazol-1-yl) (phenyl) methanone derivatives were synthesized and evaluated in vitro for cyclooxygenase (COX) inhibition as well as anti-oxidant potential by the FRAP assay. The compounds with significant in vitro COX-1/COX-2 inhibitory activity and antioxidant activity were further screened in vivo for their anti-inflammatory and analgesic activities. Moreover, the ulcerogenic potential of test compounds was also studied. To gain insight into the plausible mode of interaction of compounds within the active sites of COX-1 and COX-2, molecular docking simulations were performed. RESULTS: Among the various synthesized molecules, most of the compounds showed good cyclooxygenase inhibitory activity and efficient antioxidant activity in FRAP assay. After preliminary and indicative in vitro assays, three compounds exhibited most significant antiinflammatory and analgesic activity with better gastric tolerability during their in vivo evaluation. Ligand interaction studies indicated highest dock score -43.05 of 1,2- disubstituted benzimidazole derivatives in comparison to the reference ligand -30.70. Overall studies provided us (2-((4-methoxyphenylamino) methyl) -1h-benzo [d] imidazol- 1-yl) (phenyl) methanone as a lead with potent gastro-protective anti-inflammatory and analgesic activities that can be used for future research. CONCLUSION: From the above results, it can be concluded that designing of multifunctional molecules with COX-1/COX-2 inhibitory and anti-oxidant activities could hold a great promise for further development of GI-safer NSAIDs.
Mitigation of Radiation-induced Pneumonitis and Lung Fibrosis using Alpha-lipoic Acid and Resveratrol.
Azmoonfar R, Amini P, Yahyapour R … +7 more , Rezaeyan A, Tavassoli A, Motevaseli E, Khodamoradi E, Shabeeb D, Musa AE, Najafi M
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30892165 · Full text
BACKGROUND: Lung is a radiosensitive organ. Studies have shown that exposure of the lung to acute and high doses of radiation following inhalation of radioactive agents or an accidental radiological event may lead to pne...
BACKGROUND: Lung is a radiosensitive organ. Studies have shown that exposure of the lung to acute and high doses of radiation following inhalation of radioactive agents or an accidental radiological event may lead to pneumonitis and fibrosis, which are associated with a risk of death. So far, some agents have been studied for mitigation of pneumonitis and fibrosis following exposure of murine lung tissues to ionizing radiation. In this study, we aimed to detect the possible mitigatory effect of alpha-lipoic acid, resveratrol and their combination on mice pneumonitis and fibrosis markers following irradiation. METHODS: 25 mice were divided into 5 groups: control, radiation; radiation plus alpha-lipoic acid; radiation plus resveratrol; and radiation plus both resveratrol and alpha-lipoic acid. Mice chest regions were irradiated with 18 Gy using a cobalt-60 gamma rays source. Treatments started 24 h after irradiation and continued for two weeks. After 100 days, all mice were sacrificed and their lung tissues removed for histopathological evaluation. RESULTS: Pathological study showed that exposure to radiation led to severe pneumonitis and moderate fibrosis after 100 days. Both resveratrol and alpha-lipoic acid, as well as their combination could mitigate pneumonitis and fibrosis markers. Although, resveratrol could not mitigate infiltration of most inflammatory cells as well as inflammation and vascular damage, alpha-lipoic acid and its combination were able to mitigate most damaged markers. CONCLUSION: Alpha-lipoic acid and its combination with resveratrol were able to mitigate fibrosis and pneumonitis markers in mice lung tissues following lung irradiation. Although resveratrol has a protective effect on some markers, it has a weaker effect on lung injury. In conclusion, our results suggest that the combination of resveratrol and alpha-lipoic acid has a potent mitigatory effect compared to the single forms of these agents.
Optimization of Microemulgel for Tizanidine Hydrochloride.
Jagdale S, Brahmane S, Chabukswar A
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30854978 · Full text
BACKGROUND: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle...
BACKGROUND: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine hydrochloride belongs to BCS class II. It has low oral bioavailability and short halflife. Incorporating this drug in microemulgel is an excellent way to overcome problems associated with the drug. OBJECTIVES: Present research work was aimed to develop and optimize a microemulsion based gel system for tizanidine hydrochloride. METHODS: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram was constructed to obtain concentration range of components. The prepared microemulsion was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity. 32 level factorial design was applied to study the effect of concentration of carbopol 934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis, drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study. RESULTS: Microemulsion was prepared by using isopropyl myristate as oil, tween 80 as a surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was found with Smix ratio of 1:1. FE-SEM showed globule size 28μm for batch B1 and zeta potential was -1.27mV indicating good stability of the microemulsion. Optimised batch was F6 which showed 92% drug release within 8 hours. It followed the Korsmeyer-Peppas model. CONCLUSION: A stable, effective and elegant microemulgel formulation, exhibiting good in-vitro and ex-vivo drug release was formulated.
Design, Synthesis and Molecular Docking Studies of Novel Thiadiazole Analogues with Potential Antimicrobial and Antiinflammatory Activities.
Mehta DK, Taya P, Das R … +1 more , Dua K
Antiinflamm Antiallergy Agents Med Chem · 2019 · PMID 30848217 · Publisher ↗
BACKGROUND: Chemical modification of thiadiazole may lead to a potent therapeutic agent. In this study, biological properties of thiadiazole derivatives were evaluated by assessing their antimicrobial and anti-inflammato...
BACKGROUND: Chemical modification of thiadiazole may lead to a potent therapeutic agent. In this study, biological properties of thiadiazole derivatives were evaluated by assessing their antimicrobial and anti-inflammatory activities. METHODS: A series of novel derivatives of N-(5-(1-methyl-indol-3-yl)-1,3,4-thiadiazol-2- yl)-2-(5-substitutedphenyl)-3-(phenylamino)-4,5-dihydropyrazol-1-yl) acetamide have been synthesized and evaluated for their antimicrobial activity. Anti-inflammatory activity was done using carrageenan-induced inflammation in rat paw edema model. In-silico molecular docking studies of the synthesized compounds were performed on crystal structures of Aspergillus niger, Bacillus subtilis, Candida albicans, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Cyclooxygenase-2 (obtained from www.rcsb.org) using GRIP batch docking method of V-life MDS 3.0 software. The structures of the newly synthesized compounds were confirmed by FT-IR, 1H-NMR, 13C-NMR and Mass spectroscopy. RESULTS: Antimicrobial and Anti-inflammatory activity study of the novel synthesized compounds were screened. Synthesized compounds having methoxy substitution on the 3rd and 4th positions of aromatic ring are utmost active amongst all the derivatives. Compounds 6d, 6i, 6j and 6l were found to possess good anti-inflammatory activity having percentage of inhibition to the extent of 46.8%, 48.1%, 49.4%, and 48.5% as compared with Diclofenac. CONCLUSION: The experimental results were further supported by molecular docking analysis describing the better interaction patterns.
Synthesis of Some New Hydroxytriazenes and their Antimicrobial and Anti-inflammatory Activities.
Jain S, Dayma V, Sharma P … +3 more , Bhargava A, Baroliya PK, Goswami AK
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30827265 · Publisher ↗
BACKGROUND: Hydroxytriazenes and their derivatives have been studied for the biological and pharmacological applications in the past few years. These compounds possess antibacterial, antifungal, anti-inflammatory, analge...
BACKGROUND: Hydroxytriazenes and their derivatives have been studied for the biological and pharmacological applications in the past few years. These compounds possess antibacterial, antifungal, anti-inflammatory, analgesic and wound healing activities. In this study, we report the synthesis of ten hydroxytriazenes in two series derived from disubstituted aniline and studied for antimicrobial and anti-inflammatory activities. METHODS: For this purpose, 2-methyl-5-chloroaniline and 2-trifluoromethyl-5-chloroaniline were used to synthesize compounds A1-5 and B1-5 series, respectively. All compounds were synthesized by the reported method which involves three steps of the method (i) Reduction, (ii) Diazotization, (iii) Coupling. All synthesized compounds were characterized by various techniques CHN elemental analysis, FTIR, 1H NMR, and MASS spectral analysis. The antibacterial activities of the compounds were screened against S. aureus, S. pyogenes, E. coli, P. aeruginosa, and antifungal activities were against C. albicans, A. clavatus by the zone of inhibition method. In addition, anti-inflammatory activity was also evaluated by carrageenan-induced paw edema method and results were reported as % inhibition. RESULTS: All the synthesized compounds were obtained in pure form and their spectral data are in good agreement with their structure. The synthesized compounds have shown good antimicrobial activity and zone of inhibition was ranging 21 to 24 mm. Further antiinflammatory effect of the compounds was 96.58 to 98.71 % inhibition. CONCLUSION: The results of the present study indicate that chloro and trifluoromethyl substitution at hydroxytriazenes skeleton could improve anti-inflammatory and antimicrobial activities.
Anti-inflammatory and Antioxidant Effects of on Paracetamol-induced Hepatitis in Rats.
Baali N, Mezrag A, Bouheroum M … +3 more , Benayache F, Benayache S, Souad A
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30799800 · Full text
BACKGROUND: Herbal medicines have been used in the treatment of liver diseases for a long time. The current study was elaborated to evaluate in vitro and in vivo antioxidant and anti-inflammatory effects of Lotus cornicu...
BACKGROUND: Herbal medicines have been used in the treatment of liver diseases for a long time. The current study was elaborated to evaluate in vitro and in vivo antioxidant and anti-inflammatory effects of Lotus corniculatus (L. corniculatus) butanolic extract. METHODS: The in vitro antioxidant and anti-inflammatory properties of L. corniculatus were investigated by employing DPPH radical scavenging, H2O2 scavenging and BSA denaturation assays. In vivo antioxidant and anti-inflammatory effects of L. corniculatus were evaluated against paracetamol (APAP)-induced hepatitis in rats. L.corniculatus at doses of 100 and 200 mg/kg was administered orally once daily for seven days. Serum transaminases (AST and ALT) and lactate dehydrogenase (LDH), total bilirubin levels, liver malondialdehyde (MDA), reduced glutathione (GSH), glutathione S- transferase (GST) and superoxide dismutase (SOD) levels and inflammatory markers, such as serum Creactive protein (CRP), circulating and liver myeloperoxidase (MPO) levels were investigated. Further histopathological analysis of the liver sections was performed to support the effectiveness of L. corniculatus. RESULTS: L. corniculatus exhibited strong antioxidant and anti-inflammatory effects in vitro. In the in vivo study, our findings demonstrate that L. corniculatus (100 and 200 mg/kg) administration led to an amelioration of APAP effects on liver histology, liver functions parameters (AST, ALT, LDH, and total bilirubin levels) and liver oxidative stress markers (MDA, GSH, GST and SOD levels). Furthermore, serum CRP, circulating MPO and liver MPO levels were declined by both doses of L. corniculatus extract. The best benefits were observed with 200 mg/kg of L. corniculatus extract. CONCLUSION: Antioxidant and anti-inflammatory effects of L. corniculatus extract may be due to the presence of active components.
Anti-inflammatory Effect of Leaves Ethanolic Extract on Adjuvant and Carragenan Treated Rats.
Raj H, Gupta A, Upmanyu N
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30799799 · Full text
BACKGROUND: Woodfordia fructicosa is used traditionally for the treatment of inflammation associated with arthritis. METHODS: In the present study, the anti-inflammatory activity of W. fructicosa (WFE) leaves ethanolic e...
BACKGROUND: Woodfordia fructicosa is used traditionally for the treatment of inflammation associated with arthritis. METHODS: In the present study, the anti-inflammatory activity of W. fructicosa (WFE) leaves ethanolic extract was assessed in Sprague Dawley rats by giving 200 mg/kg dose orally. Inflammation was studied by using carrageenan induced paw edema, Freund's adjuvant (FA) and monosodium iodo acetate (MIA) induced arthritis as animal models. Serum tumor necrosis factor-alpha (TNF-α) was estimated in blood sample of animals treated with FA. The one way ANOVA followed by Bonferroni's test was used for statistical analysis. RESULTS: WFE significantly decreased (P<0.05, P<0.001) paw thickness in carrageenan induced paw edema and FA induced arthritis. The significant decrease in knee diameter (P<0.001) in MIA induced arthritis as well as inhibitory effect (P<0.001) on elevated TNF- α was observed. CONCLUSION: These results showed that the WFEexerted an inhibitory effect on TNF-α and carrageenan paw edema which may justify its traditional use in inflammatory conditions. Thus, the study shows that leaves of W. fruticose afford anti-inflammatory activity by preventing the inflammation in different animal models.
Screening of NO Inhibitor Release Activity from Soft Coral Extracts Origin Palu Bay, Central Sulawesi, Indonesia.
Tanod WA, Yanuhar U, Maftuch … +2 more , Putra MY, Risjani Y
Antiinflamm Antiallergy Agents Med Chem · 2019 · PMID 30799798 · Full text
BACKGROUND: As a marine organism, soft corals can be utilized to be various bioactive substances, especially terpenoids and steroids. The soft corals family which produces bioactive generally come from clavulariidae, alc...
BACKGROUND: As a marine organism, soft corals can be utilized to be various bioactive substances, especially terpenoids and steroids. The soft corals family which produces bioactive generally come from clavulariidae, alcyoniidae, nephtheidae and xeniidae family. OBJECTIVE: To investigate the bioactivity of Nitric Oxide (NO) inhibitor release from soft coral crude extracts of Sinularia sp. (SCA), Nephthea sp. (SCB), Sarcophyton sp. (SCC), Sarcophyton sp. (SCD), Sinularia sp. (SCE) and Sinularia sp. (SCF). MATERIALS AND METHODS: Soft coral is collected from Palu Bay (Central Sulawesi). NO inhibitory release activity measured according to the Griess reaction. Soft corals sample macerated with 1:2 (w/v). Then, Soft coral extracts with the best NO Inhibitor activity partitioned with Dichloromethane, Ethyl acetate, and n-butanol. The bioactive of all crude extracts were identified by GC-MS to find compounds with anti-inflammatory potential. RESULTS: Sarcophyton sp. (SCC) and Sinularia sp. (SCF) are able to inhibit NO concentrations of 0.22 ± 0.04 and 0.20 ± 0.04 µM at 20 mg/mL, respectively. The chemical constituents determined and showed the potential as anti-inflammatory in the crude of Sinularia sp. (SCA) were Octacosane (3.25%). In Nephthea sp., (SCB) were Cyclohexene, 6-ethenyl-6- methyl-1-(1-methylethyl)-3-(1-methylethylidene)-,(S)- (0.55%); Azulene, 1,2,3,4,5,6,7,8- octahydro-1,4-dimethyl-7-(1-methylethylidene)-, (1S-cis)- (0.53%); and 1,7,7-Trimethyl- 2-vinylbicyclo[2.2.1]hept-2-ene (4.72%). In Sarcophyton sp, (SCC) were Eicosane (0.12%); Nonacosane (10.7%); 14(β)-Pregnane (0.87%); Octacosane 6.39%); and Tricosane (1.53%). In Sarcophyton sp. (SCD) were 14(β)-Pregnane (2.69%); and Octadecane (27.43%). In crude of Sinularia sp. (SCE) were Oleic Acid (0.63%); 7,10-Hexadecadienoic acid, methyl ester (0.54%); 14(β)-Pregnane (1.07%); 5,8,11,14-Eicosatetraenoic acid, ethyl ester, (all-Z)- (4.60%); Octacosane (7.75%); and 1,2-Benzisothiazole, 3-(hexahydro-1Hazepin- 1-yl)-, 1,1-dioxide (1.23%). In the crude of Sinularia sp., (SCF) were Oxirane, decyl- (1.38%); Nonacosane (0.57%); Cyclohexanol, 5-methyl-2-(1-methylethenyl)- (0.61%); 14B-Pregnane (0.76%); and Tetratriacontane (1.02%). CONCLUSION: The extract of Sarcophyton sp. (SCC) and Sinularia sp. (SCF) showed the best NO inhibitory release activity. This study is making soft corals from Central Sulawesi, Indonesia can become a potential organism in the discovery and development of bioactive substances anti-inflammatory.
Preface.
Carradori S
Antiinflamm Antiallergy Agents Med Chem · 2019 · PMID 30777578 · Publisher ↗
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Study of Anti-inflammatory Activity of a New Non-opioid Analgesic on the Basis of a Selective Inhibitor of TRPA1 Ion Channels.
Beskhmelnitsyna EA, Pokrovskii MV, Kulikov AL … +2 more , Peresypkina AA, Varavin EI
Antiinflamm Antiallergy Agents Med Chem · 2019 · PMID 30734687 · Publisher ↗
INTRODUCTION: Nowadays, the group of NSAIDs is used the most widely in order to treat the inflammatory process. But its long-term administration increases the risk of complications of pharmacotherapy. Therefore, today it...
INTRODUCTION: Nowadays, the group of NSAIDs is used the most widely in order to treat the inflammatory process. But its long-term administration increases the risk of complications of pharmacotherapy. Therefore, today it is urgent to search for new molecules that can selectively block biological targets that directly perceive inflammatory mediators. One of such targets is TRPA1. ZC02-0012, a compound from the group of substituted pyrazinopyrimidinones, which is a selective inhibitor of TRPA1 ion channel. OBJECTIVE: The aim of our study was to study the anti-inflammatory activity of an innovative molecule under the laboratory code ZC02-0012 from the group of selective inhibitors of TRPA1 ion channel. MATERIALS AND METHODS: Anti-inflammatory activity of ZC02-0012 was studied on the model of acute exudative inflammation of the paw in response to subplantar injection in the right hind paw of mice with 0.02 ml of 2% formaldehyde solution. The mass of the paw was measured after 4 hours (peak edema) after phlogistic injection. The test substance and the reference drug was administered intragastrically or intramuscularly 45 minutes before the injection of formaldehyde solution. The presence and intensity of antiinflammatory activity was judged by the inhibitory effect, represented in percent. RESULTS AND DISCUSSION: Selective inhibitor of the TRPA1 ion channel ZC02-0012 revealed the anti-inflammatory activity at doses of 3 and 9 mg/kg, its intensity is comparable to diclofenac sodium. CONCLUSION: The selective inhibitor of the ion channel TRPA1, a substance under code ZC02-0012, has an anti-inflammatory activity comparable with diclofenac sodium.
Antioxidant Effects of Oleuropein on Hydrogen Peroxide-Induced Neuronal Stress- An Study.
Kucukgul A, Isgor MM, Duzguner V … +2 more , Atabay MN, Kucukgul A
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 30714532 · Full text
BACKGROUND: Persistent oxidative stress can lead to chronic inflammation and mediate most chronic diseases including neurological disorders. Oleuropein has been shown to be a potent antioxidant molecule in olive oil leaf...
BACKGROUND: Persistent oxidative stress can lead to chronic inflammation and mediate most chronic diseases including neurological disorders. Oleuropein has been shown to be a potent antioxidant molecule in olive oil leaf having antioxidative properties. OBJECTIVE: The aim of this study was to investigate the protective effects of oleuropein against oxidative stress in human glioblastoma cells. METHODS: Human glioblastoma cells (U87) were pretreated with oleuropein (OP) essential oil 10 µM. After 30 minutes, 100 µM H2O2 was added to the cells for three hours. Cell survival was quantified by colorimetric MTT assay. Glutathione level, total oxidant capacity, total antioxidant capacity and nitric oxide levels were determined by using specific spectrophotometric methods. The relative gene expression level of iNOS was performed by qRT-PCR method. RESULTS: According to viability results, the effective concentration of H2O2 (100µM) significantly decreased cell viability and oleuropein pretreatment significantly prevented the cell losses. Oleuropein regenerated total antioxidant capacity and glutathione levels decreased by H2O2 exposure. In addition, nitric oxide and total oxidant capacity levels were also decreased after administration of oleuropein in treated cells. CONCLUSION: Oleuropein was found to have potent antioxidative properties in human glioblastoma cells. However, further studies and validations are needed in order to understand the exact neuroprotective mechanism of oleuropein.
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