Antiinflamm Antiallergy Agents Med Chem [JOURNAL]
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Anti-Inflammatory, Antimicrobial and Insecticidal Properties of Daucus Gracilis Steinh Flowers Essential Oil.
Nadia B, Merad-Boussalah N, Benyoucef F … +3 more , Zoheir A, Muselli A, El Amine Dib M
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33292157 · Publisher ↗
BACKGROUND: Daucus gracilis Steinh belongs to the Apiaceae family. The flowers of this plant have been used by the population of western Algeria for the treatment of mouth ulcers. However, very few studies exist concerni...
BACKGROUND: Daucus gracilis Steinh belongs to the Apiaceae family. The flowers of this plant have been used by the population of western Algeria for the treatment of mouth ulcers. However, very few studies exist concerning the biological properties of essential oil of Daucus gracilis Steinh flowers. OBJECTIVES: The purpose of this work was to study the chemical composition of the essential oil of Daucus gracilis flowers and to evaluate their antimicrobial, insecticidal and anti-inflammatory properties. METHODS: The distilled essential oil was analyzed by GC and GC-MS. The antimicrobial activity of the essential oil was evaluated using two methods i) diffusion method, and ii) micro dilution technique. The insecticidal activity of essential oil was evaluated against adults of Tribolium confusum by fumigant test. The in vitro assessment of the anti-inflammatory property of essential oil was assessed by the protein denaturation method. RESULTS: Daucus gracilis flowers essential oil mainly represented oxygenated monoterpenes such as geranyl acetate (18.3%), lavandulyl acetate (15.2%), lavandulyl isobutyrate (13.6%) and citronellyl isobutyrate (6.8%). According to the results of antimicrobial activity, the essential oil of flowers presented prominent inhibitory action against Aspergillus flavus (0.06 μg/mL), followed by Staphylococcus aureus, Escherichia faecalis, Bacillus cereus and Candida albicans with MIC values of 0.125 μg/mL. The Daucus gracilis essential oil flowers proved to be very biocidal toward adults of Tribolium confusum; mortality of 100% of the population was noted with a dose of 2 μl/L air after 24 hours of exposure. Furthermore, the oil has shown a very good inhibition of protein denaturation comparable to Diclofenac at a concentration of 30 μL/mL. CONCLUSION: Daucus gracilis essential oil can be used as a pharmacological tools for inflammatory, antimicrobial and insecticidal properties.
Covid-19: Urgent Call to Action.
Mohamed AA, Tantawi OI, Fathalla LA … +6 more , El-Hassib DMA, El-Toukhy NER, Salah W, Elkadeem M, Ezzat O, Abd-Elsalam S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33267767 · Publisher ↗
Novel Corona Virus 2019 (COVID-19) is a new virus spread rapidly all over the world. It has specific respiratory or gastrointestinal tract symptoms. Its reported complications include respiratory distress, systemic infla...
Novel Corona Virus 2019 (COVID-19) is a new virus spread rapidly all over the world. It has specific respiratory or gastrointestinal tract symptoms. Its reported complications include respiratory distress, systemic inflammatory response syndrome, and septic shock. Due to heavy cytokines released by the virus; corticosteroids (40-120 mg / day) were given to severe cases to reduce pneumonia. It's a difficult task to control the spread of SARS-CoV-2, and to invent proper vaccines and treatments. In this review, the existing understanding of fatal, pandemic human coronavirus SARS-Cov2 (COVID-19), with special reference to its diagnosis, origin, transmission, and different approaches to develop its therapeutics, will be discussed.
Synthesis of Novel Aryl (4-Aryl-1H-Pyrrol-3-yl) (Thiophen-2-yl) Methanone Derivatives: Molecular Modelling, In Silico ADMET, Anti-Inflammatory and Anti-Ulcer Activities.
Pasha A, Mondal S, Panigrahi N
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33200699 · Publisher ↗
BACKGROUND: Due to the presence of both five-membered heterocyclics like pyrrole and thiophene in one molecule considerable attention was made for their enormous pharmacological activities out of which include anti-infla...
BACKGROUND: Due to the presence of both five-membered heterocyclics like pyrrole and thiophene in one molecule considerable attention was made for their enormous pharmacological activities out of which include anti-inflammatory and anti-ulcer activities. OBJECTIVE: Chalcones with toluenesulfonylmethyl isocyanide (TosMIC) undergo synthesis to form some new aryl (4-aryl-1H-pyrrol-3-yl) (thiophen-2-yl) methanone derivatives. Molecular docking of synthesized compounds with protein receptors of anti-inflammatory COX-1(3N8Y), COX-2 (1PXX) along with anti-ulcer H+/K+ATPase enzyme (2XZB) followed with drug-likeness, and in silico ADMET properties. MATERIALS AND METHODS: The multicomponent reaction was carried out by the intermediate formation of α, β-unsaturated ketone from carbonyl compounds which on sequential addition undergoes [3+2] cycloaddition reaction in same medium affords aryl (4-aryl-1H-pyrrol-3-yl) (thiophen-2-yl) methanone derivatives by addition of TosMIC in basic medium had resulted in series of compounds PY1 to PY12. All the new synthesized compounds were screened for their in-vitro anti-inflammatory activity by bovine serum albumin method followe with COX assay, and in-vivo by using carrageenan-induced rat paw edema method of the selected compounds PY1, PY5 and PY12 which is also screened for anti-ulcer activity by pylorus ligation method, respectively. Molecular docking was performed using autodock tools, drug-likeness by OSIRIS property explorer and admetSAR properties. RESULTS AND DISCUSSION: From the synthesized compounds of aryl (4-aryl-1H-pyrrol-3-yl) (thiophen- 2-yl) methanone derivatives PY5 showed decent in-vitro and in-vivo anti-inflammatory along selectivity index of 6.2 for COX-1 with IC50(μM) value of 9.54 over diclofenac with 8.74 and PY1 showed decent in-vivo anti-ulcer activities along with drug-likeness and in silico ADMET predictions revealed that all the synthesized compounds have minimal toxic effects with good absorption as well as solubility characteristics. The selected compounds may serve as potential lead compounds for developing new anti-inflammatory and anti-ulcer drugs. CONCLUSION: From the newly synthesized molecules PY5 was found to be effective for anti-inflammatory and PY1 was found to be effective for anti-ulcer activities further derivitization and designed of modification to achieve more compounds with potent anti-inflammatory and anti-ulcer activities.
Peripheral Anti-nociceptive and Anti-inflammatory Effect of Oleanolic Acid in a Rat Model of Osteoarthritis.
Salman I, Fakhoury M, Fouani M … +1 more , Lawand N
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33183210 · Publisher ↗
BACKGROUND: Oleanolic acid (OA) is a naturally occurring pentacyclic triterpenoid with multifarious actions. The anti-inflammatory effect it exerts when taken orally is the most important; however, the underpinning mecha...
BACKGROUND: Oleanolic acid (OA) is a naturally occurring pentacyclic triterpenoid with multifarious actions. The anti-inflammatory effect it exerts when taken orally is the most important; however, the underpinning mechanisms of such effects have not yet been fully explored. METHODS: In the present study, we evaluated the anti-inflammatory and anti-nociceptive effect of OA by injecting it directly into the knee joint using an animal model of osteoarthritis. Behavioral and electrophysiological studies were conducted to determine whether OA exerts a direct modulatory effect on primary sensory afferents that can lead to a decrease in pain-related behaviors and inflammatory responses. Rats were divided into two main groups: a pre- and a post-treatment group. Knee joint inflammation was induced by injecting a mixture of 3% kaolin and carrageenan (K/C). In the pre-treatment group, two different doses of OA [5 mg/ml (n=5) and 30 mg/ml (n=4); 0.1 ml per injection] were administered into the synovial cavity of the knee joint before induction of inflammation. In the post-treatment group, rats received only one dose [5 mg/ml (n=5)] of OA after induction of inflammation. RESULTS: Results indicate that intra-articular injection of OA improves motor coordination and attenuates nociceptive behavior and inflammatory reactions. More importantly, we observed a direct depolarizing action of OA on articular sensory fibers, a crucial mechanism that activates descending inhibitory pathways and controls incoming nociceptive signals to the spinal cord. CONCLUSION: Overall, our findings suggest that OA can be used as a preventive and therapeutic approach for the management of osteoarthritis.
In-silico Prediction of the Beta-carboline Alkaloids Harmine and Harmaline as Potent Drug Candidates for the Treatment of Parkinson's disease.
Banerjee R, Kumar M, Gaurav I … +6 more , Thakur S, Thakur A, Singh K, Karak S, Das R, Chhabra M
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33183209 · Publisher ↗
BACKGROUND: Parkinson's disease (PD) is a progressive neurodegenerative disease manifested by core symptoms of loss of motor control and postural instability. Loss of dopaminergic neurons is the cause of PD, thus enhanci...
BACKGROUND: Parkinson's disease (PD) is a progressive neurodegenerative disease manifested by core symptoms of loss of motor control and postural instability. Loss of dopaminergic neurons is the cause of PD, thus enhancing dopamine level by pharmacological treatment is one of the key treatment strategies for PD. However, the limitations of current treatment strategies open the possibility of novel drug candidates for the treatment of PD. OBJECTIVE: To investigate the anti-PD potential of Harmine and Harmaline. We aim to evaluate the therapeutic potential of Harmine and Harmaline by in-silico approaches; molecular docking, pharmacokinetic and Prediction of Activity Spectra for Substances (PASS) analysis were used for evaluating the therapeutic potential of Harmine and Harmaline and standard drug levodopa (L-DOPA). METHODS: Auto dock vina was used for molecular docking of all three compounds against D2- and D3- dopamine receptors. The pharmacokinetics (PKs) and toxicity profile were predicted by pkCSM, and the pharmacological activity was predicted by PASS analysis. RESULTS: Molecular docking showed a higher binding affinity of Harmine and Harmaline as compared to L-DOPA, and these results were supported by in-silico pharmacokinetic and toxicity profiling. Moreover, PASS analysis showed anti-PD activity of Harmine and Harmaline. CONCLUSION: Harmine and Harmaline exhibit higher binding affinity towards D2- and D3- dopamine receptors compared to L-DOPA, and PKs and toxicity profile support their potential as drug candidates for PD therapy.
Common Issues Among Asthma, Epilepsy, and Schizophrenia: From Inflammation to Ca/cAMP Signalling.
Bergantin LB
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33176668 · Publisher ↗
BACKGROUND: A large amount of evidence has described that asthma may be associated with a high epilepsy risk, and epilepsy may be linked with high asthma risk, especially among children and individuals in their 30s. Curi...
BACKGROUND: A large amount of evidence has described that asthma may be associated with a high epilepsy risk, and epilepsy may be linked with high asthma risk, especially among children and individuals in their 30s. Curiously, asthma has also been associated with an increased risk for schizophrenia. Most interestingly, a bidirectional link between schizophrenia and epilepsy has also been established and has been of interest for many years. OBJECTIVE: Bearing in mind the experience of our group in the field of Ca/cAMP signalling pathways, this article discussed, beyond inflammation, the role of these signalling pathways in this link among epilepsy, asthma, and schizophrenia. METHODS: Publications involving these signalling pathways, asthma, epilepsy, and schizophrenia (alone or combined) were collected by searching PubMed and EMBASE. RESULTS AND CONCLUSION: There is a clear relationship between Ca signalling, e.g. increased Ca signals and inflammatory responses. In addition to Ca, cAMP regulates pro- and anti-inflammatory responses. Then, beyond inflammation, the comprehension of the link among epilepsy, asthma, and schizophrenia could improve the drug therapy.
Modulation of Proinflammatory Bacteria- and Lipid-Coupled Intracellular Signaling Pathways in a Transwell Triple Co-Culture Model by Commensal Bifidobacterium Animalis R101-8.
Ghadimi D, Nielsen A, Hassan MFY … +6 more , Fölster-Holst R, Ebsen M, Frahm SO, Röcken C, de Vrese M, Heller KJ
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33135616 · Publisher ↗
BACKGROUND AND AIMS: Following a fat-rich diet, alterations in gut microbiota contribute to enhanced gut permeability, metabolic endotoxemia, and low grade inflammation-associated metabolic disorders. To better understan...
BACKGROUND AND AIMS: Following a fat-rich diet, alterations in gut microbiota contribute to enhanced gut permeability, metabolic endotoxemia, and low grade inflammation-associated metabolic disorders. To better understand whether commensal bifidobacteria influence the expression of key metaflammation-related biomarkers (chemerin, MCP-1, PEDF) and modulate the pro-inflammatory bacteria- and lipid-coupled intracellular signaling pathways, we aimed at i) investigating the influence of the establishment of microbial signaling molecules-based cell-cell contacts on the involved intercellular communication between enterocytes, immune cells, and adipocytes, and ii) assessing their inflammatory mediators' expression profiles within an inflamed adipose tissue model. MATERIAL AND METHODS: Bifidobacterium animalis R101-8 and Escherichia coli TG1, respectively, were added to the apical side of a triple co-culture model consisting of intestinal epithelial HT-29/B6 cell line, human monocyte-derived macrophage cells, and adipose-derived stem cell line in the absence or presence of LPS or palmitic acid. mRNA expression levels of key lipid metabolism genes HILPDA, MCP-1/CCL2, RARRES2, SCD, SFRP2 and TLR4 were determined using TaqMan qRT-PCR. Protein expression levels of cytokines (IL-1β, IL-6, and TNF-α), key metaflammation-related biomarkers including adipokines (chemerin and PEDF), chemokine (MCP- 1) as well as cellular triglycerides were assessed by cell-based ELISA, while those of p-ERK, p-JNK, p-p38, NF-κB, p-IκBα, pc-Fos, pc-Jun, and TLR4 were assessed by Western blotting. RESULTS: B. animalis R101-8 inhibited LPS- and palmitic acid-induced protein expression of inflammatory cytokines IL-1β, IL-6, TNF-α concomitant with decreases in chemerin, MCP-1, PEDF, and cellular triglycerides, and blocked NF-kB and AP-1 activation pathway through inhibition of p- IκBα, pc-Jun, and pc-Fos phosphorylation. B. animalis R101-8 downregulated mRNA and protein levels of HILPDA, MCP-1/CCL2, RARRES2, SCD and SFRP2 and TLR4 following exposure to LPS and palmitic acid. CONCLUSION: B. animalis R101-8 improves biomarkers of metaflammation through at least two molecular/signaling mechanisms triggered by pro-inflammatory bacteria/lipids. First, B. animalis R101-8 modulates the coupled intracellular signaling pathways via metabolizing saturated fatty acids and reducing available bioactive palmitic acid. Second, it inhibits NF-kB's and AP-1's transcriptional activities, resulting in the reduction of pro-inflammatory markers. Thus, the molecular basis may be formed by which commensal bifidobacteria improve intrinsic cellular tolerance against excess pro-inflammatory lipids and participate in homeostatic regulation of metabolic processes in vivo.
In Silico and In Vitro Studies of the Inhibitory Effect of Antihistamine Drug Cyproheptadine Hydrochloride on Human Salivary Alpha Amylase.
Madjda B, Khedidja B, Samira N … +1 more , Mohamed Y
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 33100209 · Publisher ↗
BACKGROUND: For the first time, the inhibitory effects on the human salivary alpha-amylase activity of the anti-inflammatory drugs indomethacin, diclofenac sodium, ketoprofen, diclofenac potassium, diclofenac, triamcinol...
BACKGROUND: For the first time, the inhibitory effects on the human salivary alpha-amylase activity of the anti-inflammatory drugs indomethacin, diclofenac sodium, ketoprofen, diclofenac potassium, diclofenac, triamcinolone acetonide, and the antihistamine drugs levocetirizine dihydrochloride, desloratadine, cycloheptadine hydrochloride, have been investigated to confirm the other properties of these drugs. OBJECTIVE: This study aimed to determine the effect of nine known drugs on human salivary α-amylase in vitro and the nature of interactions with structure-activity relationship using molecular docking experiments. METHODS: The inhibition of human salivary alpha amylase by the six anti-inflammatory and three antihistamine drugs has been carried out using the new method that has been proved in our previous work. Molecular docking has been achieved for the first time for these drugs using the Auto- Dock Vina program. RESULTS: Cyproheptadine hydrochloride presented the highest inhibitory activity against α-amylase with IC=0.7 mg/ml, while the other drugs showed weak activities (IC > 2 mg/ml). CONCLUSION: We conclude that Cyproheptadine hydrochloride, which was studied by docking experiments, exhibited the best inhibitory activity on salivary α-amylase in vitro & in silico.
Betulinic Acid-Azaprostanoid Hybrids: Synthesis and Pharmacological Evaluation as Anti-inflammatory Agents.
Khlebnicova TS, Piven YA, Lakhvich FA … +4 more , Sorokina IV, Frolova TS, Baev DS, Tolstikova TG
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 33001006 · Full text
BACKGROUND: Prevention and treatment of chronic inflammatory diseases require effective and low-toxic medicines. Molecular hybridization is an effective strategy to enhance the biological activity of new compounds. Trite...
BACKGROUND: Prevention and treatment of chronic inflammatory diseases require effective and low-toxic medicines. Molecular hybridization is an effective strategy to enhance the biological activity of new compounds. Triterpenoid scaffolds are in the focus of attention owing to their anti-inflammatory, antiviral, antiproliferative, and immunomodulatory activities. Heteroprostanoids have different pleiotropic effects in acute and chronic inflammatory processes. OBJECTIVE: The study aimed to develop structurally new and low toxic anti-inflammatory agents via hybridization of betulinic acid with azaprostanoic acids. METHODS: A series of betulinic acid-azaprostanoid hybrids was synthesized. The synthetic pathway included the transformation of betulin via Jones' oxidation into betulonic acid, reductive amination of the latter and coupling obtained by 3β-amino-3-deoxybetulinic acid with the 7- or 13-azaprostanoic acids and their homo analogues. The hybrids 1-9 were investigated in vivo on histamine-, formalin- and concanavalin A-induced mouse paw edema models and two models of pain - the acetic acid-induced abdominal writhing and the hotplate test. The hybrids were in vitro evaluated for cytotoxic activity on cancer (MCF7, U- 87 MG) and non-cancer humane cell lines. RESULTS: In the immunogenic inflammation model, the substances showed a pronounced anti-inflammatory effect, which was comparable to that of indomethacin. In the models of the exudative inflammation, none of the compounds displayed a statistically significant effect. The hybrids produced weak or moderate analgesic effects. All the agents revealed low cytotoxicity on human immortalized fibroblasts and cancer cell lines compared with 3β- amino-3-deoxybetulinic acid and doxorubicin. CONCLUSION: The results indicate that the principal anti-inflammatory effect of hybrids is substantially provided with the triterpenoid scaffold and in some cases with the azaprostanoid scaffold, but the latter makes a significant contribution to reducing the toxicity of hybrids. Hybrid 1 is of interest as a potent low toxic agent against immune-mediated inflammation.
Energy Provisioning and Inflammasome Activation: The Pivotal Role of AMPK in Sterile Inflammation and Associated Metabolic Disorders.
Shrungeswara AH, Unnikrishnan MK
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32938355 · Publisher ↗
BACKGROUND: Body defenses and metabolic processes probably co-evolved in such a way that rapid, energy-intensive acute inflammatory repair is functionally integrated with energy allocation in a starvation/ infection / in...
BACKGROUND: Body defenses and metabolic processes probably co-evolved in such a way that rapid, energy-intensive acute inflammatory repair is functionally integrated with energy allocation in a starvation/ infection / injury-prone primitive environment. Disruptive metabolic surplus, aggravated by sedentary lifestyle induces chronic under-activation of AMPK, the master regulator of intracellular energy homeostasis. Sudden increase in chronic, dysregulated 'sterile' inflammatory disorders probably results from a shift towards calorie rich, sanitized, cushioned, injury/ infection free environment, repositioning inflammatory repair pathways towards chronic, non-microbial, 'sterile', 'low grade', and 'parainflammation'. AMPK, (at the helm of energy provisioning) supervises the metabolic regulation of inflammasome activation, a common denominator in lifestyle disorders. DISCUSSION: In this review, we discuss various pathways linking AMPK under-activation and inflammasome activation. AMPK under-activation, the possible norm in energy-rich sedentary lifestyle, could be the central agency that stimulates inflammasome activation by multiple pathways such as 1: decreasing autophagy, and accumulation of intracellular DAMPs, (particulate crystalline molecules, advanced glycation end-products, oxidized lipids, etc.) 2: stimulating a glycolytic shift (pro-inflammatory) in metabolism, 3: promoting NF-kB activation and decreasing Nrf2 activation, 4: increasing reactive oxygen species (ROS) formation, Unfolded Protein Response (UPR) and Endoplasmic Reticulum (ER) stress. CONCLUSION: The 'inverse energy crisis' associated with calorie-rich, sedentary lifestyle, advocates dietary and pharmacological interventions for treating chronic metabolic disorders by overcoming / reversing AMPK under-activation.
Effects of Kolaviron on Pneumonia-like Infection Induced in Albino Wistar Rats.
Dozie-Nwakile OC, Dozie NC, Kingsley UI … +2 more , Catherine OF, Felicia ON
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32933465 · Publisher ↗
BACKGROUND: Pneumonia is an acute or chronic inflammatory disorder of the lungs, affecting the mucosal areas of the lung. It can be caused by bacteria, viruses or fungi. In some cases, it may be caused by physical or che...
BACKGROUND: Pneumonia is an acute or chronic inflammatory disorder of the lungs, affecting the mucosal areas of the lung. It can be caused by bacteria, viruses or fungi. In some cases, it may be caused by physical or chemical irritants. Kolaviron, a natural bioflavonoid extract from Garcinia kola seeds, has been shown to possess anti-inflammatory properties in Flu-like conditions which are associated with cough. There has been a paucity of information on the likelihood of the effectiveness of kolaviron against pneumonia infections. OBJECTIVE: To evaluate the antibacterial and anti-inflammatory effects of kolaviron on albino Wistar rats induced with pneumonia using Klebsiella pneumonia. MATERIALS AND METHODS: Powdered Garcinia kola seeds were extracted with n-hexane and 100% methanol as solvents by using Soxhlet extractor. A standard method was used to obtain kolaviron from the seed extracts. A total of 24 albino Wistar rats were randomly divided into six groups A to F, each comprising four rats. The rats were allowed to acclimatize for 1 hour in very cold environments using ice packs. A standardized 1.0 x10 mg/ml culture suspension was intranasally inoculated to the rats for 10 days to induce pneumonia-like symptoms. Thereafter, the kolaviron was administered to the rats such that a 500mg/kg kolaviron extract was given once daily to groups A (male rats) and B (female rats). Groups C (male rats) and D (female rats) received 250mg/kg of kolaviron extract once daily, while group E rats were given 0.5 ml of dimethyl sulfoxide (DMSO) once daily, which served as the negative control. The rats in Group F received 2.86 mg/kg of ofloxacin once daily and served as the positive control. All the treatments were done for a period of 5 days. Then 10 days after the treatments, the animals were sacrificed and the lungs were harvested for hydrostatic lung test and histopathological examination. An overnight broth culture of Klebsiella pneumonia was streaked in sterile molten nutrient agar maintained at 37°C for 24hrs. Later, a stock of 500mg/ml of kolaviron was prepared in DMSO. Two-fold dilutions were performed to obtain the following concentrations of 100%, 50%, 25%, 12.5%, 6.25%, 3.125%, and 1.565% with the stock. The anti-Klebsiella pneumonia activity of the kolaviron extract was determined using agar well diffusion methods and incubation was done at 37 o C for 24 hrs. Student t-test and Oneway Analysis of variance (ANOVA) were used for comparison of mean differences between and among the groups. RESULTS AND DISCUSSION: The sensitivity of Klebsiella pneumonia to kolaviron was concentration- dependent. There was an increase in anti-Klebsiella pneumonia activity with a decrease in kolaviron concentration. Kolaviron (KV), at 500mg/kg concentration, was efficacious and showed significant anti-inflammatory effects (P<0.0001). This was also confirmed in the histopathological examinations. The 3.125% concentration of the kolaviron gave IZDs that ranged from 25.68±3.33 mm on day 1 to 27.33±2.78 mm on day 5. Treatment with kolaviron showed to be sex-dependent with a significant difference (p<0.0001), when pre-treatment and post-treatment effects were compared between male and female rats. CONCLUSION: Kolaviron can be used as an agent in the treatment of pneumonia as it possesses anti- inflammatory and anti-Klebsiella pneumonia activities.
Anti-Nociceptive and Anti-Inflammatory Effects of Stem Bark Extract of Ficus Capensis Thunb (Moraceae) by Bioactivity Fractionation.
Wakeel OK, Abe AI, Awosan OB … +4 more , Olapade MK, Olatoyan-Layonu TJ, Olowe OA, Adeyeba OA
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32842947 · Publisher ↗
OBJECTIVE: This study investigated the antinociceptive and anti-inflammatory activities of the aqueous extract of Ficus capensis (AEFC) by bio-guided fractionation. METHODS: The anti-nociceptive and anti-inflammatory eff...
OBJECTIVE: This study investigated the antinociceptive and anti-inflammatory activities of the aqueous extract of Ficus capensis (AEFC) by bio-guided fractionation. METHODS: The anti-nociceptive and anti-inflammatory effects of AEFC (250, 500, 1000 mg/kg, i.p) were assessed using acetic acid-induced writhing, hot plate, tail-flick, formalin tests, and carrageenan- induced paw edema, respectively. The AEFC was fractionated base on polarity difference into butanol, ethyl acetate, and n-hexane fractions. The fractions (500 mg/kg) obtained were subjected to the same experimental procedures mentioned above. The EAF, which exerted the most productive activities, was further subjected to fractionation procedures that yielded six fractions (labeled CF1-CF6). These fractions (200 mg/kg) were tested for potential antinociceptive and anti-inflammatory activities. Notable antagonists (Naloxone and atropine) of the nociceptive pathway were used to evaluate the mechanism of the antinociceptive action of F. capensis. RESULTS AND DISCUSSION: The AEFC, BF, EAF, and CF4 caused a significant (p<0.05) reduction in the number of abdominal writhes, an increase in reaction time against the hot plate, tail-flick tests, and a significant (p<0.05) inhibition in both phases of formalin test. The AEFC, BF, EAF, CF4, and CF6 caused a significant (p<0.05) inhibition of paw edema development due to carrageenan. Atropine significantly reversed the antinociceptive effect of CF4 in both phases of the formalin test. The results obtained revealed that CF4 produced central and peripheral antinociceptive effects, while CF6 is peripherally mediated. CONCLUSION: The results support the traditional uses of F. capensis in the treatment of various diseases associated with pain and inflammation. The column fraction CF4 exhibited muscarinic receptor- mediated antinociceptive activity.
Newborn Screening through TREC, TREC/KREC System for Primary Immunodeficiency with limitation of TREC/KREC. Comprehensive Review.
Shinwari K, Bolkov M, Tuzankina IA … +1 more , Chereshnev VA
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32748762 · Publisher ↗
INTRODUCTION: Newborn screening (NBS) by quantifying T cell receptor excision circles (TRECs) and Kappa receptor excision circles in neonatal dried blood spots (DBS) enables early diagnosis of different types of primary...
INTRODUCTION: Newborn screening (NBS) by quantifying T cell receptor excision circles (TRECs) and Kappa receptor excision circles in neonatal dried blood spots (DBS) enables early diagnosis of different types of primary immune deficiencies. Global newborn screening for PID, using an assay to detect T-cell receptor excision circles (TREC) in dried blood spots (DBS), is now being performed in all states in the United States. In this review, we discuss the development and outcomes of TREC, TREC/KREC combines screening, and continued challenges to implementation. OBJECTIVE: To review the diagnostic performance of published articles for TREC and TREC/ KREC based NBS for PID and its different types. METHODS: Different research resources were used to get an approach for the published data of TREС and KREC based NBS for PID like PubMed, Scopus, Google Scholar, Research gate EMBASE. We extracted TREC and KREC screening Publisher with years of publication, content and cut-off values, and a number of retests, repeat DBS, and referrals from the different published pilot, pilot cohort, Case series, and cohort studies. RESULTS: We included the results of TREC, combined TREC/KREC system based NBS screening from different research articles, and divided these results between the Pilot studies, case series, and cohort. For each of these studies, different parameter data are excluded from different articles. Thirteen studies were included, re-confirming 89 known SCID cases in case series and reporting 53 new SCID cases in 3.15 million newborns. Individual TREC contents in all SCID patients were <25 TRECs/μl (except in those evaluated with the New York State assay). CONCLUSION: TREC and KREC sensitivity for typical SCID and other types of PID was 100 %. It shows its importance and anticipating the significance of implementation in different undeveloped and developed countries in the NBS program in upcoming years. Data adapting the screening algorithm for pre-term/ill infants reduce the amount of false-positive test results.
Piperine from Black Pepper Decreased the Expression of Intercellular Adhesion Molecule-1 in Macrophages.
Gholijani N, Hashemi E, Amirghofran Z
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32614754 · Publisher ↗
BACKGROUND: Macrophages are the main players involved in inflammation. Intercellular adhesion molecule-1 (ICAM-1) facilitates macrophage polarization prior to extravasation into inflamed tissue. Piperine, a natural produ...
BACKGROUND: Macrophages are the main players involved in inflammation. Intercellular adhesion molecule-1 (ICAM-1) facilitates macrophage polarization prior to extravasation into inflamed tissue. Piperine, a natural product derived from black pepper, possesses useful biological and pharmacological activities. In the current study, the possible anti-inflammatory effect of piperine on the expression of ICAM-1 on J774.1 murine macrophage cell line was investigated. METHODS: Lipopolysaccharide (LPS)-stimulated J774.1 cells were cultured in the presence of different concentrations of piperine to examine the changes in ICAM-1 expression by real-time PCR and flow cytometry. RESULTS: We found that piperine decreased ICAM-1 gene expression level from 2.4 ± 0.25 RFC (relative fold change) in LPS-only treated cells to 0.85 ± 0.525 RFC at 1µg/ml (p<0.05), 0.43 ± 0.27 RFC at 10µg/ml (p<0.01), and 0.26 ± 0.25 RFC at 20µg/ml (p<0.01). In flow cytometry, piperine at all concentrations significantly decreased ICAM-1 surface expressions (P<0.05). The geometric mean fluorescence intensity (g-MFI) in LPS-only treated cells (792 ± 57.3) decreased to 482±70 g-MFI at 20 μg/ml piperine. CONCLUSION: According to the results of this study, by decreasing the expression of ICAM-1, piperine has been suggested to reduce inflammation and have the potential to provide therapeutic benefits for immune-mediated diseases.
C1 Inhibitor Administration Reduces Local Inflammation and Capillary Leakage, Without Affecting Long-term Wound Healing Parameters, in a Pig Burn Wound Model.
Korkmaz HI, Ulrich MMW, Wieringen WNV … +11 more , Doǧan H, Vlig M, Emmens RW, Meyer KW, Sinnige P, Zeerleder S, Wouters D, Ham MSV, Zuijlen PPMV, Krijnen PAJ, Niessen HWM
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32614753 · Publisher ↗
BACKGROUND: Burns induce a boost in local and systemic complement levels as well as immune cell infiltration in the burn wound, which may negatively affect wound healing. OBJECTIVE: In this study, the effects of long-ter...
BACKGROUND: Burns induce a boost in local and systemic complement levels as well as immune cell infiltration in the burn wound, which may negatively affect wound healing. OBJECTIVE: In this study, the effects of long-term treatment with complement inhibitor C1 esterase inhibitor (C1inh) on post-burn inflammation and wound healing parameters were analyzed in time up to 60 days post-burn. METHODS: Burned pigs were treated either with or without C1inh up to 15 days post-burn. Burn wound biopsies and blood were collected at different time points up to 60 days post-burn. Thereafter, complement in blood as well as complement and immune cells in the wound, capillary leakage, necrosis, reepithelialization and wound contraction were quantified. RESULTS: No significant differences in complement C3 blood levels were observed at any time point between C1inh-treated and control pigs. In the wound, complement C4 levels were significantly lower in the C1inh group than in controls at day 3-6 and 21-30 post-burn. Similarly, C3 levels, neutrophil and macrophage infiltration in the wound were, although not statistically significant, reduced in C1inh-treated pigs at day 9-14 post-burn. No differences in lymphocyte infiltration in the wound were found between C1inh and control pigs. C1inh-treated pigs also showed reduced capillary leakage. Despite these effects, no significant differences in the long-term wound healing parameters necrosis, reepithelialization and wound contraction were observed between C1inh and control pigs. CONCLUSION: In pigs, 15 days of C1inh treatment after burn, leads to a reduction in local inflammation and capillary leakage in the burn wound without affecting long-term wound healing parameters.
Predictive and Prognostic Value of Ascitic Fluid Mannose Binding Lectin in Patients with Spontaneous Bacterial Peritonitis.
Mohamed AA, Abdelhamid M, El-Toukhy N … +6 more , Sabry A, Khattab RA, El-Damasy DA, Ahmed A, Elkadeem M, Abd-Elsalam S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32552645 · Publisher ↗
BACKGROUND: Spontaneous bacterial peritonitis is a common bacterial infection of ascitic fluid, mainly in ascites due to liver cirrhosis. Mannose-binding lectin (MBL) can activate phagocytosis and the complement system....
BACKGROUND: Spontaneous bacterial peritonitis is a common bacterial infection of ascitic fluid, mainly in ascites due to liver cirrhosis. Mannose-binding lectin (MBL) can activate phagocytosis and the complement system. Spontaneous bacterial peritonitis was detected to be higher in MBL deficiency. This study aimed to assess ascitic fluid MBL in liver cirrhosis and spontaneous bacterial peritonitis. METHODS: Ninety patients with cirrhotic ascites were included. Forty five of them had SBP. Child- Pugh score, Model for End Stage Liver Disease (MELD) and its update (uMELD) scores were used to assess the severity of liver cirrhosis. Ascitic fluid samples were obtained for differentiation of leucocytic count, estimation of albumin, protein, glucose, and serum-ascitic albumin gradient. Ascitic fluid levels of MBL were measured for all patients. SBP was documented if polymorphonuclear leucocytic count ≥250/mm in ascitic fluid. RESULTS: Ascitic fluid MBL level was significantly lower in patients with SBP. MBL had a significant negative correlation with ascitic total leukocytic count (TLC), also with serum creatinine, bilirubin, PT, INR and MELD score among SBP patients. However, it had a significant positive correlation with ascitic protein and with platelets. According to multivariate analysis, fever, TLC, platelets, creatinine, MBL, glucose and polymorphs were independent predictors for SBP development. CONCLUSION: Ascitic fluid MBL could be a good predictive and prognostic marker in patients with cirrhosis and spontaneous bacterial peritonitis.
Antioxidant, Anti-Inflammatory and Cytotoxic Properties of Lamk var. [Bonnet] M].
Hadjira S, Mansour A, Berkel C … +6 more , Seghiri R, Menad A, Benayache F, Benayache S, Cacan E, Ameddah S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32516104 · Publisher ↗
BACKGROUND: In Algerian traditional medicine, Centaurea species are well known in traditherapy. Centaurea africana has been used in folk medicine for the treatment of several inflammatory disorders. OBJECTIVE: This study...
BACKGROUND: In Algerian traditional medicine, Centaurea species are well known in traditherapy. Centaurea africana has been used in folk medicine for the treatment of several inflammatory disorders. OBJECTIVE: This study aims to examine the antioxidant, anti-inflammatory and anti-proliferative potential of both n-Butanol (BECA) and ethyl acetate (EAECA) extracts of Centaurea africana. METHODS: The phytochemical analysis of both BECA and EAECA were explored and the antioxidant activities were investigated by measuring the DPPH° scavenging effect, the reducing power and the inhibition of lipid peroxidation (LPO) induced by by Fe/ ascorbic acid system. The antiinflammatory properties were determined by measuring the NO° scavenging effect and by using carrageenan-induced rat paw oedema. The antiproliferative activity was studied on HT29 (human colorectal adenocarcinoma), OV2008 (human ovarian cancer) and C6 (Rattus norvegicus brain glioma) cell lines using the Sulforhodamine B assay. RESULTS: The total polyphenol contents (TPC) of EAECA and BECA are recorded at 125.24±10.14 and 53.03±2.50 mgGAE/g extract, respectively. Both extracts revealed the antioxidant activity in a concentration-dependent manner; this effect is more pronounced with EAECA. The BECA exhibited a higher anti-inflammatory activity. This anti-inflammatory activity was reflected in a reduction of swelling of carrageenan-evoked edemas (48.45 %), inhibition of nitric oxide (84.7 %), effective decrease in myeloperoxidase activity (58.82 %) and malondialdehyde level (65.58 %). The cytotoxic effect of BECA was found to be more pronounced against C6 cell lines (IC value: 131.93 μg/mL) while the cytotoxic activity of EAECA was more effective against HT29 and OV2008 cell lines. CONCLUSION: The obtained results indicated that EAECA exhibited a high antioxidant activity, while BECA has significant anti-inflammatory activity. Both extracts showed cytotoxic effects against cancer cell lines at certain concentrations in a cell-specific manner.
Novel Coronavirus Disease and the Current Scenario of the Global Health Emergency.
Baruah G, Sahu J
Antiinflamm Antiallergy Agents Med Chem · 2020 · PMID 32479247 · Publisher ↗
Abstract loading — click title to view on PubMed.
Dietary Technologies to Optimize Healing from Injury-Induced Inflammation.
Sears B, Perry M, Saha AK
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32394845 · Full text
Inflammation is an acute adaptive response to injury. However, if the initial inflammatory response to an injury is not completely healed, it becomes chronic low-level inflammation that is strongly associated with many c...
Inflammation is an acute adaptive response to injury. However, if the initial inflammatory response to an injury is not completely healed, it becomes chronic low-level inflammation that is strongly associated with many chronic disease states, including metabolic (obesity and diabetes), cardiovascular, auto-immune, and neurogenerative disorders as well as cancer. The healing process is far more complex than the initiation of inflammation. Within that complexity of healing is a sequence of events that are under profound dietary control and can be defined by specific blood markers. Those molecular events of the healing process that are under significant dietary control are termed as the Resolution Response. The purpose of this review is to describe the molecular components of the Resolution Response and how different dietary factors can either optimize or inhibit their actions. In particular, those dietary components that optimize the Resolution Response include a calorie-restricted, protein-adequate, moderate-carbohydrate, low-fat diet referred to as the Zone diet, omega-3 fatty acids, and polyphenols. The appropriate combination of these dietary interventions constitutes the foundation of Pro-Resolution Nutrition. The effect of these dietary components the actions of NF-κB, AMPK, eicosanoids, and resolvins are described in this review, as well as ranges of appropriate blood markers that indicate success in optimizing the Resolution Response by dietary interventions.
Substituted 3-R-2,8-Dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4] triazino [2,3-c]quinazoline-5a(6H)carboxylic Acids and their Salts - a Promising Class of Anti-inflammatory Agents.
Stavytskyi V, Antypenko O, Nosulenko I … +3 more , Berest G, Voskoboinik O, Kovalenko S
Antiinflamm Antiallergy Agents Med Chem · 2021 · PMID 32368980 · Publisher ↗
BACKGROUND: Computer-aided drug design is among the most effective methods of medicinal chemistry. The above mentioned approach is used for the purposeful search of antiinflammatory agents among quinazoline condensed der...
BACKGROUND: Computer-aided drug design is among the most effective methods of medicinal chemistry. The above mentioned approach is used for the purposeful search of antiinflammatory agents among quinazoline condensed derivatives. OBJECTIVE: The study aimed to conduct a purposeful synthesis of novel 3-R-2,8-dioxo-7,8-dihydro- 2H-pyrrolo[1,2-a][1,2,4]triazino[2,3-c]quinazoline-5a(6H)carboxylic acids and their salts as promising anti-inflammatory agents, evaluate their structure by physicochemical methods and establish their anti-inflammatory activity. METHODS: The structures of target compounds were proposed due to their structure similarity to existing drugs and experimental agents with anti-inflammatory activities. The features of the synthesized compounds structures were evaluated by IR-, NMR spectroscopy and chromatography-mass spectrometry and discussed in detail. Probable molecular mechanisms of activity were predicted by molecular docking. The anti-inflammatory activity was determined by their ability to reduce the formalin- and carrageenan-induced paw edema in rats. RESULTS: It was found that the condensation of 3-(2-aminophenyl)-6-R-1,2,4-triazin-5(2H)ones with 2-oxoglutaric acid yielded 3-R-2,8-dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4]triazino[2,3-c]quinazoline- 5a(6H)carboxylic acids which may be considered as a promising anti-inflammatory agent. An in silico study showed that the obtained compounds revealed affinity to the molecular targets and corresponded to the drug-like criteria. Additionally docking study allowed to estimate the nature of interactions between synthesized compounds and molecular targets. The in vivo experiments showed that the obtained compounds demonstrated significant anti-inflammatory activity comparable or higher than the activity of the reference drug Diclofenac. CONCLUSION: The developed and implemented search strategy of the anti-inflammatory agents was justified. 3-R-2,8-dioxo-7,8-dihydro-2H-pyrrolo[1,2-a][1,2,4]triazino[2,3-c]quinazoline5a(6H)carboxylic acids possessed the anti-inflammatory activity and additional introduction of fluorine atoms in position 11 or 12 of the heterocyclic system led to amplification of this activity.
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